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可巴胺修饰的胆固醇-氨酸合物:合成和生物活性

Natallia V Dubashynskaya¹, Anton N Bokatyi¹, Tatiana S Sall²

¹Institute of Macromolecular Compounds of the Russian Academy of Sciences, Bolshoi VO 31, St. Petersburg 199004, Russia.

International journal of molecular sciences

|July 29, 2023

概括

新的维生素B12修饰的氨酸合物增强了胆固醇的输送. 这些系统改善了肠道吸收并降低了毒性,提供了一个有前途的口服抗生素选择.

科学领域:

* 制药科学制药科学
* 聚合物化学的研究.
* 药物交付服务 * 药物交付服务

背景情况:

*聚合物系统可以提高抗生素的生物可用性,控制释放,减少毒性.
* 提高肠道透性对于口服抗菌剂,如胆素 (CT) 至关重要.

研究的目的:

* 开发和描述维生素B12修饰的氨酸-胆固醇合物 (HA-CT-B12) 以改善口服输送.
* 评估新联体的药物释放,抗菌活性,毒性和肠道透性.

主要方法:

* 合成和表征HA-CT-B12合物,包括B12和CT含量,粒子大小和z电位.
*在不同pH值 (7.4和5.2) 的体外释放研究.
*评估HEK 293细胞中的抗菌活性 (最小抑制度) 和毒性.
* 用表面透率来测量肠道透率.

主要成果:

*HA-CT-B12结合物含有95微克/毫克维生素B12和335微克/毫克CT,颗粒大小为98和702纳米.
* 超缓慢的胆固醇释放 (10小时后<1%) 在pH值7.4和5.2.2时观察到.
*结合剂保留了抗菌活性 (MIC 2μg/mL),并将CT毒性降低了30-40%.
*显著改善肠道透率 (3.5 × 10−6 cm/s),表明50-100%的体内吸收.

结论:

* 维生素B12修饰的HA-CT合物显示出作为口服药物递送系统的优秀潜力.
* 这些结合物提供了增强的生物制药性质,包括改善对胆固醇素的吸收和降低毒性.

关键词:

科里斯 (Colistin) 是一个古老的城市.亚诺科巴胺是什么意思氨酸是什么? 氨酸是什么?肠道的通透性肠道的通透性口服药物输送是通过口服药物进行的.聚合物合物是一种聚合物.

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