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基于烟酰胺的分子印迹微球的合成及体外控制释放研究。

Synthesis of nicotinamide-based molecularly imprinted microspheres and in vitro controlled release studies.

机构信息

Department of Engineering for Innovation, University of Salento, via per Monteroni, 73100 Lecce, Italy.

出版信息

Drug Deliv. 2010 Apr;17(3):130-7. doi: 10.3109/10717541003587418.

DOI:10.3109/10717541003587418
PMID:20163194
Abstract

Nicotinamide (NAM), which is one of the two principal forms, together with nicotinic acid, of vitamin B3, is both a food nutrient and a drug. Controlled NAM release systems are useful to extend the duration of the drug's pharmacological activity and to minimize administration frequency. In this paper, molecularly imprinted polymers (MIPs) have been used as unconventional synthetic polymeric carriers, to prepare drug delivery systems for sustained release of NAM molecules. In the present study, various MIPs micro-spheres have been synthesized by using methacrylic acid as a functional monomer and ethylene glycol dimethacrylate (EGDMA) as a cross-linker. Different stoichiometric ratios of the reagents have been used, in order to evaluate their influence on NAM recognition and release properties. Non-imprinted systems have been also been prepared as controls. MIPs binding capacity has been evaluated; NAM loading and in vitro release studies, in buffer solution (pH 7.2), that mimics blood plasma conditions, have been performed. Polymer P4 has given the best results since it enables it to rebind selectively and to prolong the release of NAM with higher performance than the non-imprinted one.

摘要

烟酰胺(NAM)是维生素 B3 的两种主要形式之一,与烟酸一起,既是食物营养素,也是药物。控制 NAM 的释放系统可用于延长药物的药理活性持续时间,并最小化给药频率。在本文中,使用分子印迹聚合物(MIPs)作为非常规合成聚合物载体,来制备用于 NAM 分子持续释放的药物输送系统。在本研究中,通过使用甲基丙烯酸作为功能单体和乙二醇二甲基丙烯酸酯(EGDMA)作为交联剂来合成各种 MIPs 微球。使用不同的试剂化学计量比,以评估它们对 NAM 识别和释放性能的影响。也制备了非印迹系统作为对照。评估了 MIPs 的结合能力;在缓冲溶液(pH 7.2)中进行了 NAM 负载和体外释放研究,该溶液模拟了血浆条件。聚合物 P4 给出了最佳结果,因为它能够选择性地重新结合并延长 NAM 的释放,性能优于非印迹聚合物。

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