Amer Reham I, El-Osaily Ghada H, Gad Sameh S
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
Department of Pharmaceutics, October University for Modern Sciences and Arts, Giza, Egypt.
J Adv Pharm Technol Res. 2020 Jan-Mar;11(1):13-19. doi: 10.4103/japtr.JAPTR_85_19.
Terbinafine hydrochloride (THCl) has a broad-spectrum antifungal activity. THCl has oral bioavailability 40%, which increases dosing frequency of the drug, thus leads to some systemic side effects. Sustained release THCl nanosponges hydrogel was fabricated to deliver the drug topically. Pure THCl (drug), polyvinyl alcohol (emulsifier), and ethyl cellulose (EC, polymer to produce nanosponges) were used. THCl nanosponges were produced successfully by the emulsion solvent evaporation method. Based on a 3 full factorial design, different THCl: EC ratios and stirring rates were used as independent variables. The optimized formula selected based on the particle size and entrapment efficiency % (EE) was formulated as topical hydrogel. All formulations were found in the nanosize range except Fand F. EE was ranged from 33.05% to 90.10%. THCl nanosponges hydrogel released more than 90% of drug after 8 h and showed the highest skin deposition and antifungal activity. The increase in drug: EC ratio was observed to increase EE and the particle size while higher stirring rate resulted in finer emulsion globules and significant reduction in EE. The drug release profile was slow from dosage form when it was incorporated in entrapped form as nanosponges rather than unentrapped one. The nanosponges hydrogel succeeded to sustain THCl release over 8 h. It showed the highest antifungal activity and skin deposition. THCl nanosponges hydrogel represents an enhanced therapeutic approach for the topical treatment of fungal infection.
盐酸特比萘芬（THCl）具有广谱抗真菌活性。THCl的口服生物利用度为40%，这增加了药物的给药频率，从而导致一些全身副作用。制备了盐酸特比萘芬缓释纳米海绵水凝胶用于局部给药。使用了纯THCl（药物）、聚乙烯醇（乳化剂）和乙基纤维素（EC，用于制备纳米海绵的聚合物）。通过乳液溶剂蒸发法成功制备了THCl纳米海绵。基于三因素全因子设计，将不同的THCl:EC比例和搅拌速率用作自变量。根据粒径和包封率（EE）选择的优化配方被制成局部水凝胶。除F和F外，所有制剂均在纳米尺寸范围内。EE范围为33.05%至90.10%。THCl纳米海绵水凝胶在8小时后释放了超过90%的药物，并表现出最高的皮肤沉积和抗真菌活性。观察到药物:EC比例的增加会提高EE和粒径，而较高的搅拌速率会导致乳液小球更细，EE显著降低。当药物以纳米海绵包封形式而非未包封形式掺入剂型时，药物释放曲线较慢。纳米海绵水凝胶成功地使THCl释放持续超过8小时。它表现出最高的抗真菌活性和皮肤沉积。THCl纳米海绵水凝胶代表了一种用于真菌感染局部治疗的增强治疗方法。
