Drug-resistance and drastic side effects are two major issues of traditional chemotherapy which may result in trail failure even death. Nanoparticle-mediated multidrug combination treatment has been proven to be a feasible strategy to overcome these challenges. In the present study, amphipathic block polymer of methoxyl poly(ethylene glycol)-poly(aspartyl(dibutylethylenediamine)-co-phenylalanine) (mPEG-P(Asp(DBA)-co-Phe)) was synthesized and self-assembled into pH-responsive polymeric vesicle. The vesicle was utilized to co-deliver cancer-associated epidermal growth factor (EGFR) inhibitor of afatinib and DNA-damaging chemotherapeutic doxorubicin hydrochloride (DOX) for enhanced non-small-cell lung cancer (NSCLC) therapy. As evaluated in vitro, the pH-responsive design of nanovesicle resulted in a rapid release of encapsulated drugs into tumor cells and caused enhanced cell apoptosis. In addition, in vivo therapeutic studies were conducted and the results evidenced that the co-delevery of DOX and afatinib using pH-sensitive nanovector was a promising strategy for NSCLC treatment.

耐药性和严重的副作用是传统化学疗法的两个主要问题，可能导致试验失败甚至死亡。纳米粒子介导的多药联合治疗已被证明是克服这些挑战的可行策略。在本研究中，合成了甲氧基聚（乙二醇）-聚（天冬氨酰（二丁基乙二胺）-共-苯丙氨酸）（mPEG-P（Asp（DBA）-共-Phe））的两亲嵌段聚合物，并自组装为pH反应性聚合物囊泡。该囊泡用于共同递送阿法替尼的癌症相关表皮生长因子（EGFR）抑制剂和DNA损伤性阿霉素盐酸盐（DOX），用于增强型非小细胞肺癌（NSCLC）治疗。如体外评估，纳米囊泡的pH响应设计导致封装的药物快速释放到肿瘤细胞中，并导致细胞凋亡增强。此外，进行了体内治疗研究，结果证明使用pH敏感纳米载体共同抑制DOX和阿法替尼是NSCLC治疗的一种有前途的策略。