Development and Characterization of Liposomal Vaginal Gel Loaded With Spironolactone For The Treatment of PCOS/PCOD

Abstract

Oral spironolactone is mainly used in the treatment of polycystic ovarian disease (PCOD) but it has concerns high first pass metabolism and systemic side effects. The current study optimized a localized liposomal vaginal gel of spironolactone for sustained release and reduced systemic exposure. Liposomes were formulated by ether injection method and optimized by using 32 factorial designs (soya phosphatidylcholine: cholesterol ratios). Liposomes were converted into a gel matrix by using gelling agent like Carbopol 934P. The optimized liposomes (L2) showed vesicle size, zeta potential and entrapment efficiency of 198.7 nm, -30.1 mV and 91.75%, respectively. The final vaginal gel (G8) showed a high drug content (95.22%), excellent spreadability and shows zero-order sustained release (93.34% in 24h). The formulation was found to be physically and chemically stable for 3 months as per standard ICH conditions (30°C/65% RH). This novel localized delivery system provides the targeted anti-androgenic therapy and a safer and more effective way for the management of PCOD.