【作者】 杨凯； 王昌美； 温玉明； 李龙江； 王晓毅； 陈绍维；

【Author】 Yang Kai Department of stomatology, The first Medical Hospital, Chongqing, Medical University Wang Changmei Wen Yuming Li Longjiang et al College of stomatology, West China University of Medical Sciences

【机构】 重庆医科大学附属第一医院口腔颌面外科； 四川大学华西口腔医学院口腔颌面外科；

【摘要】 <正>目的:根据口腔癌周毛细淋巴管的解剖生理特点和行口腔癌颈淋巴结转移灶靶向化疗的目的。合成制备具有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(PLA)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,用乳化-溶剂挥发法制备葫芦素BE聚乳酸纳米微粒(CuBE-PLA-NP),然后冰更多还原

【Abstract】 Objective: Anticancer nanoparticles for targeting cervical lymph nodes are designed and prepared on the bases of the physiologic and anatomic properties of the perioralcancer lymphatic capillaries. Methods: The biodegradable polylactic (PLA) is selected as the carrier material, CuncurbitacinBE (CuBE) with very high anticancer activity against oral squamouc cell carcinoma as the model drug, the nanoparticle diameter, drug loading (DL) and embedding ration (ER) rare uses as the criterion, CucurbitacinBE polylactic acid nanoparticles (CuBE-PLA-NP) is prepared by the emulsion solvent evaporation method, then, CuBE-PLA-NP lyophilization injection is prepared by using 10% manninositose as the supporting agent, Estabished oral cervical lymph node metastasis model in mice, CuBE-PLA-NP is injected in pericancer Submucosal of model mice, compared with injection of CuBE, Targeted Cervical lymph nodes is evaluated by targeting index,Selectivity index, relatie targeting efficiency, targeting efficiency, total targeting efficiency and ratio of maximum concentrations, and the treatment efficiency is ohserverd. Results: The diameter distribution for optimized CuBE-PLA-NP lyophilizaiton injections is from 47nm～120nm, the average diameter is 85nm, DL and ER are (23.03±0.10%) respectively, the release study of the thermostatic has shown that the Higuchi equation is adequate to fit the release Curve of CuBE-PLA-NP. Six targeted indexs suggests that CuBE-PLA-NP has high targeting Cervical lymph node, The histopathology also shows that degenerative and necrotic changes are found in Cervical lymph node metastatic foci after CuBE-PLA-NP is administered. Conclusion: CuBE-PL-NP is the release agent. CuBE-PLA-NP has high targeting Cervical lymph nodes by pericancer Submucosal injection, enchances effcinecy, decrease the side effect.更多还原