平阳霉素量子点聚乳酸羟基乙酸纳米粒的制备  

Preparation of pingyangmycin quantum dot polylactic-co-glycolic acid nanoparticles

作　　者：李振平[1,2] 赵建江[1] 

机构地区：[1]南方医科大学附属口腔医院.广东省口腔医院,广东广州510280 [2]南方医科大学

出　　处：《广东牙病防治》2012年第5期245-250,共6页Journal of Dental Prevention and Treatment

基　　金：国家自然科学基金(30672340);广东省科技计划项目(2008B030301183);广东省科技计划项目(2010B031500032)

摘　　要：目的为研究靶向治疗口腔癌颈淋巴结转移灶,制备一种集靶向化疗、定位、实时监测为一体的纳米粒(Nanoparticles,NPs)。方法以平阳霉素(pingyangmycin,PYM)为模型药物,以量子点(quantum dots,QDs)为荧光探针,以聚乳酸羟基乙酸(polylactic-co-glycolic acid,PLGA)为载体,以粒径、荧光性能、载药量和包封率为质量控制指标,通过正交实验设计,用复乳法制备平阳霉素量子点聚乳酸羟基乙酸纳米粒(PYM-QD-PLGA-NPs)。结果经优化制备的PYM-QD-PLGA-NPs包封率为(78.1±2.1)%,载药率为(5.9±0.3)%,平均粒径245.4 nm,电位(-6.68±4.11)mV,具备与QDs相似的荧光性能。结论 PYM-QD-PLGA-NPs具备一定的PYM包载率和QDs荧光性能,符合淋巴靶向的粒径要求,理论上通过口腔癌周注射,可靶向、定位、监测并治疗颈淋巴结转移灶。Objective A nanoparticle with combination of targeted chemotherapy,localization and real-time monitoring for cervical lymph node metastasis resulted from oral cancer was designed and synthesized.Methods Pingyangmycin（PYM） was selected as the model drug,and quantum dots（QDs） was used as fluorescent probe,while polylactic-co-glycolic acid（PLGA） was served as the carrier material.According to the quality controlling index of diameter,fluorescent property,drug loading（DL） and embedding ratio（ER）,pingyangmycin quantum dot polylactic-co-glycolic acid nanoparticles（PYM-QD-PLGA-NPs） were prepared with the method of multiple emulsion solvent evaporation and optimized through orthogonal experimental design.Results The average diameter for optimized PYM-QD-PLGA-NPs was245.4 nm,zeta potential was（-6.68±4.11） mV,DL and ER were 5.90%±0.29% and 78.1%±2.1% respectively.The nanoparticle was shared the similar fluorescence with QDs.Conclusion PYM-QD-PLGA-NPs can not only provide a certain drug loading/embedding capacity for a model anticancer drug PYM and fluorescent property of QDs,but also offer a suitable diameter for lymphatic targeting.By means of targeting,identification,surveillance and chemotherapy,in theory,it will provide a new approach to cervical lymph node metastasis by the peri-oral cancer injection.

关 键 词：平阳霉素 量子点 聚乳酸羟基乙酸 纳米粒 靶向化疗 

分 类 号：R73-36[医药卫生—肿瘤]