Development Of Intravaginal Liposomal Gel Of Clomiphene Citrate For Treatment Of Polycystic Ovary Syndrome

Abstract

Polycystic ovary syndrome is one of the most common hormonal disorders among women of newlinereproductive age presenting with infertility. Due to its complex pathogenesis and newlineunrecognized etiology, there is no effective preventive measure available for PCOS until now. newlineThe present study was to design and evaluate an intra-vaginal site-specific, liposomal gel newlinecontaining clomiphene citrate, which can be targeted to the uterus (vagina) and timedependent newlinemanner, to modulate the drug level in PCOS. Liposomes were prepared with LS75 newlineas phospholipid, Chloroform as the solvent, both Phospholipid and cholesterol in a ratio of newline0.02:0.01 at 600C temperature. Prepared liposomes were showed 80.303±0.199% drug newlineentrapment efficiency. Liposomes were optimized using 3 level factorial designs which newlinepredicted the response 79.699%, whereas observed response was found 80.121% with newlinepercentage error 0.299. Intravaginal gel was prepared with different concentrations of newlinecarbopol 934 and chitosan. Based on evaluation results CCG-3 formulation considered as best newlineformulation which shows pH 4.231±0.002, drug content 97.500±0.454%, viscosity newline8777±1.527cp, spreadability 7.1±0.033cm, gel strength 5.42±0.389gm mm-1 sec-1 and newlinecumulative drug release 76.991± 0.404%. Drug kinetic study shows and verified the sustained newlinerelease mechanism of the formulation. The gel was found stable as per stability studies newlineprotocol. IN VIVO study clearly showed that Clomiphene citrate intravaginal liposomal gel newlineformulation recovered or balanced the reproductive hormonal level and its secondary newlineassociated diseases after seven days of treatment in PCOS Wistar female rats. Thus from the newlinepresent study, it can be concluded that intravaginal liposomal gel of Clomiphene citrate has a newlinebeneficial action on hormonal activity level and potential to selectively improve PCOS and its newlinesecondary associated complications, like hypertension, diabetes, and dyslipidemia. newline