Synthesis of targeted drug delivery system for fluorouracil using sulfadiazine as the carrier.
OBJECTIVE
To synthesize a targeted drug delivery system for 5-fluorouracil (5Fu) using sulfadiazine (SF) as a carrier with reduced side-effects and strong antitumor activity.


METHODS
SF-poly (ethylene glycol) (PEG) conjugate was initially synthesized. 5Fu was subjected to reaction with trichloromethyl chloroformate to prepare chloroformyl 5Fu, which was linked to a spacer hydroxyl group of PEG that served as a macromolecular linking arm between SF and 5Fu. The content of 5Fu in the conjugate was determined by ultraviolet spectrophotometry. Spectrum of ultraviolet and infrared along with differential scanning calorimetry were employed to identify the structure of the conjugate of SFPEG-end capped 5Fu.


RESULTS
The drug loading content of the conjugate was 3.2 %, and structural analysis confirmed the linkage between 5Fu and SF via PEG.


CONCLUSIONS
Targeted drug delivery system for 5Fu using SF as a carrier has been successfully synthesized by this means.
Hu
Xi-Gang
XG
Department of Oncology, Zhujiang Hospital, First Military Medical University, Guangzhou 510282, China.
Wang
Sen-Ming
SM
Zhang
Qi-Xing
QX
Cao
Man-Ming
MM
Lu
Yang
Y
D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry; D004337:Drug Carriers; D016503:Drug Delivery Systems; D019855:Ethylene Glycol / Q000737:chemistry; D005472:Fluorouracil / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry; D013056:Spectrophotometry, Ultraviolet; D013411:Sulfadiazine / Q000737:chemistry*
D000964:Antimetabolites, Antineoplastic; D004337:Drug Carriers; C470226:schSFPEG 5-fluorouracil; D013411:Sulfadiazine; D011092:Polyethylene Glycols; D019855:Ethylene Glycol; D005472:Fluorouracil