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在空气/水界面的单层中,阿昔洛韦及其鲨烯酰-阿昔洛韦前药与 DMPC 的相互作用。

Interaction of acyclovir and its squalenoyl-acyclovir prodrug with DMPC in monolayers at the air/water interface.

机构信息

Dipartimento di Scienze Chimiche, Università degli Studi di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

出版信息

Int J Pharm. 2010 Aug 16;395(1-2):167-73. doi: 10.1016/j.ijpharm.2010.05.035.

DOI:10.1016/j.ijpharm.2010.05.035
PMID:20635474
Abstract

Acyclovir has been conjugated to the acyclic isoprenoid chain of squalene to form the squalenoyl-acyclovir prodrug. Its interaction with biomembrane models constituted by dimyristoylphosphatidylcholine (DMPC) monolayers has been studied by employing the Langmuir-Blodgett technique. The aim of the work was to gain information on the interaction of these compounds with phospholipid membranes. DMPC/acyclovir or squalenoyl-acyclovir prodrug mixed monolayers have been prepared at increasing molar fractions of the compound and the isotherm mean molecular area/surface pressure has been registered at 10 and 37 degrees C. Results reveal that the squalenoyl moiety enhances the affinity of acyclovir for the biomembrane model.

摘要

阿昔洛韦已与鲨烯的无环异戊二烯链缀合形成鲨烯酰基阿昔洛韦前药。通过Langmuir-Blodgett 技术研究了它与由二肉豆蔻酰磷脂酰胆碱(DMPC)单层组成的生物膜模型的相互作用。这项工作的目的是获取有关这些化合物与磷脂膜相互作用的信息。已在增加化合物的摩尔分数的情况下制备了 DMPC/阿昔洛韦或鲨烯酰基阿昔洛韦前药混合单层,并且在 10 和 37 摄氏度下记录了等温平均分子面积/表面压力。结果表明,鲨烯酰部分增强了阿昔洛韦对生物膜模型的亲和力。

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