Mucoadhesive nanoliposomal formulation for vaginal delivery of an antifungal

Abstract

Context: Ciclopirox olamine (CPO) is indicated in the treatment of vaginal fungal infections. The frequent and large dosing of available vaginal CPO creams gives rise to poor compliance amongst females. In such a situation a delivery system capable of providing sustained release of CPO is warranted and can be realized through incorporation of its liposomal formulation into a mucoadhesive gel base. The liposomal formulation would offer sustained release whereas mucoadhesive gel would prolong the contact with vaginal wall; thus avoiding frequent and large dosing.

Objective: The present study aimed at investigating mucoadhesive liposomal CPO gel for vaginal use.

Method: The study embarked on evaluating liposomal CPO and its Carbopol 974^®P gel for stability at vaginal pH, release profile, rheological characteristics, mucoadhesive behavior and finally antifungal activity.

Results: The results revealed that CPO liposomes were stable at vaginal pH; its Carbopol gel released 58.75 ± 6.4% of CPO at the end of 24 h which suggested sustained release. Rheology via viscometric, oscillatory stress sweep and oscillatory frequency sweep testing of the gel, studied at different temperatures and under different dilutions with vaginal fluid simulant testified pseudoplastic behavior of the gel. It also pointed towards the predominance of elastic behavior of the gel at all the dilutions. The gel exhibited good mucoadhesivity to sheep vaginal tissue. Furthermore, CPO entrapped in liposome too displayed antifungal activity.

Conclusion: The study undertaken recommended Carbopol 974^®P gel loaded with CPO liposomes as a potential delivery system for treatment of fungal vaginal infections.

Keywords::

• Ciclopirox olamine
• liposome
• vulvovaginal candidiasis
• rheology
• mucoadhesion
• elastic