DataSheet1_PSMA-Targeted Supramolecular Nanoparticles Prepared From Cucurbit[8]uril-Based Ternary Host–Guest Recognition for Prostate Cancer Therapy.docx

Nanomedicines play an important role in cancer therapy; however, some drawbacks including unsatisfactory efficacy and side effects arising from indiscriminate drug release retard their clinical applications. Although functionalization of nanomedicines through covalent interactions can improve the pharmacokinetics and efficacy of the loaded drugs, complicated and tedious synthesis greatly limits the exploration of multifunctional nanoparticles. Herein, we utilize a supramolecular strategy to design a nanomedicine for targeted drug delivery through cucurbit[8]uril-based host–guest ternary complexation and successfully prepare prostate-specific membrane antigen (PSMA)-targeted supramolecular nanoparticles encapsulating doxorubicin (DOX). In vitro studies exhibit targeted modification via noncovalent enhance anticancer efficiency of DOX due to the increased cell uptake on account of receptor-mediated endocytosis. This design provides a new strategy for the development of sophisticated drug delivery systems and holds perspective potentials in precise cancer treatments.

纳米药物在癌症治疗中扮演着至关重要的角色；然而，诸如疗效不理想及因药物无差别释放而引发的副作用等不足之处，阻碍了其在临床应用中的推广。尽管通过共价相互作用对纳米药物进行功能化能够提升负载药物的药代动力学和疗效，但复杂的合成过程及繁琐的操作极大地限制了多功能纳米粒子的研究。本研究中，我们采用超分子策略，通过基于葫芦脲的宿主-客体三元复合，设计了一种靶向药物递送纳米药物，并成功制备了针对前列腺特异性膜抗原（PSMA）的超分子纳米粒子，其内封装有阿霉素（DOX）。体外研究显示，通过非共价修饰实现了靶向性，并因受体介导的内吞作用而增加了细胞摄取，从而提高了DOX的抗癌效率。此设计为开发复杂的药物递送系统提供了一种新的策略，并在精准癌症治疗领域展现出巨大的应用潜力。