【作者】 施天一； 谷连帅； 孙玉； 王森林； 张向阳； 朱进； 孙柏旺；

【Author】 Tianyi Shi;Lianshuai Gu;Yu Suna;Senlin Wang;Chaoqun You;Xiangyang Zhang;Jin Zhu;Baiwang Sun;School of Chemistry and Chemical Engineering, Southeast University;Laboratory of Organic Chemistry,ETH Zurich;Key Laboratory of Antibody Technique of Ministry of Health, School of Pathology, Nanjing Medical University;

【机构】 东南大学化学化工学院； 苏黎世联邦理工大学有机化学系； 南京医科大学生命科学院；

【摘要】 目前,人们用顺铂治疗癌症遇到了一系列的临床瓶颈,为了解决所遇到的问题,通过纳米载药体系来解决临床问题,得到越来越多的关注。我们合成了包载了顺铂和吲哚菁绿的聚乳酸羟基乙酸共聚物-(二硬酯酰基磷脂酰乙醇胺-聚乙二醇2000)纳米球和在其基础上偶联了甘氨酸-半胱氨酸-甘氨酸-丙氨酸-丙氨酸-天冬酰胺-亮氨酸的七肽的纳米球。该纳米粒子的粒径在110纳米左右。在近红外光的下,纳米球中的吲哚菁绿被激发,释放出热量,达到控制释放药物的作用。同时,纳米球表面修饰的七肽可以智能识别胃癌细胞表面高度表达的豆荚蛋白酶,起到增加药物特异性的效果。更多还原

【Abstract】 Cisplatin-therapy has faced limitations in the process of clinical application.To settle the bottleneck,nanotechnology has emerged as an effective method.We synthesize cisplatin and indocyanine green（ICG） loaded PLGA-（DSPE-PEG2000）nanoparticles（CINPs） and ACINPs conjugated with Gly-Cys-Gly-Ala-Ala-Asn-Leu（GCGAANL）heptapeptide onto CINPs.ACINPs with nearly 110 nm exhibited good monodispersity and size stability.The EE and LE of cisplatin loaded into ACINPs were optimized as 29.81%and 3.88%.Under irradiation of 808 nm NIR,the temperature of ACINPs could rapidly rise up to 60℃ and nanoparticles were disrupted to release the cisplatin.In vitro studies have suggested ACINPs,compared with CINPs,could be recognized by MGC803 cells overexpressing the legumain upon cell surface and efficiently killed the cancer cells.However,ACINPs was harmless to MKN₂8 cells,negative expressing the legumain,which indicated the specificity and safety of ACINPs.Hence,the ACINPs exhibit great potential in avoiding the side effects of cisplatin and enhancing the chemo-photothermal therapy.更多还原