Self/co-assembling peptide, EAR8-II, as a potential carrier for a hydrophobic anticancer drug pirarubicin (THP)--characterization and in-vitro delivery.
Self/co-assembling peptide, EAR8-II, as a potential carrier for a hydrophobic anticancer drug pirarubicin (THP)--characterization and in-vitro delivery.
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DOI：
10.3390/ijms141223315
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发表时间：
2013-11-26
影响因子：
5.6
通讯作者：
Chen P
中科院分区：
文献类型：
--
作者：
Sadatmousavi P;Chen P
采用短的离子互补肽EAR 8-II包封疏水性抗癌药物吡拉西坦（THP）。EAR 8-II被设计为在其自组装/共组装中继承两种先前引入的肽AAP 8和EAK 16-II的优点。这种肽短，简单，合成成本低，同时具有低的临界组装浓度（CAC）。肽序列中丙氨酸（A）残基的选择提供了适度的疏水相互作用，与其他更疏水的残基相比，引起最小程度的聚集。EAR 8-II是与EAK 16-II类似的离子互补肽，可以与疏水性化合物如THP自组装/共组装，并在水溶液中形成稳定的腓骨纳米结构。评价了EAR 8-II和THP复合物的理化性质和细胞活性，并显示依赖于肽与药物的比例。肽与药物质量比为5：1的复合物提供了稳定的溶液、均匀的纳米结构和针对各种癌细胞系的高效抗癌活性。这项工作的基础上，EAR 8-II和THP配方在体外和体内的详细研究，为未来开发的肽为基础的疏水性抗癌药物的传递系统。
A short ionic-complementary peptide, EAR8-II, was employed to encapsulate the hydrophobic anticancer drug pirarubicin (THP). EAR8-II was designed to inherit advantages from two previously introduced peptides, AAP8 and EAK16-II, in their self/co-assembly. This peptide is short, simple, and inexpensive to synthesize, while possessing a low critical assembly concentration (CAC). The choice of alanine (A) residues in the peptide sequence provides moderate hydrophobic interactions, causing a minimal degree of aggregation, compared with other more hydrophobic residues. EAR8-II is an ionic-complementary peptide, similar to EAK16-II, can self/co-assemble with hydrophobic compounds such as THP, and forms a stable fibular nanostructure in aqueous solution. Physiochemical properties and cellular activities of the EAR8-II and THP complexes were evaluated and show dependency on the peptide-to-drug ratio. The complex at the peptide-to-drug mass ratio of 5:1 provides a stable solution, uniform nanostructure, and highly effective anticancer activity against various cancer cell lines. This work forms the basis for detailed studies on EAR8-II and THP formulations in vitro and in vivo, for future development of peptide-based delivery systems for hydrophobic anticancer drugs.
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