口服胰岛素载体的高分子生物材料

背景：利用具有生物相容性和生物可降解性的高分子材料作为载体，通过化学结合或物理包裹胰岛素，可提高胰岛素在体内的稳定性和生物利用度。 目的：从类型、制备方法、特征、药理作用等方面综述国内外口服胰岛素载体的高分子材料的研究进展。 方法：由作者应用计算机检索中国知网数据库、PubMed数据库和Elsevier 数据库2002年1月至2013年2月，与高分子生物材料和口服胰岛素载体相关的文章，中文关键词为“高分子生物材料、口服胰岛素、载体”，英文关键词为“polymeric biomaterials，oral insulin，carrier”。 结果与结论：目前，主要用于口服胰岛素系统控缓释的高分子生物材料可分为天然高分子生物材料和合成高分子生物材料两大类。用于口服胰岛素载体研究的天然高分子材料，以壳聚糖、藻酸盐多见。合成高分子生物材料中聚酯类、聚丙烯酸酯类及其共聚物，因具有良好的生物相容性、生物降解性和生理性能，被用作口服胰岛素制剂的载体材料的研究报道较多。国内外有关口服胰岛素制剂的研究报道虽多，也有一些商品型口服胰岛素进入临床试验阶段，但至今尚未见到实际应用的临床报告。其主要原因是作为载体的高分子材料、胰岛素的生物利用度低、制剂的质量标准及稳定性问题尚未解决。因此，未来的研究将主要集中在：载体材料的选择或者对现有高分子聚合物进行物理和化学的修饰，研发出新型的聚合物基材料作为载体，以避免胃肠道对胰岛素的破坏和改善胰岛素在体内的吸收，获得理想的释药速度和良好缓控释效果。

Biodegradable polymeric biomaterials as oral insulin carriers

Abstract： BACKGROUND：The carriers made from biodegradable and biocompatible polymeric materials represent an exciting approach to increase the bioavailability and stability of oral y administered insulin by the chemical reaction or physical encapsulation of insulin.
OBJECTIVE：To mainly review the research progress of the material types, preparation methods, physicochemical characteristics, in vitro release kinetics, and bioavailability of polymeric materials adopted as oral insulin carriers.
METHODS：The first author searched PubMed, Elsevier and CNKI databases for articles （2002-01/2013-02） concerning the polymeric materials and oral insulin carriers with the key words of“polymeric biomaterials, oral insulin, carrier”in English and in Chinese.
RESULTS AND CONCLUSION：Currently, there are mainly two kinds of polymeric biomaterials used for oral insulin delivery systems, that is, natural polymeric biomaterials （such as chitosan and alginates） and synthetic polymeric biomaterials. The most commonly used synthetic polymeric materials for the preparation of these vehicles are polyesters, polyacrylates and their copolymers, which are wel known for their good biodegradability, biocompatibility, and physiological properties. Although researchers have tried to develop promptly oral insulin formulation using various technologies, the reports about clinical application or commercial success have not been seen because of several questions such as polymer material as a carrier, the lower bioavailability of insulin, the quality standards and stability of the formulation. Hence, future studies wil focus on the development of a new type of polymer-based material as carriers by choosing the new materials or modifying physical and chemical characteristics of existing polymers, to avoid gastrointestinal destruction of the insulin and increase bioavailability of insulin in the body, so as to obtain the good control ed release rate and effect.