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目的 :为治疗口腔癌颈淋巴结转移灶 ,合成制备颈淋巴结靶向性的抗癌纳米微粒。方法 :选择可在体内生物降解的聚乳酸 (PAL)为载体 ,对口腔鳞癌细胞有强大杀伤作用的葫芦素BE(CuBE)为模型药物 ,以微粒粒径、载药量和包封率为质量控制指标 ,在单因素实验的基础上用均匀设计法优化工艺 ,以乳化—溶剂挥发法制备葫芦素BE聚乳酸纳米微粒 (CuBE_PLA_NP) ,然后加入 10 %甘露醇作支架剂 ,通过冷冻干燥即得CuBE_PLA_NP冻干针剂。结果 :经优化的CuBE_PLA_NP冻干针剂。其粒径分布范围为 4 7～ 12 0nm ,平均粒径为 85nm ,载药量为 2 3 0 3%± 0 4 7% ,包封率为 93 0 0 %± 0 10 % ,体外释药规律表明与Higuchi方程拟合。结论 :CuBE_PLA_NP冻干针剂为缓释剂 ,用CuBE_PLA_NP冻干针剂行口腔癌周局部注射 ,从理论上它对颈淋巴结转移灶具有靶向性 ,为以后的动物实验和临床实验提供了基础
Objective: To prepare cervical lymph node-targeted anticancer nanoparticles for the treatment of oral cancer cervical lymph node metastases. Methods: Cucurbitacin BE (CuBE), a biodegradable polylactic acid (PAL) carrier in vivo, was used as a model drug to kill oral squamous cell carcinoma cells. The particle size, drug loading and entrapment efficiency Based on the single factor experiment, the optimization design was made by the uniform design method. Cucurbitacin BE polylactic acid nanoparticles (CuBE_PLA_NP) were prepared by emulsification-solvent evaporation method, and then 10% mannitol was added as the scaffold. The freeze-dried CuBE_PLA_NP freeze-dried injection. Results: Optimized CuBE_PLA_NP freeze-dried injection. The particle size distribution ranged from 47 to 120 nm with an average particle diameter of 85 nm. The drug loading was 2300 ± 0.477% and the encapsulation efficiency was 93 0% ± 0 10%. The in vitro drug release Show fitting with Higuchi equation. CONCLUSION: The CuBE_PLA_NP freeze-dried injection is a sustained-release agent. The injection of CuBE_PLA_NP freeze-dried injection in the perianal period can theoretically target the cervical lymph node metastasis and provide the basis for later animal experiments and clinical trials