Traditional
azole antifungal formulations suffer from poor retention in the vaginal cavity, irritation and burning of the vaginal area. In the present work, we aim at the development of a novel
miconazole (MCZ) microsponges gel as an attractive
dosage form for vaginal
candidiasis. The proposed formula has the potential to minimize the local side effects of the
drug due to the controlled release characteristic, which increases patient compliance. Moreover, the mucosal retention effect of the microsponges in addition to the bioadhesion property of
Carbopol gel prolongs the retention of the
dosage form in the vagina and consequently improves the therapeutic efficiency. MCZ microsponges were prepared applying Quasi
emulsion method using
Eudragit RS100. The effect of formulation factors, namely,
drug:
polymer ratio (1:1, 2:1 and 4:1), the amount of poly vinyl alcohol (PVA) (25, 50 and 75mg) and the volume of organic
solvent (2.5, 5, 10mL) on the characteristics of MCZ microsponges has been investigated. The microsponges were optimized regarding the production yield (68.8±6.4%), particle size (78.2±2.1μm), entrapment efficiency (92.9±1.9%) and release rate (Q150 51.8±2.5%). The selected formula was further evaluated for its, flowability, porosity and surface morphology. MCZ microsponges were incorporated into
Carbopol gel, then the viscosity and bioadhesion were examined. The in vitro antifungal activity of MCZ microsponges gel was comparable to the market product. In vivo, MCZ microsponges
vaginal gel was more effective than the market product (p<0.05) in eradicating
Candida infection in rats, which was supported by the histopathological findings.