Biomaterials Research Center, Korea Research Institute of Chemical Technology, Yuseong, Daejeon, South Korea.
Colloids Surf B Biointerfaces. 2011 May 1;84(1):82-7. doi: 10.1016/j.colsurfb.2010.12.019. Epub 2010 Dec 30.
Gadolinium (Gd)-based cancer therapeutic liposomes can be used for chemotherapeutics and diagnostics. In this study, dual functional liposomes co-encapsulating doxorubicin (Dox) and Gd were prepared by Dox-transition metal complexation. Preparation conditions were optimized to obtain liposomes containing high concentrations of Dox and Gd. The optimized liposomes Gd250 co-encapsulated 3.6 mM of Dox and 1.9 mM of Gd. The magnetic resonance (MR) properties of Gd250 liposomes were determined using a 4.7 T MR system. Cellular uptake of Dox was determined using a flow cytometer and a confocal microscopy and that of Gd was measured using an inductively coupled plasma-atomic emission spectrometer. Although encapsulated Gd exhibited lower relaxivity than MRbester®, which is widely used for clinical diagnosis, because of limited diffusion across the liposome membrane, Gd250 liposomes showed much higher cellular uptake than that of MRbester®. In Gd250 liposomes, Gd was highly accumulated in B16F10 cells, which could provide improved contrast sensitivity for molecular imaging. Additionally, in Gd250 liposomes, Dox was highly internalized, which could enhance its cancer therapeutic effects. Consequently, we suggest that dual functional liposomes can be used as therapeutic and diagnostic carriers.
基于钆（Gd）的癌症治疗脂质体可用于化疗和诊断。在这项研究中，通过阿霉素（Dox）与过渡金属的配位作用共包封阿霉素（Dox）和 Gd 的双功能脂质体。优化了制备条件，以获得高浓度 Dox 和 Gd 的脂质体。优化的 Gd250 脂质体共包封了 3.6mM 的 Dox 和 1.9mM 的 Gd。使用 4.7T MR 系统测定 Gd250 脂质体的磁共振（MR）性质。使用流式细胞仪和共聚焦显微镜测定 Dox 的细胞摄取，使用电感耦合等离子体质谱仪（ICP-AES）测定 Gd 的细胞摄取。尽管包封的 Gd 的弛豫率低于广泛用于临床诊断的 MRbester®，但由于其在脂质体膜内的扩散受限，Gd250 脂质体的细胞摄取率远高于 MRbester®。在 Gd250 脂质体中，Gd 高度积聚在 B16F10 细胞中，可为分子成像提供更高的对比敏感度。此外，在 Gd250 脂质体中，Dox 高度内化，可增强其癌症治疗效果。因此，我们建议双功能脂质体可用作治疗和诊断载体。
