紫杉醇-汉防己甲素复合纳米粒的制备及其逆转MCF-7/ADR细胞多药耐药的研究  

The preparation of paclitaxel-tetrandrine combined nanoparticles and its effect on overcoming multidrug resistance of MCF-7 / ADR cells

作　　者：宁婷[1] 李月[1] 徐翀[1] 

机构地区：[1]中国医科大学附属第一医院药学部,辽宁沈阳110001

出　　处：《广东药学院学报》2015年第5期566-570,共5页Academic Journal of Guangdong College of Pharmacy

摘　　要：目的制备载有紫杉醇和汉防己甲素的复合纳米粒,并进行逆转肿瘤细胞多药耐药性研究。方法采用纳米沉淀法制备紫杉醇-汉防己甲素复合纳米粒,对其载药量、包封率、粒径进行测定,并对其体外释放行为进行考察。采用体外细胞毒试验和Western blot法考察复合纳米粒逆转多药耐药的效果。结果复合纳米粒的紫杉醇和汉防己甲素载药量分别为0.49%和0.20%,包封率分别为98.3%和99.6%,粒径为(107.3±15.6)nm。体外释放试验表明,紫杉醇和汉防己甲素几乎同步释放。MCF7/ADR细胞毒试验结果显示,相比于游离紫杉醇,紫杉醇-汉防己甲素复合纳米粒的IC50从6.7μmol/L降为1.1μmol/L。Western blot试验结果表明汉防己甲素有效地抑制了P-gp的表达。结论中药汉防己甲素能够有效地改善紫杉醇对耐药细胞株的耐药性。Objective To prepare combined nanoparticles loading paclitaxel and tetrandrine and study its effect on overcoming multidrug resistance of tumor cells. Methods The combined nanoparticles were prepared using nano-precipitation methods. The drug loading,encapsulation efficiency and particle size were determined,and the release behavior in vitro was investigated. The effect of overcoming multidrug resistance was studied using MTT assay and Western blot assay. Results The loading efficiency of the combined nanoparticles for paclitaxel and tetrandrine were 0. 49% and 0. 20%,respectively. The encapsulation efficiency of the combined nanoparticles for paclitaxel and tetrandrine were 98. 3% and 99. 6%,respectively. The mean particle size of prepared nanoparticles was（ 107. 3 ± 15. 6） nm. In vitro release experiment showed that paclitaxel and tetrandrine were simultaneously released. Compared with free paclitaxel,the combined nanoparticles decreased IC50 value from 6.7 μmol / L to 1.1 μmol / L. Western blot assay showed that the expression of P-gp was inhibited by tetrandrine. Conclusions Traditional Chinese medicine tetrandrine could overcome the multidrug resistance of paclitaxel effectively.

关 键 词：紫杉醇 汉防己甲素 纳米粒 多药耐药性 

分 类 号：R943[医药卫生—药剂学] R96[医药卫生—药学]