以羧甲基壳聚糖为原料,聚乙二醇二缩水甘油醚为交联剂,通过反相微悬浮聚合方法,制备出粒径在300～600μm的交联羧甲基壳聚糖微球,再以硝酸铈铵为引发剂,使2-丙烯酰胺-2-甲基丙磺酸在微球表面进行接枝聚合,得到含离子交换基团(—COOH、—SO3H)的可载药栓塞微球。该微球对抗癌药物盐酸阿霉素载药率24h内可达34.6%,较纯羧甲基壳聚糖微球提高了49.8%。该微球在介入疗法治疗肿瘤领域具有很好的应用前景。
Surface modified carboxymethyl chitosan embolic microspheres were prepared by crosslinking reaction of carboxymethyl chitosan in a reverse suspension system using poly(ethylene glycol diglycidyl ether)(PEGDE) as the crosslinking agent,followed by graft polymerization of 2-acrylamido-2-methyl propanesulfonic acid on the surface of microspheres.The microspheres showed regular spherical shapes with size distribution ranging from 300 μm to 600μm.The ion exchange groups (—COOH,—SO3H) were introduced into the microspheres which could load doxorubicin with loading rate as high as 34.6% in 24 hours,raising 46.8% compared to that of pure carboxymethyl chitosan microspheres.The product had bright prospect in the field of interventional treatment of tumor.
[1] 吴汉平.肝癌介入治疗的现状与展望[J].临床放射学杂志,2005,24(3):273-276.
[2] Liu X H,Heng W S,Li Q,et al.Novel polymeric microspheres containing norcantharidin for chemoembolization[J].Journal of Controlled Release,2006,116(1):35-41.
[3] Juang R S,Wu F C,Tseng R L.Solute adsorption and enzyme immobilization Oil chitosan beads prepared from shrimp shell wastes[J].Bioresource Technology,2001,80(3):187-193.
[4] Vaghani S S,Patel M M,Satish C S.Synthesis and characterization of pH-sensitive hydrogel composed of carboxymethyl chitosan for colon targeted delivery of ornidazole[J].Carbohydrate Research,2012,347(1):76-82.
[5] He Q F,Li G M,Wu H Z,et al.Preparation of porous chitosan particles for pulmonary drug delivery[J].Journal of Functionl Materials,2004,21(2):192-195.
[6] 袁文,尹学琼,冯玉红,等.羧甲基壳聚糖的制备及其抗菌性能研究进展[J].食品研究与开发,2007,28(11):185-189.
[7] Florence Croisier.Chitosan-based biomaterials for tissue engineering[J].European Polymer Journal,2013,49(4):780-792.
[8] Baldrick P.The safety of chitosan as a pharmaceutical excipient[J].Regulatory Toxicology and Pharmacology,2010,56(3):290-299.
[9] Majeti N V,Ravi Kumar.A review of chitin and chitosan applications[J].Reactive & Functional Polymers,2000,46(1):1-27.
[10] Chen L Y,Du Y M,Wu H Q,et al.Relationship between molecular structure and moisture-retention ability of carboxymethyl chitin and chitosan[J].Appl Polym Sci,2002,83(6):1233-1241.
[11] Weng L,Le H C,Lin J,et al.Doxorubicin loading and eluting characteristics of bioresorbable hydrogel microspheres:in vitro study[J].International Journal of Pharmaceutics,2011,409(1/2):185-193.
基金资助
江苏省自然科学基金(BK20161128);中央高校基础研究基金(JUSRP51626B)
PDF
(1830KB)
