pH响应性的虾青素壳聚糖微球制备及应用

Preparation and in vitro release of pH-responsive astaxanthin chitosan microspheres

摘要:

以氯乙酸和壳聚糖为原料，通过N,O-羧甲基化化学改性方法制备了水溶性羧甲基壳聚糖，并以此为原料通过乳液法制备羧甲基壳聚糖微球和羧甲基壳聚糖负载虾青素微球。考察了羧甲基壳聚糖微球的形态、分散性和粒径。结果表明，微球最佳制备条件为：羧甲基壳聚糖含量（以水相即去离子水质量为基准，下同）1.0%，油水体积比1∶1，表面活性剂Span 80含量（以油相即液体石蜡体积为基准，下同）4.0%，交联剂戊二醛含量（以油相即液体石蜡体积为基准，下同）7.5%，剪切速率4000 r/min。红外测试表明，微球成功负载虾青素，在虾青素初始添加量为20mg的载药率和包封率分别为10.74%和67.24%。在模拟胃液和模拟肠液中，负载虾青素微球的释放率分别为10%和85%。羧甲基壳聚糖可以用作药物载体。

Abstract:

Water-soluble carboxymethyl chitosan was prepared by chemical modification of N,O- carboxymethyl chitosan with chloroacetic acid and chitosan as raw materials. Carboxymethyl chitosan microspheres and carboxymethyl chitosan microspheres loaded with astaxanthin were prepared by emulsion method. The morphology, dispersion and particle size of carboxymethyl chitosan microspheres were investigated. The results show that the optimal preparation conditions of microspheres are as follows: The content of carboxymethyl chitosan (based on water phase mass, the same below) was 1.0%, the volume ratio of oil to water was 1∶1, the content of Span 80 (based on oil phase volume, the same below) was 4.0%, the content of glutaraldehyde (based on oil phase volume, the same below) was 7.5%, and the shear rate was 4000 r/min., IR test showed that the microspheres were successfully loaded with astaxanthin, and the loading rate and encapsulation rate were 10.74% and 67.24%, respectively, when the initial astaxanthin dosage was 20mg.The release rates of astaxanthin microspheres loaded in simulated gastric juice and simulated intestinal juice were 10% and 85%, respectively. Carboxymethyl chitosan can be used as a drug carrier.