a Grup d'Enginyeria de Materials (GEMAT), Institut Químic de Sarrià , Universitat Ramon Llull , Barcelona , Spain.
b Centro de Investigación Biomédica en Red en Bioingeniería , Biomateriales y Nanomedicina (CIBER-BBN) , Zaragoza , Spain.
Drug Deliv. 2018 Nov;25(1):1137-1146. doi: 10.1080/10717544.2018.1472678.
A dual doxorubicin/camptothecin (DOX/CPT) pH-triggered drug delivery mesoporous silica nanoparticle (MSN)-based nano-vehicle has been prepared. In this drug-delivery system (DDS), CPT is loaded inside the pores of the MSNs, while DOX is covalently attached to the surface of an aldehyde-functionalized MSN through a dihydrazide-polyethylene glycol chain. Thus, DOX and the linker act as pH-sensitive gatekeeper. The system is versatile and easy to assemble, not requiring the chemical modification of the drugs. While at physiological conditions the release of the drugs is negligible, at acidic pH a burst release of DOX and a gradual release of CPT take place. In vitro cytotoxicity tests have demonstrated that this DDS can deliver efficiently DOX and CPT for combination therapy.
一种双阿霉素/喜树碱（DOX/CPT）pH 触发药物输送介孔硅纳米粒子（MSN）基纳米载体已被制备。在这个药物输送系统（DDS）中，CPT 被装载在 MSNs 的孔内，而 DOX 通过二酰肼-聚乙二醇链共价连接到醛功能化 MSN 的表面。因此，DOX 和连接物充当 pH 敏感的门控物。该系统具有多功能性且易于组装，不需要对药物进行化学修饰。在生理条件下，药物的释放可以忽略不计，而在酸性 pH 值下，DOX 会爆发释放，CPT 则会逐渐释放。体外细胞毒性试验表明，这种 DDS 可以有效地输送 DOX 和 CPT 进行联合治疗。
