Development of non-invasive transdermal patch of Emblica officinalis for anti atherosclerotic activity
Keywords:
Transdermal, polymers, permeation, atherosclerosisAbstract
The present study was designed to formulate matrix type transdermal patches of a potent anti atherosclerotic botanical Emblica officinalis on a mercury substrate and evaluated for physicochemical parameters like thickness, % flatness, weight variation, moisture uptake, moisture content, folding endurance, elongation and drug content values. Further, in vivo drug release was also observed by HPLC in rabbit serum. Four formulations were prepared using different ratio of matrix forming polymers, plasticizer and penetration enhancers. Formulations E-1, E-2, E-3 and E-4 were composed of Ethyl cellulose (EC) and Hydroxypropyl Methylcellulose (HPMC) with the following ratios: 6:4, 7:3, 8:2 and 9:1. In vitro cumulative amounts of the permeated drug were observed 48.53, 55.46, 73.26 and 99.72% in 48 hrs from the four formulations. The release profile of the optimized formulation E-4; r2 = 0.984 (Higuchi) showed that permeation of the drug controlled by a diffusion mechanism. The cumulative amount of the permeated drug after 48hrs from E-4 was 343.95mcg/cm2. Permeability coefficient was calculated 7.16mcg/cm2/hr. Based on physicochemical and in vitro skin permeation studies, E-4 was chosen for further in vivo studies. Blood plasma concentration of E-4 after 48 hrs was 0.2914mcg/cm2. Skin permeation performance and scanning electron microscopic studies revealed that formulation E-4 was found to be better than other formulations and it was selected as the optimized formulation. The skin irritation tests showed negligible erythema and edema. The developed transdermal patches may increase the efficacy of E. officinalis for the therapy of atherosclerosis.
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