Studies on statistically optimized binary ethosomal gel encapsulated with Carvedilol: Ex-vivo permeation and Pharmacodynamic assessment in male Wistar albino rats

Abstract

The current study entails novel advanced formulation approach binary ethosomal gel containing Carvedilol and evaluating the optimized formulation for hypertension. Carvedilol is an antihypertensive agent, which undergoes hepatic metabolism and shows poor bioavailability of just 20 %. Carvedilol binary ethosomal suspension was optimized using central composite design (CCD). In which quantities of lipid (A), ethanol (b), and propylene glycol (C) were selected independent variables; vesicle size (Y1), entrapment efficiency (Y2) and cumulative %drug release (Y3) were selected as dependent variables. The composition of optimum formulation was found as 2 % of lipid (Soya lecithin), 20 % of ethanol, and 10 % of propylene glycol. The optimized binary ethosomal suspension (OBE) had shown a vesicle size, poly dispersable index, ztapotential, cumulative % drug release, and %entrapment efficiency of 130±1.72nm, 0.230±0.03,-31±1.8MV, 97.89±3.7 %, and 99±2.96 % respectively. This was further evaluated and compared with liposomes. Scanning electron microscopy studies revealed that OBE was in spherical shape. The OBE was converted to hydrogel and evaluated for rheological properties. The OBE-Gel (OBE-G) attained mean transdermal flux of 0.0644±0.002 mg/cm 2 .h through rat skin. This formulation showed a substantial and constant decrease SciForum in blood pressure, for up to 24 h. The OBE-G was found to be effective, with reduction in blood pressure by virtue of better permeation through rat skin. In conclusion, OBE-G accentuate the transdermal flux and the results obtained encouraged its use for hypertension treatment.