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Int. J. Mol. Sci. 2013, 14(12), 23315-23329; doi:10.3390/ijms141223315

Self/Co-Assembling Peptide, EAR8-II, as a Potential Carrier for a Hydrophobic Anticancer Drug Pirarubicin (THP)—Characterization and in-Vitro Delivery

Department of Chemical Engineering and Waterloo Institute of Nanotechnology, University of Waterloo, Waterloo, ON N2L 3G1, Canada
* Author to whom correspondence should be addressed.
Received: 17 October 2013 / Revised: 13 November 2013 / Accepted: 14 November 2013 / Published: 26 November 2013
(This article belongs to the Special Issue Bioactive Nanoparticles 2013)
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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.
Keywords: ionic-complementary; self/co-assembly; encapsulation; stability; anticancer activity ionic-complementary; self/co-assembly; encapsulation; stability; anticancer activity
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Sadatmousavi, P.; Chen, P. Self/Co-Assembling Peptide, EAR8-II, as a Potential Carrier for a Hydrophobic Anticancer Drug Pirarubicin (THP)—Characterization and in-Vitro Delivery. Int. J. Mol. Sci. 2013, 14, 23315-23329.

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