pH敏感的肿瘤靶向聚合物胶束的体外性质
In vitro properties of p H sensitive tumor cell targeting polymer micelles
作者：刘妍曦;黄园;周洲;
Author：
收稿日期： 年卷（期）页码：2017,32(05):-459-463
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：FQS多肽;整合素α_vβ_3;融合肽;肿瘤微环境;肿瘤细胞靶向;聚合物胶束;HPMA聚合物;阿霉素
Key words：
基金项目：
中文摘要
目的制备肿瘤微环境敏感、具有肿瘤细胞靶向能力和穿膜能力的融合肽FQSIYPp IKRRRRRRRRHHHHC(FRH)修饰的聚合物胶束,并对其体外性质进行初步考察。方法采用FRH修饰N-(2-羟丙基)-甲基丙烯酰胺(HPMA)聚合物-β-谷甾醇(β-SITO),形成HPMA聚合物胶束(FRH-M),考察其理化性质、肿瘤细胞的摄取和抑制肿瘤细胞生长的效果。结果透射电镜显示:胶束为均匀的类球形。FRH-M胶束粒径约为55 nm,阿霉素载药量8.3%。该胶束在p H7.4条件下,Zeta电位为-3.01±0.05 m V,在p H6.4条件下,电荷翻转为5.27±0.32 m V。FRH-M的药物释放速度随释放介质的p H降低而加快。FRH-M的细胞摄取较未经修饰胶束的P-M提升了1.9倍;且在p H6.4条件下的细胞摄取明显高于p H7.4的,FRH-M的IC50值为1.40±0.41μg·m L~(-1),明显低于未经配体修饰的胶束(5.08±0.33μg·m L~(-1))。结论经FRH多肽修饰的聚合物胶束具有良好的肿瘤微环境响应能力,且有更好的细胞摄取能力和体外抗肿瘤活性,极具发展前景。
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