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植物研究 ›› 2013, Vol. 33 ›› Issue (4): 484-489.doi: 10.7525/j.issn.1673-5102.2013.04.016

• 论文 • 上一篇    下一篇

叶酸偶联牛血清白蛋白负载卡铂和紫杉醇肿瘤靶向纳米粒制备、表征及体外释放性能评价

单常;祖元刚*;赵修华;桑梅   

  1. 东北林业大学森林植物生态学教育部重点实验室,哈尔滨 150040
  • 收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2013-07-20 发布日期:2013-07-20
  • 通讯作者: 祖元刚
  • 基金资助:
     

Preparation, Characterization and Evaluation of in vitro Release of Folate-Conjugated Carboplatin and Paclitaxel -loaded Bovine Serum Albumin Tumor-targeting Nanoparticles

SHAN Chang;ZU Yuan-Gang*;ZHAO Xiu-Hua;SANG Mei   

  1. Key Laboratory of Forest Plant Ecology,Northeast Forestry University,Ministry of Education,Harbin 150040
  • Received:1900-01-01 Revised:1900-01-01 Online:2013-07-20 Published:2013-07-20
  • Contact: ZU Yuan-Gang
  • Supported by:
     

摘要: 紫杉醇(Paclitaxel,商品名Taxol)是一种在红豆杉科(Taxaceae L.)红豆杉属(Taxus L.)生长缓慢的常绿乔木中分离提取的天然化合物。卡铂和紫杉醇均是目前临床上使用率很高的抗肿瘤药物,并在临床上经常配伍使用治疗不同的癌症。本研究以叶酸偶联的牛血清白蛋白作为药物载体,采用去溶剂技术制备了叶酸靶向卡铂—紫杉醇的白蛋白纳米粒,并研究了靶向制剂体外释放性质。研究结果表明:卡铂—紫杉醇白蛋白纳米粒平均粒径为199.4 nm,Zeta电位为-30.90 mV。卡铂包封率为91.4%;紫杉醇包封率为56.1%,药物总载药量为21%。其冻干粉复溶12 h后各项数据未发生较大变化,说明其具有良好的稳定性。体外释放结果表明叶酸—卡铂—紫杉醇白蛋白纳米粒与卡铂和紫杉醇原粉比较具有明显的缓释效果,体外释药时间可达120 h。

关键词: 叶酸, 卡铂, 紫杉醇, 牛血清白蛋白, 靶向, 去溶剂化

Abstract: Paclitaxel under the trade name Taxol, is a natural compounds isolated and purified from the trees of the Taxus(Taxaceae L.) belonging to taxus(Taxus L.). Paclitaxel and carboplatin are anti-cancer drugs currently with high clinical utility rates, which often used in combination on the clinical treatment of different types of cancer. Coupling folic acid in bovine serum albumin as a drug carrier, surface coating using nano-particle and solvent technology, folate-targeted carboplatin-paclitaxel albumin nanoparticles were prepared, and the in vitro release properties of targeted drug were studied. Research results are as follows: the mean grain size of carboplatin-paclitaxel albumin nanoparticles was 199.4 nm, the zeta electric potential was -30.90 mV; the envelope rates were 91.4% for carboplatin and 56.1% for paclitaxel, respectively; the drug loading capacity was 21%. It was proven that within 12 h a good stability was maintained through the reconstitution of the fa-carboplatin-paclitaxel albumin nanoparticles. In addition, the folic acid-carboplatin-paclitaxel albumin nanoparticles showed an evident slow-release effect as compared with the carboplatin and paclitaxel original powder, the in vitro release time was up to 120 h.

Key words: folic acid, carboplatin, paclitaxel, bovine serum albumin, target, desolvation

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