克洛特里马在水溶液中的增强溶解性和生物可用性与疏水性高分支多聚甘油醇,以改善抗真菌活性
Daria Jaworska-Krych1, Monika Gosecka1, Mateusz Gosecki1
1Centre of Molecular and Macromolecular Studies, Polish Academy of Sciences, Sienkiewicza 112, 90-363 Lodz, Poland.
ACS applied materials & interfaces
|April 5, 2024
概括
使用高分支多糖醇 (HbPGL) 的新水性配方改善了用于治疗 vulvovaginal candidiasis 的 clotrimazole 输送. 这些结构化液体增强了药物的溶解性,透性和抗真菌活性,提供了一个有前途的治疗选择.
科学领域:
- 聚合物化学 聚合物化学
- 药品制造 药品制造 药品制造
- 药物运输 药物运输 药物运输
背景情况:
- 克洛特里马的水溶性较差限制了其在治疗 vulvovaginal candidiasis 的疗效.
- 传统的配方,比如 suppositories 遭受不受控制的药物释放.
研究的目的:
- 开发使用双胞胎高分支多糖醇 (HbPGL) 结构的克洛特里马新型水性配方.
- 为了提高克洛特里马的溶解性,透性和抗真菌活性,用于妇科应用.
主要方法:
- 合成基改性HbPGL聚合物与疏水核的合成.
- 通过溶剂蒸发,然后添加水来封装克洛特里马.
- 使用FTIR和DSC进行表征;评估质性,透性 (弗朗兹扩散细胞) 和抗真菌活性.
主要成果:
- 阿里尔-HbPGL构造物形成了非牛顿结构流体与封装的克洛特里马.
- 富含双的HbPGL促进了分子分布和透明配方.
- 与对照组相比,配方显示克洛特里马的透性显著增加 (5-50倍).
- 增强和持续的抗真菌活性对抗Candida物种长达7天.
结论:
- 基于二基改性HbPGL的水性注射性克洛特里马配方提供了更好的治疗潜力.
- 开发的结构化液体克服了传统的克洛特利马输送系统的局限性.
- 这种方法证明了提高水溶性较差药物的输送的可行策略.
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