Carbohydrate polymers · 2025
Fabrication of sodium alginate-hydroxypropyl methylcellulose based bioadhesive eutectogel of Eberconazole for improved anti-fungal activity.
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Chachad Jay, Dey Shidhanto, Sherje Atul, Dangre Pankaj, Borkar Maheshkumar R
Аннотация
The present study focuses on the development of a bioadhesive eutectogel (BAEgel) incorporating deep eutectic solvents (DESs) to enhance the solubility of Eberconazole (EBER), a poorly water-soluble yet highly permeable Biopharmaceutics Classification System (BCS) Class II antifungal drug. Among the various DESs evaluated, the combination of choline chloride (ChCl) and propylene glycol (PG) in a 1:2 M ratio, DES (plain) demonstrated the highest solubility for EBER, achieving 63.75 ± 3.3 mg/mL, which represents a significant enhancement. This DES-EBER system was subsequently incorporated into several BAEgel formulations prepared using various polymers such as carbopol, sodium alginate, and hydroxypropyl methylcellulose K15 (HPMC k15). Among these, the BAEgel-F5 formulation batch, comprising 2.25 % sodium alginate and 0.5 % HPMC K15, was selected based on its optimal performance. BAEgel-F5 exhibited favorable physicochemical properties, including suitable viscosity, pH, spreadability, and good drug content. In vitro drug release studies revealed a sustained release profile over 12 h, with 93.85 ± 2.81 % drug release, which was significantly higher compared to the pure drug that showed only 32.21 ± 2.46 % release. Antifungal activity studies further demonstrated that BAEgel-F5, despite containing only half the EBER concentration (0.5 %) of the marketed formulation (1 %), achieved comparable antifungal efficacy. The accelerated stability studies also revealed excellent chemical and physical stability of BAEgel-F5 formulation. Overall, this study highlights the potential of BAEgel as an effective topical delivery platform for antifungal drugs, offering improved therapeutic efficacy with lower drug concentration.