透析法制备紫杉醇聚合物胶束给药系统

摘要以4-二甲氨基吡啶(DMAP)和二环己基碳二亚胺(DCC)作催化剂和缩合剂,合成聚乙二醇-共轭亚油酸(PEG-CLA)聚合物;以PEG-CLA为载体,采用透析法制备了紫杉醇聚合物胶束给药系统;利用动态光散射法(DLS)、透射电镜(TEM)、X-射线光电能谱(XPS)表征了紫杉醇胶束的粒径与粒径分布、形貌以及表面组分特性,分别在pH值为7.4的磷酸盐缓冲溶液(PBS)和1 mol/L水杨酸钠溶液中进行了紫杉醇胶束的体外药物释放试验。研究结果表明,所制备的紫杉醇胶束外形大致呈球状,粒径在100 nm左右,且粒径分布较窄。X-射线光电能谱显示,胶束表面没有吸附紫杉醇。在体外药物释放实验中,发现水杨酸钠对紫杉醇的释放起促进作用。

	Service

	把本文推荐给朋友
	加入我的书架
	加入引用管理器
	Email Alert
	RSS
	作者相关文章
	王彩霞
	冯霞
	徐芳
	吝保瑞

关键词：紫杉醇聚合物胶束

Abstract： Poly(ethylene glycol)(PEG)-conjugated linoleic acid(CLA)(PEG-CLA) polymeric conjugate was synthesized using 4-dimethylaminopyridine(DMAP) and dicyclohexycarbodiimide(DCC) as catalyst and coupling agent,respectively.PEG-CLA polymer was employed as carrier,the paclitaxel-loaded micelles were prepared by dialysis method.The size and size distribution,the structure and the surface chemistry of micelles were characterized by dynamic light scattering(DLS),transmission electron microscopy(TEM) and X-ray photoelectron spectroscopy(XPS),respectively.The in vitro release profiles of paclitaxel from polymeric micelles were investigated in pH7.4 phosphate buffer solution(PBS) and 1 mol/L sodium salicylate medium.The results show that the paclitaxel-loaded micelles have spherical shapes,particle size of 100 nm and narrow size distribution.XPS indicates that the drug is not absorbed on the micelles surface and sodium salicylate medium can accelerate the release rate of paclitaxel from polymeric micelles.

Keywords：

Received 2007-01-15; published 2007-01-15

引用本文:

王彩霞;冯霞;徐芳;吝保瑞;.透析法制备紫杉醇聚合物胶束给药系统[J]. 化学工业与工程, 2007,24(1): 24-27

WANG Cai-xia,FENG Xia,XU Fang,LIN Bao-rui.Preparation of Paclitaxel-Loaded Polymeric Micelles by Dialysis Method[J]. Chemcial Industry and Engineering, 2007,24(1): 24-27

[1]	CROSASSO P,CERUTI M,BRUSA P.Preparation,characterization and properties of sterically stabilizedpaclitaxel-containing liposomes[J].Journal of ControlledRelease,2000,63(1):19-30.
[2]	RODRIGUES P C A,SCHEUERMANN K,STOCKMAR C.Synthesis and in vitro efficancy of acid-sensitive poly(ethylene glycol)paclitaxel conjugates[J].Bioorganic&Medicinal Chemistry Letters.2003,13(3):355-360
[3]	ZHANG C,QINENG P,ZHANG H.Self-assembly andcharacterization of paclitaxel-loaded N-octyl-O-sulfatechitosan micellar system[J].Colloids and Surfaces B:Biointerfaces.2004,39(2):69-75
[4]	KIM S Y,LEE Y M.Taxol-loaded block copolymernanospheres composed of methoxy poly(ethylene glycol)andpoly(-εcaprolactone)as novel anticancer drug carriers[J].Biomaterials.2001,22(13):1-
[5]	LIU X M,WANG L S.A one-pot synthesis of oleic acid end-capped temperature-and pH-sensitive amphiphilic polymers[J].Biomaterials.2004,25(10):1-
[6]	LA S B,OKANO T,KATAOKA K.Preparation andcharacterization of the micelle-forming polymeric drugindomethacin-incorporated poly(ethylene oxide)-poly(β-benzylL-aspartate)block copolymer micelles[J].Journal ofPharmaceutical Science.1996,85:85-90
[7]	LAVASANIFAR A,SAMUEL J,KWON G S.Micelles self-assembled from poly(ethylene oxide)-block-poly(N-hexylstearate-Laspartamide)by a solvent evaporation method:Effect on the solubilization and haemolytic activity ofamphotericin B[J].Journal of Controlled Release.2001,77(2):155-160
[8]	GARCIA H S,ARCOS J A,KEOUGH K J.Immobilizedlipase-mediated acidolysis of butter oil with conjugatedlinoleic acid:Batch reactor and packed bed reactor studies[J].Journal of Molecular Catalysis B:Enzymatic.2001,11(5):623-632
[9]	PALOMBO J D,GANGULY A,BISTRIANB R.Theantiproliferative effects of biologically active isomers ofconjugated linoleic acid on human colorectal and prostaticcancer cells[J].Cancer Letters.2002,177(2):163-172
[10]	董岸杰,邓联东,孙多先.紫杉醇两亲嵌段共聚物纳米囊的研究[J].药学学报,2004,39(2):149-152.
[11]	CHO Y W,LEE J,LEE S C.Hydrotropic agents for study ofin vitro paclitaxel release from polymeric micelles[J].Journal of Controlled Release.2004,97(2):249-257
[12]	LEE J,LEE S C,ACHARYA G.Hydrotropic solubilization ofpaclitaxel:Analysis of chemical structures for hydrotropicproperty[J].Pharmaceutical Research.2003,20(7):1-