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。
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 carboplatin-paclitaxel albumin nanoparticles was 199.4 rim, the zeta electric potential was - 30. envelope rates were 91.4% for carboplatin and 56.1% for paclitaxel, respectively; the drug loading grain size of 90 mV; the 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.
出处
《植物研究》
CAS
CSCD
北大核心
2013年第4期484-489,共6页
Bulletin of Botanical Research
基金
公益性行业科研专项经费项目:目的林药组分资源定向培养与高值化产品开发(201204601)
关键词
叶酸
卡铂
紫杉醇
牛血清白蛋白
靶向
去溶剂化
folic acid
carboplatin
paclitaxel
bovine serum albumin
target
desolvation
