ABSTRACT
Objective: To study the preparation technique and release characteristic of 5- fluorouracil-loaded chitosan microspheres for the intranasal administration. Methods:Using the liquid paraffin as the oil phase,and span-80 as the emuifier; 5- fluorouracil-loaded chitosan microspheres were achieved by emulsion-chemical crosslink technique. The orthogonal experimental design was applied to optimize the preparation procedure. 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.The degree of mucoadhesion was investigated by determining the mucociliary transport rate(MTR) of the microparticle across a frog palate. Results: Microspheres with a good shape and narrow size distribution were prepared. The average diameter was (43?4) ?m. The drug loading was 38.5%? 1.0%. The entrapment efficiency was 79.0%?1.8%.The drug release profile in vitro could be described by Higuichi eqution Q=0.1035t 1/2 +0.0284 (r=0.9965). Chitosan had good mucoadhesive property and caused a siginificant reduction in MTR(P
ABSTRACT
0.1%EDTA≈5% HP ? CD≈1%lecithin. Conclusion: The three methods have good correlation.