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作 者 ：单常;祖元刚*;赵修华;桑梅

期 刊 ：植物研究 2013年 33卷 4期 页码：484-489

关键词：叶酸；卡铂；紫杉醇；牛血清白蛋白；靶向；去溶剂化；

Keywords:folic acid, carboplatin, paclitaxel, bovine serum albumin, target, desolvation,

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。

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.

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