title: Nanostructured lipid carriers (NLC) based topical gel of flurbiprofen: design, characterization and in vivo evaluation.
abstract: Nanostructured lipid carriers (NLC)-based gel was developed as potential topical system for flurbiprofen (FP) topical delivery. The characterizations of the prepared semisolid formulation for topical application on skin were assessed by means of particle size distribution, zeta potential analysis, X-ray analysis, in vitro percutaneous penetration, rheological study, skin irritation test, in vivo pharmacodynamic evaluation and in vivo pharmacokinetic study. The NLC remained within the colloidal range and it was uniformly dispersed after suitably gelled by carbopol preparation. It was indicated in vitro permeation studies through rat skin that FP-NLC-gel had a more pronounced permeation profile compared with that of FP-loaded common gel. Pseudoplastic flows with thixotropy were obtained for all NLC-gels after storage at three different temperatures. No oedema and erythema were observed after administration of FP-NLC-gel on the rabbit skin, and the ovalbumin induced rat paw edema could be inhibited by the gel. The maximum concentration in plasma was 29.44 μg/ml and 2.49 μg/ml after oral and topical administration, respectively. While the amount of drug accumulated in skin after topical application was much higher than oral application. In conclusion, NLC-based gel could be a promising vehicle for topical delivery of FP.
authors.affiliation: School of Pharmaceutics, Pharmaceutical University of Shenyang, Shenyang 110016, People's Republic of China.
authors.forename: Fei
authors.initials: F
authors.lastname: Han
authors.forename: Ran
authors.initials: R
authors.lastname: Yin
authors.forename: Xin
authors.initials: X
authors.lastname: Che
authors.forename: Jing
authors.initials: J
authors.lastname: Yuan
authors.forename: Yanan
authors.initials: Y
authors.lastname: Cui
authors.forename: He
authors.initials: H
authors.lastname: Yin
authors.forename: Sanming
authors.initials: S
authors.lastname: Li
mesh_terms: D000287:Administration, Topical; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005227:Fatty Acids / Q000737:chemistry; D005480:Flurbiprofen / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D005782:Gels; D066298:In Vitro Techniques; D008297:Male; D049329:Nanostructures / Q000008:administration & dosage* / Q000737:chemistry; D010047:Ovalbumin; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000033:anatomy & histology / Q000187:drug effects / Q000378:metabolism; D012869:Skin Absorption; D023422:Skin Irritancy Tests; D013501:Surface-Active Agents / Q000737:chemistry; D014280:Triglycerides / Q000737:chemistry
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D005227:Fatty Acids; D005782:Gels; D013501:Surface-Active Agents; D014280:Triglycerides; C086409:glyceryl behenate; C022834:miglyol 812; D005480:Flurbiprofen; D010047:Ovalbumin