Purpose

The purpose of this study was to develop fluconazole microsponges loaded bioadhesive film, rolled into a torpedo-shaped capsule, to achieve ease of application and reduce application frequency for the treatment of vulvovaginal candidiasis. This was accomplished by using biodegradable polymer blend specifically designed to cater the busy lifestyle of working women.

Methods

Microsponges were prepared using the quasi-emulsion solvent diffusion method. Herein, fluconazole: ethyl cellulose (1:2.5, 1:3, 1:3.5) and polyvinyl alcohol (used as the external phase) were dissolved in dichloromethane (12.5, 15, 17.5 ml). Three-level, two-factor full-factorial design optimized the above process. Next, the developed microsponges were thoroughly evaluated for entrapment efficiency, drug release and antimicrobial study. Lastly, film was developed which was made up of blend of bioadhesive polymers, namely pectin and xanthan gum. Subsequently, film was rolled into a torpedo-shaped capsule shell.

Results

The spherical-shaped porous microsponges exhibited a notable entrapment efficiency (94.17%), size 14.68 μm and rapid drug release of 91.1 ± 1.54% within 10 h. Further, bioadhesive film revealed thickness 92 μm, folding endurance 440, moisture content 5.66 ± 0.51% w/w, and good tensile strength to withstand vaginal pressure and remarkable zone of inhibition against Candida albicans (19.1 mm).

Conclusion

Fluconazole microsponges loaded bioadhesive film, rolled into a torpedo-shaped capsule, exhibited an excellent aesthetic appearance. Moreover, strong bioadhesivity ensured a high efficacy in combating disease.

中文翻译：

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氟康唑微海绵负载生物粘附阴道膜治疗外阴阴道念珠菌病

目的

本研究的目的是开发装载氟康唑微海绵的生物粘附膜，卷成鱼雷形胶囊，以实现使用方便并减少治疗外阴阴道念珠菌病的使用频率。这是通过使用专门为满足职业女性忙碌的生活方式而设计的可生物降解聚合物混合物来实现的。

方法

采用准乳液溶剂扩散法制备微海绵。在此，将氟康唑:乙基纤维素(1:2.5、1:3、1:3.5)和聚乙烯醇(用作外相)溶解在二氯甲烷(12.5、15、17.5ml)中。三水平、二因素全因子设计优化了上述过程。接下来，对开发的微海绵的包封效率、药物释放和抗菌研究进行了彻底评估。最后，开发了由生物粘附聚合物（即果胶和黄原胶）混合物制成的薄膜。随后，将薄膜卷成鱼雷形胶囊壳。

结果

球形多孔微海绵表现出显着的包封率（94.17％），尺寸为14.68μm，10小时内药物快速释放为91.1±1.54％。此外，生物粘附膜的厚度为92μm，耐折度为440，水分含量为5.66±0.51％w/w，具有良好的拉伸强度以承受阴道压力和显着的白色念珠菌抑制区（19.1mm）。

结论

氟康唑微海绵负载生物粘附膜，卷成鱼雷形胶囊，表现出优异的美观外观。此外，强大的生物粘附性确保了对抗疾病的高效能。