| 紫杉醇棕榈酸酯的合成及其脂质体的制备与处方研究 |
| 投稿时间：2024-04-17 修订日期：2024-07-18 点此下载全文 |
| 引用本文：陈炳辰,王思真,郭贝贝,杨峰.紫杉醇棕榈酸酯的合成及其脂质体的制备与处方研究[J].药学实践杂志,2024,42(9):379~384,410 |
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| 基金项目:国家自然科学基金（82304455）；海军军医大学校级课题（2023MS009） |
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| 中文摘要:目的 通过对紫杉醇（PTX）的结构改造联合相应脂质体的构建，改善肿瘤细胞摄取，增加药物疗效。方法 通过酯化反应制备了紫杉醇前药PTX-PA，并建立含量方法学研究。采用单因素筛选，结合粒径、包封率等指标评价不同方法、条件下制备的PTX-PA/Lip，确定其最佳处方和制备工艺。结果 通过酯化反应成功制备PTX-PA，且建立的HPLC定量分析方法符合方法学要求。利用单因素筛选，确定了PTX-PA/Lip的最佳处方和制备工艺，通过最优处方制备的PTX-PA/Lip纳米粒径为（2.75±1.81） nm，PDI为（0.076±0.020），药物包封率达到90%以上。结论 基于纳米技术成功制备出棕榈酸修饰的紫杉醇脂质体，增强了紫杉醇在靶细胞的递送，为PTX-PA的药效学研究奠定基础。 |
| 中文关键词:紫杉醇 棕榈酸 脂质体 前药 制剂学研究 |
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| Synthesis of paclitaxel palmitate and the formulation optimization of its liposomes |
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| Abstract:Objective To improve the cellular uptake efficiency and the therapeutic effect through the structural modification of paclitaxel （PTX） and the preparation of corresponding liposomes. Methods The prodrug of paclitaxel, PTX-PA, was prepared by esterification reaction, and the quantitative detection method of PTX-PA was established. Next,the optimal formulation and preparation of PTX-PA/Lip was obtained through single factor screening based on their appearance, particle size, and encapsulation efficiency. Results The PTX-PA was successfully synthesized, and the established HPLC quantitative analysis method for PTX-PA met the methodological requirements. After the optimal preparation and formulation research through single factor screening, the particle size of optimized PTX-PA/Lip was （62.75±1.81） nm with a PDI of （0.076±0.02）, while the drug encapsulation rate reached more than 90%. Conclusion This research successfully prepared palmitic acid modified paclitaxel liposomes based on nanotechnology, enhancing the drug delivery efficiency of paclitaxel and laying the foundation for the pharmacodynamics research of PTX-PA. |
| keywords:paclitaxel palmitic acid liposomes prodrug pharmaceutical research |
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