寡核苷酸微球制剂研究进展  

Progress in Research on Oligonucleotide Microspheres

作　　者：张雪妍 崔雅欣 祝天宇 孙凤英[1] 滕乐生[1] ZHANG Xueyan;CUI Yaxin;ZHU Tianyu;SUN Fengying;TENG Lesheng(School of Life Sciences,Jilin University,Changchun 130012)

机构地区：[1]吉林大学生命科学学院

出　　处：《中国医药工业杂志》2019年第10期1136-1142,共7页Chinese Journal of Pharmaceuticals

摘　　要：寡核苷酸能够针对特定致病基因进行特异性干扰,是当前肿瘤、炎症等疾病治疗的新热点;但生物学稳定性差、体内半衰期短、核酸酶降解、对细胞膜的渗透性低、靶部位浓度低等缺点使其难以直接作为治疗药物。药物传递系统是目前常用的解决寡核苷酸递送问题的方案,其中,微球制剂以其能够提高药物稳定性、控制药物平稳释放等特点成为解决寡核苷酸递送问题的新热点。寡核苷酸药物可以直接包载或与阳离子材料形成复合物后包载进入微球。本文综述了近年来微球制剂在寡核苷酸递送系统中的研究进展。Oligonucleotides can specifically interfere with specific pathogenic genes,which is a new hotspot in the treatment of tumor,inflammation and other diseases.However,oligonucleotides are not suitable for direct administration due to the poor biological stability,short half-life in vivo,nuclease degradation,poor cell membrane permeability,and low concentration in target tissues.In recent years,in order to achieve stable and efficient delivery of oligonucleotide drugs,researchers dedicated to drug delivery systems around the world have made great efforts.Microsphere preparations have become one of the hotspots of oligonucleotide drug delivery systems,because microsphere preparations can improve drug stability and release the oligonucleotide drugs in a sustained and controlled manner.Therefore,microsphere preparations are suitable for the delivery of drugs with high activity and long-term using.Microspheres can be prepared by encapsulating oligonucleotides directly or the composites with cationic materials in them.In this paper,recent studies on microsphere preparations in oligonucleotide delivery systems are reviewed.

关 键 词：寡核苷酸 微球制剂 药物递送 直接包载 复合微球 

分 类 号：R944.9[医药卫生—药剂学]