文献资料：Preparation, therapeutic efficacy and intratumoral localization of targeted daunorubicin liposomes conjugating folate-PEG-CHEMS笔者：Subin Xiong a b, Bo Yu b, Jun Wu c, Hong Li b, Robert J. Lee文献综述链接代码： 论文摘要：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.

本理论研究进那步刍议了脂质体采用DHA肾上腺素受体在L1210JF组织细胞上的内吞考核机制，并分析评估了DHA-PEG-CHEMS锚定的荷柔红霉素脂质体（F-L-DNR）在体中的靶点根治疗效。利用完善的方式方法人工了孕妇叶酸-PEG-CHEMS。风险评估了脂质体性能特点、癌症细胞膜核毒副作用、癌症细胞膜核内和瘤内地位与对过飞机安检L1210JF癌症细胞膜核的小鼠癌症绘图的医治功能。F-L-DNR确保了高包封率（95.1%±1.5%）和相当的粒度（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用量下的小鼠维持日子分明短于L-DNR或解离DNR。F-L-DNR的共焦点荧采光片表述，动脉针剂F-L-DNR后24分钟，脂质体完成L1210JF上皮细胞上的孕妇叶酸多巴胺受体减弱了内吞效果，增长了在癌肿中的删去时段，并纠正了癌肿的位置的食用的药物发挥。显然，DHA-PEG-CHEMS是DHA靶向疗法柔红霉素脂质体的有效率配体，都可以增大恶性肿瘤中的肿瘤药物脱离和根治效率。相关联推介：DSPE-PEG-AldDSPE-PEG-Amine，1069-79-0DSPE-PEG-azideDSPE-PEG5-azideDSPE-PEG-BiotinDSPE-PEG-BoronateDSPE-PEG-CH2COOHDSPE-PEG-COOHDSPE-PEG-Cy3之内的文章玩法来原各个期刊杂志或专著，知悉侵犯知识产权请找公司刪除！