Studies on nonionic surfactant bilayer vesicles of ciclopirox olamine

Abstract

Context: Niosomal delivery can prove an alternative to improve the poor skin penetration and residence of the topical antifungal drugs that account for the long treatment regimes in cutaneous mycosis. Objective: To investigate niosomes as carriers for dermal delivery of ciclopirox olamine (CPO), a broad spectrum antifungal drug. Materials and methods: Niosomes were prepared by ethanol injection method using Span 60, cholesterol, diacetyl phosphate according to 3² factorial design and evaluated for physicochemical parameters, in vitro and ex vivo deposition in skin and stability study. Results: Unilamellar CPO niosomes of size 170–280 nm, entrapment efficiency 38–68%, and sufficient electrokinetic stability were obtained. Percent drug deposition in artificial membrane varied from 12.75 to 92.74. Deposition of CPO into rat skin from niosomal dispersion and its gel was significantly higher than that of plain CPO solution and its marketed product. Obtained niosomes possessed sufficient stability on storage. Discussion: Increasing amounts of Span 60 and cholesterol increase the vesicle size probably because of entrapment of CPO-ionized molecules in the aqueous compartment and interaction of its unionized counterpart with the bilayer constituents leading to increase in bilayer thickness. Consequently, the percent entrapment efficiency also increased. However, increasing Span 60 levels decreased the in vitro percent drug deposition. This might be attributed to the larger size of vesicles produced by high amounts of surfactant that showed poor deposition. The optimized batch possessed sufficient stability. Conclusions: The results of this investigation suggest that niosomes are promising tools for cutaneous retention of CPO.

Keywords:

• Antifungal
• cholesterol
• cutaneous deposition
• ethanol injection
• niosomes
• Span 60
• topical
• unilamellar

Acknowledgments

The authors thank Cipla Ltd., Mumbai, for supplying gift sample of CPO. The authors are highly grateful to Dr. B.L.V. Prasad, National Chemical Laboratory, Pune, for providing fluorescence spectrophotometer for use. K.S. Shaikh is thankful to All India Council for Technical Education for financial assistance in the form of National Doctoral Fellowship.