叶酸修饰黄连总生物碱壳聚糖纳米粒处方优化

Formulation Optimization of Coptis Chinensis Total Alkaloid Chitosan Nanoparticles Modified by Folic Acid

目的:优化叶酸修饰黄连总生物碱壳聚糖纳米粒的制备工艺,并对其进行质量评价。方法:采用离子交联法制备叶酸修饰黄连总生物碱壳聚糖纳米粒,在单因素考察的基础上,通过星点设计-效应面法优化处方并验证。结果:最佳处方工艺为2.0 mg·ml-1的壳聚糖溶液4.75 ml,pH 4.52,黄连总生物碱加入量0.54 mg。制备出的纳米粒平均粒径为(245.6±17.9) nm(n=3),PDI(0.323±0.027)(n=3),包封率(74.36±4.76)%(n=3),Zeta电位(27.8±4.36) mV(n=3)。体外释放试验显示,普通纳米粒和叶酸修饰纳米粒在12 h内累计释放率为83.69%、81.95%。结论:成功制备出叶酸修饰的黄连总生物碱壳聚糖纳米粒且纳米粒的理化性质较为理想。

Objective: To optimize the preparation technology of folic acid modified Coptis chinensis total alkaloid chitosan nanoparticles and evaluate the quality. Methods: Coptis chinensis total alkaloid chitosan nanoparticles were prepared by an ion crosslinking method. On the basis of single factor investigation,the formulation and preparation process were optimized by central composite designresponse surface methodology followed by verification. Results: The optimal formulation process was as follows: 2.0 mg·ml-1 chitosan solution was 4.75 ml,the p H was 4.52,and the added amount of Coptis chinensis total alkaloid was 0.54 mg. The size and the entrapment efficiency of Coptis chinensis total alkaloid chitosan nanoparticles were promising with the average particle size of( 245.6±17.9)nm,the PDI of( 0.323±0.027),the encapsulation efficiency of( 74.36±4.76) %( n = 3),and the zeta potential of( 27.8±4.36) m V( n= 3). The in vitro release test showed that the cumulative release rate of the common nanoparticles and folic acid modified nanoparticles respectively was 83.69% and 81.95% within 12 h. Conclusion: Folic acid modified Coptis chinensis total alkaloid chitosan nanoparticles are successfully prepared,and the physical and chemical properties of the nanoparticles are satisfactory.