壳聚糖以及其他生物材料作为胰岛素载体的释药性能特征  

Characteristics of drug release of chitosan and other biomaterials as insulin carriers

作　　者：侯桂梅[1] 卢林娜[1] 

机构地区：[1]大连市中心医院内分泌科,辽宁省大连市116033

出　　处：《中国组织工程研究与临床康复》2009年第42期8349-8352,共4页Journal of Clinical Rehabilitative Tissue Engineering Research

摘　　要：目的:探讨壳聚糖作为胰岛素载体的释药特性,展望高分子材料在胰岛素载体中的应用。方法:以胰岛素,载体,壳聚糖,脂质体,聚合物为检索词,检索中国期刊全文数据库(1999-01/2009-06);以insulin,carriers,chitosan,liposomes,polymer为检索词,检索Pubmed数据库(1999-01/2009-06),文献检索语种限制为中文和英文。以药物生物利用度、药物包埋率、药物的释放率为评价指标,纳入壳聚糖及其他生物材料作为口服胰岛素载体的研究,排除注射给药及其他给药方式的研究。结果:计算机初检得到543篇文献,根据纳入排除标准,对壳聚糖及其他生物材料作为胰岛素载体的释药特性进行分析。壳聚糖及其衍生物纳米粒作为胰岛素给药系统的研究备受关注。它在黏膜给药系统中表现出独特的纳米效应,不但可以改变药物的动力学,而且可以延长在黏膜内的滞留时间,改变膜转运机制,增加药物对膜的通透性,有效地克服了酶等生物屏障,解决了胰岛素在体内易失活及半衰期短等问题。近年来,胰岛素载体的释药性研究已经取得了一些进展,但面临的困难仍然很多,主要是包封率较低,吸收有限,而且制剂质量方法不成熟,剂量较难控制,成本较高,以及对吸收部位的损坏乃至可能对人体脏器功能带来影响。随着许多新性能高分子材料的涌现以及医药制剂工业的迅猛发展,高分子载体被越来越广泛地应用于新药的研究与开发中。结论:生物相容性、生物可降解性是选择胰岛素载药体系时需要首先考虑的问题。胰岛素载体的合成,胰岛素与载体的联接方式,间隔基对释放药物性能的影响,载体结构与单克隆抗体特异性的关系对胰岛素载体的释药性有决定性的影响。OBJECTIVE： To explore the characteristics of drug release of chitosan as insulin vector, and to prospect application of polymer materials to insulin vector. METHODS： We researched China Journal Full-text Database in Chinese from January 1999 to June 2009, and Pubmed database in English from January 1999 to June 2009 with the key words of “insulin, carriers, chitosan, liposomes, polymer”. Drug bioavailability, embedding rate, release rate were used as evaluation indexes. Studies concerning chitosan and other biological materials as insulin carrier for oral use were included. Studies describing injection administration and other administration methods were excluded. RESULTS： 543 literatures were selected by computer. According to exclusion criteria, characteristics of drug release of chitosan and other biomaterials as insulin carriers were analyzed. Chitosan and its derived nanoparticle as insulin administration system have received high attention, and presented special nanometer effects in mucosa administration system, not only can change drug dynamics, but also prolong residence time in mucosa, change membrane transport mechanism, enhance drug permeability to membrane. These effectively overcome biological barrier such as enzyme, solve some problems such as easy to inactivation and short half-life period of insulin in vivo. Recently, drug release research of insulin carrier has obtained some progresses, but we still face many difficulties, including low entrapment efficiency, limited absorption, immature evaluation method for preparation quality, difficult to control, high cost, destroy to absorption area, and effects on human organs. With the appearance of many new functional polymers and rapid development of medical preparation industry, polymer carrier has been widely used in the research and development of new drugs. CONCLUSION： Biocompatibility and biodegradability should be firstly considered when selecting insulin drug carrier system. Synthesis of insulin carrier, connection manner of insulin a

关 键 词：胰岛素 载体 壳聚糖 脂质体 聚合物 

分 类 号：R318[医药卫生—生物医学工程]