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聚(N-异丙基丙烯酰胺)共聚物的pH依赖性粘膜粘附揭示了药物递送的设计规则。

pH-dependent mucoadhesion of a poly(N-isopropylacrylamide) copolymer reveals design rules for drug delivery.

作者信息

Zhu X, Degraaf J, Winnik F M, Leckband D

机构信息

Department of Chemical and Biomolecular Engineering, University of Illinois at Urbana-Champaign, 600 South Mathews Avenue, Urbana, Illinois 61801, USA.

出版信息

Langmuir. 2004 Nov 23;20(24):10648-56. doi: 10.1021/la048363q.

Abstract

This study investigated the mucoadhesive property of a hydrophobically modified copolymer N-isopropylacryamide and glycidylacrylamide NIPAM-N-Gly-(C18)2 (NIPAM-Gly). Prior studies demonstrated that the interfacial properties of this copolymer are pH dependent and that the chains form strong hydrogen bonds at pH < 7 via the carboxylic acid side chains of the glycine moieties. Mucin interactions with the copolymer brushes were investigated by surface plasmon resonance and by direct force measurements. Mucin adsorption was determined as a function of pH, ionic strength, and mucin concentration. It adsorbs to the copolymer strongly at pH 5, but the adsorption decreases with increasing pH. The adsorbed amount is also ionic-strength dependent, decreasing with increasing monovalent salt concentrations at all pH values investigated. When compared with similar investigations with poly(ethylene oxide), these results provide insights into both the chemical characteristics and the solution conditions that determine the mucoadhesive properties of polymers.

摘要

本研究考察了疏水改性共聚物N-异丙基丙烯酰胺与N-(十八烷基)2-丙烯酰胺缩水甘油(NIPAM-N-Gly-(C18)2,简称NIPAM-Gly)的黏膜黏附特性。先前的研究表明,该共聚物的界面性质依赖于pH值,且在pH < 7时,其链段通过甘氨酸部分的羧酸侧链形成强氢键。通过表面等离子体共振和直接力测量研究了黏蛋白与共聚物刷的相互作用。测定了黏蛋白吸附量随pH值、离子强度和黏蛋白浓度的变化。在pH 5时,黏蛋白强烈吸附于共聚物,但随着pH值升高,吸附量降低。在所研究的所有pH值下,吸附量也依赖于离子强度,随着单价盐浓度增加而降低。与聚环氧乙烷的类似研究相比,这些结果为决定聚合物黏膜黏附特性的化学特性和溶液条件提供了见解。

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