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克洛法齐明的封装使用环氧:制备,表征和体外释放特性

Seong-Jin Hong¹, Young-Min Kim¹

¹Department of Integrative Food, Bioscience and Biotechnology, Chonnam National University, Gwangju 61186, Republic of Korea.

International journal of molecular sciences

|May 27, 2023

概括

循环德克斯 (CD) 和基于循环德克斯的复合物 (CI) 显著提高了克洛法胺 (CFZ) 的溶解性和稳定性. CI-9表现出卓越的性能,为开发有效的CFZ药物输送系统提供了一个有前途的战略.

科学领域:

制药科学制药科学
药物输送系统药物输送系统
材料科学材料科学材料科学

背景情况:

像克洛法齐明 (CFZ) 这样的药物的水溶性差,限制了它们的治疗效果.
环极素 (CD) 和基于环极素的复合物 (CI) 是已知的助剂,可以提高药物溶解度.
开发稳定和有效的配方,用于难以溶解的药物仍然是制药开发的一个重大挑战.

研究的目的:

评估和比较各种循环素 (CD) 和基于循环素的复合物 (CI) 在提高克洛法胺 (CFZ) 的水溶性和稳定性方面的疗效.
为了确定 clofazimine 配方的最佳循环德克斯基复合物.
评估包容性复合体对环境压力的保护作用.

主要方法:

选各种循环素 (CDs) 和基于循环素的复合物 (CI) 进行查,以检测 clofazimine (CFZ) 的含量.
可溶性和封装效率的确定.
扫描电子显微镜 (SEM) 用于复杂的形成分析.
在体外溶解研究.
对抗环境压力的稳定性测试,包括紫外线照射.

主要成果:

CI-9表现出克洛法胺 (CFZ) 的最高药物含量百分比和溶解度.
确定CFZ:CI-9的最佳摩尔比为0.2:1,实现了高封装效率.
SEM证实了CFZ/CI和CFZ/CD纳入综合体的形成,导致迅速溶解.
与自由CFZ和CFZ/CD相比,CFZ/CI-9表现出最高的药物释放率 (高达97%) 和优越的抗UV辐射保护.
CFZ/CI复合体显示出对环境压力的增强稳定性.

结论:

CI-9是一种高效的基于循环德的复合物,可提高克洛法胺 (CFZ) 的溶解性,溶解率和稳定性.
CFZ/CI复合物代表了开发稳定和有效的克洛法胺药物产品的有希望的配方策略.
需要进一步的体内研究来评估这些新型药物输送系统的药理动力学特征和安全性.

关键词:

克洛法齐米因 (Clofazimine) 是一种类药物.循环德克斯特兰 (Cyclodextran) 是一种循环德克斯特兰.循环德克斯林 (Cyclodextrin) 是一种循环德克斯林.药物释放性质药物释放性质包容复杂的包容复杂的包容

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