Studies On Adriamycin Gelatin Microspheres

Adriamycin (ADM) is used in treatment of lung cancer, but it's toxicity is serious, especial heart toxicity, it's clinical application is confined. So it is necessary to develop a targeting preparation of adriamycin. In this paper, the study was aimed to develop an adriamycin gelatin microspheres (ADM-GMS), which would be lung-targeting with low distribution in other tissues, and would increase curative effect and reduce the side-effect. ADM-GMS was prepared by emulsifying. By using single-factor test and orthogonal test, preparation technology was optimized. The particle size and distribution, appearance, mobility, characters, drug-loading rate and entrapment rate were used to evaluate the quality of the microspheres. The results showed that the particle size and distribution was suitable, quality was stable, drug-loaded and entrapment rate were fine. Dialysis method was used to test the property of microspheres in vitro release. With the ultraviolet and visible spectrophotometry (UV) as the test means, the accumulated release curve of microspheres was studied. The consequence indicated that release of ADM-GMS was fine and was much better than ADM. 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 accumulated release rate were detected for the stability studies. The outcome manifested that microspheres were affected by high temperature and high humidity, and the others were stable for the test, so the adriamycin gelatin microspheres should be stored in place of shady and cool ,dry hermetic. In vivo experiment of ADM-GMS, the high performance liquid chromatography (HPLC) with UV detector was utilized for the determination of adriamycin contention in mice tissues, the results showed that compared with the regular adriamycin solutions, the adriamycin gelatin microsphere was obviously concentrated on lung, and contention of adriamycin in heart tissues were decreased, and the adriamycin could be released slowly.