Effect of the chemical structure on the drug release from brinzolamide based nano eye-drops
Effect of the chemical structure on the drug release from brinzolamide based nano eye-drops
复制标题
化学结构对布林佐胺纳米滴眼液药物释放的影响
DOI：
10.1080/15421406.2020.1743447
复制
发表时间：
2020
影响因子：
0.7
通讯作者：
Kasai Hitoshi
中科院分区：
文献类型：
--
作者：
Koseki Yoshitaka;Ikuta Yoshikazu;Sato Kota;Aoyagi Shigenobu;Inada Satoshi;Onodera Tsunenobu;Oikawa Hidetoshi;Nishiguchi Koji M.;Nakazawa Toru;Kasai Hitoshi
由于角膜位于眼睛表面，具有阻挡异物进入的屏障功能，因此市售的眼药水几乎无法渗入眼睛。为了提高滴眼剂的渗透率，我们提出了纳米尺寸的滴眼剂，称为“纳米滴眼剂”。合成了一系列由青光眼治疗剂布林佐胺衍生的三甲基锁（TML）基团的前药化合物，并通过再沉淀法成功制备了所得前药的纳米滴眼剂。我们发现纳米滴眼剂的药物释放很大程度上取决于包含纳米滴眼剂的前药的化学结构。因此，通过改变布林佐胺前药的化学结构来控制降眼压作用的时间。这些结果为有效控制释放的药物设计提供了见解。
Commercially available eye-drops scarcely penetrate the eye because of the cornea, which is located at the surface of the eye and function of barrier to keep out foreign matter. To enhance the penetration ratio of eye-drop, we have proposed nanometer-sized eye-drops called “nano eye-drops.” A series of prodrug compounds derived from brinzolamide, a glaucoma therapeutic agent, connected with a trimethyl lock (TML) group were synthesized and the nano eye-drops of the resulting prodrugs were successfully fabricated by the reprecipitation method. We found that the drug release of nano eye-drops critically depended on the chemical structure of the prodrugs comprising the nano eye-drops. As a result, the timing of the ocular hypotensive effect was controlled by altering the chemical structure of brinzolamide prodrug. These results provide insight into drug design for effective controlled release.