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.

Keywords::

• Topical delivery
• Elastic vesicles
• Ketoconazole
• skin
• edge activator

Acknowledgements

Fluorescence micrroscopy studies were carried out at Central Scientific Instruments Organisation (CSIO), Chandigarh, India. We acknowledge the contribution of Dr Shashi Bhushan, Indian Institute of Integrative Medicine (IIIM), Jammu, India for his help in the conduct of cytotoxicity assays.

Declaration of interest

The authors declare no conflict of interest.