【摘要】 本文综述了pH敏感聚合物(pH-sensitive polymer)载体靶向输送抗肿瘤药物的研究进展。肿瘤组织的细胞间质呈弱酸性(pH值<7),而肿瘤细胞内的溶酶体和内涵体具有更强的酸性(pH值4~6)。pH敏感聚合物在酸性介质中能发生质子化或化学反应,使其物理或化学性质发生改变。使用pH敏感型聚合物做成的药物载体能够对肿瘤酸性微环境产生响应,实现药物的快速释放、激活载体的靶向传输功能、促进载体的细胞内吞。大量实验表明,pH敏感型药物载体输送抗肿瘤药物可以明显增加药物在作用部位的浓度,从而饱和肿瘤细胞的多种抗药机制,克服肿瘤细胞的耐药性,提高抗癌药物的治疗效果同时减少其毒副作用。更多还原

【Abstract】 This review presents the state of the art of pH- sensitive polymeric carriers for cancer drug delivery. Solid tumors have a weakly acidic extracellular pH( pH < 7),and cancer cells have even much acidic pH in endosomes and lysosomes( pH 4 ~6). The physical or chemical properties of pH- sensitive polymers can be changed by the occurrence of proton or chemical reaction in acid medium. The drug carriers made of pH- sensitive polymers can respond to the acidic microenvironment of the tumor,which could be utilized to achieve the sharply release of the drug,activate the targeting group and accelerate the endocytosis of drug- loaded polymeric carriers. Various experiments demonstrated that pH- sensitive carriers of antitumor drugs can significantly increase the concentration of the drug in the related fields,overcome the multidrug resistance( MDR) against anticancer drugs of tumor cells,and reduce side effect of cancer chemical therapy.更多还原