Assembly of poly[N-(2-hydroxypropyl)methacrylamide] having cholesteryl moiety as terminal groups
Assembly of poly[N-(2-hydroxypropyl)methacrylamide] having cholesteryl moiety as terminal groups
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具有胆固醇基部分作为端基的聚[N-(2-羟丙基)甲基丙烯酰胺]的组装
DOI：
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发表时间：
2000
期刊：
影响因子：
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通讯作者：
Minoru Sugiyama
中科院分区：
文献类型：
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作者：
K. Sugiyama;R. Hanamura;Minoru Sugiyama
聚[N-在聚合物末端具有一个侧链胆固醇基部分和在两个聚合物末端具有两个侧链胆固醇基部分作为端基的（2-羟丙基）甲基丙烯酰胺（PHPMA）（PHPMA-2Chol和PHPMA-2Chol）通过N-甲基吡咯烷酮的自由基聚合来制备。（2-羟丙基）甲基丙烯酰胺用4引发，4′-偶氮双-[（3-胆固醇基）4-氰基戊酸酯]分别在2-巯基乙醇和硫代胆固醇作为链转移试剂的存在下进行。通过荧光光谱和核磁共振氢谱分析了PHPMAs的自组织性。临界胶束浓度（CMC）随着PHPMA聚合度的降低而降低。PHPMA-Chol的CMC比PHPMA-2Chol大得多。PHPMA-2Chol存在时，凝血酶与合成底物S-2238的酶促反应的米氏常数测定表明，PHPMA具有良好的血液相容性。根据小角X射线散射测量，PHPMA-2Chol可以将胆固醇分子作为亲脂性药物模型保持在由PHPMA-2Chol中位于末端的胆固醇基形成的疏水层中。© 2000 John Wiley & Sons，Inc.聚合物科学杂志A：聚合物化学38：3369-3377，2000
Poly[N-(2-hydroxypropyl)methacrylamide]s (PHPMAs) with one pendant cholesteryl moiety at the polymer end and two pendant cholesteryl moieties at both polymer ends as terminal groups (PHPMA-Chol and PHPMA-2Chol) were prepared by the radical polymerization of N-(2-hydroxypropyl)methacrylamide initiated with 4,4′-azobis-[(3-cholesteryl) 4-cyanopentanoate] in the presence of 2-mercaptoethanol and thiocholesterol as chain-transfer reagents, respectively. The self-organization of the PHPMAs was analyzed by fluorescence and 1H NMR measurements. The critical micelle concentration (CMC) decreases with a decreasing PHPMA degree of polymerization. The CMC of PHPMA-Chol is much larger than that of PHPMA-2Chol. PHPMA exhibits an excellent blood compatibility, as determined from the Michaelis constant for the enzymatic reaction of thrombin and a synthetic substrate, S-2238, in the presence of PHPMA-2Chol. According to a small-angle X-ray scattering measurement, PHPMA-2Chol can hold the cholesterol molecule as a lipophilic drug model in a hydrophobic layer formed by terminal-located cholesteryl groups in PHPMA-2Chol. © 2000 John Wiley & Sons, Inc. J Polym Sci A: Polym Chem 38: 3369–3377, 2000