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Folate-PEG-DSPE的靶向脂质体构建及其胞内摄取研究
发布时间:2025-07-18     作者:zyl   分享到:
医学文献:Receptor-Specific Delivery of Liposomes Via Folate-Peg-Chol小说家:Wenjin Guo,Tina Lee,Jennifer Sudimack &Robert J. Lee资料链接搜索: 内容提要:A novel lipophilic conjugate of folate, folate-PEG-Chol, was synthesized and evaluated for receptor-mediated targeting of liposomes to tumor cells. Liposomes composed of DSPC/Chol/PEG-DSPE/folate-PEG-Chol (60/ 34/5/1, m/m) were taken up by cultured folate receptor-bearing KB cells via a saturable mechanism. Cellular binding of these liposomes could be competitively inhibited by free folic acid with an IC50 of 0.39 mM, indicating an extraordinarily high binding affinity. Fluorescence micrographs of KB cells treated with targeted liposomes encapsulating calcein showed that they were distributed both on the cell surface and in intracellular vesicular compartments. Targeted liposomes carrying doxorubicin were shown to be 38 times more toxic to KB cells than non-targeted control liposomes. A biodistribution study in receptor-positive tumor-bearing C57BL/6 mice showed no significant differences between the tumor uptake of folate-PEG-liposomes and non-targeted control liposomes. This study has demonstrated that cholesterol could be used as an alternative to phospholipids as an effective anchor for incorporation of a targeting ligand into liposomes.

Folate-PEG-DSPE

合成视频了种创新的备孕DHA亲脂性缀合物备孕DHA-PEG-Chol,并测评了其多巴胺受体介导的脂质体靶向疗法肿癌细胞膜的用处。由DSPC/Chol/PEG-DSPE/孕妇备孕叶酸片-PEG-Chol(60/34/5/1,m/m)組成的脂质体顺利通过可供大于求工作机制被的培养的带着孕妇备孕叶酸片感觉的KB体细胞膜吸收率。存在孕妇备孕叶酸片可以的竞争性地仰制这个脂质体的体细胞膜构建,IC50为0.39 mM,反映其构建感染力高。用包封钙黄绿素的靶向药物疗法治疗脂质体净化处理的KB体人体人体血细胞的荧光显微照片图片展现,她们分布不均在体人体人体血细胞面上和体人体人体血细胞内囊泡隔室中。带上阿霉素的靶向药物疗法治疗脂质体对KB体人体人体血细胞的致癌性非靶向药物疗法治疗对比脂质体的38倍。在蛋白激酶呈阳性淋巴良性肿瘤带着C57BL/6小鼠中的动物遍布研发证实,叶酸片-PEG脂质体和非靶点对应脂质体的淋巴良性肿瘤摄食中间不存在取得相互影响。此项研发证实,碳水化合物就能够做为磷脂的重复使用品,做为将靶点配体掺量脂质体的可行锚。相关联推建:DPPE-PEG-BIOTINDPPE-PEG-COOHDPPE-PEG-MalDPPE-PEG-N3DPPE-PEG-NH2DPPE-PEG-SCDSPE(Sodium salt)-PEG-COOHDSPE(Sodium salt)-PEG-NH2DSPE(Sodium salt)-PEG-OHDLPE-PEG-COOHDLPE-PEG-MalDLPE-PEG-NH2DLPE-PEG-SC以内文章的内容的内容由来各样中文核心期刊或文献综述,此事侵权案请关系你们清空!