焦脱镁叶绿酸-a (PPa)是光动力治疗(PDT)中的第二代光敏剂。但游离的PPa仍存在一些缺陷，导致临床疗效降低，如在生理环境下容易自聚集，在肿瘤组织中积累较差。为了解决这些问题，我们通过溶剂法和自组装的方法构建了一种基于聚烯丙胺盐酸盐(PAH)修饰的以Zr4+为中心离子，2-氨基对二苯甲酸为骨架(Zr-MOF)负载PPa (Zr-MOF-PPa@PAH)的光动力治疗纳米平台。Zr-MOF-PPa@PAH具有良好的包封效率、有效的细胞吸收能力和良好的生物相容性。此外，体外细胞摄取实验表明，Zr-MOF-PPa@PAH纳米材料可以加速PPa药物进入肿瘤细胞核，药物释放行为具有pH敏感性。对人肝癌细胞系HepG-2的MTT检测结果清楚表明，Zr-MOF-PPa@PAH复合材料在光照下能有效导致细胞损伤和凋亡细胞死亡，纳米复合材料能提高PS类药物的PDT抗肿瘤作用，但暗毒作用可以忽略。总之，本研究制备出生物相容性好和全身毒性低的光动力治疗的纳米粒子，提高了光动力疗效。 Pyropheophorbide‐a (PPa) is the second generation photosensitizer in photodynamic therapy (PDT). But free of PPa there are still some defects, which leads to reduced clinical curative effect. For example, it is easy to self-aggregate in the physiological environment and accumulates poorly in the tumor tissue. In order to solve these problems, we constructed a photodynamic therapy nanoplatform based on polyallylamine hydrochloride (PAH) modified with Zr4+ as the central ion and 2-amino p-benzoic acid as the skeleton (Zr-MOF) to support PPa (Zr-MOF-PPa@PAH), by solvent method and self-assembly method. Zr-MOF-PPa@PAH has good encapsulation efficiency, effective cell absorption capacity and good biocompatibility. In addition, the cells in vitro experiments show that the intake Zr-MOF-PPa@PAH nanomaterials can accelerate PPa drugs into the tumor cell nucleus, and drug release behavior is pH sensitive. The results of MTT assay on human hepatoma cell line HepG-2 clearly show that Zr-MOF-PPa@PAH composites under light can cause cell injury and apoptotic cell death, nano composite materials can improve the PDT of PS drugs’ antitumor effect, but the dark poison effect can be ignored. In conclusion, the photodynamic therapy nanoparticles with good biocompatibility and low systemic toxicity were prepared in this study, which improved the photodynamic efficacy.