文章：Preparation, therapeutic efficacy and intratumoral localization of targeted daunorubicin liposomes conjugating folate-PEG-CHEMS我们：Subin Xiong a b, Bo Yu b, Jun Wu c, Hong Li b, Robert J. Lee专著网页链接： 结语：Folate polyethylene glycol-cholesterol hemisuccinate (folate-PEG-CHEMS) is a novel folate ligand firstly synthesized by our group and demonstrated good stability and potential targeting results on KB cells in vitro. The current study further explored endocytosis mechanisms of liposomes via folate receptor on L1210JF cells and assessed targeted therapeutic efficacy of folate-PEG-CHEMS anchored liposomes loading daunorubicin (F-L-DNR) in vivo. Folate-PEG-CHEMS was synthesized by a modified method. The liposome properties, cell cytotoxicity, intracellular and intratumoral localization, and therapeutic efficacy on a murine tumor model bearing L1210JF cells were evaluated. High encapsulation efficiency (95.1% ± 1.5%) and appropriate particle size (76.0 ± 35.5 nm) and zeta potential (−12.83 ± 1.36 mV) were achieved for F-L-DNR. IC50 of F-L-DNR on L1210JF cells was 2–3-folds lower than that of non-targeted liposomal daunorubicin (L-DNR). Anticancer efficacy on L1210JF tumor model indicated that mice survival time of F-L-DNR group at doses of 5 mg/kg and 10 mg/kg was significantly longer than that of L-DNR or free DNR. Confocal fluorescence photographs of F-L-DNR indicated enhanced endocytosis of liposomes via folate receptor on L1210JF cells, prolonged retaining time in tumors and improved drug release in the tumor site at 24 h post intravenous injection of F-L-DNR. In conclusion, folate-PEG-CHEMS is an effective ligand for folate-targeted daunorubicin liposomes to achieve increased drug release in tumor and therapeutic efficacy.

本科学研究进的一步研究综述了脂质体利用DHA多巴胺受体在L1210JF细胞膜上的内吞机制化，并监测了DHA-PEG-CHEMS锚定的荷柔红霉素脂质体（F-L-DNR）在里面的靶点根治郊果。主要采用完善的方式方法获得了孕妇叶酸-PEG-CHEMS。考核了脂质体属性、组织致毒、组织内和瘤内分析甚至对挟带L1210JF组织的小鼠癌肿整治的诊疗使用效果。F-L-DNR变现了高包封率（95.1%±1.5%）和合适的的孔径（76.0±35.5 nm）和ζ电势（-12.83±1.36 mV）。F-L-DNR对L1210JF癌细胞的IC50比非靶向治疗柔红霉素脂质体（L-DNR）低2-3倍。F-L-DNR组在5mg/kg和10mg/kg服用量下的小鼠能活精力非常明显立于L-DNR或悬浮DNR。F-L-DNR的共焦聚荧太阳光照片显示，门静脉注塑F-L-DNR后24个小时，脂质体依据L1210JF受损细胞上的叶酸片多巴胺受体增加了内吞帮助，加长了在肉瘤中的永久保存时间段，并改进了肉瘤脏器的药物剂量产生。自始至终，DHA-PEG-CHEMS是DHA靶点柔红霉素脂质体的很好的配体，都可以提升肺部肿瘤中的中药施放和中药治疗感觉。有关推送：DSPE-PEG-AldDSPE-PEG-Amine，1069-79-0DSPE-PEG-azideDSPE-PEG5-azideDSPE-PEG-BiotinDSPE-PEG-BoronateDSPE-PEG-CH2COOHDSPE-PEG-COOHDSPE-PEG-Cy3以上的项目项目从何而来各种杂志期刊或参考文献，如无图片侵权请找话题企业删除文件！