Centro di Imaging Molecolare e Preclinico, Dipartimento di Biotecnologie Molecolari e Scienze della Salute, Università di Torino, Via Nizza 52, 10126 Torino, Italia.
Dipartimento di Scienze e Innovazione Tecnologica, Università del Piemonte Orientale "Amedeo Avogadro", Viale T. Michel 11, 15121 Alessandria, Italia.
J Control Release. 2017 Feb 28;248:45-52. doi: 10.1016/j.jconrel.2017.01.010. Epub 2017 Jan 7.
Amphiphilic Janus-dendrimers are able to self-assemble into nanosized vesicles named dendrimersomes. We recently synthesized the 3,5-C-EG-(OH) dendrimer that generates dendrimersomes with very promising safety and stability profiles, that can be loaded with different contrast agents for in vivo imaging. In this contribution, nanovesicles were loaded with both the Magnetic Resonance Imaging (MRI) reporter GdDOTAGA(C) and the glucocorticoid drug Prednisolone Phosphate (PLP), in order to test their effective potential as theranostic nanocarriers on murine melanoma tumour models. The incorporation of GdDOTAGA(C) into the membrane resulted in dendrimersomes with a high longitudinal relaxivity (r=39.1mMs, at 310K and 40MHz) so that, after intravenous administration, T-weighted MRI showed a consistent contrast enhancement in the tumour area. Furthermore, the nanovesicles encapsulated PLP with good efficiency and displayed anti-tumour activity both in vitro and in vivo, thus enabling their practical use for biomedical theranostic applications.
两亲性 Janus 树状大分子能够自组装成纳米尺寸的囊泡，称为树状大分子囊泡。我们最近合成了 3,5-C-EG-(OH) 树状大分子，它生成的树状大分子囊泡具有非常有前景的安全性和稳定性特征，可以负载不同的对比剂用于体内成像。在本研究中，纳米囊泡同时负载了磁共振成像 (MRI) 报告剂 GdDOTAGA(C)和糖皮质激素药物磷酸泼尼松龙 (PLP)，以测试它们作为治疗诊断性纳米载体在小鼠黑色素瘤肿瘤模型中的有效潜力。GdDOTAGA(C)掺入到膜中导致树状大分子囊泡具有高纵向弛豫率（r=39.1mMs，在 310K 和 40MHz 下），因此，静脉给药后，T1 加权 MRI 显示肿瘤区域有一致的对比增强。此外，纳米囊泡以良好的效率包封了 PLP，并在体外和体内均显示出抗肿瘤活性，从而使其能够实际用于生物医学治疗诊断应用。
