| 郑宏志,刘 阳,周晓东,张军千.载多西紫杉醇脂质微泡制备及特性考察[J].,2025,(18):2890-2896 |
| 载多西紫杉醇脂质微泡制备及特性考察 |
| Preparation and Characterization of Docetaxel-loaded Lipid Microbubbles |
| 投稿时间：2025-07-14 |
| DOI：10.13241/j.cnki.pmb.2025.18.002 |
| 中文关键词: 多西紫杉醇 脂质微泡 HepG2细胞 |
| 英文关键词: Docetaxel Lipid microbubbles HepG2 cells |
| 基金项目:国家自然科学基金项目（81071169）；河南省医学科技攻关计划项目（LHGJ20230478） |
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| 中文摘要: |
| 摘要 目的：制备纳米级载多西紫杉醇脂质微泡（DLLM），表征其理化性质，并评估其生物安全性及体外抗肿瘤效果，探讨其作为化疗药物靶向递送系统的潜力。方法：采用薄膜水化法制备DLLM；利用透射电子显微镜、扫描电子显微镜和粒径分析仪表征其形态、粒径及分布，采用高效液相色谱法测定药物包封率；以人肝癌HepG2细胞为模型，设置对照组（Control组）、多西紫杉醇组（DOC组）、载多西紫杉醇脂质微泡组（DLLM组）及载多西紫杉醇脂质微泡+超声组（DLLM+US组），通过光学显微镜观察细胞形态，CCK-8法检测细胞存活率，流式细胞术检测细胞凋亡，评估微泡的生物相容性及其介导的超声增效抗肿瘤作用。结果：制备的DLLM呈规则球形，粒径分布范围为200-600 nm，平均粒径为380 nm，包封率80.3%±2.6%。DOC组和DLLM+US组细胞存活率显著低于Control组（P＜0.01），凋亡率显著升高（P＜0.01）。DLLM+US组细胞存活率低于DOC组（P＜0.05），凋亡率高于DOC组（P＜0.05）。DLLM组与Control组相比，细胞存活率及凋亡率均无显著性差异（P＞0.05）。结论：本实验制备的纳米级DLLM，其粒径均一、包封率高、稳定性及生物相容性良好。DLLM在超声辐照触发下可增强多西紫杉醇对HepG2细胞的杀伤及促凋亡作用。 |
| 英文摘要: |
| ABSTRACT Objective: To prepare nanoscale docetaxel-loaded lipid microbubbles (DLLM), characterize their physical and chemical properties, evaluate their biosafety and anti-tumor effects in vitro, and explore their potential as a targeted delivery system for chemotherapeutic drugs. Methods: DLLM was prepared by thin film hydration method. The morphology, particle size and distribution were characterized by transmission electron microscopy, scanning electron microscopy and particle size analyzer. The drug encapsulation efficiency was determined by high performance liquid chromatography. Human hepatoma HepG2 cells were used as a model to set up the control group (Control group), the docetaxel group (DOC group), the docetaxel-loaded lipid microbubbles group (DLLM group) and the docetaxel-loaded lipid microbubbles+ ultrasound group (DLLM+ US group). The cell morphology was observed by optical microscope, the cell survival rate was detected by CCK-8 method, and the apoptosis was detected by flow cytometry. The biocompatibility of microbubbles and their mediated ultrasound-enhanced anti-tumor effect were evaluated. Results: The prepared DLLM was regular spherical, with a particle size distribution range of 200-600 nm, an average particle size of 380 nm, and an encapsulation efficiency of 80.3%±2.6%. The cell viability of the DOC group and the DLLM+US group was significantly lower than that of the Control group (P＜0.01), and the apoptosis rate was significantly increased (P＜0.01). The cell viability of the DLLM+US group was lower than that of the DOC group (P＜0.05), and the apoptosis rate was higher than that of the DOC group (P＜0.05). There was no significant difference in cell viability and apoptosis rate between the DLLM group and the Control group (P＞0.05). Conclusion: The nano-scale DLLM prepared in this experiment has uniform particle size, high encapsulation efficiency, good stability and biocompatibility. DLLM can enhance the killing and pro-apoptotic effects of docetaxel on HepG2 cells under ultrasound irradiation. |
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