两种使用不同固化技术的自纳米乳化药物输送系统的比较,以提高水溶性较差的赛莱科西布的可溶性和口服生物利用性
Mi Ran Woo1, Sanghyun Woo1, Young-Woo Bak1
1College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea.
Colloids and surfaces. B, Biointerfaces
|July 4, 2024
概括
一种新型的固体自纳米乳化颗粒系统 (S-SNEGS) 显著提高了赛莱可克西布的溶解性和口服生物利用性. 与固体自纳米乳化药物输送系统 (S-SNEDDS) 和赛莱可西布粉相比,该系统提供了优越的性能.
科学领域:
- 制药技术 制药技术 制药技术
- 药物输送系统 药物输送系统
- 纳米技术纳米技术
背景情况:
- 塞莱科克西布是一种非类固醇抗炎药物,具有较差的水溶性,限制了其口服生物利用性.
- 开发先进的药物输送系统对于提高难溶性药物的治疗疗效至关重要.
研究的目的:
- 开发和比较两个新的固体自纳米乳化系统:固体自纳米乳化药物输送系统 (S-SNEDDS) 和固体自纳米乳化颗粒系统 (S-SNEGS).
- 为了提高塞莱科西布的可溶性,溶解率和口服生物可用性.
- 评估开发系统的物理化学和流量特性.
主要方法:
- 使用Captex,Tween 80和TPGS制备液体自纳米乳化药物输送系统 (L-SNEDDS).
- 通过喷雾干燥将L-SNEDDS固化为S-SNEDDS,通过流体床颗粒化进行S-SNEGS.
- 在老鼠中对溶解性,溶解性,物理化学性质,流动性和体内口服生物利用性的比较分析.
主要成果:
- 与S-SNEDDS和赛莱可西布粉相比,S-SNEGS显示了显著改善的溶解性和溶解率.
- 无论是S-SNEDDS还是S-SNEGS,都能将晶体的赛莱科克西布转化为无形的形式.
- 与S-SNEDDS相比,S-SNEGS表现出优越的流量特性 (减少静止角度,压缩性指数和豪斯纳比率).
- 在老鼠中,S-SNEGS增加了口服生物利用率 (AUC),比S-SNEDDS增加了1.3倍,比塞莱科克西布粉增加了4.5倍.
结论:
- S-SNEGS是一种高效的固体自纳米乳化系统,用于增强口服输送水溶性较差的赛莱科克西布.
- S-SNEGS的卓越表现突显了其作为一个有前途的药物交付平台的潜力.
- 流体床颗粒化为开发S-SNEGS提供了优势,比喷雾干燥的S-SNEDDS具有更好的特性.
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