Institute of Nanobiotechnology, School of Materials Science and Engineering, Tianjin University, Tianjin 300072, PR China; Tianjin Key Laboratory of Composites and Functional Materials, Tianjin 300072, PR China.
Department of Neurosurgery, Laboratory of Neuro-Oncology, Tianjin Medical University General Hospital, Tianjin 300052, PR China.
Int J Pharm. 2012 Apr 15;426(1-2):170-181. doi: 10.1016/j.ijpharm.2012.01.013. Epub 2012 Jan 14.
Polymeric liposomes (PEG/RGD-MPLs), composed of amphiphilic polymer octadecyl-quaternized modified poly (γ-glutamic acid) (OQPGA), PEGylated OQPGA, RGD peptide grafted OQPGA and magnetic nanoparticles, was prepared successfully. These PEG/RGD-MPLs could be used as a multifunctional platform for targeted drug delivery. The results showed that PEG/RGD-MPLs were multilamellar spheres with nano-size (50-70 nm) and positive surface charge (28-42 mV). Compared with magnetic conventional liposomes (MCLs), PEG/RGD-MPLs exhibited sufficient size and zeta potential stability, low initial burst release and less magnetic nanoparticles leakage. The cell uptake results suggested that the PEG/RGD-MPLs (with RGD and magnetic particles) exhibited more drug cellular uptake than non RGD and non magnetism carriers in MCF-7 cells. MTT assay revealed that PEG/RGD-MPLs showed lower in vitro cytotoxicity to GES-1cells at ≤ 100 μg/mL. These data indicated that the multifunctional PEG/RGD-MPLs may be an alternative formulation for drug delivery system.
成功制备了由两亲性聚合物十八烷基季铵化改性聚（γ-谷氨酸）（OQPGA）、聚乙二醇化 OQPGA、RGD 肽接枝 OQPGA 和磁性纳米粒子组成的聚合物脂质体（PEG/RGD-MPLs）。这些 PEG/RGD-MPLs 可用作靶向药物传递的多功能平台。结果表明，PEG/RGD-MPLs 为具有纳米尺寸（50-70nm）和正表面电荷（28-42mV）的多层球体。与磁性常规脂质体（MCLs）相比，PEG/RGD-MPLs 表现出足够的粒径和zeta 电位稳定性、低初始突释和较少的磁性纳米粒子泄漏。细胞摄取结果表明，在 MCF-7 细胞中，具有 RGD 和磁性粒子的 PEG/RGD-MPLs 比非 RGD 和非磁性载体具有更高的药物细胞摄取率。MTT 试验表明，PEG/RGD-MPLs 在≤100μg/mL 时对 GES-1 细胞的体外细胞毒性较低。这些数据表明，多功能 PEG/RGD-MPLs 可能是药物传递系统的替代制剂。
