药物缓释载体烷基化壳聚糖的性能研究
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刘利萍，鲁越青
(绍兴文理学院 化学系， 浙江 绍兴 312000)
摘要：目的 对壳聚糖进行烷基化改性，制备药物缓释载体材料。方法 在碱性介质中，卤代烷与壳聚糖分子中的氨基反应得到烷基化壳聚糖，并测定其对模型药物5-Fu的渗透性能。结果 在反应温度40～60 ℃、反应2～4 h，随着卤代烷链长的增长其取代度也提高，乙基壳聚糖、庚烷基壳聚糖和十六烷基壳聚糖的取代度分别为7.3%、17.0% 和68.1%。IR谱数据表明，取代反应主要发生在壳聚糖分子的氨基上。在pH≤7.4的缓冲溶液中，烷基化壳聚糖膜对5-Fu的渗透系数的影响随着烷基链长的增长而减小。结论 烷基化壳聚糖对5-Fu的缓释作用优于壳聚糖。
关键词：药剂学；药物载体；烷基化壳聚糖；取代度；渗透系数
中图分类号：R94 文献标识码：A
Study on properties of alkyl-modified chitosan as drug carrier
LIU Li-ping, LU Yue-qing
(Department of Chemistry, Shaoxing Arts and Sciences College, Shaoxing 312000, China)
Abstract: Objective To modify chitosan with alkyl halides to be used as sustained-release drug carrier. Method N-alkyl chitosan was prepared by introducing alkyl groups into the amine groups of chitosan via Schiff 's base intermediates under alkaline condition. Result Under same conditions of preparation, namely reaction temperature 40～60 ℃ and time 2～4 h, the more carbon chain length of alkyl-groups were, the more substitution degrees of N-alkyl chitosan were. They were 7.3%, 17.0% and 68.1% for N-ethyl, N-heptyl and N-cetyl chitosan respectively. The permeability coefficient of N-alkyl chitosan films for model drug 5-Fu decreased with increasing the carbon chain length of the alkyl substituent in PBS solution of pH≤7.4, and that of same N-alkyl chitosan film decreased with increaseing pH of PBS solution. Conclusion The decrease of permeability coefficient could be ascribed to the increased hydrophobic properties of alkyl-chitosan.
Key words: pharmaceutics; drug carrier; alkyl-modified chitosan; substitution degree; permeability coefficient
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