血管抑制剂康普瑞汀和康普瑞汀磷酸二钠纳米制剂研究进展  

Nanoformulations of the vascular inhibitors:combretastatin A4 and combretastatin A4 phosphate

作　　者：马娟娟[1] 陈建明[1,2] 

机构地区：[1]第二军医大学药学院药剂教研室,上海200433 [2]江苏天士力帝益药业有限公司,淮安223003

出　　处：《国际药学研究杂志》2016年第5期893-898,共6页Journal of International Pharmaceutical Research

摘　　要：血管抑制剂康普瑞汀(风车子抑素,CA4)可靶向微管蛋白,抑制其聚合,从而抑制肿瘤组织血管,起到抗肿瘤作用,但CA4水溶性差,生物利用度很低。CA4衍生物康普瑞汀磷酸二钠(CA4P)增加了水溶性,进入体内可转化为CA4,在国外已进入Ⅱ/Ⅲ期临床试验,但存在毒副作用大、体内消除快等问题。纳米剂型可增加药物溶出和吸收,获得控释、靶向、延长药效、减小副作用等效果。针对CA4和CA4P的物理化学特点和生物药剂学缺陷,纳米制剂可望改变药物溶出、吸收和分布。本文综述了近年来关于CA4和CA4P纳米制剂的研究进展,涉及树状大分子、聚合物胶束(PM)、纳米粒(NP)、长循环脂质体(LCL),并对其研发和应用前景进行展望。Combretastatin A4（CA4）,a vascular inhibitor,can target tubulin and inhibit tubulin polymerization,thus it can inhibit the tumor blood vessels and has antitumor effect. But it is insoluble in water and has low bioavailability. CA 4 phosphate （CA4P）,the derivative of CA4,can improve the solubility of CA4 and convert into CA4. CA4P is undergoing phaseⅡ/Ⅲclinical tri-als abroad. However,CA4P has several undesirable side effects and relative short half-life in vivo. Nanoformulations can increase the dissolution and absorption of the drug and obtain controlled release and targeting,prolong the efficacy and reduce side effects. Work-ing on the physical and chemical characteristics and biological pharmacy defects of CA4 and CA4P,nanoformulations may change the dissolution,absorption and distribution of the drug. This paper reviews the current nanoformulations of CA4 and CA4P,including den-drimer,polymeric micelle（PM）,nanoparticles（NP）,long-circulating liposome（LCL）,and discusses the prospects of their nanofor-mulations.

关 键 词：康普瑞汀 树状大分子 聚合物胶束 纳米粒 长循环脂质体 

分 类 号：R943[医药卫生—药剂学]