Palomba Francesco, Genovese Damiano, Rampazzo Enrico, Zaccheroni Nelsi, Prodi Luca, Morbidelli Lucia
Dipartimento di Chimica "Giacomo Ciamician", Alma Mater Studiorum, Università di Bologna, Via Selmi 2, 40126 Bologna, Italy.
Dipartimento di Scienze della Vita, Università di Siena, Via A. Moro 2, 53100 Siena, Italy.
ACS Omega. 2019 Aug 14;4(9):13962-13971. doi: 10.1021/acsomega.9b01699. eCollection 2019 Aug 27.
Silica nanostructures are widely investigated for theranostic applications since relatively mild and easy synthetic methods allow the fabrication of multicompartment nanoparticles (NPs) and fine modulation of their properties. Here, we report the optimization of a synthetic strategy leading to brightly fluorescent silica NPs with a high loading ability, up to 45 molecules per NP, of Sorafenib, a small molecule acting as an antiangiogenic drug. We demonstrate that these NPs can efficiently release the drug and they are able to inhibit endothelial cell proliferation and migration and network formation. Their lyophilization can endow them with long shelf stability, whereas, once in solution, they show a much slower release compared to analogous micellar systems. Interestingly, Sorafenib released from Pluronic silica NPs completely prevented endothelial cell responses and postreceptor mitogen-activated protein kinase signaling ignited by vascular endothelial growth factor, one of the major players of tumor angiogenesis. Our results indicate that these theranostic systems represent a promising structure for anticancer applications since NPs alone have no cytotoxic effect on cultured endothelial cells, a cell type to which drugs and exogenous material are always in contact once delivered.
由于相对温和且简便的合成方法能够制备多室纳米颗粒(NPs)并对其性质进行精细调控,二氧化硅纳米结构在诊疗应用方面受到了广泛研究。在此,我们报告了一种合成策略的优化,该策略可制备出具有高负载能力的明亮荧光二氧化硅 NPs,每个 NPs 最多可负载 45 个索拉非尼分子,索拉非尼是一种具有抗血管生成作用的小分子药物。我们证明这些 NPs 能够有效释放药物,并且能够抑制内皮细胞的增殖、迁移和网络形成。它们的冻干处理可赋予其长期的储存稳定性,然而,一旦处于溶液中,与类似的胶束系统相比,它们的释放速度要慢得多。有趣的是,从普朗尼克二氧化硅 NPs 中释放出的索拉非尼完全阻止了内皮细胞反应以及由血管内皮生长因子引发的受体后丝裂原活化蛋白激酶信号传导,血管内皮生长因子是肿瘤血管生成的主要参与者之一。我们的结果表明,这些诊疗系统是抗癌应用中一种很有前景的结构,因为单独的 NPs 对培养的内皮细胞没有细胞毒性作用,而内皮细胞是药物和外源性物质给药后始终会接触到的一种细胞类型。