新型多西紫杉醇载药纳米微球的制备及其评价  被引量:3

Preparation and evaluation of novel docetaxel-loaded nanoparticles

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作  者:张文君 刘芹[2] 

机构地区:[1]南京公安消防医院内科,江苏南京210008 [2]南京大学医学院附属鼓楼医院肿瘤中心,江苏南京210008

出  处:《中华肿瘤防治杂志》2012年第8期579-582,共4页Chinese Journal of Cancer Prevention and Treatment

基  金:国家自然科学基金(81071815;81101751)

摘  要:目的:采用自行合成的高分子载体,制备负载多西紫杉醇(DOC)的纳米微球,全面评价其性质。方法:通过开环聚合法,制备单甲氧基聚乙二醇-聚己内酯(mPEG-PCL)两嵌段聚合物载体,考察载体的结构、相对分子质量、纳米微球粒径、形貌、生物相容性等性质。以改良的丙酮-纳米沉淀法制备负载DOC的载药纳米微球,以CCK-8法,评价该载药微球在体外对于肝癌细胞株H22的抗肿瘤活性,并与泰素帝相比较。结果:通过开环聚合法合成mPEG-PCL两嵌段聚合物,测定相对分子质量和设计相对分子质量相近。DOC纳米微球为不规则的圆形,表面光滑,其粒径<100nm。载体在高浓度时对细胞生长无抑制作用,毒性低。DOC的载药效率为81.3%,载药量为18.7%。体外细胞毒性显示,DOC纳米载体组IC50略小于裸药泰素帝。结论:该实验制备并评估了DOC载药纳米微球,为进一步研究提供了实验依据。OBJECTIVE:To prepare docetaxel(DOC)-loaded nanoparticles with bi-block copolymers mPEG-PCL and evaluate their characters. METHODS: mPEG-PCL was synthesized by ring-opening polymerization method. The structure, molecular weight, diameters, morphology and biocompatibility of the nanoparticles were investigated. The DOC loaded nanodrug was prepared by a modified acetone nano-precipated method. The in vitro cytotoxicity of DOC-loaded nanoparticles against Taxotere was evaluated by CCK-8 assay on murine hepatic carcinoma H22 ceils. RESULTS: mPEG-PCL copolymers were synthesized with desired molecular weight. The Doc-toaded nanoparticle was a monolayer spherical particle with a diameter less than 100 nm. The blank nanoparticles were non-toxic to the H22 cells. The encapsulation efficiency and drug loading content were 81.3 % and 18. 7%, respectively. In vitro cytotoxicity test demonstrated that the IC50 of DOC-loaded nanoparticles was slightly lower than that of Taxotere. CONCLUSION: This study was prepared,eval- uated the DOC-loaded nanopartheles and provided an experimental basis for further research.

关 键 词:多西紫杉醇 纳米微球 生物相容性 抗肿瘤 纳米沉淀法 

分 类 号:R94[医药卫生—药剂学]

 

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