京尼平交联制备5-fu-壳聚糖微球及其体外释放研究-preparation and in vitro release of 5 - fu - chitosan microspheres crosslinked by genipin.docxVIP

AbstractDrug-loaded chitosan microsphere was prepared when genipin was crosslinking agent and 5-Fu was model drug. To date, chitosan is the only positively charged dietary fiber and natural basic polysaccharide with properties as biological adhesion, biocompatibility, non-toxic, biodegradable, stong targeting. In this paper, genipin was chosen as crosslinking agent with good biocompatibility, low toxicity. And genipin can not easily be rapidly degraded. So it replaces the traditional chemical crosslinkers. The traditional mode of adminstration of drugs was changed, it entered body in the form of microsphere. It avoided the shortcoming of common oral administration of drugs that was likely to stimulate the gastrointestinal tract.This paper studied the preparation of drug-loaded chitosan microsphere by W/O emulsion dispersion. And the best conditions were found through by single factor and orthogonal experiment. The optimum conditions of chitosan drug-loaded microsphere as followed. The dosage of chistan, Secretary Ban-80 and Tween-20 were 0.090g, 0.80g and 0.060g, respectively. The mass ratio of chitosan and genipin and 5-Fu was 1.0:0.20:0.60. The other optimum conditions were found that magnetic stirrer speedwas 600rpm, the reaction time was 3h, the temperature of reaction was 35℃，theemulsification time was 1.5h, mass fraction of acetic acid was 2.0%, the concentration of CS acetic acid was 30g/L, and the ratio of O/W was 40:3.0.The samples pepared in optimum conditions were characterized, and the results showed that, the appearance of chitosan was sphere, the particle size distribution was uniform, the dispersion was good, the surface of the blank microsphere was smooth. The range of particle size was from 40nm to 60nm. Drug loading, encapsulation efficiency and in vitro release were analyzed by UV spectrophotometry. Afer determination we found that the drug loading and encapsulation efficiency of microsphere and the reaction temperature, the