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EPR效应是指实体瘤的高通透性和滞留效应,通过EPR效应可实现纳米药物对肿瘤的靶向治疗,目前靶向抗癌药物的设计即基于此。理想的基于EPR效应靶向肿瘤药物的设计应包括三个关键点:在血液循环中稳定存在;选择性肿瘤部位蓄积(EPR效应);肿瘤细胞对活性药物的主动吸收。据此,我们研发了N-(2-羟丙基)甲基丙烯酰胺(HPMA)和吡柔比星(THP)的聚合物P-THP,二者经腙键连接。该聚合物在体内具有更长的循环时间,因而可以更
The EPR effect refers to the high permeability and retention effect of solid tumors. Targeted therapies of the drugs by the EPR effect can be realized by the EPR effect. At present, the design of the targeted anticancer drugs is based on this. The ideal design of a targeted oncology drug based on the EPR effect should include three key points: stable presence in blood circulation; selective tumor site accumulation (EPR effect); and active recruitment of active drug by tumor cells. Accordingly, we developed polymer P-THP of N- (2-hydroxypropyl) methacrylamide (HPMA) and pirarubicin (THP), both of which are hydrazone-linked. The polymer has a longer cycle time in the body and can therefore be more