中国生物工程杂志

Objective To prepare cisplatin polybutylcyanoacrylate stleath nanoparticle (CDDP-PBCA-mPEG ) and observe the different tissue distributions of the nanoparticles in the mice body after the injection via lateral tail vein , and to study the targeting distribution of CDDP-PBCA-mPEG on normal mice livers. Methods CDDP-PBCA-mPEG was prepared by double emulsion method，with the surface modified by methoxypolyethyleneglycol.High-performance liquid chromatography (HPLC) method was established using methyl alcohol and water(55 ：45) as mobile phase；detection was done at 210nm.Sixty mice were randomly divided into 2 groups with 30 mice in each group:non conjugated free CDDP group and CDDP-PBCA-mPEG group, A single dose of either conjugated or free cisplatin equaled 5mg / kg of body weight was delivered via the tail vein. Five mice in each trail were sacrificed at 15 , 30 minutes, 1 ,2，6 and 12 hours after the injection , respectively. The cisplatin concentrations in the collected livers, kidneys, spleens, hearts, lungs and plasma were demonstrated using a high performance liquid chromatography with fluorescence detector. Results The mean diameter of the prepared CDDP-PBCA-mPEG was 170.9 nm；the mean entrapment efficiency of the particles was 60.1% ；and the drug loading rate was 3.88%．The cisplatin concentrations of the mice liver in the experimental groups was significantly higher than those in the control groups( P < 0. 01 ) .The nanoparticle conjugated cisplatin was significantly lower than those in the control groups( P < 0. 01 ) and cleaned up quickly from the kidney tissues. Cisplatin was released slowly in the liver and plasma during the detection period in the experimental groups. Conclusion 　CDDP-PBCA-mPEG has the liver targeting with slow medicine release. It also decreases the medicine distribution in the kidney and other organs. In the treatment of liver cancer, the polybutylcyanoacrylate stleath nanoparticle system has a good liver targeting ability, which increases the anticancer activity and markedly decreases the toxicity of cisplatin.