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Effect of the chemical structure on the drug release from brinzolamide based nano eye-drops
Molecular Crystals and Liquid Crystals ( IF 0.7 ) Pub Date : 2020-07-23 , DOI: 10.1080/15421406.2020.1743447
Yoshitaka Koseki 1 , Yoshikazu Ikuta 1 , Kota Sato 2, 3 , Shigenobu Aoyagi 4 , Satoshi Inada 4 , Tsunenobu Onodera 1 , Hidetoshi Oikawa 1 , Koji M. Nishiguchi 2, 5 , Toru Nakazawa 2, 3, 5, 6 , Hitoshi Kasai 1
Affiliation  

Abstract 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.

中文翻译:

化学结构对布林佐胺基纳米滴眼液药物释放的影响

摘要 由于角膜位于眼睛表面,具有阻挡异物的屏障功能,市售的眼药水几乎不能穿透眼睛。为了提高滴眼液的渗透率,我们提出了一种称为“纳米滴眼液”的纳米级滴眼液。合成了一系列源自青光眼治疗剂布林佐胺的前药化合物,并与三甲基锁(TML)基团相连,并通过再沉淀法成功制备了所得前药的纳米滴眼剂。我们发现纳米滴眼液的药物释放严重依赖于包含纳米滴眼液的前药的化学结构。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。
更新日期:2020-07-23
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