Abstract

Objective: Luliconazole (LZL) has low aqueous solubility that limits its dermal bioavailability and acts as a barrier to topical delivery. The conventional topical formulations have a limited ability to retain the drug over the skin for a prolonged period. The main objective of the study was to formulate and characterize LZL loaded ethyl cellulose (EC) nanoparticles and formulate them as a film-forming gel (FFG) for prolonged delivery in fungal skin infections.Methods: The solvent evaporation technique was used for the preparation of nanoparticles of LZL by using EC as a polymer. The prepared nanoparticles were evaluated for physical appearance, production yield, entrapment efficiency, drug content, particle size, zeta potential, Polydispersity index (PDI), and in vitro drug release. Then the nanoparticles were incorporated into FFG formulation by using polyvinyl pyrrolidone (PVP) and polyvinyl alcohol (PVA) as the gelling agent. The prepared FFG was evaluated for pH, Viscosity, Spreadability, in vitro drug release studies, in vitro antifungal studies, and release kinetic studies.Results: The optimized nanoparticle formulation F5 having drug to polymer ratio of 1:2 showed satisfactory production yield (86.32%), entrapment efficiency (83.36%), drug content (42.86), particle size (125.3), and 93.72% of in vitro drug release after 24 h (h). The optimized FFG formulation FFG4 showed the shortest film-forming time of 5.06 min (min), percentage Cumulative drug release of 92.18% after 24 h, and had promising in vitro antifungal activity.Conclusion: The prepared FFG could be used with promising potential for fungal infection of the skin.

Highlights

  • LZL is a topical broad-spectrum antifungal drug approved by the USFDA in November 2013

  • Zeta potential, Polydispersity index (PDI), drug content, entrapment efficiency, and in vitro drug release, nanoparticles formulation F5 was selected as an optimized batch

  • Based on the film-forming time, pH, in vitro drug release, formulation FFG4 was selected as the optimized batch

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Summary

Introduction

LZL is a topical broad-spectrum antifungal drug approved by the USFDA in November 2013. It has lower aqueous solubility that limits dermal bioavailability and acts as a barrier to topical delivery [1]. The solubility of the drug in the lipid phase of the stratum corneum acts as a rate-limiting step for permeation. The current dosage forms are associated with several limitations such as skin irritation, do not ensure persistent contact with the skin surface, and can be wiped off by the patient's clothes; repeated application is required. These leave a sticky and greasy feel after application leading to poor patient compliance [3]

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