Preparation And Drug Releasing Evaluation Of Chitosan-5-fluoruracil Drug-polymer Conjugates In Vitro

As a focus of current research in the field of targeted drugs, drug-polymer conjugatescan couple drugs on the polymeric based on chemical bonding in order to control therelease of drugs. In this paper, carboxymethyl chitosan drug-polymer conjugates,succinylated chitosan-5-fluorouracil, LA-Chitosan/5-fluorouracil (LA-CTS-5FuCOOH) andFA-Chitosan/5-fluorouracil (FA-CTS-5FuCOOH) of three targeting drug-polymer conjugateswere synthesized using chitosan (CTS) as drug carrier,5-fluorouracil (5-Fu) as drug model.1Carboxymethyl chitosan-5-fluorouracil drug-polymer conjugates (CMCS-5FuOH)was synthesized using carboxymethyl chitosan as drug carrier,5-fluorouracil (5-FuOH) asdrug model. The drug loading efficiency was13.4%.The chemical structure and crystallization behavior of the obtained samples werecharacterized infrared spectroscopy (IR), nuclear magnetic resonance (1H-NMR) and X-raypowder diffraction (XRD). The grafting rate of5-FuOH and the in vitro release performancewas analyzed by ultraviolet spectrum (UV). The results indicated that SUCS and5-FuOHwere chemically bonded through ester linkage, and CMCS-5FuOH had good releaseproperties in different pH mediums.2Succinylated chitosan-5-fluorouracil drug-polymer conjugates (SUCS-5FuOH) wasprepared using succinylated chitosan (SUCS) as drug carrier,5-fluorouracil (5-FuOH) as drugmodel, DCC as condensation agent and4-dimethyl-aminopyridine (DMAP) as catalyst. Thechemical structure, thermal stability and crystallization behavior of the obtained sampleswere characterized infrared spectroscopy (IR), nuclear magnetic resonance (1H-NMR),thermal gravimetric analysis (TG) and X-ray powder diffraction (XRD). The grafting rate of5-FuOH and the in vitro release performance analyzed by ultraviolet spectrum (UV). Theresults indicated that SUCS and5-FuOH were chemically bonded through ester linkage, thegrafting rate of SUCS-5FuOH was18.7%, and it had good sustained-release performance under the condition of simulated body fluids and enzymes.3FA-CTS-5FuCOOH and LA-CTS-5FuCOOH liver targeting drug-polymer conjugateswas prepared using CTS as coupled drug carrier, carboxymethyl-5-fluorouracil (5-FuCOOH)as drug model, folic acid (FA) and lactobionic acid (LA) as target group material, which thedrug loading efficiency was4.5%. Infrared spectroscopy (IR), nuclear magnetic resonancespectroscopy (1H-NMR) and X-ray powder diffraction (XRD) were utilized to confirm itschemical structure, and The grafting rate of5-FuCOOH was analyzed by ultraviolet spectrum(UV).