| 宋飞钰,张雪琼,代福笠,等.Box-Behnken响应面法优化辛伐他汀纳米粒的处方工艺[J].安徽医药,2025,29(9):1751-1757. |
| Box-Behnken响应面法优化辛伐他汀纳米粒的处方工艺 |
| Formulation optimization of simvastatin nanoparticle by Box-Behnken response surface method |
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| DOI：10.3969/j.issn.1009-6469.2025.09.011 |
| 中文关键词: 辛伐他汀 纳米粒子 羧甲基壳聚糖 处方工艺 Box-Behnken响应面法 |
| 英文关键词: Simvastatin Nanoparticles Carboxymethyl chitosan Prescription process Box-Behnken response surface method |
| 基金项目:湖北省自然科学基金项目( 2023AFC043) |
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| 中文摘要: |
| 目的采用 Box-Behnken响应面法优化辛伐他汀纳米粒( SIM-NPs)的处方工艺。方法 2024年 5―7月，采用离子交联法制备 SIM-NPs。Box-Behnken响应面法对纳米粒的制备工艺进行优化，考察辛伐他汀与羧甲基壳聚糖的质量比、羧甲基壳聚糖与氯化钙的质量比、氯化钙的浓度、羧甲基壳聚糖的浓度对 SIM-NPs包封率的影响。通过透射电子显微镜观察纳米粒的形态；测定纳米粒的粒径分布和 Zeta电位；测定粒径和多分散系数的变化考察纳米粒的稳定性；并进行体外释放与细胞毒性评价。结果最佳处方工艺为羧甲基壳聚糖与氯化钙的质量比 1.9∶1.0，氯化钙浓度 0.95 g/L，羧甲基壳聚糖浓度 1.90 g/L。制备得到的 SIM-NPs的粒径为 83.64 nm，Zeta电位为 .13.07 mV，多分散系数为 0.170，包封率为 95.11%，载药量为 4.14%，纳米粒在 1周内具有较好的稳定性，并具有良好的体外缓释性能和细胞相容性。结论 Box-Behnken响应面法优化得到的 SIM-NPs处方工艺合理可行，所得的纳米粒包封率较高，理化性能良好，具有缓释作用。 |
| 英文摘要: |
| Objective The prescription process for simvastatin nanoparticles (SIM-NPs) was enhanced by utilizing the Box-Behnken response surface methodology. Methods SIM-NPs were synthesized by the ionic-gelation method from May to July 2024. The Box-Behnken design of response surface methodology was employed to enhance the formulation process of nanoparticles. This study primari-ly focused on analyzing the impact of various parameters, including the mass ratio of the drug to carboxymethyl chitosan and carboxy-methyl chitosan to calcium chloride, the concentrations of calcium chloride and carboxymethyl chitosan, on the encapsulation efficien-cy of the nanoparticles. The morphology of the nanoparticles was observed using transmission electron microscopy. The particle size dis-tribution and zeta potential of the nanoparticles were determined; and the stability of the nanoparticles was investigated by measuringchanges in particle size and the polydispersity coefficient. The in vitro release and cytotoxicity of the nanoparticles were also evaluated.Results The ideal formulation for the prescription process involved a carrier-to-crosslinker mass ratio of 1.9∶1.0, with a crosslinkerconcentration of 0.95 g/L, and a carboxymethyl chitosan concentration of 1.9 g/L. The encapsulation efficiency of SIM-NPs of simvas-tatin was measured at 95.11%, with a drug loading capacity of 4.14%.The average diameter of the nanoparticles was 83.64 nm, comple-mented by a zeta potential of . 13.07 mV. The nanoparticles exhibit excellent stability over a week, demonstrating favorable in vitroslow release characteristics and cytocompatibility. Conclusion The Box-Behnken response surface methodology optimization has yielded a feasible formulation process for SIM-NPs,resulting in a high encapsulation efficiency of the nanoparticles,along with favorablephysicochemical properties and sustained release capabilities. |
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