李近,蒋国强,丁富新

• 1:清华大学化学工程系

摘要(Abstract)：

改变嵌段材料PLGA-mPEG亲、疏水端的分子量,通过体外降解和释药实验,考察材料性质对PLGA-mPEG载药微球的性质、降解以及释药行为的影响。当亲水链段mPEG较短时,PLGA-mPEG材料疏水链段的分子量越高,微球对药物包封率越高;微球的降解取决于材料的性质和水渗入的速度,亲水链段mPEG的引入增强了微球的吸水性,加速了材料的水解,释药速率相应提高,低分子量mPEG加速水解的效应更明显;但mPEG对微球有增塑作用,使微球在降解过程中维持了一定机械强度和完整形态,降低了降解后期微球崩解造成药物突释的风险。

关键词(KeyWords)： PLGA-mPEG;微球;药物控释;分子量;降解

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金(20576057);; 清华大学基础研究基金(JCqn2005033)

作者(Author): 李近,蒋国强,丁富新

参考文献(References)：

• [1]ZHANG Lei(张磊),YANG Song(杨松),GE Zhi-qiang(葛志强)et al.Study on the preparation of recombinant humanα-2b interferon slowly realeasing microcapsules and its in-vitro release properties(重组α-2b干扰素缓释微囊制备工艺及体外释药过程研究)[J].J Chem Eng of Chinese Univ(高校化学工程学报),2004,18(5):628-632.
• [2]Kumar N,Ravikumar M N V,Domb A J.Biodegradable block copolymers[J].Adv Drug Deliv Rev,2001,53(1):23-44.
• [3]Zhou S,Liao X,Li X et al.Poly-D,L-lactide–co-poly(ethylene glycol)microspheres as potential vaccine delivery systems[J].J Control Release,2003,86(2-3):195-205.
• [4]MallardéD,Boutignon F,Moine F et al.PLGA–PEG microspheres of teverelix:influence of polymer type on microsphere characteristics and on teverelix in vitro release[J].Int J Pharm,2003,261(1-2):69-80.
• [5]Jeong B,Bae Y H,Kim S W.Biodegradable thermosensitive micelles of PEG-PLGA-PEG triblock copolymers[J].Colloids Surf B Biointerfaces,1999,16(1-4):185-193.
• [6]Luo W J,Li S M,Bei J Z et al.Synthesis and characterization of Poly(L-lactide)-poly(ethylene glycol)multiblock copolymers[J].J Appl Polym Sci,2002,84(9):1729-1736.
• [7]Penco M,Marcioni S,Ferruti P et al.Degradation behaviour of block copolymers containing poly(lactic-glycolic acid)and poly(ethylene glycol)segments[J].Biomaterials,1996,17(16):1583-1590.
• [8]Fang C,Shi B,Pei Y Y et al.In vivo tumor targeting of tumor necrosis factor-α-loaded stealth nanoparticles:Effect of MePEG molecular weight and particle size[J].Eur J Pharm Sci,2006,27(1):27-36.
• [9]Lee C M,Choi Y,Huh E J et al.Polyethylene glycol(PEG)modified99mTc-HMPAO-liposome for improving blood circulation and biodistribution:The effect of the extent of PEGylation[J].Cancer Biother Radio,2005,20(6):620-628.
• [10]Avgoustakis K,Beletsi A,Panagi Z et al.PLGA-mPEG nanoparticles of cisplatin:in vitro nanoparticle degradation,in vitro drug release and in vivo drug residence in blood properties[J].J Control Release,2002,79(1-3):123-135.
• [11]Rosca I D,Watari F,Uo M.Microparticle formation and its mechanism in single and double emulsion solvent evaporation[J].J Control Release,2004,99(2):271-280.
• [12]Siepmann J,Faisant N,Akiki J et al.Effect of the size of biodegradable microparticles on drug release:experiment and theory[J].J Control Release,2004,96(1):123-134.