高等学校化学学报

高等学校化学学报 ›› 2003, Vol. 24 ›› Issue (11): 2103.

• 论文 • 上一篇    下一篇

靶向抗肿瘤药物甲氨喋呤-琥珀酰壳聚糖缀合物的制备及其体外稳定性的初步探讨

王银松, 李英霞, 宋妮, 张华   

  1. 中国海洋大学海洋药物与食品研究所, 青岛 266003
  • 收稿日期:2002-10-14 出版日期:2003-11-24 发布日期:2003-11-24
  • 通讯作者: 李英霞(1964年出生),女,博士,教授,从事糖化学研究.E-mail:liyx417@ouc.edu.cn E-mail:liyx417@ouc.edu.cn
  • 基金资助:

    2002年青岛市科技攻关项目资助

Preparation and in Vitro Stability of Targeting Antitumor Drug: Methotrexate-Succinyl-Chitosan Conjugate

WANG Yin-Song, LI Ying-Xia, SONG Ni, ZHANG Hua   

  1. Institute of Marine Drugs and Food, Ocean University of China, Qingdao 266003, China
  • Received:2002-10-14 Online:2003-11-24 Published:2003-11-24

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被引次数

42

摘要： 报道了甲氨喋呤-琥珀酰壳聚糖缀合物的合成方法,并通过紫外光谱、红外光谱及核磁共振谱进行了结构验证.流式细胞仪的检测结果表明,N-琥珀酰壳聚糖对K562白血病肿瘤细胞具有较强的亲和性;溶解性实验结果表明,甲氨喋呤-琥珀酰壳聚糖缀合物的水溶性较好(pH=1～14);体外释放实验结果表明,缀合物性质稳定,能明显延缓甲氨喋呤的释放,为抗肿瘤药物的靶向及缓控释给药体系的研究提供了初步参考.

关键词: N-琥珀酰壳聚糖, 甲氨喋呤, 靶向抗癌药物, 缓控释

Abstract: Methotrexate-succinyl-chitosan conjugate was synthesized and its structure was confirmed by UV, IR, 1HNMR and 13CNMR.The flow cytometry analysis shows that N-succinyl-chitosan demonstrated a high affinity for K562 leukemia cells.This conjugate was water-soluble in the range of pH1-14, and the dynamic dialysis study shows that the conjugate was stable.These results provided references for the study of targeting, sustained and controlled release delivery systems of antitumor drugs.

Key words: N-Succinyl-chitosan, Methotrexate, Targeting antitumor drug, Sustained and controlled release

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