载有10-羟基喜树碱的纳米颗粒：小鼠体内的制备及抗肿瘤活性
10-Hydroxycamptothecin loaded nanoparticles: preparation and antitumor activity in mice.
作者信息
Zhang Leyang, Yang Mi, Wang Qin, Li Yuan, Guo Rui, Jiang Xiqun, Yang Changzheng, Liu Baorui
机构信息
Laboratory of Mesoscopic Chemistry and Department of Polymer Science and Engineering, College of Chemistry and Chemical Engineering, Nanjing University, Nanjing, 210093, PR China.
出版信息
J Control Release. 2007 Jun 4;119(2):153-62. doi: 10.1016/j.jconrel.2007.02.013. Epub 2007 Mar 1.
10-Hydroxycamptothecin (HCPT) loaded nanoparticles made from poly(caprolactone-co-lactide)-b-PEG-b-poly(caprolactone-co-lactide) (PCLLA-PEG-PCLLA) block copolymer, were prepared by a novel two-step nanoprecipitation method using an interior-chemistry strategy. The satisfactory drug loading content (>13%) as well as high encapsulation efficiency (>85%) was achieved. Cytotoxicity test indicated that the HCPT-loaded nanoparticles had enhanced in vitro cytotoxicity compared to free drug. Progressively, in vivo antitumor activity and HCPT biodistribution in sarcoma-180 (S-180) bearing mice after intravenous injection of the HCPT-loaded nanoparticles show that HCPT-loaded nanoparticles exhibited superior in vivo antitumor effect and remarkably different biodistribution than the commercially available HCPT injection.
采用一种新型的两步纳米沉淀法并运用内部化学策略，制备了由聚（己内酯-共-丙交酯）-b-聚乙二醇-b-聚（己内酯-共-丙交酯）（PCLLA-PEG-PCLLA）嵌段共聚物制成的载10-羟基喜树碱（HCPT）纳米粒。获得了令人满意的载药量（>13%）以及高包封率（>85%）。细胞毒性试验表明，与游离药物相比，载HCPT纳米粒具有增强的体外细胞毒性。进一步地，在静脉注射载HCPT纳米粒后，对荷肉瘤-180（S-180）小鼠的体内抗肿瘤活性和HCPT生物分布研究表明，载HCPT纳米粒表现出优于市售HCPT注射液的体内抗肿瘤效果和显著不同的生物分布。
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