Martí Del Rio Andrea, Sánchez-García David
Grup d'Enginyeria de Materials, Institut Químic de Sarrià, Universitat Ramon Llull, Via Augusta 390, Barcelona 08017, Spain.
ACS Appl Polym Mater. 2025 Jun 3;7(11):7013-7024. doi: 10.1021/acsapm.5c00608. eCollection 2025 Jun 13.
A potent drug delivery system (DDS) based on poly-(β-amino ester)-s (pBAEs) to tackle multidrug resistance (MDR) in lung cancer by codelivering siRNA targeting antiapoptotic BCL-2 and doxorubicin (DOX) has been prepared. Engineered via strain-promoted azide-alkyne cycloaddition (SPAAC) to attach a tripeptide end-chain moiety and thiol-disulfide exchange to conjugate DOX, the system employs a hydrazone linker for dual pH- and redox-responsive release. This ensures precise tumor targeting with minimal leakage in the circulation. In multidrug-resistant lung cancer cells (GLC-4/ADR), it sharply downregulates BCL-2 expression, amplifying DOX's therapeutic impact.
一种基于聚（β-氨基酯）（pBAEs）的高效药物递送系统（DDS）已被制备出来，该系统通过共递送靶向抗凋亡蛋白BCL-2的小干扰RNA（siRNA）和多柔比星（DOX）来解决肺癌中的多药耐药性（MDR）问题。该系统通过应变促进的叠氮化物-炔烃环加成反应（SPAAC）进行工程改造，以连接一个三肽端链部分，并通过硫醇-二硫键交换来共轭DOX，它采用腙连接子实现pH和氧化还原双重响应释放。这确保了精确的肿瘤靶向性，同时在循环中泄漏最小。在多药耐药肺癌细胞（GLC-4/ADR）中，它能显著下调BCL-2的表达，增强DOX的治疗效果。
Zotero 插件
