A pH-Responsive Nanoparticle Library with Precise pH Tunability by Co-Polymerization with Non-Ionizable Monomers

Ruiyang Zhao; Chuanxun Fu; Zenghui Wang; Meijie Pan; Bin Ma; Qingqing Yin; Binlong Chen; Jianxiong Liu; Heming Xia; Fangjie Wan; Letong Wang; Qiang Zhang; Yiguang Wang

doi:10.1002/anie.202200152

A pH-Responsive Nanoparticle Library with Precise pH Tunability by Co-Polymerization with Non-Ionizable Monomers

Angew Chem Int Ed Engl. 2022 May 2;61(19):e202200152. doi: 10.1002/anie.202200152. Epub 2022 Mar 10.

Authors

Ruiyang Zhao^{1

2}, Chuanxun Fu^{1

2}, Zenghui Wang^{1

2}, Meijie Pan², Bin Ma², Qingqing Yin², Binlong Chen^{1

2}, Jianxiong Liu², Heming Xia², Fangjie Wan², Letong Wang², Qiang Zhang^{1

2}, Yiguang Wang^{1

2}

Affiliations

¹ State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China.
² Beijing Key Laboratory of Molecular Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China.

PMID: 35218123
DOI: 10.1002/anie.202200152

Abstract

Precise monitoring of the subtle pH fluctuation during biological events remains a big challenge. Previously, we reported an ultra-pH-sensitive (UPS) nanoprobe library with a sharp pH response using co-polymerization of two tertiary amine-containing monomers with distinct pK_a . Currently, we have generalized the UPS nanoparticle library with tunable pH transitions (pH_t ) by copolymerization of a tertiary amine-containing monomer with a series of non-ionizable monomers. The pH_t of nanoparticles is fine-tuned by the non-ionizable monomers with different hydrophobicity. Each non-ionizable monomer presents a constant contribution to pH tunability regardless of tertiary amine-containing monomers. Based on this strategy, we produced two libraries of nanoprobes with continuous pH_t covering the entire physiological pH range (5.0-7.4) for fluorescent imaging of endosome maturation and cancers. This generalized strategy provides a powerful toolkit for biological studies and cancer theranostics.

Keywords: Fluorescence Imaging; Nanoparticles; Non-Ionizable Monomers; Polymerization; pH Tunability.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amines
Hydrogen-Ion Concentration
Hydrophobic and Hydrophilic Interactions
Nanoparticles*
Polymerization

Substances

Amines