资料：Synthesis and Evaluation of a Novel Lipophilic Folate Receptor Targeting Ligand诗人：YING LIU, SONGLIN XU, LESHENG TENG, BRYANT YUNG, JING ZHU, HONG DING and ROBERT J. LEE文章网页链接： 文献综述：Background: Folate receptor (FR)-targeted liposomes have been investigated as delivery vehicles for anticancer drugs. A novel lipophilic FR ligand, folate-glutathione-polyethyleneglycol-distearoyl phosphatidylethanolamine (F-GSH-PEG-DSPE), was synthesized, incorporated into liposomes and evaluated for FR targeting efficiency. These liposomes were then evaluated as carriers of the chemotherapy agent vincristine (VIN). Materials and Methods: F-GSH-PEG-DSPE was synthesized and FR-targeted liposomes loaded with either calcein (F-L-Calcein) or VIN (F-L-VIN) were prepared by thin film hydration followed by polycarbonate membrane extrusion and, in the case of VIN, by remote loading. To assess liposome stability, the uptake of F-L-VIN in KB (FR+) cancer cells was measured after storage under 4°C for 3 months. Comparative pharmacokinetic studies were carried out with F-L-VIN and L-VIN (non-targeted control liposomes). Results: F-L-Calcein showed significantly higher cellular uptake in KB cells compared to non-targeted liposomes. In addition, F-L-VIN showed enhanced cytotoxicity in KB cells in vitro compared to control liposomes. Pharmacokinetic parameters indicated that both F-L-VIN and control liposomes had higher area under the curve (AUC), mean residence time (MRT), elimination half life (t1/2-β) and lower total body clearance (CL) than those of free VIN, while there were no significant differences between these liposomal formulations. Conclusion: F-GSH-PEG-DSPE is effective as a novel ligand for the synthesis of FR-targeted liposomes.

转化成没事种创新亲脂性FR配体，DHA-谷胱甘肽聚乙二醇二硬脂酰磷脂酰甲醇胺（F-GSH-PEG-DSPE），将其掺加脂质体中，并鉴定了FR靶向疗法利用率。并且将这样的脂质体看做放化疗治疗药物齐齐哈尔新碱（VIN）的各种载体实行鉴定。材料和措施：合并F-GSH-PEG-DSPE，在透气膜水合、聚碳酸膜一挤和手机远程跳转制取载荷钙黄绿素（F-L-calcein）或VIN（F-L-VIN）的FR靶向药物脂质体。方便评估报告格式脂质体的平稳性，在4°C下存储3个月时间后，測量KB（FR+）癌细胞对F-L-VIN的摄食。用F-L-VIN和L-VIN（非靶点對照脂质体）实施了非常药代动力机学调查。的结果：或非靶向疗法脂质体差距，F-L-Calcein在KB人体生殖受损受损细胞中的人体生殖受损受损细胞摄取量凸显高。最后，与对比脂质体差距，F-L-VIN在身体KB人体生殖受损受损细胞中现示出开展的人体生殖受损受损细胞毒素。药代原因学因素表面，F-L-VIN和对比脂质体的的身材曲线现在积（AUC）、的平均等待时光（MRT）、消掉半衰期（t1/2-β）和周身清楚率（CL）均过于悬浮VIN，但这个脂质管理体制剂当中不会有特殊不同。理论依据：F-GSH-PEG-DSPE看作合成视频FR靶向药物脂质体的新配体是有效的的。相关的推建：DSPE-PEG-BiotinDSPE-PEG-BoronateDSPE-PEG-CH2COOHDSPE-PEG-COOHDSPE-PEG-Cy3DSPE-PEG-Cy5DSPE-PEG-DBCODSPE-PEG-FITCDSPE-PEG-FolateDSPE-PEG-IADSPE-PEG-Mal以上项目的文章项目來源当下期刊论文或资料，比如侵犯知识产权请认识人们删除图片！