Effect of Surface Chemistry of Polymeric Nanoparticles on Cutaneous Penetration of Cholecalciferol

Publication date: Available online 11 October 2018Source: International Journal of PharmaceuticsAuthor(s): Augustine Lalloz, Marie-Alexandrine Bolzinger, Jimmy Faivre, Pierre-Luc Latreille, Araceli Garcia Ac, Cyrielle Rakotovao, Jean-Michel Rabanel, Patrice Hildgen, Xavier Banquy, Stéphanie BriançonAbstractWe investigated the influence of nanoparticle (NP) surface composition on different aspects of skin delivery of a lipophilic drug: chemical stability, release and skin penetration. Cholecalciferol was chosen as a labile model drug. Poly(lactic acid) (PLA)-based NPs without surface coating, with a non-ionic poly(ethylene glycol) (PEG) coating, or with a zwitterionic poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC) coating were prepared using flash nanoprecipitation. Process was optimized to obtain similar hydrodynamic diameters. Polymeric NPs were compared to non-polymeric cholecalciferol formulations. Cholecalciferol stability in aqueous medium was improved by polymeric encapsulation with a valuable effect of a hydrophilic coating. However, the in vitro release of the drug was found independent of the presence of any polymer, as for the drug penetration in an intact skin model. Such tendency was not observed in impaired skin since, when stratum corneum was removed, we found that a neutral hydrophilic coating around NPs reduced drug penetration compared to pure drug NPs and bare PLA NPs. The nature of the hydrophilic block (PEG or PMPC) had however no impact. We hypot...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research