有效的药物加载方法,通过被动扩散将水溶性较差的药物加载到双体中
Yuta Arai1,2, Yasunori Iwao3, Yoshio Muguruma4
1Analytical Development, Pharmaceutical Sciences, Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
Molecular pharmaceutics
|October 12, 2023
概括
一种新的被动扩散方法简化了将药物加载到双细胞,一种固体脂质纳米粒子. 这种方法提高了药物封装效率,为早期药物开发提供了有价值的工具.
科学领域:
- 纳米技术 纳米技术
- 药物运输 药物运输 药物运输
- 材料科学 材料科学 材料科学
背景情况:
- 双体是固体脂质纳米粒子,能够溶解水溶性较差的药物.
- 传统的双药物加载方法复杂且耗时,涉及热循环或联合研磨.
- 对双胞胎来说,需要更简单,更有效的药物加载技术.
研究的目的:
- 开发一种简单的,被动的药物加载方法,用于使用扩散的双细胞.
- 为了研究聚乙烯糖醇 (PEG) 链长度对药物加载到双细胞中的影响.
- 评估负载因子对基托可纳 (KTZ) 封装成双细胞的效率的影响.
主要方法:
- 在透析装置内,在和基托可纳 (KTZ) 溶液中化了没有药物的双细胞.
- 双制备有或没有不同长度的聚乙烯糖醇 (PEG) 链 (PEG2K和PEG5K).
- 随着时间的推移,分析了形态变化,封装速度和度.
主要成果:
- 被动扩散成功地将KTZ装入裸双细胞中,封装度取决于脂质度.
- 双细胞的PEGylation减轻了形态变化和改善了封装率.
- 与PEG2K双胞胎相比,PEG5K双胞胎显示出最大的形态变化预防,但24小时后封装度较低,表明被动负荷的最佳PEG长度.
- 温度和车辆的选择影响了KTZ封装速度.
结论:
- 已经开发出一种简单的被动扩散方法,用于将药物装入双细胞中.
- 基化可以提高双胞胎的药物载荷能力和效率,确定了最佳的PEG链长度.
- 这种高吞吐量,资源最小的方法对早期药物开发有希望.
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