Hu Xi-Gang, Wang Sen-Ming, Zhang Qi-Xing, Cao Man-Ming, Lu Yang
Department of Oncology, Zhujiang Hospital, First Military Medical University, Guangzhou 510282, China.
Di Yi Jun Yi Da Xue Xue Bao. 2002 Nov;22(11):1042-4.
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.
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.
The drug loading content of the conjugate was 3.2 %, and structural analysis confirmed the linkage between 5Fu and SF via PEG.
Targeted drug delivery system for 5Fu using SF as a carrier has been successfully synthesized by this means.
以磺胺嘧啶（SF）为载体合成一种用于5-氟尿嘧啶（5Fu）的靶向给药系统，以降低副作用并增强抗肿瘤活性。
首先合成SF-聚乙二醇（PEG）共轭物。使5Fu与双光气反应制备氯甲酰基5Fu，其与PEG的间隔羟基相连，PEG作为SF与5Fu之间的大分子连接臂。通过紫外分光光度法测定共轭物中5Fu的含量。采用紫外光谱、红外光谱以及差示扫描量热法鉴定SF-PEG封端5Fu共轭物的结构。
共轭物的载药量为3.2%，结构分析证实了5Fu与SF通过PEG相连。
通过这种方法成功合成了以SF为载体的5Fu靶向给药系统。
