title: Nanostructured lipid carriers-based flurbiprofen gel after topical administration: acute skin irritation, pharmacodynamics, and percutaneous absorption mechanism.
abstract: In order to assess the preliminary safety and effectiveness of nanostructured lipid carriers-based flurbiprofen gel (FP NLC-gel), the acute irritation test, in vivo pharmacodynamics evaluation and pharmacokinetic study were investigated after topical application. No dropsy and erythema were observed after continuous dosing 7 d of FP NLC-gel on the rabbit skin, and the xylene-induced ear drossy could be inhibited by FP NLC-gel at different dosages. The maximum concentration of FP in rats muscle was 2.03 μg/g and 1.55 μg/g after oral and topical administration, respectively. While the peak concentration in untreated muscle after topical administration was only 0.37 μg/mL. And at any time, following topical administration the mean muscle-plasma concentration ratio Cmuscle/CPlasma was obviously higher than that following oral administration. Results indicated that FP could directly penetrate into the subcutaneous muscle tissue from the administration site. Thus, the developed FP NLC-gel could be a safe and effective vehicle for topical delivery of FP.
authors.affiliation: a College of Pharmacy , Shenyang Pharmaceutical University , Shenyang , PR China and.
authors.forename: Aihua
authors.initials: A
authors.lastname: Song
authors.forename: Zhen
authors.initials: Z
authors.lastname: Su
authors.forename: Sanming
authors.initials: S
authors.lastname: Li
authors.forename: Fei
authors.initials: F
authors.lastname: Han
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D005480:Flurbiprofen / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D005782:Gels; D008055:Lipids / Q000737:chemistry*; D008297:Male; D051379:Mice; D049329:Nanostructures; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption; D023422:Skin Irritancy Tests; D014018:Tissue Distribution
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D005782:Gels; D008055:Lipids; D005480:Flurbiprofen
keywords: Acute irritation; flurbiprofen; nanostructured lipid carriers; percutaneous absorption mechanism; pharmacodynamics evaluation