Lignin is a product of the secondary metabolism of plants that arise from phenylalanine through the phenylpropanoid pathway. The resulting structure of lignin is strongly dependent on its origin and the isolation process. In general, it is a complex and biodegradable polymer with antimicrobial properties, antioxidant effects,and low cytotoxicity. As a result of these properties, lignin has high potentials for valorisation, which could alsofind application in medicine. The application of lignin in the form of nanoparticles, for example, as a drug delivery system, is currently being considered. To enable their use in niche applications, their preparation and characterization ought to be developed and optimized. Here, we discuss the essentials for the successful application of these systems in the production of value-added products.