正交试验优选羧甲基壳聚糖-醋甲唑胺纳米微球的制备方案

目的：制备羧甲基壳聚糖载药纳米微球,醋甲唑胺为模型药物,测量药物的包封率和纳米微球形态.方法：采用乳化交联法,在微乳液的基础上制备载药纳米微球,对可能影响药物包封率的处方因素进行优化设计,筛选出最优配方.结果：羧甲基壳聚糖溶液的浓度对包封率有显著性影响,三聚磷酸钠溶液浓度和醋甲唑胺药量对包封率未见影响.优化方案的载药纳米微球包封率为49.36％,其电镜下为较规整的球型纳米微球,平均粒径386.0 nm.结论：采用乳化交联法,可形成较高包封率的羧甲基壳聚糖-醋甲唑胺纳米微球.

Otimization on preparation technology of carboxymethyl chitosan-methazolamide nanoparticles by orthogonal design

Objective： To prepare carboxymethyl chitosan （CMC） drug - loaded nanoparticles, with methazolamide as model drug. The drug encapsulation efficiency and morphology should be measured. Methods ： Drug - loaded nanoparticles were preparated in microemulsion by emulsion crosslinking method. The design of formulation factors that may affect the drug entrapment efficiency was optimized to select optimal formulation. Results ： The concentration of carboxymethyl chitosan solution has a significant effect on the entrapment efficiency, when sodium tripolyphosphate （TPP） solution concentration and weight of methazolamide don＇ t effect on the entrapment efficiency. Entrapment efficiency of optimization of drug - Loaded nanoparticles was 49.36%. The nanoparticles is regular and baLL - type, with average particle size in 386.0 nm on electron microscope. Conclusion： Nanoparticles can be formated with hydrophilic carboxymethyl - chitosan coating lipophilic methazolamide by emulsion crosslinking method, and high encapsulation efficiency can be achieved.