载TNP-470 mPEG-PLA纳米粒制备及体外生物活性评价  

Preparation and in vitro evaluation of mPEG-PLA nanoparticles containing TNP-470

作　　者：王云飞[1,2] 狄文 邱丽华[1,2] 

机构地区：[1]上海交通大学医学院附属仁济医院妇产科 [2]上海交通大学医学院妇产科学研究所 上海市妇科肿瘤重点实验室,上海200127

出　　处：《中国实用妇科与产科杂志》2012年第11期861-864,共4页Chinese Journal of Practical Gynecology and Obstetrics

基　　金：上海市科委纳米专项基金(编号:1052nm04800)

摘　　要：目的评价载O-(氯乙酰-氨甲酰基)烟曲霉醇(TNP-470)甲氧基聚乙二醇-聚乳酸(mPEG-PLA)纳米粒的载药量、包封率、粒径、电位、形态、体外释放及活性。方法采用单乳法制备载TNP-470的mPEG-PLA纳米粒,透射电镜观察纳米粒形态,马尔文激光粒度仪测定其粒径分布及Zeta电位,高效液相色谱仪(HPLC)法测定纳米粒包封率、载药量及体外释药特性;CCK-8试剂盒检测对人脐静脉内皮细胞(HUVEC)的细胞毒作用;细胞划痕试验检测对HUVEC细胞迁移力的影响。结果制备的载TNP-470纳米粒为类球形,平均粒径131.25nm,Zeta电位-14.17mV,包封率66.24%,载药量3.31%,制剂72h体外累计释药百分率为60.15%,细胞增殖和划痕实验表明载TNP-470纳米粒能够显著抑制HUVEC细胞的增殖和迁移。结论对难溶性不稳定药物TNP-470制得的纳米粒具有合适的粒径及包封率,可提高其在水相中的浓度,并达到缓释作用,同时保留有原有的生物活性。Objective To prepare TNP-470-loaded mPEG-PLA nanoparticles（TNP-470-mPEG-PLA-NPs） and evaluate loading capacity,encapsulation efficiency,particle size,Zeta potential,morphology,in vitro release and bioactivity of the NPs.Methods TNP-470-mPEG-PLA-NPs were prepared by emulsion/solvent evaporation method（o/w）.The morphology of the NPs was observed by TEM.The distribution of particle size and Zeta potential of the NPs were determined by Malvern particle size analyzer.The encapsulation efficiency,drug-loading and in vitro release were examined by HPLC method.Cell counting kit-8（CCK-8） was used to detect the cell viability.Their migration were measured by wound assay.Results TNP-470-mPEG-PLA-NPs were spherical with an average diameter 131.25 nm,Zeta potential of-14.17 mV,drug loading of 3.31% and encapsulation efficiency of 66.24% and 72h accumulated release ratio of 60.15%.Cell experiments indicated that TNP-470-mPEG-PLA-NPs significantly inhibited HUVEC cells proliferation and migration.Conclusion These results indicated that TNP-470-mPEG-PLA-NPs possessed appropriate particle size and encapsulation efficiency,significantly increased the concentration of TNP-470 in water,exhibited sustained release in vitro,and retained the bioactivity of TNP-470.

关 键 词：O-(氯乙酰-氨甲酰基)烟曲霉醇 甲氧基聚乙二醇-聚乳酸 纳米粒 缓释 

分 类 号：R71[医药卫生—妇产科学]