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Andrographolide(ADG), a main component in herb Andrographis paniculata, has been identified as one of the most promising anti-tumor agents.However, high hydrophobicity greatly restricts its efficacy and application in cancer therapy.In the present study, PLGA-PEG-PLGA amphipathic copolymers were synthesized by gentle chemical grafting methods to formulate nanoparticles(NPs) for ADG delivery.AGP NPs with a high encapsulation and loading efficiency about 92% and 9% were obtained by optimization.Presenting as inerratic nanospheres in nano solution, the average size, zeta potential and critical micelle concentration of ADG NPs were about 124nm,-13mV and 1.98 x 10-5 g/mL, respectively.In comparison to free ADG, ADG NPs exhibita sustained drug release profilein vitro.More importantly, the enhanced cytotoxic effectsof ADG NPson breast cancer MAD-MB-231 cells were revealed in vitro, after co-incubation with drugs for 24h.Both stronger cell cycle arrest effects at G1 phase and pro-apoptosis effectswere observed in the correspondingconcentration of ADG (15μM) to investigateits potential mechanism.It is also shown that the internalization of NPs could be observed in cytoplasm by laser confocal microscopy.The quantitative results of in vitro cellular uptake showed that after co-incubation for 4h, theintemalization amounts of NPs would significantly more about 2.3 times than that of flee agents, which would contribute to its enhanced efficacy.In a word, these results demonstrated ADG encapsulated in PLGA-PEG-PLGANPs may be a new drug delivery strategy for improving efficacy in cancer therapy.