Preparation and in vitro Release of 5-Fluorouracil-Loaded Chitosan Microspheres for the Intranasal Administration

AIM:To study chitosan used as a carrier,5- fluorouracil as a model drug,the preparation technique and release characteristic of 5- fluorouracil-loaded chitosan microspheres for the intranasal administration.METHOD: 5-Fluorouracil-loaded chitosan microspheres were achieved by emulsion-chemical crosslink technique.The orthogonal experimental design was applied to optimize the preparation procedure.The desirability function was introduced as a total index for the multiple variable of microsphere formulation.The surface morphology of the microspheres was observed by scanning electron microscope.Dynamic dialysis method was used to determine the releasing characteristic of microspheres in vitro and it influencing fators.Swelling behavior was expressed by swelling ratio.RESULT: Microspheres with a good shape and narrow size distribution were prepared.The average diameter was 43.2±4.17 μm.The drug loading was (38.48±1.03)%.The entrappment efficiency was (78.96±1.77)%.The drug release profile in vitro could be described by Higuichi eqution Q=0.1035t 1/2+0.0284(r=0.9965).Drug release was fast at the initial period in parallel to swelling behavior,however,the release was slow at the later time period followed by a diffusion-controlled mechanism. CONCLUSION: The optimized technique has a good reproducibility and a high entrappment efficiency,so it could be used to prepare 5-fluorouracil-loaded chitosan microspheres for the intranasal administration. [