目的 构建载葛根素（Pur）聚乙烯亚胺/海藻酸钠（PEI/ALG）自组装纳米粒（Pur-PEI/ALG-NPs），并考察其制备工艺与性能。方法 采用自组装法制备Pur-PEI/ALG-NPs；采用UV法定量，采用马尔文粒度仪对Pur-PEI/ALG-NPs进行表征；并考察其体外释放行为；以包封率和载药量为评价指标，采用中心组合设计-效应面法（CCD-RSM）优化Pur-PEI/ALG-NPs处方。结果 优化后的处方：PEI质量浓度为3.2 mg/mL，ALG质量浓度为1.3 mg/mL，PEI-ALG质量比为3.75：1，平均粒径为（118.0±0.4）nm，Zeta电位为（35.2±0.7）mV，包封率为（24.13±1.78）%，载药量为（11.17±0.71）%；体外释放结果表明Pur-PEI/ALG-NPs加快了Pur的释放速率。结论 成功制备了Pur-PEI/ALG-NPs，粒径小且分布集中，表面具有丰富的正电荷，为葛根素在临床眼部治疗奠定了基础。

Objective To develop the puerarin-loaded polyethyleneimine/alginate nanoparticles (Pur-PEI/ALG-NPs) and investigate their physicochemical properties. Methods The Pur-PEI/ALG-NPs were prepared by electrostatic interaction. The particle size and Zeta potential of nanoparticles were measured by laser light scattering using a Zeta sizer ZEN3600, in vitro release curves for which were studied. The formulation variables were optimized by central composite design-response surface methodology (CCD-RSM) with entrapment efficiency and drug loading as dependent variables. Results An optimal formulation was confirmed as follows:polyethyleneimine concentration was 3.2 mg/mL, alginate concentration was 1.3 mg/mL and the mass ratio of PEI/ALG was 3.75. The resulting nanoparticles exhibited entrapment efficiency of (24.13 ±1.78)% and drug loading of (11.17 ±0.71)%, respectively. Zeta potential of nanoparticles was found to be (35.2 ±0.7) mV, with the average diameter of (118.0 ±0.4) nm. In vitro release test proved that nanoparticles accelerated the release rate of Pur. Conclusion Pur-PEI/ALG-NPs are prepared successfully with narrow particle size distribution and rich positive charge, which may lay the foundation for further clinical ocular application of Pur.

重庆市自然科学基金资助项目（cstc2016jcyjA0068）