摘要
目的考察一种新型两亲性壳聚糖衍生物———聚乙二醇(PEG)/β谷甾醇双接枝壳聚糖(PSC)在水中自组装形成的纳米粒的性能及组织分布,为作为抗肿瘤药物载体的可行性进行理论探讨。方法采用芘荧光探针技术测定PSC的临界聚集浓度(CAC);用香豆素-6为模型药物,透析法考察胶束的体外释放度行为;考察载香豆素-6的PSC纳米粒在小鼠体内的组织分布。结果 CAC为0.02 g/L,载药量为3.3%,包封率为75%。较长链PEG的纳米粒比修饰短链PEG的纳米粒在脑部的分布有所增加;两种载药PSC纳米粒在肺部浓度较高;修饰PSC纳米粒在肾、心中分布均较少。结论 PSC胶束可作为香豆素的载体,具有良好的应用前景。
Objective To investigate the performance and the tissue distribution of the nanoparticles formed by self- assembling in water with a novel amphiphilic chitosan derivant-polyethylene glycol（PEG）/β sitosterol double grafted ehitosan（PSC） so as to theoretically explore the feasibility as anti- tumor drug carrier. Methods The critical aggregation concentration（CAC） of the copolymer PSC was measured by the pyrene fluorescent probe technique; with coumarin- 6 as the model drug, the in vitro release behavior of the micelle was investigated by the dialysis method; the tissue distribution of the PSC nanoparticles carrying coumarin- 6 in mice in vivo were in- vestigated. Results CAC was 0. 02 g/L, the drug-loading capacity was 3.3% and the encapsulation rate was 75%. The distribution in brain of nanoparticles of longer- chain PEG was increased to some extent compared with the modified short chain PEG; the two kinds of drug- loading PSC nanoparticles had the higher concentration in lung; at the same time the modified PSC nanoparticles were distributed little in kidney and heart. Conclusion The PSC micelle may be used as the coumarin carrier and has better application prospect.
出处
《中国药业》
CAS
2014年第7期17-20,共4页
China Pharmaceuticals
