OPTIMIZATION AND CHARACTERIZATION OF NOVEL VESICULAR CARRIER SYSTEM FOR TOPICAL DELIVERY OF SOME NSAIDs

Abstract

newline The present research was focused to optimize naproxen sodium vesicular carriers incorporated in newlinetransdermal gel formulation. Box Behnken experimental design was utilized for optimization using newlinedifferent variables. Three vesicular formulations were investigated as drug carriers niosomes, newlinetransfersomes and transethosomes. The prepared formulations were evaluated for drug entrapment newlineefficiency, vesicle size and zeta potential for finding out a optimized formula through point newlineprediction method. newlineAll the excipients selected were found to be compatible with the drug based on the results of drug newlineexcipient compatibility studies. The % drug entrapment, particle size and zeta potential of optimized newlineniosomal formulation were 74.23 %, 105.11 nm and -34 mv for transfersomes 80.11 newline%, 114.91 nm and -37 mv and for transethosomes 86.97 %, 102.91 nm and -35 mv respectively newline, which were significantly in agreement by predicted responses through point prediction method. newlineThe rheological properties of all optimized gel formulations were found acceptable for ease of newlineapplication. Drug release from transethosomal gel formulation shows highest 82% release in 24 newlinehours while transfersomal, niosomal and marketed gel formulation shows 79 % 72% and 67.65 newlinerespectively. The Ex Vivo Permeation Studies shows highest Permeation flux of newline28.36 ± 0.98 and#956;g/cm 2 /h for transethosome formulation. In addition, Skin irritation test in rats newlineconfirmed that the formulations are safe for skin application and are non irritant in nature. The newlinetransethosomal gel formulation showed highly significant inhibition (pandlt;0.001) in paw edema newlinevolume at all time points in comparison with the control group. The difference was found significant newlineat 4 h after carageenan administration, when maximum inhibition of paw volume (87.02 %) was newlinerecorded. Stability tests indicated that the vesicular formulations were stable over three months. newlineTherefore, among the various vesicular formulations examined in the research study ultra- newlinedeformable transethosmal gel formulation co