Construction of 5-Fluorouracil Delivery System Based on Chitosan/Poly(Vinyl Alcohol) Complex Hydrogel with Built-in Composite Microspheres of Gelatin and PLGA
ZHU Xiao-jing，QIU Li-yan，ZHU You-fen，JIN Yi
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College of Pharmaceutical Science，Zhejiang University，Hangzhou 310058，China
OBJECTIVE To develop a 5-fluorouracil(5-Fu) sustained delivery system based on chitosan/poly(vinyl alcohol)(PVA) complex hydrogel with built-in gelatin-PLGA composite microspheres.METHODS 5-Fu loaded gelatin microspheres were prepared by emulsification-chemical crosslinking method then incorporated into PLGA matrix by oil-in-oil emulsification extraction technique to obtain the composite microspheres.The shape,size,the encapsulation efficiency of 5-Fu,and in vitro drug release profiles of prepared microspheres were investigated.Chitosan/PVA hydrogels were prepared by freeze-thaw circle method.5-Fu release profiles from gelatin-PLGA microspheres entrapped in chitosan/PVA hydrogels were investigated.RESULTS The composite microspheres were in good shape and the encapsulation efficiency of 5-Fu was over 85%.The burst release was decreased while the polymer concentration was increased and drug loading was decreased.The in vitro release profile of 5-Fu composite microspheres with low drug content was fitted with first-order kinetic equation while that of 5-Fu composite microspheres with high drug content was discribed by Higuchi equation.Moreover,the release profiles were manipulated by regulating the concentration of PLGA in the composite microspheres.The burst effect was ameliorated by entrapping the composite microspheres into chitosan/PVA hydrogels.CONCLUSION By the combination of gelatin-PLGA composite microspheres and chitosan/PVA hydrogel,a controlled delivery system for 5-Fu was developed.This drug delivery system prepared by composite microspheres into chitosan/PVA hydrogels has the potential use in early entrapping intraperitoneal chemotherapy for advanced gastrointestinal carcinoma.
ZHU Xio-jing;QIU Li-yn;ZHU You-fen;JIN Yi.
Construction of 5-Fluorouracil Delivery System Based on Chitosan/Poly(Vinyl Alcohol) Complex Hydrogel with Built-in Composite Microspheres of Gelatin and PLGA [J]. Chinese Pharmaceutical Journal, 2008, 43(11): 844-847
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