新型生物黏附性材料巯基壳聚糖的合成与表征

巯基聚合物利用二硫键的形成, 以共价键黏附于黏膜表面, 可以延长药物在黏膜上的滞留时间, 有利于药物分子的吸收. 本文合成了一种新型巯基聚合物——N-乙酰基-L-半胱氨酸-g-壳聚糖(CS-NAC), 并进行了表征, 同时对材料的溶胀度、黏附性和细胞毒性进行了测试. 结果表明, 这种巯基聚合物具有较高的巯基含量, 最高可达到589.3 μmol/g; 具有快速的溶胀性能; 黏附性显著增强, 黏附时间和黏附力分别是壳聚糖的30和3倍; 无明显的细胞毒性. 因此, CS-NAC是一种很有应用前景的生物黏附性材料.

Synthesis and Characterization of Novel Bioadhesive Material Thiolated Chitosan

The use of mucoadhesive thiolated polymers as the carriers can improve the adsorption of drugs by prolonging the residence time on the nasal mucosa on the basis of the formation of disulphide bonds between thiol groups on polymer and cysteine-rich domains of mucus glycoproteins. In this study, a novel thiolated polymer, N-acetyl-L-cysteine-g-chitosan conjugate(CS-NAC) was synthesized and characterized. Swelling and mucoadhesive properties of CS-NAC conjugates were evaluated in vitro. The cytotoxicity of CS-NAC conjugates was measured on L-929 mouse fibroblast cells by utilizing MTT method. The obtained CS-NAC conjugate displayed the most content of thiol group (589.3±38.6) μmol/g. The conjugates exhibited a fast swelling behavior in comparison to the unmodified chitosan. The mucoadhesive properties of CS-NAC conjugate showed more than 30-fold increase in mucoadhesion time and 3-fold increase in adhesive force versus the unmodified chitosan. Moreover, CS-NAC did not cause a significant increase in cytotoxicity. Therefore, the novel thiolated chitosan is a promising potential bioadhesive material.