文献：Easy formulation of liposomal doxorubicin modified with a bombesin peptide analogue for selective targeting of GRP receptors overexpressed by cancer cells

作者：Antonella Accardo, Silvia Mannucci, Elena Nicolato, Federica Vurro, Carlo Diaferia, Pietro Bontempi, Pasquina Marzola & Giancarlo Morelli

文献链接：https://link.springer.com/article/10.1007/s13346-018-00606-x

摘要：

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.

本文涉及阿霉素脂质体（Dox）的获得，其中脂质体用靶向肽进行外部修饰，能够以选择性的方式在肿瘤中过表达的膜受体上驱动制剂。我们开发了一种由三个不同小瓶组成的试剂盒：（a）一个装有阿霉素脂质体药物（Doxil®）无菌、半透明、红色分散体的小瓶，（B）一个装满具有反应功能的改性磷脂（DSPE-Peg maleimide）冻干粉末的小瓶，以及（C）一个含有1-9蛙皮素肽类似物（Cys-BN-AA1）的小瓶，该类似物经过化学修饰，可与DSPE-Peg-maleimid以化学计量比反应。所选肽是野生型1-9蛙皮素肽的稳定类似物拮抗剂；在血清中非常稳定；对胃泌素释放肽受体（GRPR也称为BB2）保持高特异性，具有纳摩尔亲和力；并且在一些癌症细胞中过表达。动物研究结果清楚地表明，在用试剂盒产品（即用蛙皮素类似物Doxil-BN-AA1修饰的聚乙二醇化脂质体Dox）治疗的小鼠中，肿瘤生长减少，与用非修饰聚乙二醇化脂质体制备Dox或生理盐水治疗的小鼠相比，疗效有所提高。

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DSPE-PEG-TH

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DSPE-PEG-CREKA

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DSPE-PEG-M2pep

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