| Gambogic acid(GA) as one of the good antineoplastic drugs found in the past decades. has been used to heal many cancers. Like many other anticancer drugs, there are difficulties in its clinical administration due to its poor solubility. In order to increase its solubility, In this paper,Nanoparticles of biodegradable polymers such as Poly(D,L-lactic acid) (PLA) was used to prepare Gambogic Acid-Loaded PLA Nanopaticles(GA-PLA-NPs).And the characteristics and inhibitory effect on hepatocellular carcinoma cells HepG2 In vitro has been studied.The gambogic acid-loaded PLA nanoparticles were prepared by a self-emulsion solvent evaporation method. And a single and multi-factor experiment was enhanced to inspect the effect regularity of various factors on the size and process of nanoparticles. The content of Gambogic acid was measured by ultraviolet speetro- photometer.The shape of nanoparticles was observed by transmission electron microscope (TEM).The size distribution and mean diameter were measured by laser particle size analyzer. The entrapment efficiency and content of drug loading were determined by Ultraviolet Spectrophotometer after ultracentrifugation. The Stability and release behavior in vitro was carried out. The acute toxicity was carried out to study the Security of GA-PLA-NPs. The effect of GA and GA-PLA-NPs on the growth of HepG2 cells was evaluated by MIT assay. The growth curve was drawn by means of cell culturing and counting cell number. The morphology was observed by hematoxylin-eoxin staining and phase-contrast microscope.The GA-PLA-NPs prepared Clarify and transparent. The Ultraviolet Spectrophotometer methods for drug concentration measure was accurate and receivable, The RSD of the recovery,precision with-day and between-day are less than 0.6%. It conforms to the request of nanoparticles in the experiment of DL,RY and the recovery. In the single factor experiment, The preparation of GA-PLA-NPs were also effected by the Surfactant, Organic phase, Stirring speed, Stirring time, evaporating temperature, volume ratio of water phase and oil phase ,the content of the PLA,surfactant and GA. Both the increase of the water volume and the content of the PLA can increase the mean diameter of the nanoparticles. In a multi-factors experiment, a homogeneous design was employed to analyze the effect regularity of the ratio GA and PLA, the content of PLA in water phase and the volume ratio of Water phase and oil phase on the mean diameter and the polydispersity coefficient of GA-PLA-NPs. The preparation process adapted to the formulation was as follows: the volume ratio of the aqueous and organic was 1∶1(v/v),the surfactant concentration in aqueous was 0.5%,the PLA concentration in water phase was 70 g/20 mL (w/v), GA∶PLA was 1∶6(w/w).Under TEM observation, the nanoparticles all had a fine spherical shape. GA was adsorpted or mosaiced in the surface of the PLA-NPs. the mean diameter of the GA-PLA-NPs was 51.2 nm.The size of 95% GA-PLA-NPs was in the range 30～70 nm,the amount of the nanoparticles whose size were more than 100nm was less than 1%, The entrapment efficiency and content of drug loading were 98.87 % and 13.3 %,the mean recovery was bigger than 99%,RSD was 3.37%, the GA-PLA-NPs prepared by above conditions has the accelerate, light, cold and hot stability. The release behavior of drug in vitro showed an initial burst effect, subsequently a slower rate stage.The accumulation LD50 of GA-PLA-NPs prepared by above conditions is 26.605 mg/kg, Bigger than the LD50 of GA, Which was 20.000 mg/Kg.Cell experiment results were as follows: compared with the control group, the optical density of 100μg/mL Blank nanoparticles group has no significant effect on cells, GA and GA-PLA-NPs groups both has a significant effect on cancer cells, The IC50 of the GA- PLA- NPs and the GA we drawn were 1.6377, 3.8598μg / mL respectively.The GA-PLA-NPs prepared has a feasibility process, reduced toxicity, has an clear inhibitory effect on tumor, can be used as a new type of pharmaceutical preparations...
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