Formulation and development of posaconazole topical gel: impact of polymer variability on antifungal efficacy

Harshit Gautam*, Abhishek Nagar

School of Health & Allied Science, Career Point University, Kota, Rajasthan, India

Refer this article

Harshit Gautam, 2026. Formulation and development of posaconazole topical gel: impact of polymer variability on antifungal efficacy. Journal of medical pharmaceutical and allied sciences, V 15, I 3, Pages 87 – 93. Doi: https://doi.org/10.55522/jmpas.V15I3.7088.

ABSTRACT

Superficial fungal infections represent a significant global health burden, affecting approximately 40 million individuals worldwide, particularly in developing nations. Posaconazole, a potent broad-spectrum triazole antifungal agent, exhibits poor aqueous solubility (0.02 mg/mL) and limited permeability, presenting formulation challenges for topical delivery. The present investigation aimed to formulate and evaluate Posaconazole topical gels using different polymers and study the effect of polymer variation on physicochemical properties, drug release behaviour, and antifungal efficacy. Five gel formulations (F1–F5) were prepared using gelling agents such as Carbopol 934P (1% w/w), Carbopol 940 (1% w/w), HPMC K4M (2% w/w), HPMC K15M (2% w/w) and Poloxamer 407 (20% w/w). Organoleptic characterization, determination of melting point, solubility profile, FTIR spectroscopy, DSC analysis and development of a UV spectrophotometric method were carried out as preformulation studies. The formulations were evaluated for: pH, viscosity, spreadability, extrudability, drug content uniformity, in vitro drug release, release kinetics, antifungal activity and stability. Preformulation studies showed the identity and purity of Posaconazole (melting point 168-172°C) and maximum solubility in DMSO (25.76 ± 0.32 mg/mL). The drug-excipient compatibility was demonstrated by FTIR and DSC. All the formulae showed acceptable physicochemical properties. The formulation F4 (HPMC K15M) showed the best properties: pH 6.72, viscosity 34,760 cP, spreadability 24.38 g·cm/sec, extrudability 95.74% and drug content 99.58%. In-vitro drug release by Higuchi kinetics (R2 = 0.992) was found, with 12 hours cumulative release of 97.84% in F4. The formulation was confirmed to be effective against the antifungal activity of Candida albicans, Aspergillus niger and Trichophyton rubrum. No significant changes were observed in the stability studies carried out under accelerated conditions (40 ± 2°C / 75 ± 5% RH) for three months. The HPMC K15M-based posaconazole gel is a promising topical formulation with desirable physicochemical properties, sustained drug release and excellent stability for effective treatment of superficial fungal infections.

Keywords:

Posaconazole, Topical gel, Antifungal activity, Polymer variability, Drug release kinetics.

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