Formulation, Development and Characterization of PLGA-Luliconazole Nanoparticles Loaded Gel System for Topical Fungal Treatment

Abstract:

Background: Fungal infections are the primary cause of skin diseases. Topical application of antifungal drugs is the most preferred treatment which is associated with key limitations viz. need for high doses and frequency of application. By considering the limitations of current topical treatment, the present study involves the formulation and characterization of luliconazole nanogel. Materials and Methods: The luliconazole nanoparticles were prepared by using biodegradable polymer PLGA 50:50 and dispersed in polymeric dispersion prepared by Carbopol 940 and HPMC K4M. For optimization of nanoparticles as well as their polymeric dispersion a factor-three level (32 ) design was implemented. Optimized nanoparticles were characterized for various parameters viz. particle size, PDI, entrapment efficiency, XRD, SEM, whereas the nanogel was investigated for viscosity, cumulative drug release, spreadability, extrudability, skin irritation test, and antifungal activity. Results: The nine batches of nanoparticles as well as nanogel were prepared. Nanoparticles prepared by using 100 mg PLGA at 6 HPH cycles showed size, PDI, and % entrapment as 406 nm and 87% respectively was the desired batch. The XRD and SEM study ensured the encapsulation of drug with satisfactory surface morphology. Nano-gel formulated with 0.3% Carbopol and 1.0% HPMC was selected as optimized; it showed viscosity and % cumulative drug release as 3650 cP and 54% respectively. Nanogel showed significant sustained luliconazole release (54.12%) in comparison to simple nanoparticles (65.22%). The formulation showed improved antifungal activity than standard treatment without any skin irritation signs. Conclusion: Prepared nano-gel is a promising alternative to the current treatment.

Keywords: Nanoparticles, Nano-gel, Optimization, Antifungal, Skin test.