Efficacy of Gelling Agents on the In-vitro Release and Physical Properties of Loxoprofen Sodium Gel Containing Ultra Elastic Vesicles

Abstract

Objective: Preparation of a topical prolong release gel for loxoprofen sodium using optimized nano-sized transfersome dispersion using different gelling agents with in vitro and in vivo evaluation in comparison to the marketed gel prepared by a conventional method. Method: The optimum nano transfersome dispersion containing 5% egg lecithin (as an oil phase) 1% span 60 (as an emulsifying agent) was converted into a gel using different gelling agents including carbopol 974p, carbopol 940, carbopol 934 and hydroxyl propyl methylcellulose (HPMC K100) at ratio of (1:1). Each prepared gel was then evaluated in vitro to determine the homogenisity, consistency, spreadability, viscosity, and in vitro drug release as well as skin permeation test, human skin irritation test, and in vivo effectiveness. Result: The selected gel formula (TG3) showed best homogenisity, consistency and spreadability as well as it produced initial burst release of 60.3% (within 1 hour) followed by the prolonged release of 95.4% continued for 6 hours. In addition, the optimum gel formula (TG3) has shown remarkable prolong release, which was significantly higher than the marketed gel (loxonin® gel 1%) without any sign of skin irritation with better effectiveness Conclusion: This work succeeded in preparing topical gel for loxoprofen sodium using carbopol 974p as gelling agent and utilizing ultra elastic lipid vesicles (transfersomes) with prolong release that reduces dose frequency and improves patient compliance