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Issue 16, 2017
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A dendrimer–hydrophobic interaction synergy improves the stability of polyion complex micelles

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Abstract

Polyion complex (PIC) micelles incorporating PEG-dendritic copolymers display an unprecedented stability towards ionic strength that is amplified via hydrophobic interactions. The tridimensional orientation of peripheral hydrophobic linkers between charged groups and the globular/rigid dendritic scaffold maximizes this stabilization compared to PIC micelles from linear polymers. As a result, micelles stable at concentrations higher than 3 M NaCl are obtained, which represents the highest saline concentration attained with PIC micelles. Advantages of this stabilizing dendritic effect have been taken for the design of a robust, pH-sensitive micelle for the controlled intracellular release of the anticancer drug doxorubicin. This micelle displays a slightly higher toxicity, and distinctive mechanisms of cell uptake and intracellular trafficking relative to the free drug. The preparation of mixed PIC micelles by combining differently functionalized PEG-dendritic block copolymers has allowed the fine-tuning of their stability, paving the way towards the facile modulation of properties like biodegradability, drug loading, or the response to external stimuli.

Graphical abstract: A dendrimer–hydrophobic interaction synergy improves the stability of polyion complex micelles

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Supplementary files

Article information


Submitted
22 Feb 2017
Accepted
24 Mar 2017
First published
28 Mar 2017

Polym. Chem., 2017,8, 2528-2537
Article type
Paper

A dendrimer–hydrophobic interaction synergy improves the stability of polyion complex micelles

M. Fernandez-Villamarin, A. Sousa-Herves, S. Porto, N. Guldris, J. Martínez-Costas, R. Riguera and E. Fernandez-Megia, Polym. Chem., 2017, 8, 2528
DOI: 10.1039/C7PY00304H

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