开发和优化一种自我微乳化药物输送系统 (SMEDDS),用于同时使用索拉费尼布和黄素
Xingzhen Huang1,2, Lizhen Feng3, Xuefang Lu4
1School of Pharmacy, Guangxi Medical University, Nanning, Guangxi, 530000, PR China. huangxingzhen@gxmu.edu.cn.
Drug delivery and translational research
|August 29, 2024
概括
一种新型的自我微乳化药物输送系统 (SMEDDS) 能够同时输送黄素和索拉芬尼,显著提高抗瘤功效. 这种配方可改善肝细胞癌治疗的药物溶解性和口服生物可用性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术纳米技术
背景情况:
- 肝细胞癌 (HCC) 治疗面临着药物溶解性和生物可用性方面的挑战.
- 黄素和索拉费尼布是潜在的抗癌药物,其发射能力有限.
- 需要新的药物输送系统来提高这些化合物的疗效.
研究的目的:
- 开发和描述一种自我微乳化药物输送系统 (SMEDDS),用于同时使用黄素和索拉芬尼布.
- 评估结合SMEDDS的体外抗瘤疗效和药物释放概况.
- 评估同时服用药物的体外药理动力学改善,特别是口服生物可用性.
主要方法:
- 索拉费尼布-库尔库明自微乳化药物输送系统 (SOR-CUR-SMEDDS) 的配方,采用响应表面方法来优化.
- 试验室表征包括颗粒大小,多分散率指数 (PDI) 和泽塔潜力 (ZP).
- 在体外对HepG2细胞的抗瘤活性评估,药物释放研究和药物动力学分析.
主要成果:
- SOR-CUR-SMEDDS表现出最优的纳米乳液特性 (13.48 nm大小,0.228 PDI,-12.4 mV ZP). 在这种情况下,SOR-CUR-SMEDDS具有最佳的纳米乳液特性.
- 该组合显示显著降低了对HepG2细胞的IC50值 (曲素为3倍,索拉芬尼为5倍).
- 实验室研究显示,黄素释放量增强 (79.20%),口服索拉费尼布 (1239.88倍) 和黄素 (3.64倍) 的生物可用性大幅增加.
结论:
- 开发的SOR-CUR-SMEDDS有效地提高了黄素和sorafenib的可溶性和抗瘤功效.
- 这种新的配方显著提高了这两种药物的口服生物可用性.
- SMEDDS代表了一种有前途的策略,用于提高结合性肝细胞癌治疗的治疗潜力.
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