Chitosan-coated liposomes for topical vaginal therapy: Assuring localized drug effect

Abstract

The choice of drug therapy in pregnant patients suffering from vaginal infections is limited by the safety profile of the drug. Assuring the efficient topical therapy to avoid systemic absorption is considered the best therapy option. Chitosan-coated liposomes have been developed and optimized to assure localized therapy of clotrimazole. Chitosan was selected as mucoadhesive polymer both to prolong system's retention at the vaginal site and act on biofilms responsible for high recurrence of infections. Sonicated liposomes were coated with chitosan in three different concentrations, namely 0.1, 0.3 and 0.6% (w/v). Clotrimazole-containing (22 μg/mg lipid) chitosan-coated liposomes were in the size range of 100–200 nm. The <i>in vitro</i> release studies confirmed prolonged release of clotrimazole from both non-coated and chitosan-coated liposomes as compared to control. The <i>ex vivo</i> penetration experiments performed on the pregnant sheep vaginal tissue showed that coated liposomes assured increased clotrimazole tissue retention and reduced its penetration as compared to the control. Mucin studies revealed that the coating with lower chitosan concentration increased the system's mucoadhesive potential, as compared to coating with higher concentrations. These results provide a good platform for further <i>in vivo</i> animal studies on mucoadhesive liposomes destined to localized vaginal therapy.