The present invention relates to a conjugate of hydrophilic polymer-multicarboxyl oligopeptide and drug molecule of the following formula:
wherein: P is a water soluble polymer; m is an integer of 2˜12; j is an integer of 1˜6; R
i
is a group selected from H, C
1-12
alkyl, substituted aryl, aralkyl, heteroalkyl and substituted alkyl; X and Z are linking groups; and TA is drug molecule. The conjugate has low toxicity and an ability to carry more than one drug molecule to improve solubility, sustain and control drug release, and has a remarkably enhancing effect especially to antitumor drug such as paclitaxel and camptothecin etc.
本发明涉及一种亲
水聚合物-多羧基寡肽和以下式的药物分子的结合物:
其中:P是
水溶性聚合物;m是2~12的整数;j是1~6的整数;Ri是从H、C1-12烷基、取代芳基、芳基烷基、杂原子烷基和取代烷基中选择的基团;X和Z是连接基团;TA是药物分子。该结合物具有低毒性,并能携带多种药物分子以提高溶解度,维持和控制药物释放,并对
抗肿瘤药物如
紫杉醇和
喜树碱等具有显著增强作用。