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基于DSPE-PEG-Maleimide的靶向肽偶联脂质体构建及评价方法研究
发布时间:2025-07-21     作者:zyl   分享到:
文章:Easy formulation of liposomal doxorubicin modified with a bombesin peptide analogue for selective targeting of GRP receptors overexpressed by cancer cells小说作者:Antonella Accardo, Silvia Mannucci, Elena Nicolato, Federica Vurro, Carlo Diaferia, Pietro Bontempi, Pasquina Marzola & Giancarlo Morelli资料连接://link.springer.com/article/10.1007/s13346-018-00606-x文献综述:The article concerns the obtainment of liposomal doxorubicin (Dox) in which liposomes are externally modified with a targeting peptide able to drive the formulation in a selective way on membrane receptors overexpressed in tumors. We developed a kit composed by three different vials: (A) a vial containing a sterile, translucent, red dispersion of the liposomal doxorubicin drug (Doxil®), (B) a vial filled with a lyophilized powder of a modified phospholipid with a reactive function (DSPE-Peg-maleimide), and (C) a vial containing a 1–9 bombesin peptide analogue (Cys-BN-AA1) chemically modified to react in stoichiometric ratio respect to DSPE-Peg-maleimide. The chosen peptide is a stable analogue antagonist of the wild-type 1–9 bombesin peptide; it is very stable in serum; maintains high specificity, with nanomolar affinity, towards gastrin release peptide receptors (GRPRs indicated also as BB2); and is overexpressed in some cancer cells. Results on animal studies clearly indicate that in mice treated with the kit product (i.e., pegylated liposomal Dox modified with the bombesin analogue, Doxil-BN-AA1), tumor growth is reduced, with an improved efficacy respect to mice treated with non-modified pegylated liposomal Dox or with saline solution.


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文章设及阿霉素脂质体(Dox)的赢得,这当中脂质体用靶向医治肽开始外链遮盖,也可以以挑选性的方式在肿癌中过证实的膜感觉上动力药品。他们发掘这个多种由两个各种小瓶组合的制剂盒:(a)这个装用阿霉素脂质体药剂(Doxil®)灭菌、半透明的、粉红色不集中体的小瓶,(B)这个装进极具想法工作的渗透型磷脂(DSPE-Peg maleimide)冻干颗粒的小瓶,与(C)这个有1-9蛙皮素肽像物(Cys-BN-AA1)的小瓶,该像物通过化工物质遮盖,可与DSPE-Peg-maleimid以化工物质计量检验比想法。所选择肽是野山型1-9蛙皮素肽的增强像物拮抗剂;在血清中是非常增强;对胃泌素释放出来肽感觉(GRPR也称呼BB2)保持稳定高特女性朋友,极具纳摩尔感染力;还有在一定癌病细胞系中过证实。爬行动物深入分析可是模糊地证实,用制剂盒企业产品(即用蛙皮素像物Doxil-BN-AA1遮盖的聚乙二醇化脂质体Dox)医治的小鼠中,肿癌滋生减掉,与用非遮盖聚乙二醇化脂质机制备Dox或生理上蒸馏水医治的小鼠对比,效用进行增长。相应个性化推荐:DSPE-PEG-THDSPE-PEG-YIGSRDSPE-PEG-NGRDSPE-PEG-Angiopep-2DSPE-PEG-CREKADSPE-PEG-RVG29DSPE-PEG-M2pep不低于好的文章相关内容源头各大期刊杂志或专著,予以侵权行为请关系大家刪除!