title: Nanostructured lipid carriers for transdermal delivery of acid labile lansoprazole.
abstract: The aim of this study was to develop nanostructured lipid carriers (NLCs) for transdermal delivery of acid-labile lansoprazole (LPZ). The drug loading, particle size, zeta potential, thermal behavior and stability of NLCs were evaluated. The particle size of NLCs was in the range of 90-210nm and the zeta potential was -61.9 to +3.2mV dependent of the compositions. Stearylamine (SA) prevented lansoprazole degradation and maintained drug stable in NLCs. The anionic sodium dodecyl sulfate (SDS) adsorbed on the lipid surface and formed complex with cationic SA to prevent NLCs aggregation. The effects of type (e.g., isopropyl myristate (IPM), menthol) and concentration (e.g., 1.25, 2.50, 3.75%w/w) of enhancers on penetration of lansoprazole NLC hydrogels were investigated in vitro using Wistar rat skin. The steady-state flux of lansoprazole NLC hydrogel containing 3.75% IPM was the highest which was enhanced by 2.7 folds as compared to enhancer-free NLC hydrogel. In vivo pharmacokinetics of lansoprazole following transdermal delivery of NLC hydrogel showed that the elimination of drug was significantly reduced and the mean residence time of drug was prominently prolonged as compared to intravenous drug solution (p<0.005). The accumulation of drug in the skin and continuous penetration of drug through the skin accounted for the maintenance of drug concentration for at least 24h.
authors.affiliation: Graduate Institute of Pharmaceutical Sciences, School of Pharmacy, National Taiwan University, Taipei, Taiwan; Drug Research Center, College of Medicine, National Taiwan University, Taipei, Taiwan. Electronic address: wjlin@ntu.edu.tw.
authors.forename: Wen Jen
authors.initials: WJ
authors.lastname: Lin
authors.affiliation: Graduate Institute of Pharmaceutical Sciences, School of Pharmacy, National Taiwan University, Taipei, Taiwan.
authors.forename: Yi Shein
authors.initials: YS
authors.lastname: Duh
mesh_terms: D000279:Administration, Cutaneous; D000588:Amines / Q000737:chemistry; D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage; D002851:Chromatography, High Pressure Liquid; D004058:Diffusion; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D006358:Hot Temperature; D020100:Hydrogels / Q000737:chemistry; D064747:Lansoprazole / Q000008:administration & dosage*; D008055:Lipids / Q000737:chemistry; D008297:Male; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry; D013552:Swine
chemical_list: D000588:Amines; D000897:Anti-Ulcer Agents; D004337:Drug Carriers; D020100:Hydrogels; D008055:Lipids; D064747:Lansoprazole; D012967:Sodium Dodecyl Sulfate; C009317:stearylamine
keywords: Lansoprazole; Nanostructured lipid carrier; Penetration; Pharmacokinetics; Transdermal delivery