Abstract: N-[(2-hydroxy-3-trimethylammonium) propyl] chitosan chloride (HTCC) was synthesized by quaternisation and the folate group was conjugated on the N-quarternary ammonium chitosan. The target product was characterized by FTIR and 1H NMR. The result showed that both HTCC and FA-HTCC had good water solubility. Particle size and zeta potential were 188 nm and 15.4 mV at N/P ratio of 4. In contrast with other carriers, FA-HTCC had comparatively high transfection efficiency and low cytotoxicity on Hela cells in vitro.

Key words: chitosan, quaternized, folate, gene delivery

摘要： 首先对壳聚糖进行季铵化改性合成N-季铵化壳聚糖（HTCC），再接枝叶酸基团制备了叶酸偶联N-季铵化壳聚糖（FA-HTCC），用FTIR和1H NMR等对产物进行表征，并对其作为基因载体进行研究。结果表明，合成产物具有较好的水溶性，N/P为4的FA-HTCC/DNA复合物粒径为188 nm、Zeta电位为15.4 mV。与PEI和阳离子脂质体相比，FA-HTCC具有更低的细胞毒性和更高的转染效率。

关键词: 壳聚糖, 季铵化, 叶酸, 基因载体