环糊精(准)聚轮烷在药物控制释放应用中的研究进展

Progress in Application of Controlled Drug Release Based on Cyclodextrins( Pseudo) Polyrotaxanes

在药物控制释放系统中,药物能够按照设计的剂量在要求的时间范围内以均匀速率持续释放,达到低剂量、高疗效的效果.利用天然或合成的聚合物作为药物载体或介质来构建药物控制释放系统可以有效地降低药物的毒副作用,减少患者耐药性,提高药物的稳定性和生物利用度.环糊精和聚合物可以通过疏水力、氢键、范德华力等驱动力相互作用形成环糊精(准)聚轮烷,因其具有独特的结构、良好的生物相容性、易于化学修饰以及环糊精在聚合物轴上可迁移等特点.既可以将药物包结在环糊精(准)聚轮烷中的环糊精空腔中,也可以将药物键合在环糊精外侧的羟基上,从而可以增大药物载药量、溶解性以及稳定性.环糊精(准)聚轮烷药物控制释放系统可以有效地将环糊精的包结、易修饰技术和聚合物纳米给药技术融合一体,使药物能够达到定点、定时以及定量的释放效果.然而,到目前为止,基于环糊精(准)聚轮烷构建的药物控制释放系统大多只停留在体外实验研究阶段,需要加快其相关理论以及其在生物体内的研究进度,从而获得具有更高的载药量和包封率、更好的药物控制释放效率和真正能适用于生物体内的新型环糊精(准)聚轮烷药物控制释放体系.本文综述了近年来基于环糊精(准)聚轮烷构建的药物控制释放系统在药物控制释放中的应用的最新研究进展,并对其发展作了进一步的展望.

Drugs can achieve the effect of sustained and controlled release, low dose and high curative in the controlled drug release system according to the design of drug dose in the required time range at a uniform rate. It can effectively reduce adverse reaction as well as resistance in patients, and improve stability and biological a- vailability to use natural and synthetic ploymers as drugs carrier or medium to build controlled drug release system. Cyclodextrins（CDs） and linear polymer molecule can form polypseudorotaxane（PPR） under the driving of hydrophobic interaction, hydrogen bond and Van der Waals force. Due to the unique structure, good biocompatibility, facile functionalization of（pseudo） polyrotaxanes and the mobility of CD rings on the linear polymer molecule, drugs can not only be wrapped in the cavity of cyclodextrin of（pseudo） polyrotaxane, but also be bonded to the hydroxyl group of cyclodextrin of（pseudo） polyrotaxane. The （pseudo） polyrotaxane of cyclodextrin would be a new type of drug sustained and controlled release vector which can increase the drug loading, solublity and stability. The controlled drug release system of（pseudo） polyrotaxane can be effectively integrated with the inclu- sion of cyclodextrin, the modified of cyclodextrin technology and the polymer nano drug delivery technology, in which the drug can achieve fixed - point, timed and quantitative release. However, the controlled drug release system based on cyclodextrin（pseudo） polyrotaxane has only confined to vitro experimental research stage up to now. In order to obtain the novel cyclodextrin of（pseudo） polyrotaxane drug controlled release system of higher drug loading and encapsulation and better efficiency of the drug control release with real application to organisms, the related theories and the rate of study progress in vivo should be enhanced. The latest progress in application of controlled drug release based on cyclodextrins（pseudo） polyrotaxanes are summarized in this paper. In addition, some personal perspectives on this field are also presented.