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Dermal Formulation Incorporating Isoconazole Nitrate Nanoparticles Offers High Absorption into Skin and Antimicrobial
Ayako Harada1, Rie Tanaka2, Hiroko Otake2
1ROHTO Pharmaceutical Co., Ltd., 1-8-1 Tatsuminishi, Ikuno-ku, Osaka 544-8666, Japan.
Pharmaceutics
|December 31, 2025
Summary
This study developed an isoconazole nitrate nanoparticle (ISN-NP) gel for enhanced topical delivery. The nanogel formulation significantly improved antifungal activity and transdermal permeation compared to microparticle gels.
Area of Science:
- Pharmaceutical Sciences
- Dermatology
- Mycology
Background:
- Isoconazole nitrate (ISN) is an antifungal agent targeting ergosterol synthesis.
- Improving ISN skin retention and permeability can enhance therapeutic efficacy for candidiasis.
- Nanoparticle formulation aims to optimize ISN topical delivery.
Purpose of the Study:
- To develop and evaluate an isoconazole nitrate nanoparticle (ISN-NP) gel for improved topical delivery.
- To assess the antifungal activity and skin permeation of the ISN-NP gel.
- To compare the performance of ISN-NP gel with microparticle-based gels.
Main Methods:
- Isoconazole nitrate nanoparticles (ISN-NPs) were prepared using wet-bead milling with methylcellulose.
- ISN-NPs were incorporated into a Carbopol hydrogel.
- High-performance liquid chromatography (HPLC) measured ISN concentration.
- In vivo studies used Wistar rats for skin absorption and *Candida albicans* for antifungal activity.
Main Results:
- The ISN-NP gel showed stable nanoparticles with a size distribution of 60-220 nm.
- ISN-NP gel demonstrated superior antifungal activity against *Candida albicans*.
- Compared to ISN-MP gels, ISN-NP gel exhibited 1.54-fold enhanced drug release and 1.7-fold increased transdermal permeation.
Conclusions:
- Incorporating ISN nanoparticles into a Carbopol gel is a promising strategy for enhancing topical delivery of poorly water-soluble ISN.
- The nanogel system offers a valuable platform for transdermal delivery in clinical applications.
- This formulation improves the therapeutic efficacy of isoconazole nitrate for topical antifungal treatment.

