Robust Polyion Complex Vesicles (PICsomes) under Physiological Conditions Reinforced by Multiple Hydrogen Bond Formation Derived by Guanidinium Groups

Biomacromolecules
Mao HoriKazunori Kataoka

Abstract

Polyion complex vesicles (PICsomes) formed from a self-assembly of an oppositely charged pair of block- and homo-polyelectrolytes have shown exceptional features for functional loading of bioactive agents. Nevertheless, the stability of PICsomes is often jeopardized in a physiological environment, and only PICsomes having chemically cross-linked membranes have endured in harsh in vivo conditions, such as in the bloodstream. Herein, we developed versatile PICsomes aimed to last in in vivo settings by stabilizing their membrane through a combination of ionic and hydrogen bonding, which is widely found in natural proteins as a salt bridge, by controlled introduction of guanidinium groups in the polycation fraction toward concurrent polyion complexation and hydrogen bonding. The guanidinylated PICsomes were successfully assembled under physiological salt conditions, with precise control of their morphology by tuning the guanidinium content, and the ratio of anionic and cationic components. Guanidinylated PICsomes with 100 nm diameter, which are relevant to nanocarrier development, were stable in high urea concentration, at physiological temperature, and under serum incubation, persisting in blood circulation in vivo.

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Citations

May 27, 2020·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Luisa ZartnerCornelia G Palivan
Dec 18, 2020·Advanced Drug Delivery Reviews·Yong Liu, Lichen Yin
Apr 4, 2021·Macromolecular Bioscience·Xin LiXikuang Yao
May 7, 2021·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Akihiro Kishimura

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