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Studies on statistically optimized binary ethosomal gel encapsulated with Carvedilol: Ex-vivo permeation and Pharmacodynamic assessment in male Wistar albino rats
* 1 , 2
1  Associate Professor, Department of Pharmaceutics, Anurag Group of Institutions, Venkatapur, Ghatkesar, Medchal, Hyderabad-500088
2  Department of Pharmaceutics, University college of Pharmaceutical Sciences (UCPSc), Kakatiya university, Vidyaranyapuri, Hanamakonda, Warangal, Telangana 506009, India.

Abstract: The current studies entail novel approaches of formulating the binary ethosomal gel containing Carvedilol and evaluating the optimized for Pharmacodynamic study through transdermal delivery. Carvedilol is an antihypertensive agent and poorly water soluble, which undergoes pre-systemic metabolism and shows lower bioavailability of 20 %. Carvedilol binary ethosomal suspension was optimized by using central composite design (CCD). In which, quantities of lipid (A), ethanol (B) and propylene glycol(PG) (C) were selected as independent variables; vesicle size (Y1), Entrapment efficiency (Y2) and cumulative % drug release (Y3) was selected as dependent variables. The composition of optimum formulation was found as 2 % of lipid (Soya lecithin), 20 % of ethanol, and 10 % of PG. The optimized binary ethosomal suspension (OBE) had shown a vesicle size, PDI, ZP, Cumulative % drug release, and % EE of 130±1.72 nm, 0.230±0.03, -31±1.8 Mv, 97.89±3.7 %, and 99±2.96 % respectively. This was further evaluated and compared with Liposomes. SEM studies revealed that OBE was in spherical shape. The OBE was further converted to the hydrogel by using Carbopol 934 (1%) and evaluated for rheological properties. The OBE- Gel (OBE-G) attained mean transdermal flux of 0.0644±0.002 mg/cm2/h through rat skin. During the antihypertensive study, the treatment group showed a substantial and constant decrease in blood pressure, for up to 24 h. The OBE-G was found to be effective, with an ameliorated reduction in blood pressure by virtue of better permeation through Wistar albino rat skin. In conclusion, the developed hydrogel containing Carvedilol OBE accentuate the transdermal flux and the results obtained encouraged its use for hypertension treatment.
Keywords: Carvedilol; Entrapment Efficiency; Central composite design; hydrogel, Wistar albino rat.