Preparation and evaluation of anti-hyperlipidaemic in topical preparation and characterization using vesicular drug delivery system

Author : Heba F. Salem, Rasha M. Kharshoum, Heba A. Aboutaleb, Hanan H. Farouk

Simvastatin is an HMG CoA reductase inhibitor used for the treatment of dyslipidemia, however the drug has two major problems; short biological half‐life and extensive first pass effect. The aim of this work was to develop Simvastatin niosomal gel to prolong the residence time at the absorption site thereby increase bioavailability and avoid extensive first pass effect. Simvastatin niosomal gel were prepared by dispersing different ratios of carbopol 940, hydroxyl propyl methyl cellulose and sodium carboxy methyl cellulose (2:3: 4%) w/v into the alcoholic solution at room temperature. The 23 factorial design was used to develop Simvastatin niosomal gel, the independent factors used are polymer types (carbapol 940, HPMC H15 and Na CMC), polymer concentrations (2,3, 4% w/v) . The developed niosomal gel were characterized by clarity, pH determination, homogeneity, rheological characteristics, entrapment efficiency and In vitro diffusion studies. The results revealed that the Simvastatin noisomal gel were clear and homogenous at pH 6.8 , viscosity ranged from 1560 to1700 cn and the efficiency of entrapment ranged from 80 to 90%.It was found that the formula contains carbapol 940 and pellets of niosome which had the highest release rate and selected as optimized formula.

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