Preparation, optimization and in vitro evaluation of core-shell paclitaxelloaded nanoparticles composed of MPEG-PLA and PLA  

载有紫杉醇的核-壳MPEG-PLA/PLA纳米微球的制备、优化及体外评价(英文)

作　　者：孙玉[1] 张新明[2] 汤琳[1] 

机构地区：[1]皖南医学院药学院,安徽芜湖241002 [2]安徽师范大学化学与材料科学学院,安徽芜湖241000

出　　处：《Journal of Chinese Pharmaceutical Sciences》2015年第2期104-110,共7页中国药学（英文版）

基　　金：Key Research Foundation of Wannan Medical College(Grant No.WK2014Z06);Doctoral Starting-up Foundation of Wannan Medical College(Grant No.201219)

摘　　要：Nanoparticles with typical core-shell structure were prepared with a blend of methoxypoly（ethylene glycol）-poly（lactide） copolymer （MPEG-PLA） and poly （lactic acid） （PLA） along with paclitaxel by the O/W solvent evaporation method. An orthogonal experiment L9（3）3 was applied to get the best preparation conditions. The core-shell paclitaxel-loaded MPEG-PLA/PLA nanoparticles with the highest drug loading efficiency were obtained when amount of MPEG-PLA, time of ultrasonication and volume of deionized water were 300 mg, 10 rain and 30 mL, respectively. The release behavior of paclitaxel from the optimal MPEG-PLA/PLA nanoparticles showed that 22% ofpaclitaxel was released in 14 d. When incubating with human nasopharyngeal carcinoma ceils expressing LMP 1, these optimal nanoparticles showed a little lower tumor growth compared with free paclitaxel.本文制备了一种具有典型核-壳结构的载药纳米微球,由甲氧基聚乙二醇-聚乳酸共聚物(MPEG-PLA)、聚乳酸(PLA)和紫杉醇通过O/W溶剂挥发法制备而成。用正交试验L9(3)3对制备过程进行优化设计,当MPEG-PLA的用量为300 mg、超声时间为10 min、去离子水的用量为30 m L时可制得包封率最高的载有紫杉醇的MPEG-PLA/PLA纳米微球。体外溶出度实验表明14天后约有22%的紫杉醇从此微球中析出,体外抗肿瘤活性实验表明此微球对LMP1细胞具有略低于等量的游离紫杉醇的抗肿瘤活性。

关 键 词：Core-shell nanoparticles MPEG-PLA/PLA PACLITAXEL Orthogonal design 

分 类 号：R943[医药卫生—药剂学]