文献：Preparation and Characterization of Angiopep-2 Functionalized Ginsenoside-Rg3 Loaded Nanoparticles and the Effect on C6 Glioma Cells

作者：Xiaomei Su, Danshen Zhang, Haiwei Zhang, Kaiyan Zhao & Wenshu Hou

相关产品：

PCL10000-PEG2000

PCL12000-PEG2000-MAL

原文摘要：The purpose of this work was to prepare and characterize Angiopep-2

functionalized ginsenoside-Rg3 loaded nanoparticles (ANG-Rg3-NP) and evaluate the therapeutic effect on C6 glioma cells. Nanoparticles were prepared by the emulsion solvent evaporation method. Angiopep-2 was functionalized to nanoparticles via a maleimide-thiol covalent binding reaction to obtain ANG-Rg3-NP. The prepared nanoparticles were evaluated for size, zeta potential, morphology, stability, encapsulation efficiency, loading capacity and

release properties. The cytotoxicity study and targeting effect of ANG-Rg3-NP were

evaluated by MTT assay. The study of cellular uptake in C6 glioma cells was performed by fluorescence microscopy and by using a microplate reader. The prepared ANG-Rg3-NP was observed to be uniformly spherical in shape with a particle size at 147.1±2.7 nm. The encapsulation efficiency and loading capacity reached 80.6±3.0% and 27.2±1.4%, respectively. Additionally, ANG-Rg3-NP exhibited a desirable sustained release behavior. In vitro cytotoxicity study indicated that ANG-Rg3-NP could inhibit the proliferation of C6 glioma cells in a concentration-dependent manner. Also, the functionalization of Angiopep-2 made nanoparticles cross the blood-brain barrier more easily and accelerated the cellular uptake of nanoparticles. The ANG-Rg3-NP was a promising brain drug delivery carrier for the treatment of glioma.

PCL-PEG-MAL是一种聚合物材料，它由聚己内酯（PCL）、聚乙二醇（PEG）和马来酰亚胺（MAL）组成。PCL是一种具有良好生物降解性和机械性能的聚合物，PEG具有良好的水溶性和生物相容性，而MAL则提供了反应活性位点。该产品可用于药物输送系统，利用PCL的可降解性和PEG的亲水性来控制药物释放速率，提高药物的生物利用度。基于此制备Angiopep-2功能化人参皂苷-rg3负载纳米颗粒（ANG-Rg3-NP）。制备过程如下：

图：PCL-PEG的化学结构

采用乳状液溶剂蒸发法制备纳米颗粒

将PCL-PEG（含有PCL-PEG-MAL的重量为1mg，PCL-PEG的重量为4 mg）溶解在二氯甲烷中。接下来，将人参皂苷-rg3溶解在甲醇中。然后将二氯甲烷和甲醇混合作为油相。以胆酸钠溶液作为水相，将油相缓慢滴入水相，然后在冰水浴中超声，直到悬浮液变成白色乳化液。用旋转真空蒸发器除有机溶剂，得到蓝色透明溶液。然后通过膜过滤溶液，去除未加入的人参皂苷-rg3离心，沉淀物用去离子水洗涤两次，用磷酸盐缓冲盐水分散，得到人参皂苷-Rg3纳米颗粒溶液（Rg3-NP）。

图：ANG-Rg3-NP和纳米颗粒穿过血脑屏障和C6 gliomas细胞的制备过程。

结论：制备的ANG-Rg3-NP呈均匀的球形，粒径为147.1±2.7 nm。封装效率和负载能力分别达到80.6±3.0%和27.2±1.4%。此外，ANG-Rg3-NP还表现出了理想的缓释行为。体外细胞研究表明，ANG-Rg3-NP可抑制C6 gliomas细胞的增殖，且呈浓度依赖性。此外，Angiopep-2的功能化使纳米颗粒更容易通过BBB，并加速了细胞对纳米颗粒的摄取。ANG-Rg3-NP是一种很有前途的药物传递载体。