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固体自我微乳化药物输送系统 (S-SMEDDS) 通过喷雾干燥制备,以提高 cinnamaldehyde (CA) 的口服生物利用性

Yun Meng¹, Ye Cai¹, Mengyao Cui¹

¹School of Pharmacy, Anhui University of Chinese Medicine, Hefei, PR China.

Pharmaceutical development and technology

|February 3, 2024

概括

这项研究开发了一种固体的自微乳化药物输送系统 (S-SMEDDS),用于甲 (CA). 在S-SMEDDS显著增强CA显著增强CA.

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:

丁甲 (CA) 具有治疗潜力,但其口服生物可用性较差.
开发有效的口服药物输送系统对于提高CA等脂性药物的治疗疗效至关重要.

研究的目的:

用喷雾干燥方法制备甲 (CA) 的固体自我微乳化药物输送系统 (S-SMEDDS).
提高CA的口服生物利用率和体外释放.
研究通过S-SMEDDS传递的CA的细胞吸收和运输机制.

主要方法:

使用喷雾干燥技术来制备CA S-SMEDDS,使用马尔托德.
优化配方参数,包括载体比,固体含量,温度,注入速度和原子化压力.
使用差分扫描热量计 (DSC) 进行表征.
在动物模型中进行体外药物释放研究和药理动力学评估.
使用Caco-2/HT29共同培养系统研究细胞吸收和运输机制.

主要成果:

优化的CA S-SMEDDS配方成功地准备了高封装效率.
DSC的分析表明,CA被封装在S-SMEDDS中的无形形式.
在体外释放研究显示,与CA悬浮相比,CA释放的1.3倍增加.
药理动力学研究表明,从S-SMEDDS中获得CA的相对口服生物利用率增加了1.6倍.
细胞吸收主要由能量依赖性内细胞分裂 (克拉和囊泡介导) 介导.
在Caco-2/HT29细胞模型中,S-SMEDDS显著提高了CA透性.

结论:

开发的S-SMEDDS是一种有效的口服固体剂型,可提高脂类药物的口服生物可用性,如肉甲.
增强的生物利用性归因于改善的体外释放,增加的透性和高效的细胞吸收机制.
这种配方策略有望提高其他水溶性较差的药物的输送.

关键词:

在Caco-2细胞中.锡纳甲锡纳甲的HT29细胞.在S-SMEDDS中使用.吸收吸收吸收吸收

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