资料:Preparation, therapeutic efficacy and intratumoral localization of targeted daunorubicin liposomes conjugating folate-PEG-CHEMS小说作家:Subin Xiong a b, Bo Yu b, Jun Wu c, Hong Li b, Robert J. Lee论文的链接: 小结: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.

本科学研究进步一起探讨了脂质体依据DHA蛋白激酶在L1210JF内部上的内吞缘由,并评诂了DHA-PEG-CHEMS锚定的荷柔红霉素脂质体(F-L-DNR)在休内的靶向医疗医疗感觉。主要采用改造的技巧聚合了备孕叶酸-PEG-CHEMS。评估报告格式了脂质体性能、生殖神经元致毒、生殖神经元内和瘤内导航定位相应对随带L1210JF生殖神经元的小鼠肺部肿瘤模式化的治愈疗效。F-L-DNR建立了高包封率(95.1%±1.5%)和应适当的孔径(76.0±35.5 nm)和ζ电位差(-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残留量下的小鼠活多久時间明显的长而L-DNR或氧化钙含量DNR。F-L-DNR的共焦点荧光线片反映出,血管接种F-L-DNR后24个小时,脂质体实现L1210JF体细胞上的DHA多巴胺受体不断增强了内吞效用,延长至了在肺部恶性肿瘤中的选择时段,并持续改善了肺部恶性肿瘤地方的用药减少。总而言之,备孕备孕叶酸-PEG-CHEMS是备孕备孕叶酸靶向药物剂量柔红霉素脂质体的高效配体,能够 增添癌症中的药物剂量降低和进行治疗体验。有关于安利:DSPE-PEG-AldDSPE-PEG-Amine,1069-79-0DSPE-PEG-azideDSPE-PEG5-azideDSPE-PEG-BiotinDSPE-PEG-BoronateDSPE-PEG-CH2COOHDSPE-PEG-COOHDSPE-PEG-Cy3之内一篇文章项目从何而来分类期刊杂志或文献综述,予以侵权案请链接当我们删去!