Abstract

FORMULATION, OPTIMIZATION AND COMPARATIVE EVALUATION OF ESTRADIOL CO-CRYSTAL LOADED VAGINAL GEL FOR POST MENOPAUSAL SYMPTOMS

Ajanya K.*, Dr. Geetha V. S. and Shahana Shoukath

ABSTRACT

The aim of the study was to formulate estradiol co-crystal loadedvaginal gel to improve drug’s solubility and bioavailability for thetreatment of postmenopausal symptoms. The estradiol co-crystals wereformulated using urea as a coformer with the aid of solventevaporation technique. The co-crystal formulation was optimized by 2level 2 factor central composite design with 13 runs using DesignExpert®13 software trial version to maximize the solubility andminimize the particle size. The co-crystals showed a 5-fold increase insolubility as compared to pure drug. The co-crystals were incorporatedto vaginal gel base with Carbopol and HPMC in differentconcentrations and comparatively evaluated. The F1 formulation withcarbopol and HPMC in 1:1 ratio was found to be optimized batch withimproved drug release of 93.3±0.8% in phosphate buffer pH 5. Theinvitro drug release kinetics shows first order kinetics with non-fickiansuper case II transport. The co-crystal loaded gel was comparatively evaluated with estradioldrug loaded gel with the same gel base. The estradiol co-crystal loaded vaginal gel withimproved drug release rate can be used as an effective treatment option for postmenopausalsymptoms.

Keywords: Postmenopausal symptoms, Estradiol, Co-crystal, Solvent evaporation, Vaginal gel.