| 星点设计-效应面法优化仑伐替尼混合胶束的制备工艺 |
| 投稿时间：2024-03-11 修订日期：2024-08-06 点此下载全文 |
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| 基金项目:新疆维吾尔自治区自然科学基金重点项目(编号：2022D01D78)通信作者:尹东锋 Tel: ( 0991) 4992862 E-mail: ydf1112@ 163.com ,李倩2,谢志2,贾文彦2,尹东锋2* |
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| 中文摘要:目的: 本研究旨在优化仑伐替尼混合胶束的处方及其制备工艺。方法: 通过薄膜水化法，利用普朗尼克P123和F127作为载体材料，制备仑伐替尼混合胶束。利用单因素实验和星点设计-响应面法筛选出最优处方并对其物理性质进行了初步的表征。结果:优化后的最佳处方和工艺条件为：P123质量百分比80%、载体材料用量90 mg、投药量10 mg、水化体积6 ml、水化时间45 min、旋蒸温度55℃。制备得到的仑伐替尼混合胶束的平均粒径为（104.0±0.32 ）nm，PDI为0.220±1.19，Zeta电位为（?2.56±0.81) mV，平均包封率为（83.33±0.30）%，平均载药量为（8.67±0.07）%。胶束形态为分布均一的规整球形，并显示出一定的缓释性能。结论：本研究开发的制备工艺简单可行，所得载药胶束具有较高的载药量和包封率，且释放稳定，为仑伐替尼混合胶束的进一步研究和开发提供了有价值的参考。 |
| 中文关键词:仑伐替尼 混合胶束 薄膜水化法 星点设计-效应面法 |
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| Optimization of the Preparation Process for Lenvatinib Mixed Micelles Using Central Composite Design-Response Surface Methodology |
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| Abstract:Objective: This study aimed to optimize the formulation and preparation process of lenvatinib mixed micelles. Methods: Lenvatinib mixed micelles were prepared using the film hydration method, employing Poloxamer P123 and F127 as carrier materials. The effects of various parameters including the mass percentage of P123, the amount of carrier material, drug loading, hydration volume, hydration time, and rotary evaporation temperature on the encapsulation efficiency and drug loading capacity were initially assessed through single-factor experiments. The optimal conditions were further refined using central composite design-response surface methodology, followed by process validation. The morphology of the micelles was observed with transmission electron microscopy, and their quality was evaluated by measuring particle size and Zeta potential. Additionally, the in vitro release behavior was investigated using the dialysis method. Results: The optimized formulation and process conditions were identified as follows: P123 mass percentage of 80%, carrier material amount of 90mg, drug loading of 10mg, hydration volume of 6ml, hydration time of 45min, and rotary evaporation temperature of 55°C. The resulting lenvatinib mixed micelles had an average particle size of (104.0±0.32) nm, a polydispersity index (PDI) of 0.220±1.19, and a Zeta potential of(?2.56±0.81)mV. The average encapsulation efficiency was (83.33±0.30)% and the average drug loading was (8.67±0.07)%. The micelles displayed a uniform spherical morphology with a certain sustained-release capability. Conclusion: The preparation process developed in this study is simple and feasible, producing drug-loaded micelles with high drug loading and encapsulation rates, and stable release. This provides valuable insights for further research and development of lenvatinib mixed micelles. |
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