Nanosponge Fortified Ciclopirox-Olamine for Antifungal Efficacy with Improved Topical Delivery.

Abstract

Background: Topical drug delivery systems are most promising in the management of fungal skin infections; however, they often face challenges to achieve therapeutic efficacy due to low solubility, particle size, molecular weight, and skin barriers. In this regard, nanosponge [NS] offers a novel solution with its three-dimensional porous networks, enhancing drug solubility, bioavailability, and providing prolonged release.

Objective: The aim of this study was to develop NS fortified with Ciclopirox olamine [CPO] with enhanced drug solubility, prolonged targeted delivery, and improved therapeutic efficacy for the management of fungal skin infections.

Method: CPO-loaded ethyl cellulose and polyvinyl alcohol NS were synthesized using the emulsion solvent technique and subsequently evaluated for particle size, surface morphology through scanning electron microscopy [SEM], polydispersity index [PDI], zeta potential [ZP], entrapment efficiency [EE %], drug loading [DL %], drug-excipient interactions via differential scanning calorimetry, and in vitro dissolution studies. Furthermore, the antifungal test was conducted to assess the inhibitory effect on fungal growth.

Results: The optimized formulation using ethyl cellulose and polyvinyl alcohol at 1.75 mg and 2 mg, respectively, emerged as the most effective, with a particle size of 526.1 nm and PDI of 0.332, indicating a uniform distribution. Moreover, the formulation demonstrated a high drug loading efficiency and sustained drug release over a 7 h period, achieving a drug release of 77.83 %. The pH of the gel formulations ranged from 5.35 to 7.40, the viscosity ranged from 3759 to 4710 cps, and the spreadability was adequate for topical application. Additionally, the optimized NS exhibited superior antifungal activity against Candida albicans and Aspergillus Niger, compared to drug alone and commercial fungicidal creams. Moreover, the in vitro studies confirmed the gel's effectiveness and its ability to sustain drug release, following Higuchi kinetics.

Conclusion: The formulated CPO-loaded NS gels exhibit enhanced solubility, stability, and sustained drug release, significantly improving topical drug delivery with exceptional therapeutic efficacy. This novel approach underscores the potential of NSs for efficient and targeted medication delivery in both the pharmaceutical and cosmetic industries. Furthermore, their effective preparation method, excellent physicochemical properties, and antifungal activity make NSs a promising strategy for the oral delivery of poorly soluble drugs. The fungal skin infections are generally not serious but can be uncomfortable and persistent. With proper hygiene and appropriate treatment, most infections can be effectively managed. Therefore, understanding the types of fungi involved and recognizing symptoms early with an effective delivery system can lead to quicker recovery and reoccurrences. The development of CPOloaded NS represents a promising advancement in topical antifungal therapy. By improving drug delivery and efficacy, this innovative formulation could significantly enhance treatment outcomes for patients suffering from fungal infections. Further, clinical studies will be essential to validate these findings and explore potential applications in broader dermatological contexts.