| Objective:TO optimize the peparation of new agents major components of traditional Chinese medicine arsenic trioxide (As2O3) and improve the quality of the new formulations of indicators, reduce the toxicity of AS2O3 and to explore its killing effect on EJ cancer, in order to further provide the experimental basis for targeted drug delivery.Methods:The prepartion technology was optimized by orthogonal design on the base of signgle factor experimentation as oil viscosity, W/O, albumin solution concentration, aqueous phase pH, type of curing agent, curing agent, emulsifier, and emulsifying time, curing time and so on. Combination of the actual situation,selected the optimal preparation conditions of new agents that arsenic trioxide albumin nanoparticles (As2O3-BSA-NP), ablumin concentration, PH value of aqueous, formalin, the dose of emulsifier,. stabilization time and the best way to preparate was chosed. Observing nanospheres,particle size by transmission electron microscopy, and arsenic standard curve which was founded by Ag(DCC) method was used to determined DL% and EE%,. Nanospheres were enclosed and stored in the refrigerator (3-5℃) at the room temperature of 37℃,then observing there stability after there month.Preparations for the micropowder, sterilization, strength, stability properties was investigated The As2O3-BSA-NP and arsenic trioxide effect on EJ cells. By MTT method to compare the two drugs for the effection on EJ cell. The apoptosis was proof from morphology by laser confocal microscopeResults:Emulsifieation-heat solidification is the best prepation teehnique for AS2O3-BSA-NS. The four factors affect DF differently, stirring rate behaves as the maximum (P<0.01),followed stabilization time and the W/O volume ratio (P<0.05).However, emulsifier dose not influence DF(P>0.05)The dimaeters of nanospheres were between 50nm and 250nm. The mean dimaeter of them was 100±50nm; the surface was smooth and spherieal and the fluidity was fine.In this experiment,durg loading, encapsulation efficiency and released dgree were investigated. The mean DL% and EE% were 19.8% and 51.3% respectively The release of nanospheres in vitro was investigated by dialysis.The result showed that the release of nanospheres prepared by chemical cross-linked method was slower than those heat-stablization mehtod.The release of nanospheres which prepared by heat-stablization method was 14.98% after 10h.The test of morphology,sterilization,intensity and stability of As2O3-BSA-NP showed that the appearance of As2O3-BSA-NP was smooth and spherical. Sterilization and storage at 4℃,25℃,37℃for 3 months did not obviously change the morphology,DL,Eeand the release rate.Experiment shows that arsenic trioxide albumin nanoparticles drug effect obviously sustained.Preparations of arsenic trioxide enhance the efficacy and the inhibition rate of EJ cell obviously improved.,the highest inhibition rate to the cells can reach 93.1%±3.1%.Apoptosis was display by LSM which was effected by two drugs.Conclusions:The result of the study showed that emulsification-heated solidification method was simple and practicable to prepare the AS2O3-BSA-NP without organic solvents.The low boiling point solvents can be recycled easilyand reduce harmful to the harm of human body. Cleaning solvent, easy recovery of low boiling point ether, reduce the environment pollution.The particle size of nanospheres fits for experiment and the release characteristics was rather slow.The chemotherapeutic drug loaded in sustained release nanospheres on EJ cell proved to be a new potental approach and effective strategy for treating the carcinoma of urinary bladder patients with an important clinical significance.
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