【摘要】 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更多还原

【Abstract】 Objective:Anti_cancer nano_particles for targeting cervical lymph nodes were designed and prepared on the basis of the physiologic and anatomic properties of the peri_oral cancer lymphatic capillaries.Methods:The biodegradable polylactic acid (PLA) was selected as the carrier material, and cucurbitacinBE (CuBE) with very high anticancer activity against oral squamous cell carcinoma was used as the model drug. According to the criteria of the diameter of the nano_particles, drug loading (DL) and embedding ratio (ER), the preparing technology was optimized by uniformly designing experiment on the basis of single_factor experiment. CucurbitacinBE poly_lactic acid nano_particles (CuBE_PLA_NP) was prepared with the method of emulsion solvent evaporation, and then CuBE_PLA_NP lyophilization injection was prepared by using 10% manninositose as the supporting agent. Results:The diameter distribution for optimized CuBE_PLA_NP lyophilization injection ranged from 47 nm to120 nm, and the average diameter was 85nm. DL and ER were 23.03%±0.47% and 93.00%±0.10% respectively. The release study of the thermostatics also demonstrated that Higuchi equation was adequate to fit the release curve of CuBE_PLA_NP.Conclusion:CuBE_PLA_NP can be used as the release agent, as CuBE_PLA_NP can enter peri_oral cancer lymphatic capillaries for targeting cervical lymph nodes by the peri_cancer submucosal injection. Therefore, it can also used for animal and clinical experiments.\;更多还原