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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:
论文资料:Easy formulation of liposomal doxorubicin modified with a bombesin peptide analogue for selective targeting of GRP receptors overexpressed by cancer cells我们:Antonella Accardo, Silvia Mannucci, Elena Nicolato, Federica Vurro, Carlo Diaferia, Pietro Bontempi, Pasquina Marzola & Giancarlo Morelli资料友链://link.springer.com/article/10.1007/s13346-018-00606-x绪论: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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本篇文章设及阿霉素脂质体(Dox)的得到 ,表中脂质体用靶点肽确定外表体现语,要以选定性的方式在肿癌中过认为的膜蛋白激酶上能够注射剂。大家研发了一大种由二个物有所不同小瓶组成的的制剂盒:(a)一名装配有阿霉素脂质体类药(Doxil®)无菌室、半透亮、红颜色分散性体的小瓶,(B)一名塞满还包括症状实用功能的改良磷脂(DSPE-Peg maleimide)冻干粉丝的小瓶,相应(C)一名包括刺激性1-9蛙皮素肽类式物(Cys-BN-AA1)的小瓶,抽象方法式物过程生物体现语,可与DSPE-Peg-maleimid以生物计量校准比症状。选取肽是原生态型1-9蛙皮素肽的安全稳定性类式物拮抗剂;在血清中至关安全稳定性;对胃泌素释放出来肽蛋白激酶(GRPR也被视为BB2)要保持高特异形,还包括纳摩尔感召力;另外在有些胃癌人体细胞中过认为。两栖动物探索的结果了解清楚地认为,用得制剂盒企业产品(即用蛙皮素类式物Doxil-BN-AA1体现语的聚乙二醇化脂质体Dox)的治疗方法的小鼠中,肿癌衍生减掉,与用非体现语聚乙二醇化脂质机制备Dox或内分泌系统氯化钠的治疗方法的小鼠相对,较果物有所从而提高。涉及到的最新推荐:DSPE-PEG-THDSPE-PEG-YIGSRDSPE-PEG-NGRDSPE-PEG-Angiopep-2DSPE-PEG-CREKADSPE-PEG-RVG29DSPE-PEG-M2pep往上好文章内部源以及中文核心期刊或学术论文,若有侵权行为请取得联系大家移除!