整合素受体靶向脂质体药物载体及其制备方法和应用技术

本发明专利技术公开了整合素受体靶向脂质体药物载体及其构建方法，还公开了该药物载体在制备靶向抗肿瘤脂质体药物中的应用。本发明专利技术将十六烷基脂肪链与ＲＧＤ肽段相缀合，对其进行疏水性修饰，合成了具备两亲性的正十六烷基和ＲＧＤ肽缀合物，即Ａｒｇ－Ｇｌｙ－Ａｓｐ－Ｘ－ＮＨ－Ｃ↓［１６］Ｈ↓［３３］，Ｘ选自缬氨酸、丝氨酸或苯丙氨酸。本发明专利技术将脂溶性的抗肿瘤药物引入到该两亲性缀合物中得到抗肿瘤靶向脂质体药物，该脂质体系统可以增加抗肿瘤药物在靶部位的浓度并可减少其在非靶部位的毒副作用，提高药物的治疗指数。本发明专利技术以荷肉瘤Ｓ１８０小鼠为模型评价了紫杉醇脂质体制剂的抗肿瘤活性，结果显示紫杉醇靶向脂质体比各对照组具有更优异的抗肿瘤活性。

Integrin receptor targeting liposome drug carrier, preparation method and application thereof

The invention discloses a integrin receptor targeting liposome drug carrier and a construction method thereof, and also discloses the application of the drug carrier in preparing a targeted anti-tumor liposome drug. In the invention, sixteen alkyl fatty chain and RGD peptide conjugated phase, hydrophobic modification of the two amphiphilic is sixteen alkyl and RGD peptide conjugates were synthesized, Arg - Gly - Asp - X - NH - C: 16 H: 33, X is selected from valine, serine or phenylalanine. The invention of fat soluble anticancer drugs into the two amphiphilic conjugates in tumor targeting liposome. The liposome system can increase the concentration of antitumor drugs in target sites and reduce its non target side effects, improve the therapeutic index. The present invention evaluates the antitumor activity of paclitaxel liposome preparations as a model for sarcoma bearing S180 mice, and results show that paclitaxel targeting liposomes have better antitumor activity than the control groups.

【技术实现步骤摘要】

【技术保护点】
具有两亲性的整合素受体靶向锚点化合物，其特征在于，其分子式为：Ａｒｇ－Ｇｌｙ－Ａｓｐ－Ｘ－ＮＨ－Ｃ↓［１６］Ｈ↓［３３］，其中，Ｘ选自缬氨酸残基、丝氨酸残基或苯丙氨酸残基。

【技术特征摘要】

【专利技术属性】
技术研发人员：崔国辉，崔纯莹，付征然，孙怡，
申请(专利权)人：首都医科大学，
类型：发明
国别省市：11[中国|北京]