Departamento de Química Inorgánica y Bioinorgánica, Facultad de Farmacia, Universidad Complutense de Madrid , 28040 Madrid, Spain.
Networking Research Center on Bioengineering, Biomaterials and Nanomedicine , Avenida Monforte de Lemos, 3-5, 28029 Madrid, Spain.
ACS Appl Mater Interfaces. 2017 Aug 16;9(32):26697-26706. doi: 10.1021/acsami.7b06906. Epub 2017 Aug 7.
The development of targeted nanocarriers able to be selectively internalized within tumor cells, and therefore to deliver anti-tumor drugs specifically to diseased cells, constitutes one of the most important goals in nano-oncology. Herein, the development of Janus mesoporous silica particles asymmetrically decorated with two targeting moieties, one of them selective for folate membrane cell receptors (folic acid) and the other one able to bind to mitochondria membrane (triphenylphosphine, TPP), is described in order to achieve sequential cell to organelle vectorization. The asymmetric decoration of each side of the particle allows fine control in the targeting attachment process in comparison with the use of symmetric nanocarriers. The presence of folic acid induces a higher increase in particle accumulation inside tumor cells, and once there, these nanocarriers are guided close to mitochondria by the action of the TPP moiety. This strategy can be applied for improving the therapeutic efficacy of current nanomedicines.
开发能够选择性地被肿瘤细胞内化的靶向纳米载体,并因此将抗肿瘤药物特异性递送至病变细胞,是纳米肿瘤学的最重要目标之一。在此,描述了具有两种靶向部分的不对称装饰的Janus 介孔硅粒子的开发,其中一种部分对叶酸膜细胞受体(叶酸)具有选择性,另一种部分能够与线粒体膜结合(三苯基膦,TPP),以实现顺序的细胞到细胞器的载体化。与使用对称纳米载体相比,粒子各侧的不对称装饰允许在靶向附着过程中进行精细控制。叶酸的存在诱导粒子在肿瘤细胞内的积累增加,一旦进入细胞,这些纳米载体在 TPP 部分的作用下被引导靠近线粒体。该策略可用于提高现有纳米药物的治疗效果。