一种潜在的共晶策略,以量身定制体外溶解,并提高caco-2的透性和berberine的口服生物可用性
Hui Chen1, Jiangpo Ma2, Feng Zhou1
1Laboratory of Advanced Theranostic Materials and Technology, Ningbo Institute of Materials Technology and Engineering, Chinese Academy of Sciences, Ningbo 315201, PR China; Ningbo Cixi Institute of Biomedical Engineering, Cixi 315300, PR China.
International journal of pharmaceutics
|October 4, 2024
概括
一种新的柏柏林化物 (BER) 和洛诺西卡姆晶 (BLCC) 显著提高了口服吸收和生物可用性. 这种协同晶体策略提供了一种有前途的方法,用于改善透性较差的化合物的药物输送.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 柏柏林化 (BER) 具有治疗潜力,但由于肠道透性较低,其口服吸收和生物利用性较差.
- 制定提高BER口服输送的策略对于其临床应用至关重要.
研究的目的:
- 开发一种柏柏林化和洛诺西卡姆共晶体 (BLCC),以改善柏柏的口服吸收和生物可用性.
- 描述开发的共晶体的物理化学性质,并评估其体外和体内性能.
主要方法:
- 使用溶剂蒸发方法形成晶.
- 通过X射线衍射,差异扫描热度计和热重度计分析进行表征.
- 在各种pH条件下进行体外溶解研究和Caco-2细胞透性测试.
- 在体内相对生物利用性的评估.
主要成果:
- BLCC表现出改进的溶解配置,在酸性条件下立即释放,在中性条件下持续释放.
- 与BER (8.82 × 10−7 cm/s) 相比,BLCC显著提高了Caco-2细胞的透率 (50.30 × 10−7 cm/s).
- 与BER相比,BLCC显示出了显著的410%的相对生物利用率,这归因于肠道透性和溶解能力的提高.
结论:
- 开发的BLCC有效地改善了柏柏林化的溶解行为,肠道透性和口服生物可用性.
- 晶形成是一种可行的策略,可以增强缺乏透性的活性药物成分的输送.
- BLCC具有显著的潜力,可以提高BER在治疗各种疾病中的疗效.
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