紫杉醇纳米粒作为药物递送载体的研究  

The research of paclitaxel-loaded nanoparticles by human serum albumin as drug delivery vectors

作　　者：潘英[1] 倪海华[2] 邹爱峰[2] 邓盛齐[3] 

机构地区：[1]江苏省肿瘤医院,南京210000 [2]扬子江药业集团,泰州225321 [3]四川抗菌素工业研究所,成都610052

出　　处：《中国抗生素杂志》2013年第11期853-858,共6页Chinese Journal of Antibiotics

摘　　要：目的制备紫杉醇纳米粒的制备,对其理化性质进行考察以及作为药物递送载体的研究。方法采用高压乳匀法制备包载紫杉醇(PTX)的人血清白蛋白纳米粒,采用透析法研究PTX-HSA在不同介质中的释放动力学,并以Taxol为对照,通过MTT试验对PTX-HSA的抗肿瘤活性进行了评价。结果白蛋白载体在水介质中能自组装形成纳米粒,对PTX具有优越的增溶效果,载药量为33.0%,包封率为98.6%,平均粒径为130.0nm,多分散系数为0.174,Zeta电位为-31.0mV;PTX-HSA纳米粒体外释放行为呈现非零级释药特征,释放速度具有一定pH依赖性。PTX-HSA纳米粒比Taxol对酸性分泌蛋白(SPARC)过度表达的人肺癌细胞A549具有更强的细胞毒性,而对不表达SPARC的中国仓鼠卵巢CHO细胞毒性没有显著差异。结论 PTX-HSA具有良好的应用前景。Objective To prepare an albumin-bound form of paclitaxel nanoparticeles by emulsion method, investigate its physico-chemical properties and research as drug delivery vectors. Methods In vitro release, PTX- HSA nanoparticles were measured using a dialysis method in various buffered solution. MTT experiments were used to evaluate the cytotoxic effect to A549 cells. Results Nanoparticles of PTX were self-assembled in water medium. HSA showed excellent drug loading capacites for PTX with drug loading of 33.0% and encapsulation efficiency of 98.6%. The mean size of PTX-HSA nanoparticle was 130.0nm with polydisperse index of 0.174. The Zeta potential was -31.0mV. Release behavior of PTX formulated in PTX-HSA nanoparticles showed non-zero order and pH- sensitive release characteristics. Compared with Taxol~, PTX-HSA nanoparticle exhibited stronger cytotoxicity to A549 and comoarble cvtotoxicv to CHO cells. Conclusion PTX-HSA nanooarticles had a bright future.

关 键 词：白蛋白 纳米粒 主动靶向 紫杉醇 体外释放 细胞毒性 

分 类 号：R9[医药卫生—药学]