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苯丁酸氮芥从带有β-环糊精基团的聚(N-异丙基丙烯酰胺)水凝胶中的释放。

Release of chlorambucil from poly(N-isopropylacrylamide) hydrogels with beta-cyclodextrin moieties.

作者信息

Liu Yu-Yang, Fan Xiao-Dong, Hu Hui, Tang Zhong-Hua

机构信息

Department of Applied Chemistry, School of Science, Northwestern Polytechnic University, Xi'an, 710072, People's Republic of China.

出版信息

Macromol Biosci. 2004 Aug 9;4(8):729-36. doi: 10.1002/mabi.200400037.

Abstract

The present work is focused on investigating the behavior of controlled drug release poly(N-isopropylacrylamide) (PNIPA) hydrogels in the presence of beta-cyclodextrin (beta-CD). For this purpose, three types of NIPA hydrogels with beta-CD moieties were synthesized with different architectures according to our previous studies. An anti-cancer drug (chlorambucil, CLB), which can form an inclusion complex with beta-CD, was selected for loading and in vitro release studies. The drug was loaded into hydrogels via a swelling method. DSC was used to study the interactions between the CLB molecules and the polymers. The results indicate that the CLB-polymer interactions are at the molecular level. Loading CLB into these polymers can result in an evident decrease in the glass transition temperature (T(g)), and the variation of T(g) (DeltaT(g)) depends on the structures of the polymers and their beta-CD content. The controlled release experiments show that the presence of beta-CD can markedly enhance CLB release from shrunken PNIPA hydrogels and increase the ratio of CLB released in total drug loading content. Release profile of CLB from hydrogels 1a-c and 4 at pH 1.4 and 7.4, at 37 degrees C.

摘要

本研究聚焦于考察含β-环糊精(β-CD)时可控药物释放聚(N-异丙基丙烯酰胺)(PNIPA)水凝胶的行为。为此,根据我们之前的研究,合成了三种具有不同结构且带有β-CD基团的NIPA水凝胶。选择了一种能与β-CD形成包合物的抗癌药物(苯丁酸氮芥,CLB)用于负载及体外释放研究。通过溶胀法将药物负载到水凝胶中。利用差示扫描量热法(DSC)研究CLB分子与聚合物之间的相互作用。结果表明CLB与聚合物之间的相互作用处于分子水平。将CLB负载到这些聚合物中会导致玻璃化转变温度(T(g))明显降低,且T(g)的变化量(ΔT(g))取决于聚合物的结构及其β-CD含量。控释实验表明,β-CD的存在能显著增强CLB从收缩的PNIPA水凝胶中的释放,并提高CLB在总药物负载量中的释放比例。在37℃、pH值为1.4和7.4条件下,CLB从水凝胶1a - c和4中的释放曲线。

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