Studies On Cisplatin Diatrizoate Gelatin Microspheres Of Bronchial Artery Embolization

Cisplatin(CDDP) is a wide antitumor drug .It is used in treatment of lung cancer, by vein injection. However,it's toxicity is serious, especial kidney toxicity, it's clinical application is confined. In this paper, the study was aimed to develop an cisplatin diatrizoate gelatin microspheres (CDDP-DTZ-GMS), which would be lung-targeting with low distribution in other tissues, and would increase curative effect and reduce the side-effect,and would manufacture some kinds of solid embolism materials that could develop under the X-ray,and so that CDDP-DTZ-GMS can be used for the embolization and chemical theraphy.CDDP-DTZ-GMS was prepared by emulsifying. By using single-factor test and the uniformity design,preparation technology was optimized. The particle size and distribution, appearance, mobility, characters, solution,suspension,drug-loading rate and entrapment rate were used to evaluate the quality of the microspheres. The results showed that the microspheres are yellow,flowable,stable.Globular powder good fluidity was obtained by scanning electron microscope.Examination usingscanning electron photomicrographs showed spherical particles size was90.8%.μmwith 91.2% of the microspheres being in the range of 45~150μm.The average drug loading and the average incorporation efficiency were 17.2%and 72.1%respectively. Development of CDDP-DTZ-GMS were studied by evaluating their physical and chemical characteristic,drug-loading of diatrizoate or harium sulfate,in vitro release and taking pictures under X-ray. The outcome manifested that CDDP-DTZ-GMS of containing high lever of developable materials,could be seen under X-ray clearly. Dialysis method was used to test the property of microspheres in vitro release and release mechanism With the high performance liquid chromatography (HPLC) as the test means, the accumulated release curve of microspheres was studied.The cisplatin release behavior from microspheres in vitron could be described by double phase dynamic model.The release mechanism was erosion and diffusion. The Cisplatin stuff release profiles in viro could be described by first order dynamic model.Experiments in vitro indicat that the CDDP-DTZ-GMS havea goodsustained release efficiency CDDP.The initial stability test of microspheres was studied. Influencing factors, including temperature and humidity were investigated. Accelerated test and long-term test were also conducted.Appearance of microspheres, mobility, content determination and development were detected for the stability studies. The outcome manifested that the microspheres were ffected by high temperature and high humidity, and the others were stable for the test, the microspheres...