Change search
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • harvard1
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf
Intranasal delivery of asenapine loaded nanostructured lipid carriers: formulation, characterization, pharmacokinetic and behavioural assessment
Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
Pharma Research, Lupin Limited (Research Park), Pune.
Luleå University of Technology, Department of Health Sciences, Medical Science.ORCID iD: 0000-0003-2645-5719
Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, Varanas.
Show others and affiliations
2016 (English)In: RSC Advances, ISSN 2046-2069, E-ISSN 2046-2069, Vol. 6, no 3, p. 2032-2045Article in journal (Refereed) Published
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

Place, publisher, year, edition, pages
2016. Vol. 6, no 3, p. 2032-2045
National Category
Other Health Sciences
Research subject
Health Science
Identifiers
URN: urn:nbn:se:ltu:diva-12569DOI: 10.1039/c5ra19793gISI: 000368191100043Scopus ID: 2-s2.0-84954116864Local ID: bbb87ad8-420c-47b4-83b9-e2aa02bed3ccOAI: oai:DiVA.org:ltu-12569DiVA, id: diva2:985520
Note
Validerad; 2016; Nivå 2; 20160205 (andbra)Available from: 2016-09-29 Created: 2016-09-29 Last updated: 2018-07-10Bibliographically approved

Open Access in DiVA

No full text in DiVA

Other links

Publisher's full textScopus

Authority records BETA

Vuddanda, Parameswara RaoVelaga, SitaramSingh, Sanjay

Search in DiVA

By author/editor
Vuddanda, Parameswara RaoVelaga, SitaramSingh, Sanjay
By organisation
Medical Science
In the same journal
RSC Advances
Other Health Sciences

Search outside of DiVA

GoogleGoogle Scholar

doi
urn-nbn

Altmetric score

doi
urn-nbn
Total: 218 hits
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • harvard1
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf