A novel nanovesicular carrier system to deliver drug topically

Abstract

Context: Ketoconazole, a lipophilic drug with a large molecular weight of 531.44 Da and a limiting aqueous solubility of 0.04 mg/ml is expected to show a poor transport across the skin.Objective: The work describes usefulness of a novel, surfactant based elastic vesicular drug carrier system (SEVs), for enhanced dermal delivery.Materials and methods: The system constitutes Span 60 and an edge activator (Tween 80) and was characterized and monitored for safety and potential to target deeper mice skin layers.Results: Nanosized (126 nm), elastic vesicles showed significantly high skin penetration and retention as compared to free drug suspension. Incorporation into different bases especially a hydrogel showed a significant retention which was even more than the market formulation (Nizral®). Safety was confirmed as cytotoxicity and acute dermal irritation/corrosion. Topically applied fluorescent vesicles labeled with 6-carboxyfluorescein, on mice skin, were observed intact in dermal layer 6 h post application.Conclusion: The results of the present study indicate that SEVs can be used to enhance skin delivery of the model high molecular weight and poorly water-soluble drug ketoconazole. The developed nanorange system is an effective system for targeting deeper mice skin layers which may be translated to human skin with suitable modifications, if required.