磷酸川芎嗪羧甲基壳聚糖纳米粒的制备及体外释放研究

目的:制备磷酸川芎嗪羧甲基壳聚糖纳米粒(CMC-TMP-NP),并对其体外释放行为进行研究。方法:采用乳化交联法制备CMC-TMP-NP,以包封率为评价指标,通过正交设计实验对处方和工艺进行优化;通过测定CMC-TMP-NP的包封率、载药量、粒径、形态和体外释放率评价其质量。结果:优选出CMC浓度为4mg/mL、投药比为1:2、交联度为3,进行制备CMC-TMP-NP;制备出的纳米粒粒径分布均匀且表面呈圆整球形,平均粒径为192.6nm、多分散系数为0.219、平均包封率为(85.17±1.25)%、平均载药量为(9.38±1.28)%。结论:实验制备的CMC-TMP-NP包封率高,粒径分布均匀,体外能显著延缓药物释放。

Preparation Technology and In-vitro Release Characteristics of Tetramethylpyrazine Phosphte-loaded Carboxymethyl Chitosan Nanoparticals

Objective:To preparet tetramethylpyrazine phosphte-loaded carboxymethyl chitosan nanoparticals and to investigate the drug release behavior in vitro.Methods:CMC-TMP-NP were prepared by the emulsion crosslinking method.The encapsulation efficiency was used to evaluate the influence of different formulation and preparation factors;the formulation was optimized by orthogonal design.The quality of CMC-TMP-NP was evaluated by determining the entrapment efficiency,the loading capacity,particle size,the morphology and the release in vitro.Results:The concentration of CMC was 4mg/mL,the dosing ratio was 1:2,the degree of cross linking was 3;the optimized nanoparticals had a spherical shape,the average diameter was 192.6nm,the PDI was 0.219,the loading capacity was(85.17±1.25)%,the entrapment efficiency was(9.38±1.28)%.Conclusion:The CMC-TMP-NP with promising encapsulation efficiency,nanometeric sizes and delayed drug release in vitro.