Transdermal delivery of flurbiprofen: permeation enhancement, design, pharmacokinetic, and pharmacodynamic studies in albino rats.

摘要

The enhancing effects of lemon oil on the transdermal penetration of flurbiprofen through rat skin invitro and in vivo was investigated. The maximum flux achieved by Isopropyl alcohol (IPA):Propylene glycol (PG) (70:30% v/v) solvent mixture was further increased by lemon oil. The flux of flurbiprofen through ethylene vinyl acetate microporous membrane was evaluated. The membrane altered the flux of flurbiprofen significantly. The reservoir type of transdermal patch was fabricated using flurbiprofen viscous system, ethylene vinyl acetate membrane, and backing film. Histological investigations were done on rat skin samples treated with solvent systems with or without penetration enhancer for 24 hr. No skin irritation was seen. Lemon oil produced more pronounced change in stratum corneum and the epidermis as compared with the control groups. The pharmacokinetics of flurbiprofen in albino rats following application of a transdermal patch for 24 hr was evaluated. The maximum plasma concentration (C(max)) and AUC(0-alpha) of the patch formulation was 1.7 and 1.6 times, increased respectively as compared with the control patch formulation. Quantity of the drug accumulated in the excised skin to which test patch formulation was applied was more than the one to which control patch formulation was applied. Anti-inflammatory effect in the Carrageenin-induced paw edema in rat was significantly higher than the control patch formulation.