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羟基喜树碱-磷脂复合物的制备、表征及细胞毒性评价 预览 被引量:2

Preparation,characterization and in vitro cytotoxicity evaluation of hydroxycamptothecin-phospholipid complex
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摘要 目的制备羟基喜树碱-磷脂复合物(HCPT-PC),对其理化性质进行表征,并考察其细胞毒性。方法采用马尔文粒径电位测定仪、扫描电镜、透射电镜对粒径和形态进行表征;采用X线粉末衍射、红外光谱对复合机制进行考察;同时考察其溶解度和抗肿瘤活性。结果 HCPT-PC粒径为(145.08±18.37)nm;扫描电镜和透射电镜下呈均匀分布的球形;粉末衍射结果显示,HCPT-PC中HCPT从结晶态转变为无定形状态;红外光谱显示HCPT与PC的极性端存在弱相互作用;HCPT-PC在水、PBS、乙醇、正辛醇中的溶解度分别提高约21.91、20.36、1.42和6.32倍;与Hep G2、SMMC-7721和H22细胞作用48和72 h后,HCPT-PC的IC50值较HCPT分别提高3.57、11.14、2.79、37.26、21.23和24.49倍。结论 HCPT通过与PC的极性端形成弱相互作用复合成无定形状态的HCPT-PC,其溶解度和抗肝癌活性较HCPT显著提高。 Objective To prepare hydroxycamptothecin-phospholipid complex(HCPT-PC),characterize its physicochemi-cal properties,and evaluate the cytotoxicity. Methods The particle size and morphology of HCPT-PC were characterized by malvern particle size potentiometer,scanning electron microscopy(TEM)and transmission electron microscopy(TEM). Its composite mecha-nism was investigated by X-ray powder diffraction and infrared spectroscopy. The solubility and antitumor activity were also investigat-ed. Results The particle size of HCPT-PC was(145.08±18.37)nm. Scanning electron microscopy and transmission electron micros-copy revealed that HCPT-PC was uniformly distributed with a spherical shape. X-ray powder diffraction indicated that HCPT changed from crystalline to amorphous state in HCPT-PC. Fourier transform infrared spectroscopy showed that there was a weak interaction be-tween HCPT and PC. The solubility of HCPT-PC in water,PBS,ethanol and n-octanol was about 21.91,20.36,1.42 and 6.32 times than that of HCPT,respectively. After treated with HepG2,SMMC-7721 and H22 cells for 48 and 72 hours,IC50 of HCPT-PC was higher than that of HCPT by 3.57,11.14,2.79,37.26,21.23 and 24.49 times,respectively. Conclusion HCPT is compounded into an amorphous-state HCPT-PC by a weak interaction with the polar end of PC. Its solubility and anti-hepatocarcinoma activity are signif-icantly higher than HCPT.
作者 张红敏 李琬晴 高静 张慧 李迎 孙建绪 李见春 郑爱萍 ZHANG Hong-min1,2, LI Wan-qing3, GAO Jing2, ZHANG Hui2, LI Ying2, SUN Jian-xu2, LI Jian-chun1, ZHENG Ai-ping2. (1. Department of Pharmacy, Bengbu Medical College, Bengbu 233000, China; 2. Department of Pharmaceutics, State Key Laboratory of Toxicology and Medical Countermeasures, Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China; 3. School of Preclinical Medicine, Beijing University of Chinese Medicine, Beijing 100029, China)
出处 《国际药学研究杂志》 CSCD 北大核心 2017年第7期714-721,共8页 Foreign Medical Sciences(Section of Pharmarcy)
基金 国家自然科学基金资助项目(81573357) 蚌埠医学院科研项目(BYKY1609ZD) 安徽省访问学者基金项目(gxfx ZD2016148) 军队医学创新工程专项(16CZX032)
关键词 羟基喜树碱-磷脂复合物 复合机制 溶解度 细胞毒性 hydroxycamptothecin-phospholipid complex compound mechanism solubility cytotoxicity
作者简介 张红敏,女,在读硕士研究生,研究方向:药物新剂型研究,E-mail:1530513071@qq.com;通讯作者:李见春,男,博士,副教授,研究方向:药物新剂型研究,E-mail:lijianchun0552@163.com;;通讯作者:郑爱萍,女,研究员,博士生导师,研究方向:纳米给药系统,分子药剂学,Tel:010-66931694,E-mail:apzheng@163.com
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