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基于Folate-PEG-Chol修饰的靶向脂质体在受体介导内吞机制中的应用研究
发布时间:2025-07-18     作者:zyl   分享到:


文献资料:Preparation, therapeutic efficacy and intratumoral localization of targeted daunorubicin liposomes conjugating folate-PEG-CHEMS作家:Subin Xiong a b, Bo Yu b, Jun Wu c, Hong Li b, Robert J. Lee论文参考文献友链: 文献综述: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.

叶酸-PEG-CHEMS

本探究更深层次的一个脚印初探了脂质体能够 备孕DHA肾上腺素受体在L1210JF肿瘤细胞上的内吞策略,并风险评估了备孕DHA-PEG-CHEMS锚定的荷柔红霉素脂质体(F-L-DNR)在身上的靶向方法方法功效。用整改的最简单的方法制作而成了叶酸片-PEG-CHEMS。分析了脂质体性质、血受损细胞膜毒素、血受损细胞膜内和瘤内wifi定位及及对攜帶L1210JF血受损细胞膜的小鼠恶性肿瘤型号的开展效果好。F-L-DNR确保了高包封率(95.1%±1.5%)和适宜的粒度(76.0±35.5 nm)和ζ电势(-12.83±1.36 mV)。F-L-DNR对L1210JF神经细胞的IC50比非靶点柔红霉素脂质体(L-DNR)低2-3倍。F-L-DNR组在5mg/kg和10mg/kg服用量下的小鼠活多久时光清晰善于L-DNR或悬浮DNR。F-L-DNR的共聚焦点荧太阳光片表述,冠状动脉打F-L-DNR后24个钟头,脂质体经由L1210JF血细胞上的孕妇叶酸多巴胺受体促进了内吞功效,不断增加了在恶性良性肿瘤中的补齐时,并改善效果了恶性良性肿瘤部件的用量宣泄。一直以来,备孕叶酸片-PEG-CHEMS是备孕叶酸片靶点柔红霉素脂质体的有使用效果配体,也可以新增良性肿瘤中的肿瘤药物降低和诊疗使用效果。相关的个性化推荐:DSPE-PEG-AldDSPE-PEG-Amine,1069-79-0DSPE-PEG-azideDSPE-PEG5-azideDSPE-PEG-BiotinDSPE-PEG-BoronateDSPE-PEG-CH2COOHDSPE-PEG-COOHDSPE-PEG-Cy3上述句子方面源几大类期刊杂志或论文,请谅解侵犯知识产权请练习小编去除!