肿瘤靶向载体N-正辛基-N′-琥珀酰基壳聚糖的制备和结构表征

Preparation and characterization of N-octyl-N'-succinyl chitosan as a tumour-targeting carrier

目的:对壳聚糖的结构进行修饰,制备N-正辛基-N′-琥珀酰基壳聚糖。方法:以壳聚糖为原料,通过与正辛醛、丁二酸酐反应,在其2位氨基引入琥珀酰基和正辛基。产物用FTIR、1HNMR、元素分析对其进行表征。用粉末X-衍射、DSC、TG对其物理性质进行分析,并初步考察了其对K562肿瘤细胞的亲和性。结果:合成了N-正辛基-N′-琥珀酰基壳聚糖,其结晶程度下降,水溶性增加,与K562肿瘤细胞亲和性较好。结论:N-正辛基-N′-琥珀酰基壳聚糖可作为新型肿瘤靶向载体。

Aim： To prepare N-octyl-N＇-succinyl chitosan by the chemical modification of chitosan. Methods： By using aldehyde and succinic anhydride incorporated with the amino group of chitosan, N-octyl-N＇-succinyl chitosan was synthesized. The chemical structure of synthesized N-octyl-N＇-succinyl chitosan was characterized by FHR, ^1 H NMR and elemental analysis. Some of the physical properties were measured by X-ray powder diffraction DSC and TG. Moreover, the affinity of N-octyl-N＇-succinyl chitesan for K562 leukemia cells was evaluated. Results： Novel Noctyl-N＇-succinyl chitosan had been synthesized with the decrease in the degree of crystallization and improve in the water-solubility. The affinity of N-octyl-N＇-succinyl chitosan to K562 leukemia cells was fairly high. Conclusion： Noctyl-N＇-succinyl chitosan could be a potential tumour-targeting carrier.