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Published on: February 14, 2018
Optimizing a Natural Oil-Based Sertaconazole Nitrate Organogel: enhanced antifungal activity through in vitro and in
Piyush Jain1, Shashikant Chandrakar1, Pushpa Prasad Gupta2
1Department of Pharmacy, Columbia Institute of Pharmacy, Raipur, India.
Objectives:
This study aimed to develop and optimize a topical organogel formulation of Sertaconazole nitrate (SN) using Cinnamon oil (CO) to enhance antifungal activity and improve dermal drug delivery.
Methods:
A 33 Box-Behnken design (BBD) was used to optimize the formulation by varying three factors- Cinnamon oil, Carbopol-934 (CP), and Polyethylene glycol-400 (PEG) at three levels. Key responses measured were viscosity (VS), spreadability (SP), and drug content (DC). The formulations underwent physicochemical evaluations including homogeneity, pH, swelling index, moisture content, and extrudability.
Results:
The organogels had a skin-friendly pH ranging from 6.11 to 6.99, VS between 0.39 and 0.49 Pa.s, and SP from 20.40 to 26.45 g.cm/s-1. DC was consistently high (91.66% to 99.33%). The optimized batch (C11) showed excellent in vitro and ex vivo drug release (97.98% and 86.14%, respectively). Zeta potential of -24.60 mV indicated good physical stability. Drug deposition studies confirmed efficient skin penetration, with 85.45% retained in skin layers. Antifungal tests demonstrated strong activity against Candida albicans and Trichophyton rubrum, outperforming plain organogels and marketed formulations. Skin irritation and histopathology studies confirmed the formulation's safety for topical use.
Conclusion:
The optimized Sertaconazole nitrate organogel (SNO) with CO is a stable, safe, and effective topical delivery system that enhances drug penetration and antifungal efficacy, making it a promising option for dermal antifungal therapy.
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