The effect of two crosslinkers in preparation of chitosan microspheres

摘要

Purpose: To investigate the effect of the two crosslinkers in preparation of 5-fluorouracil-loaded chitosan microspheres. Methods: Using the chitosan as drug carrier, sodium tripolyphosphate and glutaraldehyde as crosslinkers, the liquid paraffin as the oil phase, and span-80 as the emulsifier, 5-fluorouracil-loaded chitosan microspheres were prepared by emulsion-solidification technique. The encapsulation efficiency and the morphous of microspheres were used to evaluate the influence of different formulations and preparation factors. Results: The encapsulation efficiency of 5-fluorouracil-loaded chitosan microspheres was generally between 45% to 55% using glutaraldehyde as the crosslinker. The encapsulation efficiency of the microspheres could reach more than 70% using crosslinkers both glutaraldehyde and sodium tripolyphosphate. The infrared spectra indicated that there was strong intermolecular force between chitosan and 5-FU. This 5-fluorouracilloaded chitosan microsphere had some sustained-release in vitro. Conclusion: The encapsulation efficiency of the 5-fluorouracil-loaded chitosan microspheres was significantlyenhanced using two-step solidification method comparing to one-step solidification method.