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  • 1.
    Alomari, Mustafa
    et al.
    UCL School of Pharmacy, University College London.
    Vuddanda, Parameswara Rao
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap. UCL School of Pharmacy, University College London.
    Trenfield, Sarah J.
    UCL School of Pharmacy, University College London.
    Dodoo, Cornelius C.
    UCL School of Pharmacy, University College London.
    Velaga, Sitaram
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Basit, Abdul W.
    UCL School of Pharmacy, University College London.
    Gaisford, Simon
    UCL School of Pharmacy, University College London.
    Printing of T3 and T4 Oral Drug Combinations as a Novel Strategy for Hypothyroidism2018Ingår i: International Journal of Pharmaceutics, ISSN 0378-5173, E-ISSN 1873-3476, Vol. 549, nr 1-2, s. 363-369Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Hypothyroidism is a chronic and debilitating disease that is estimated to affect 3% of the general population. Clinical experience has highlighted the synergistic value of combining triiodothyronine (T3) and thyroxine (T4) for persistent or recurrent symptoms. However, thus far a platform that enables the simultaneous and independent dosing of more than one drug for oral administration has not been developed. Thermal inkjet (TIJ) printing is a potential solution to enable the dual deposition of T3 and T4 onto orodispersible films (ODFs) for therapy personalisation. In this study, a two-cartridge TIJ printer was modified such that it could print separate solutions of T3 and T4. Dose adjustments were achieved by printing solutions adjacent to each other, enabling therapeutic T3 (15–50 μg) and T4 dosages (60–180 μg) to be successfully printed. Excellent linearity was observed between the theoretical and measured dose for both T3 and T4 (R2 = 0.982 and 0.985, respectively) by changing the length of the print objective (Y-value). Rapid disintegration of the ODFs was achieved (< 45 seconds). As such, this study for the first time demonstrates the ability to produce personalised dose combinations by TIJ printing T3 and T4 onto the same substrate for oral administration.

  • 2.
    Chakraborty, Subhashis
    et al.
    Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi .
    Shukla, Dali
    Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi .
    Rao Vuddanda, Parameswara
    Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi .
    Mishra, Brahmeshwar
    Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi .
    Singh, Sanjay Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Effective in-vivo utilization of lipid-based nanoparticles as drug carrier for carvedilol phosphate2011Ingår i: Journal of Pharmacy and Pharmacology (JPP), ISSN 0022-3573, E-ISSN 2042-7158, Vol. 63, nr 6, s. 774-779Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Objectives Lipid nanoparticles as carrier for oral drug administration improve gastrointestinal solubility of poorly soluble drugs and thus enhance bioavailability. However, basic drugs may undergo rapid dissolution from such solid dispersions in the stomach and precipitate in the intestine due to their higher solubility in acidic medium. Therefore, the objective of this work was to study the enhancement in bioavailability of carvedilol phosphate (basic drug) by providing an alkaline gastric environment to drug-loaded solid lipid nanoparticles. Methods An alkaline gastric environment in rats was created and maintained with oral administration of an antacid suspension 5 min before and 30 min post dosing. Key findings The formulation administered orally exhibited enhanced bioavailability (∼27%) when compared with drug suspension and sustained release behaviour when compared with formulation under ideal gastric conditions. The enhanced bioavailability is due to the presence of lipid nanoparticles as drug carrier while the sustained-release characteristic may be attributed to the presence of antacid, which resulted in elevation of gastric pH and reduced the drug's solubility. Conclusions It may be concluded that although lipid nanoparticles can be instrumental in improving bioavailability, additional sustained release may be achieved by targeting intestinal release of basic drugs from lipid vehicles, which is possible by incorporating them into suitable enteric-coated formulations.

  • 3.
    Chakraborty, Subhashis
    et al.
    Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi .
    Shukla, Dali
    Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi .
    Rao Vuddanda, Parameswara
    epartment of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi .
    Mishra, Brahmeshwar
    Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi .
    Singh, Sanjay Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Utilization of adsorption technique in the development of oral delivery system of lipid based nanoparticles2010Ingår i: Colloids and Surfaces B: Biointerfaces, ISSN 0927-7765, E-ISSN 1873-4367, Vol. 81, nr 2, s. 563-569Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The objective of the present study was to employ suitable adsorbent with free flowing characteristics for improving the stability and physical properties of solid lipid nanoparticles (SLN) for oral administration. Stearic acid based nanoparticles of carvedilol phosphate were fabricated by solvent emulsification evaporation technique in sodium taurocholate solution prepared in pH 7.2 buffers (I-KH2PO4/NaOH or II-NaH2PO4/Na2HPO4) with 1% polyvinyl alcohol. Nanoparticles were then adsorbed by passing the nanodispersion through a Neusilin US2 (adsorbent) column. Interestingly, scanning electron microscopy revealed round deformed and even collapsed nanoparticles in Buffer-I and discrete spherical to ellipsoidal nanoparticles in Buffer-II which indicates the inability of nanoemulsion to crystallize and form SLN in Buffer-I. The successful formation of SLN in Buffer-II was confirmed by differential scanning calorimetry and X-ray diffraction. The retention of SLN from the nanodispersion by adsorption on the adsorbent imparted good flow property and resulted in a marked stability improvement of the formulation in terms of drug retention efficiency and release profile as compared to the simple nanosuspension. In conclusion, the adsorbent technology would be instrumental in imparting additional features to the existing conventional colloidal system for pharmaceutical application which would ease the process of capsule filling at industrial scale, simplify the handling of formulations by patients and can significantly improve the shelf life of the product for a longer period of time as compared to liquid formulations

  • 4.
    Gundampati, Ravi Kumar
    et al.
    Molecular Biology Unit, Institute of Medical Sciences, Banaras Hindu University, Varanasi.
    Sahu, Shraddha
    School of Biochemical Engineering, Indian Institute of Technology (BHU), Varanasi.
    Srivastava, Avinash Kumar
    School of Biochemical Engineering, Indian Institute of Technology (BHU), Varanasi.
    Chandrasekaran, Sambamurthy
    Department of Animal Sciences, University of Hyderabad.
    Rao Vuddanda, Parameswara
    Department of Pharmaceutics, Indian Institute of Technology (BHU), Varanasi.
    Pandey, Rajesh Kumar
    Molecular Biology Unit, Institute of Medical Sciences, Banaras Hindu University, Varanasi.
    Maurya, Radheshyam P.
    Department of Animal Sciences, University of Hyderabad.
    Singh, Sanjay Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Jagannadham, Medicherla Venkata
    Molecular Biology Unit, Institute of Medical Sciences, Banaras Hindu University, Varanasi.
    In silico and in vitro studies: Tryparedoxin Peroxidase inhibitor activity of methotrexate for antileishmanial activity2013Ingår i: American Journal of Infectous Diseses, ISSN 1553-6203, Vol. 9, nr 4, s. 117-129Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    In order to understand the mechanism of molecular interactions at the active site of Tryparedoxin Peroxidase (Try P), homology modeling and docking studies were performed. We generated a Three-Dimensional (3D) model of target protein based on the Crystal structure of Leishmania Major Try PI (PDB ID: 3TUE) using modeler software. Docking analysis was carried out to study the effects of methotrexate on Tryparedoxin Peroxidase (Try P). Inhibition of the Tryparedoxin peroxidase interaction has become a new therapeutic strategy in treating leishmaniasis. Docking analysis was carried out to study the effects of methotrexate on Tryparedoxin Peroxidase (TryP). Tryparedoxin peroxidase of Trypanosomatidae family functions as antioxidant through their peroxidase and peroxynitrite reductase activities. The theoretical docking study, conducted on a sample previously reported for anti-cancer properties of Methotrexate at the binding site of 3D models of Tryparedoxin Peroxidase of Leishmania braziliensis (L. braziliensis Try P) examine interaction energy. Our studies indicate that Methotrexate displays potent activity against Try P with lowest binding energy and RMSD values to be -14.5879 Kcal/Mol and 2.0 A. The results of the present study clearly demonstrated the Tryparedoxin Peroxidase inhibitory activity by methotrexate in in silico docking analysis and in vitro assay which contributes towards understanding the mechanism of antileishmanial activity.

  • 5.
    Jain, Achint K.
    et al.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University.
    Mishra, Sandeep Kumar
    Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi.
    Rao Vuddanda, Parameswara
    Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi.
    Singh, Sanjay Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Singh, Royana S.
    Department of Anatomy, Institute of Medical Sciences, Banaras Hindu University, Varanasi.
    Singh, Sanjay
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Targeting of diacerein loaded lipid nanoparticles to intra-articular cartilage using chondroitin sulfate as homing carrier for treatment of osteoarthritis in rats2014Ingår i: Nanomedicine: Nanotechnology, Biology and Medicine, ISSN 1549-9634, E-ISSN 1549-9642, Vol. 10, nr 5, s. 1031-1040Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Targeted delivery of antiosteoarthritic drug diacerein to articular tissue could be a major achievement and soluble polysaccharide chondroitin sulfate (ChS) may be a suitable agent for this. Therefore, diacerein loaded solid lipid nanoparticles modified with ChS (ChS-DC-SLN) were prepared for synergistic effect of these agents to combat multidimensional pathology of osteoarthritis (OA). Prepared formulation were of size range 396. ±. 2.7. nm, showed extended release up to 16. h and increased bioavailability of diacerein by 2.8 times. ChS-DC-SLN were evaluated for their effect on histopathology of femoro-tibial joint of rat knee and amount of ChS and rhein (an active metabolite of diacerein) at targeted site. Concentration of rhein was significantly higher in case of ChS-DC-SLN (7.8. ±. 1.23. μg/ml) than that of drug dispersion (2.9. ±. 0.45. μg/ml). It can be stated that ChS served as homing to articular cartilage for targeting of drug. Thus, ChS-DC-SLN have great potential to enhance the overall efficacy of treatment for OA. From the Clinical Editor: This study demonstrates the feasibility of targeted delivery of diacerein to articular tissue using soluble polysaccharide chondroitin sulfate as the targeting vector. This approach has the potential to significantly increase anti-arthritic drug concentration in joints without leading to systemic toxicity

  • 6.
    Mishra, Amit Kumar
    et al.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Rao Vuddanda, Parameswara
    Singh, Sanjay Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Intestinal lymphatic delivery of praziquantel by solid lipid nanoparticles: Formulation design, in vitro and in vivo studies2014Ingår i: Hans Journal of Nanotechnology, ISSN 2161-086X, E-ISSN 2161-0878, Vol. 2014, artikel-id 351693Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The aim of the present work was to design and develop Praziquantal (PZQ) loaded solid lipid nanoparticles (PZQ-SLN) to improve the oral bioavailability by targeting intestinal lymphatic system. PZQ is practically insoluble in water and exhibits extensive hepatic first-pass metabolism. PZQ SLN were composed of triglycerides, lecithin and various aqueous surfactants; were optimized using hot homogenization followed by ultrasonication method. The optimized SLN had particle size of 123 ± 3.41 nm, EE of 86.6 ± 5.72 %. The drug release of PZQ-SLN showed initial burst release followed by the sustained release. Inspite of zeta potential being around -10 mV, the optimized SLN were stable at storage conditions (5 ± 3 °C and 25 ± 2°C/ 60 ± 5 % RH) for six months. TEM study confirmed the almost spherical shape similar to the control formulations. Solid state characterization using differential scanning calorimeter (DSC) and powder X-ray diffraction (PXRD) analysis confirmed the homogeneous distribution of PZQ within the lipid matrix. The 5.81-fold increase in AUC 0 → ∞, after intraduodenal administration of PZQ-SLN in rats treated with saline in comparison to rats treated with cycloheximide (a blocker of intestinal lymphatic pathway), confirmed its intestinal lymphatic delivery. The experimental results indicate that SLN may offer a promising strategy for improving the therapeutic efficacy and reducing the dose.

  • 7.
    Montenegro-Nicolin, Miguel
    et al.
    Department of Pharmaceutical Science and Technology, School of Chemical and Pharmaceutical Sciences, University of Chile, Santiago.
    Reyes, Patricio E.
    Instituto de Salud Pública de Chile, Santiago.
    Jara, Miguel O.
    Department of Pharmaceutical Science and Technology, School of Chemical and Pharmaceutical Sciences, University of Chile, Santiago.
    Vuddanda, Parameswara Rao
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Neira-Carrillo, Andrónico
    Advanced Center for Chronic Diseases (ACCDiS), Santiago.
    Butto, Nicole
    Advanced Center for Chronic Diseases (ACCDiS, )Santiago.
    Velaga, Sitaram
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Morales, Javier O.
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap. Department of Pharmaceutical Science and Technology, School of Chemical and Pharmaceutical Sciences, University of Chile, Santiago.
    The Effect of Inkjet Printing over Polymeric Films as Potential Buccal Biologics Delivery Systems2018Ingår i: AAPS PharmSciTech, ISSN 1530-9932, E-ISSN 1530-9932, Vol. 19, nr 8, s. 3376-3387Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The buccal mucosa appears as a promissory route for biologic drug administration, and pharmaceutical films are flexible dosage forms that can be used in the buccal mucosa as drug delivery systems for either a local or systemic effect. Recently, thin films have been used as printing substrates to manufacture these dosage forms by inkjet printing. As such, it is necessary to investigate the effects of printing biologics on films as substrates in terms of their physical and mucoadhesive properties. Here, we explored solvent casting as a conventional method with two biocompatible polymers, hydroxypropyl methylcellulose, and chitosan, and we used electrospinning process as an electrospun film fabrication of polycaprolactone fibers due to its potential to elicit mucoadhesion. Lysozyme was used as biologic drug model and was formulated as a solution for printing by thermal inkjet printing. Films were characterized before and after printing by mechanical and mucoadhesive properties, surface, and ultrastructure morphology through scanning electron microscopy and solid state properties by thermal analysis. Although minor differences were detected in micrographs and thermograms in all polymeric films tested, neither mechanical nor mucoadhesive properties were affected by these differences. Thus, biologic drug printing on films was successful without affecting their mechanical or mucoadhesive properties. These results open way to explore biologics loading on buccal films by inkjet printing, and future efforts will include further in vitro and in vivo evaluations.

  • 8.
    Rao Vuddanda, Parameswara
    et al.
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap. Banaras Hindu University, Institute of Technology, Department of Pharmaceutics, Varanasi .
    Chakraborty, Subhashis
    Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi .
    Singh, Sanjay Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Berberine: A potential phytochemical with multispectrum therapeutic activities2010Ingår i: Expert Opinion on Investigational Drugs, ISSN 1354-3784, E-ISSN 1744-7658, Vol. 19, nr 10, s. 1297-1307Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Importance of the field: The use of traditional medicines of natural origin is being encouraged for the treatment of chronic disorders, as synthetic drugs in such cases may cause unpredictable adverse effects. Berberine, a traditional plant alkaloid, is used in Ayurvedic and Chinese medicine for its antimicrobial and antiprotozoal properties. Interestingly, current clinical research on berberine has revealed its various pharmacological properties and multi-spectrum therapeutic applications. Areas covered in this review: An extensive search in three electronic databases (Unbound Medline, PubMed and ScienceDirect) and internet search engines (Scirus and Google Scholar) were used to identify the clinical studies on berberine, without any time constraints. This review elaborates the recent studies which reveal that with time, the drug has evolved with superior therapeutic activities. In addition, this review will also attract the attention of formulation scientists towards the issues and challenges associated in its drug delivery and the probable approaches that may be explored to help patients reap the maximum benefit of this potentially useful drug. What the reader will gain: A relatively large number of studies discussed here have revealed the possible areas where this phytochemical constituent can exhibit its therapeutic activities in the treatment of chronic ailments or diseases including diabetes, cancer, depression, hypertension and hypercholesterolemia. Take home message: The potential of the drug remains to be harvested by designing a suitable formulation that could overcome its inherent low bioavailability

  • 9.
    Rao Vuddanda, Parameswara
    et al.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Mishra, Amit Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Singh, Sanjay
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Singh, Sanjay Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Development of polymeric nanoparticles with highly entrapped herbal hydrophilic drug using nanoprecipitation technique: An approach of quality by design2015Ingår i: Pharmaceutical development and technology (Print), ISSN 1083-7450, E-ISSN 1097-9867, Vol. 20, nr 5, s. 579-587Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The intention of this study is to achieve higher entrapment efficiency (EE) of berberine chloride (selected hydrophilic drug) using nanoprecipitation technique. The solubility of drug was studied in various pH buffers (1.2-7.2) for selection of aqueous phase and stabilizer. Quality by design (QbD)-based 32 factorial design were employed for optimization of formulation variables; drug to polymer ratio (X1) and surfactant concentration (X2) on entrapment efficiency (EE), particle size (PS) and polydispersity index (PDI) of the nanoparticles. The nanoparticles were subjected to solid state analysis, in vitro drug release and stability study. The aqueous phase and stabilizer selected for the formulations were pH 4.5 phthalate buffer and surfactant F-68, respectively. The formulation (F-6) containing drug to polymer ratio (1:3) and stabilizer (F-68) concentration of 50mM exhibited best EE (82.12%), PS (196.71nm), PDI (0.153). The various solid state characterizations assured that entrapped drug is amorphous and nanoparticles are fairly spherical in shape. In vitro drug release of the F-6 exhibited sustained release with non-Fickian diffusion and stable at storage condition. This work illustrates that the proper selection of aqueous phase and optimization of formulation variables could be helpful in improving the EE of hydrophilic drugs by nanoprecipitation technique

  • 10.
    Rao Vuddanda, Parameswara
    et al.
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Montenegro-Nicolini, Miguel
    Department of Pharmaceutical Sciences and Technology, University of Chile, Santiago.
    Morales, Javier O.
    Department of Pharmaceutical Sciences and Technology, University of Chile, Santiago.
    Velaga, Sitaram
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Effect of plasticizers on the physico-mechanical properties of pullulan based pharmaceutical oral films2017Ingår i: European Journal of Pharmaceutical Sciences, ISSN 0928-0987, E-ISSN 1879-0720, Vol. 96, s. 290-298Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The effect of different plasticizers (glycerol, vitamin E TPGS and triacetin) and their concentrations on the physico-mechanical properties of pullulan based oral films was studied. A full factorial (32) design of experiments was used. Elastic modulus, tensile strength, elongation at break and disintegration time were selected as response variables. Modulated differential scanning calorimeter (MDSC) was used for determining glass transition temperature (Tg) of pullulan films. The surface morphology of films was evaluated by SEM, while ATR-FTIR was used to obtain a molecular level understanding of polymer-plasticizer interactions. The DoE analysis allowed for the modelling of tensile strength and elongation at break. The highest elongations were observed in glycerol at 20% w/w. Majority of the films disintegrated within one minute without significant differences. ATR-FTIR spectra of pullulan alone and different plasticizer blend films show characteristic molecular interactions. The present study concluded that glycerol is suitable plasticizer compared to others for manufacturing pullulan based oral films.

  • 11.
    Rao Vuddanda, Parameswara
    et al.
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Montenegro-Nicolini, Miguel
    Department of Pharmaceutical Sciences and Technology, University of Chile.
    Morales, Javier O.
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Velaga, Sitaram
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Effect of surfactants and drug load on physico-mechanical and dissolution properties of nanocrystalline tadalafil-loaded oral films2017Ingår i: European Journal of Pharmaceutical Sciences, ISSN 0928-0987, E-ISSN 1879-0720, Vol. 109, s. 372-380Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The aim of the present work was to prepare tadalafil (TDF) nanocrystals-loaded oral polymeric films (OFs) and investigate the effect of hydrophilic surfactants and drug loads on the physico-mechanical and dissolution properties. The nanosuspensions of TDF were prepared by high shear homogenization. HPMC based placebo casting film gel was prepared and mixed with TDF nanosuspensions. Films were casted using an automated film applicator and dried at 60 °C for 45 min. Particle size (PS), polydispersity index (PDI), and zeta potential (ZP) of TDF nanosuspensions were measured in a Zetasizer. The films were characterized using SEM, AFM, DSC, TGA and PXRD. The mechanical properties and in vitro drug release were determined using standard methods. TDF existed in crystalline form and the particles remained in the nano-range in redispersed films. TDF nanocrystals were embedded in the polymeric matrix and the drug loaded films were rough on the surface. Mechanical properties of the films varied with changes in drug load and surfactant. Significant changes in the disintegration times were noticed in films containing surfactants compared to surfactant-free films. About 80% of the drug release was observed between 3 and 30 min. TPGS showed better TDF release from the films at different drug loads

  • 12. Rao Vuddanda, Parameswara
    et al.
    Rajamanickam, Vijayakumar Mahalingam Ahalingam
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi.
    Yaspal, Madhu
    Department of Anatomy, Institute of Medical Sciences, Banaras Hindu University, Varanasi.
    Singh, Sanjay Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Investigations on agglomeration and haemocompatibility of Vitamin E TPGS surface modified berberine chloride nanoparticles2014Ingår i: BioMed Research International, ISSN 2314-6133, E-ISSN 2314-6141, Vol. 2014, artikel-id 951942Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The objective of the present study is to investigate the influence of surface modification on systemic stability of NPs. Vitamin E TPGS (1% w/v) was used for surface modification of berberine chloride nanoparticles. Naked and surface modified NPs were incubated in different SBFs (pH 6.8 and 7.4) with or without bile salts and human plasma. NPs were observed for particle agglomeration and morphology by particle size analyzer and TEM, respectively. The haemocompatibility studies were conducted on developed NPs to evaluate their safety profile. The surface modified NPs were stable compared to naked NPs in different SBFs due to the steric stabilization property of vitamin E TPGS. Particle agglomeration was not seen when NPs were incubated in SBF (pH 6.8) with bile salts. No agglomeration was observed in NPs after their incubation in plasma but particle size of the naked NPs increased due to adhesion of plasma proteins. The TEM images confirmed the particle size results. DSC and FT-IR studies confirmed the coexistence of TPGS in surface modified NPs. The permissible haemolysis, LDH release, and platelet aggregation revealed that NPs were compatible for systemic administration. Thus, the study illustrated that the surface modification is helpful in the maintenance of stability of NPs in systemic conditions

  • 13.
    Singh, Bhupender L.
    et al.
    Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi .
    Rao Vuddanda, Parameswara
    Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi .
    Vijayakumar, M.R.
    Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi .
    Kumar, Vinod
    Department of Zoology, Faculty of Science, Banaras Hindu University, Varanasi .
    Saxena, Preeti Suman
    Department of Zoology, Faculty of Science, Banaras Hindu University, Varanasi .
    Singh, Sanjay
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Cefuroxime axetil loaded solid lipid nanoparticles for enhanced activity against S. aureus biofilm2014Ingår i: Colloids and Surfaces B: Biointerfaces, ISSN 0927-7765, E-ISSN 1873-4367, Vol. 121, s. 92-98Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The present research work is focused on the development of solid lipid nanoparticles of cefuroxime axetil (CA-SLN) for its enhanced inhibitory activity against Staphylococcus aureus produced biofilm. CA-SLN was prepared by solvent emulsification/evaporation method using single lipid (stearic acid (SA)) and binary lipids (SA and tristearin (TS)). Process variables such as volume of dispersion medium, concentration of surfactant, homogenization speed and time were optimized. The prepared SLN were characterized for encapsulation efficiency, drug polymer interaction studies (DSC and FT-IR), shape and surface morphology (SEM and AFM), in vitro drug release, stability studies and in vitro anti biofilm activity against S. aureus biofilm. Among the process variables, increased volume of dispersion medium, homogenization speed and time led to increase in particle size whereas increase in surfactant concentration decreased the particle size. SLN prepared using binary lipids exhibited higher entrapment efficiency than the single lipid. DSC and FT-IR studies showed no incompatible interaction between drug and excipients. CA-SLN showed two folds higher anti-biofilm activity in vitro than pristine CA against S. aureus biofilm.

  • 14.
    Singh, Sanjay Kumar
    et al.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Dadhania, Parth
    Pharma Research, Lupin Limited (Research Park), Pune.
    Vuddanda, Parameswara Rao
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Jain, Achint K.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Velaga, Sitaram
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Singh, Sanjay
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Intranasal delivery of asenapine loaded nanostructured lipid carriers: formulation, characterization, pharmacokinetic and behavioural assessment2016Ingår i: RSC Advances, ISSN 2046-2069, E-ISSN 2046-2069, Vol. 6, nr 3, s. 2032-2045Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The aim of the present research work was to develop asenapine (ASM) loaded nanostructured lipid carriers (ANLC) for the delivery of drugs in the brain by an intranasal route to enhance therapeutic efficacy. A quality by design approach was used for development and optimization of ANLC. A total of five independent variables were selected, in which three were compositions and two were process variables, while particle size and entrapment efficiency were selected as response variables. The final optimized batch was evaluated by various in vitro characterizations as well as in vivo brain and plasma pharmacokinetic studies. Finally, the ANLC was assessed for efficacy and safety profiling for upto three weeks by a behavior model viz. catalepsy, induced locomotor and paw test in Charles Foster rats. The observed particle size, entrapment efficiency and zeta potential of ANLC was found to be 167.30 +/- 7.52 nm, 83.50 +/- 2.48% and -4.33 +/- 1.27 mV, respectively. Surface characterization studies demonstrated a spherical shape with a smooth surface of ANLC which follows the Korsmeyer-Peppas in vitro release kinetic model (r(2) = 0.9911, n = 0.53). A brain pharmacokinetic study indicated a significantly higher (p < 0.05) peak drug concentration (C-max: 74.13 +/- 6.73 ng mL(-1)), area under the drug concentration-time curve (AUC(0-24) (h): 560.93 +/- 27.85 h ng mL(-1)) and mean residence time (MRT: 7.1 +/- 0.13 h) of ANLC compared to ASM in the brain via an intranasal route. The results of behaviour studies of ANLC showed a significant decrease in extra-pyramidal side effects with increasing antipsychotic effect after 1-2 week(s) of treatment. These findings demonstrate that nanostructured lipid carriers could be a new promising drug delivery system for intranasal delivery of asenapine in the treatment of schizophrenia

  • 15.
    Singh, Sanjay Kumar
    et al.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Kushwaha, Anand Kumar
    Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi .
    Rao Vuddanda, Parameswara
    Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi .
    Karunanidhi, Priyanka
    Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi .
    Singh, Sanjay
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Development and evaluation of solid lipid nanoparticles of raloxifene hydrochloride for enhanced bioavailability2013Ingår i: BioMed Research International, ISSN 2314-6133, E-ISSN 2314-6141, Vol. 2013, artikel-id 584549Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Raloxifene hydrochloride (RL-HCL) is an orally selective estrogen receptor modulator (SERM) with poor bioavailability of nearly 2% due to its poor aqueous solubility and extensive first pass metabolism. In order to improve the oral bioavailability of raloxifene, raloxifene loaded solid lipid nanoparticles (SLN) have been developed using Compritol 888 ATO as lipid carrier and Pluronic F68 as surfactant. Raloxifene loaded SLN were prepared by solvent emulsification/evaporation method, and different concentrations of surfactant, and homogenization speed were taken as process variables for optimization. SLN were characterized for particle size, zeta potential, entrapment efficiency, surface morphology, and crystallinity of lipid and drug. In vitro drug release studies were performed in phosphate buffer of pH 6.8 using dialysis bag diffusion technique. Particle sizes of all the formulations were in the range of 250 to 1406 nm, and the entrapment efficiency ranges from 55 to 66%. FTIR and DSC studies indicated no interaction between drug and lipid, and the XRD spectrum showed that RL-HCL is in amorphous form in the formulation. In vitro release profiles were biphasic in nature and followed Higuchi model of release kinetics. Pharmacokinetics of raloxifene loaded solid lipid nanoparticles after oral administration to Wistar rats was studied. Bioavailability of RL-HCL loaded SLN was nearly five times than that of pure RL-HCL

  • 16.
    Singh, Sanjay Kumar
    et al.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University.
    Purvin, Shah
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University.
    Rao Vuddanda, Parameswara
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University.
    Singh, Sanjay
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University.
    Jain, Achint K.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University.
    Pharmacokinetic and tissue distribution study of solid lipid nanoparticles of zidovudine in rats2014Ingår i: Journal of Nanotechnology, ISSN 1687-9503, E-ISSN 1687-9511, Vol. 2014, artikel-id 854018Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Zidovudine-loaded solid lipid nanoparticles (AZT-SLNs) and zidovudine in solution were prepared and administered in rats. The aim of this research was to study whether the bioavailability of zidovudine can be improved by AZT-SLNs perorally to rats as compared to oral administration of zidovudine. Zidovudine was determined in plasma and tissues by reverse phase high performance liquid chromatography. The pharmacokinetic parameters of zidovudine were determined after peroral administration: area under curve of concentration versus time (AUC) for AZT-SLNs was 31.25% greater than AZT solution; meanwhile mean resident time (MRT) was found to be 1.83 times higher for AZT-SLNs than AZT solution. Elimination half life of zidovudine was also increased for SLN formulation. Tissue distribution pattern of zidovudine was changed in case of AZT-SLNs. AUC of zidovudine in brain and liver was found to be approximately 2.73 and 1.77 times higher in AZT-SLNs than AZT solution, respectively, indicating that AZT-SLNs could cross blood brain barrier. Distribution of zidovudine was approximately 0.95 and 0.86 times lesser in heart and kidney, respectively. It can be concluded from the study that oral administration of AZT-SLNs modifies the plasma pharmacokinetic parameters and biodistribution of zidovudine

  • 17.
    Singh, Sanjay Kumar
    et al.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Singh, Sanjay
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Rao Vuddanda, Parameswara
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh.
    Srivastava, Avinash Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University.
    A comparison between use of spray and freeze drying techniques for preparation of solid self-microemulsifying formulation of valsartan and in vitro and in vivo evaluation2013Ingår i: BioMed Research International, ISSN 2314-6133, E-ISSN 2314-6141, Vol. 2013, artikel-id 909045Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The objective of the present study was to develop self micro emulsifying formulation (SMEF) of valsartan to improve its oral bioavailability. The formulations were screened on the basis of solubility, stability, emulsification efficiency, particle size and zeta potential. The optimized liquid SMEF contains valsartan (20% w/w), Capmul MCM C8 (16% w/w), Tween 80 (42.66% w/w) and PEG 400 (21.33% w/w) as drug, oil, surfactant and co-surfactant, respectively. Further, Liquid SMEF was adsorbed on Aerosol 200 by spray and freeze drying methods in the ratio of 2: 1 and transformed into free flowing powder. Both the optimized liquid and solid SMEF had the particle size <200 nm with rapid reconstitution properties. Both drying methods are equally capable for producing stable solid SMEF and immediate release of drug in in vitro and in vivo conditions. However, the solid SMEF produced by spray drying method showed high flowability and compressibility. The solid state characterization employing the FTIR, DSC and XRD studies indicated insignificant interaction of drug with lipid and adsorbed excipient. The relative bioavailability of solid SMEF was approximately 1.5 to 3.0 folds higher than marketed formulation and pure drug. Thus, the developed solid SMEF illustrates an alternative delivery of valsartan as compared to existing formulations with improved bioavailability

  • 18.
    Sngh, Yuvraj N.
    et al.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Vuddanda, Parameswara Rao
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Jain, Achint K.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Parihar, Sarita
    Department of Orthodontics, Institute of Medical Sciences, Banaras Hindu University, Varaansi.
    Chaturvedi, Thakur P.
    Department of Orthodontics, Institute of Medical Sciences, Banaras Hindu University, Varaansi.
    Singh, Sanjay Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Mucoadhesive gel containing immunotherapeutic nanoparticulate satranidazole for treatment of periodontitis: Development and its clinical implications2015Ingår i: RSC Advances, ISSN 2046-2069, E-ISSN 2046-2069, Vol. 5, nr 59, s. 47659-47670Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The aim of this study was to alleviate shortcomings in periodontal treatment by utilizing a mucoadhesive gel containing immunotherapeutic ganglioside coated polymeric nanoparticles (G-PNP) bearing satranidazole (SZ). Nanoprecipitation was used to fabricate SZ loaded G-PNP. In our previous deliberations aqueous dispersibility of conventional SZ had raised dose consistency issues. Usage of G-PNP allayed those fears as DSC and XRD data showed that SZ was rendered amorphous (more water dispersible than crystalline SZ) when captured in a polymeric matrix of nanoparticles. G-PNP were added to sodium carboxy methyl cellulose (SCMC 30 NP) gels and compared against SCMC 30 (gel containing conventional SZ) for texture, mucoadhesion, drug release and inhibitory susceptibility of Aggregatibacter actinomycetomicans. Subsequently a 21 day single blind clinical trial comparing the efficacy of SCMC 30 NP and SCMC 30 was conducted. SCMC 30 NP showed a maximum mucoadhesion force (43.27 ± 4.10 gf), low hardness (12.28 ± 0.17 N), moderate gel strength (8.53 ± 0.21 N) and elasticity (5.50 ± 0.03 mm). 'Well' diffusion data revealed qualitatively greater antibacterial activity of SCMC 30 NP. Dissolution studies demonstrated diffusion controlled release of SZ at concentrations above MIC. SCMC 30 NP caused a significant (P < 0.05) decrease in clinical markers of periodontitis, i.e. gingival index and pocket depth as compared to SCMC 30. Also reduction in the plaque index produced by SCMC 30 NP was highly significant (P < 0.01) as compared to SCMC 30 at the end of the 21st day of clinical study. Amelioration of disease was improved due to Th-2 biased immuno shifting mediated by G-PNPs, which increased secretion of anti-inflammatory cytokines like IL-4 and TGF-β from J774 macrophages. Clinical benefits incurred along with ease of application calls for a scaled up investigation of SCMC 30 NP

  • 19.
    Velaga, Sitaram
    et al.
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Nikjoo, Dariush
    Luleå tekniska universitet, Institutionen för teknikvetenskap och matematik, Materialvetenskap.
    Rao Vuddanda, Parameswara
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Drying Kinetics of Polymeric Films: theoretical and experimental studies2016Konferensbidrag (Refereegranskat)
  • 20.
    Velaga, Sitaram
    et al.
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Nikjoo, Dariush
    Luleå tekniska universitet, Institutionen för teknikvetenskap och matematik, Materialvetenskap.
    Rao Vuddanda, Parameswara
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap. Department of Pharmaceutics, UCL School of Pharmacy, University College London.
    Experimental Studies and Modeling of the Drying Kinetics of Multicomponent Polymer Films2018Ingår i: AAPS PharmSciTech, ISSN 1530-9932, E-ISSN 1530-9932, Vol. 19, nr 1, s. 425-435Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    The process of drying thin polymer films is an important operation that influences the film structure and solid state, and the stability of the product. The purpose of this work was to study and model the drying kinetics of multicomponent films based on two polymers: hydroxypropyl methylcellulose (HPMC, amorphous) and polyvinyl alcohol (PVA, semicrystalline). The isothermal drying kinetics of the films at different temperatures (40, 60, and 80°C) were studied using thermo-gravimetric analysis (TGA) and convection oven methods. Solid-state characterization tools used in the study included polarization and hot-stage microscopy, scanning electron microscopy (SEM), and differential scanning calorimetry (DSC). The drying kinetics of HPMC and PVA films in the TGA apparatus and convection oven were comparable. The three-parameter (Wmax, τ, n) Hill equation successfully modeled the experimental drying kinetics. The time factor τ in the Hill equation nicely explained two drying phases in the films. Solid-state phase changes occurring in the films during dehydration had a bearing on the drying kinetics and mechanisms. TGA can be used as a simple tool to determine the end points in drying processes using ovens or tunnels. The three-parameter Hill equation explained the drying kinetics and diffusion mechanisms of the solvent through the polymer films for the first time. This study advances our understanding of film drying, in particular for pharmaceutically relevant thin films.

  • 21.
    Vijayakumar, Mahalingam Rajamanickam
    et al.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Kosuru, Ramoji
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Vuddanda, Parameswara Rao
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Singh, Sanjay Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Singh, Sanjay
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Trans resveratrol loaded DSPE PEG 2000 coated liposomes: An evidence for prolonged systemic circulation and passive brain targeting2016Ingår i: Journal of Drug Delivery Science and Technology, ISSN 1773-2247, Vol. 33, s. 125-135Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Trans resveratrol (RSV) is a natural molecule proved for cardioprotective effects, vasodilation, anti-inflammatory, cancer preventive and therapeutic activities devoid of any potential side effects. Recently, anti cancer potential against glioma cells were also reported with proven molecular mechanisms. However, the therapeutic application of RSV in clinical disease management is restricted because of its rapid elimination from systemic circulation and thereby low biological half life in mammals. Therefore, the main objective of this study was to improve the systemic circulation and biological half life of RSV using DSPE PEG 2000 decorated (PEGylated) liposomes. Moreover, brain distribution of RSV loaded PEGylated liposomes (RSV-PEG-Lipo) and non-PEGylated liposomes (RSV-Lipo) was also evaluated for proving their passive brain targeting ability. In vitro drug release of both liposomes was found to be sustained up to 48 h. RSV-PEG-Lipo showed higher area under the curve, plasma half life and mean residence time and lower volume of distribution and clearance than that of pristine RSV solution and RSV-Lipo. Pharmaokinetics results clearly indicated that the RSV-PEG-Lipo will be promising tool for enhancing plasma half life and prolong the systemic circulation of RSV. Brain distribution studies revealed that the liposomal formulations can be applied as an effective tool for passive brain targeting useful in the treatment of glioma.

  • 22.
    Vijayakumar, Mahalingam Rajamanickam
    et al.
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Kumari, Lakshmi
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Patel, Krishna Kumar
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Vuddanda, Parameswara Rao
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Vajanthri, Kiran Yellappa
    School of Biomedical Engineering, Indian Institute of Technology (Banaras Hindu University).
    Mahto, Sanjeev Kumar
    School of Biomedical Engineering, Indian Institute of Technology (Banaras Hindu University).
    Singh, Sanjay
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Intravenous administration of trans-resveratrol-loaded TPGS-coated solid lipid nanoparticles for prolonged systemic circulation, passive brain targeting and improved in vitro cytotoxicity against C6 glioma cell lines2016Ingår i: RSC Advances, ISSN 2046-2069, E-ISSN 2046-2069, Vol. 6, nr 55, s. 50336-50348Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    trans-Resveratrol (RSV), a natural molecule isolated from red wine, is widely known for several therapeutic potentials. RSV is proved for cardioprotective, vasodilation, anti-inflammatory, and anticancer effects. Recently, anticancer potential against glioma cells has also been reported. However, the clinical application of RSV in glioma treatment is largely limited because of its rapid metabolism and elimination from systemic circulation thereby exhibiting low biological half-life and poor brain distribution as well. Therefore, the main objective of this study was to enhance the circulation time, biological half-life and passive brain targeting of RSV using D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS)-coated solid lipid nanoparticles (RSV-TPGS-SLN). RSV-TPGS-SLN formulations were prepared by a solvent emulsification evaporation method and evaluated for several nanoparticulate characteristics. In vitro anticancer potential and cellular internalization of nanoparticles were also investigated in C6 glioma cell lines. Pharmacokinetics and biodistribution studies were carried out following intravenous administration in healthy Charles Foster rats. RSV-TPGS-SLN showed significantly higher in vitro cytotoxicity against C6 glioma cell lines and excellent cellular internalization. RSV-TPGS-SLN showed 11.12 and 9.37 times higher area under the curve and plasma half-life than RSV solution, respectively. Moreover, brain distribution of RSV-TPGS-SLN was found to be 9.23 times higher in comparison to that of RSV alone. Thus, we anticipate that the RSV-TPGS-SLN formulation can be applied as a potential tool for improving circulation time, biological half-life and passive brain targeting of RSV, thereby being immensely useful in the treatment of glioma.

  • 23.
    Vuddanda, Parameswara Rao
    et al.
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap. Department of Pharmaceutics, UCL School of Pharmacy, University College London, London, United Kingdom.
    Alomari, Mustafa
    Department of Pharmaceutics, UCL School of Pharmacy, University College London.
    Dodoo, Cornelius C.
    Department of Pharmaceutics, UCL School of Pharmacy, University College London.
    Trenfield, Sarah J.
    Department of Pharmaceutics, UCL School of Pharmacy, University College London.
    Velaga, Sitaram
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Basit, Abdul W.
    Department of Pharmaceutics, UCL School of Pharmacy, University College London.
    Gaisford, Simon
    Department of Pharmaceutics, UCL School of Pharmacy, University College London.
    Personalisation of warfarin therapy using thermal ink-jet printing2018Ingår i: European Journal of Pharmaceutical Sciences, ISSN 0928-0987, E-ISSN 1879-0720, Vol. 117, s. 80-87Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Warfarin is a widely used anticoagulant that is critical in reducing patient morbidity and mortality associated with thromboembolic disorders. However, its narrow therapeutic index and large inter-individual variability can lead to complex dosage regimes. Formulating warfarin as an orodispersible film (ODF) using thermal ink-jet (TIJ) printing could enable personalisation of therapy to simplify administration. Commercial TIJ printers are currently unsuitable for printing the milligram dosages, typically required for warfarin therapy. As such, this study aimed to modify a commercial TIJ printing system to formulate personalised warfarin ODFs containing therapeutic dosages. A TIJ printer was modified successfully with the printer functionality intact; the substrate (paper) rolling mechanism of the printer was replaced by printing onto a stationary stage. Free film substrates were composed of hydroxypropyl methylcellulose (20%w/w) and glycerol (3%w/w). The resulting ODFs were characterised for morphology, disintegration, solid-state properties and drug content. Printed film stability was assessed at 40 °C/75% relative humidity for 30 days. Therapeutic warfarin doses (1.25 and 2.5 mg) were successfully printed onto the film substrates. Excellent linearity was observed between the theoretical and measured dose by changing the warfarin feed concentration (R2 = 0.9999) and length of the print objective, i.e. the Y-value, (R2 = 0.9998). Rapid disintegration of the ODFs was achieved. As such, this study successfully formulated personalised warfarin ODFs using a modified TIJ printer, widening the range of applications for TIJ printing to formulate narrow therapeutic index drugs.

  • 24.
    Vuddanda, Parameswara Rao
    et al.
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Mathew, Aji P.
    Luleå tekniska universitet, Institutionen för teknikvetenskap och matematik, Materialvetenskap.
    Velaga, Sitaram
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Electrospun nanofiber Mats for ultrafast release of ondansetron2016Ingår i: Reactive & functional polymers, ISSN 1381-5148, E-ISSN 1873-166X, Vol. 99, s. 65-72Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Nanofiber mats or films are promising platforms that can offer unique opportunities in oromucosoal drug delivery. However, the conventional film forming technologies are unable to produce mats with unique internal microstructure and properties. Thus, the present study was aimed to develop electrospun nanofiber mats of a model drug -ondansetron hydrochloride (OND) for ultrafast drug release. Polyvinyl alcohol (PVA), a water soluble synthetic polymer was used in the preparation of nanofiber mats and casting film. The OND nanofiber mats and conventional films were prepared by electrospinning and casting methods, respectively. Different electrospinning process variables (feed rate, electric voltage and tip to collector distance) were investigated. Nanofiber mats and casted films were characterized using Scanning electron microscopy (SEM), Atomic force microscopy (AFM), Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), and Attenuated total reflection – Fourier transform infrared spectroscopy (ATR-FTIR). The folding endurance, drug content, wetting behaviour and disintegration properties and in-vitro drug release studies were also performed.The SEM and AFM had revealed that the nanofiber mats were formed with smooth uniform texture. Solid state studies indicated that the OND was in amorphous state and uniformly dispersed in PVA mats and a film. The electrospun nanofiber mat and casted film of OND showed sufficient mechanical properties. Wet sponge method suggested that OND nanofiber mats were simultaneously wetted and disintegrated within 10 s, which is ultrafast compared to casted films. The total amount of OND was released in 90 s (1.5 min) and 1800 s (30 min) from OND-PVA electrospun nanofiber mats and casted film, respectively. OND nanofiber mats can be promising alternatives to existing solid dosage forms for ultrafast release of drugs.

  • 25.
    Vuddanda, Parameswara Rao
    et al.
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Velaga, Sitaram
    Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
    Singh, Sanjay
    Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
    Boswellic acid: medicinal use of an ancient herbal remedy2016Ingår i: Journal of Herbal Medicine, ISSN 2210-8033, Vol. 6, nr 4, s. 163-170Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Boswellic acid (BA) is an ancient herbal drug prescribed in the Indian traditional medicine systems (Ayurveda) for treatment of coughs, colds, hoarseness, bronchitis, asthma, dyspnea and diarrhea. Current research suggests it also has therapeutic potential in modern medical practice. Therefore, it is of interest to the research community to consolidate the preclinical and clinical findings on BA. The aim of this review was to comprehensively cover the plant sources, phytochemistry and physicochemical properties of BA along with its medicinal properties, safety, toxicity, and regulatory status. The review also discussed the challenges associated with drug delivery and some feasible approaches for addressing these. Four electronic databases (Scifinder, Unbound Medline, PubMed and Science Direct) and two internet search engines (Scirus and Google Scholar) were extensively searched without any time constraint.The many studies discussed in the review indicated therapeutic potential for BA in the treatment of a range of chronic diseases including arthritis, cancer, asthma and diabetes. It is hoped that this review will help researchers identify relevant research questions leading to the development of effective formulations and a better understanding of the safety of BA, with the aim of promoting it as a mainstream treatment for various diseases in clinical practice. 

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