Formulation and in vitro evaluation of coconut oil-core cationic nanocapsules intended for vaginal delivery of clotrimazole

The objective of this work was to propose coconut oil-core nanocapsules prepared from Eudragit (R) RS100, a cationic polymer, and to evaluate their potential for vaginal delivery of clotrimazole in candidiasis. Nanocapsule suspensions loaded with clotrimazole at 1.0 and 3.0 mg/mL were prepared by interfacial deposition of Eudragit (R) RS100. The physicochemical characterization showed average diameter lower than 200 nm, low polydispersity index, positive zeta potential (+10.94 to +14.57 mV), acid pH values (5.4-5.7) and encapsulation efficiencies close to 100%. After 60 days of storage at room temperature and protected from light, the nanocapsules were reasonably stable. Photodegradation studies showed that nanoencapsulation improved clotrimazole stability against UV radiation. The in vitro drug release at pH 4.5 was characterized by a prolonged release with no burst effect. The nanocapsules were more active than free clotrimazole against Candida albicans and Candida glabrata strains susceptible and resistant to fluconazole. Hence, clotrimazole-loaded coconut oil-core nanocapsules represent promising alternatives to the treatment of vulvovaginal candidiasis. (C) 2014 Elsevier B.V. All rights reserved.