Centro de Reconocimiento Molecular y Desarrollo Tecnológico, Unidad Mixta Universidad, Politécnica de Valencia-Universidad de Valencia, Camino de Vera s/n, 46022 Valencia, Spain.
Chemistry. 2013 Jan 21;19(4):1346-56. doi: 10.1002/chem.201202740. Epub 2012 Dec 7.
The preparation of a new capped silica mesoporous material, Rh-Azo-S, for on-command delivery applications in the presence of target enzymes is described. The material consists of nanometric mesoporous MCM-41-like supports loaded with Rhodamine B and capped with an azopyridine derivative. The material was designed to show "zero delivery" and to display a cargo release in the presence of reductases and esterases, which are usually present in the colon, mainly due to intestinal microflora. The opening and cargo release of Rh-Azo-S in vitro studies were assessed and seen to occur in the presence of these enzymes, whereas no delivery was noted in the presence of pepsine. Moreover, Rh-Azo-S nanoparticles were used to study controlled Rhodamine B dye delivery in intracellular media. HeLa cells were employed for testing the "non"-toxicity of nanoparticles. Moreover, delivery of the dye in these cells, through internalization and enzyme-mediated gate opening, was confirmed by confocal microscopy. Furthermore, the nanoparticles capped with the Azo group and loaded with a cytotoxic camptothecin (CPT) were also prepared (solid CPT-Azo-S) and used as delivery nanodevices in HeLa cells. When this solid was employed, the cell viability decreased significantly due to internalization of the nanoparticles and delivery of the cytotoxic agent.
描述了一种新型的 capped silica 介孔材料 Rh-Azo-S 的制备,该材料可用于在靶酶存在下进行按需递药应用。该材料由纳米级介孔 MCM-41 样载体负载罗丹明 B 并封端有偶氮吡啶衍生物。该材料被设计为表现出“零传递”,并在存在还原酶和酯酶时显示货物释放,这些酶通常存在于结肠中,主要是由于肠道微生物群。在体外研究中评估了 Rh-Azo-S 的开启和货物释放,发现其仅在存在这些酶的情况下发生,而在胃蛋白酶存在下则没有传递。此外,还使用 Rh-Azo-S 纳米颗粒研究了细胞内介质中罗丹明 B 染料的控制释放。使用 HeLa 细胞测试了纳米颗粒的“非”毒性。此外,通过细胞内吞作用和酶介导的门控开启,通过共聚焦显微镜证实了这些细胞中染料的传递。此外,还制备了用偶氮基团封端并负载细胞毒性喜树碱 (CPT) 的 CPT-Azo-S 纳米颗粒(固体 CPT-Azo-S),并将其用作 HeLa 细胞中的递药纳米器件。当使用这种固体时,由于纳米颗粒的内化和细胞毒性药物的传递,细胞活力显著降低。