Tumor targeting and pH-responsive nanoparticle system of hydrophobic drugs for liver cancer treatmen

• 作 者: Jinming Zhang Shengpeng Wang Chaomei Fu Meiwan Chen Yitao Wang
• 机 构: State Key Laboratory of Quality Research in Chinese Medicine (University of Macau),Institute of Chin
• 出 处: 2013年“好医生杯”中药制剂创新与发展论坛
• 发表日期: 2013年7期

　　A dual mediated liver tumor targeting polymer constituted with glycyrrhetinic acid (GA)-modified poly(ethylene glycol)-poly-L-histidine-poly(lactic-co-glycolic acid)(GA-PEG-PHIS-PLGA) was synthesized, in which GA contributed as liver target ligand and PHIS devoted as the trigger of tumor slight acid enviornment.Andrographolide (ADG), a diterpenoid lactone isolated from Andrographis paniculata, which exhibited anti-liver cancer activities while extremely hydrophobic character, was chosen as the model drug.Some features of liver targeted nanoparticles(NPs) via self-assembly of amphipathic copolymers including its morphology, diameter, size distribution and in vitro drug release in different pH value buffer were evaluated.The relative changes following pH 7.4 to 5.0 buffer would mean this polymer could be suitable as the drug delivery carriers for the slight acid micro-environment of solid tumor.Additionally, the results of in vitro cell cytotoxicity and cellular uptake studies showed the introduction of GA to the micelles could significantly increase the affinity for human hepatic carcinoma Hep3B cells, which induced a 2;6-fold higher endoeytosis than it for human breast carcinoma MAD-MB-231 cells.These results indicated that this eopolymer would be greatly promising in the chemotherapy of liver cancer due to its GA ligand and acid micro-environment response.