10.1021/acsbiomaterials.8b01163.s001
Yilong Cheng
Yilong
Cheng
Gary W. Liu
Gary W.
Liu
Ritika Jain
Ritika
Jain
Jeffrey W. Pippin
Jeffrey
W. Pippin
Stuart J. Shankland
Stuart
J. Shankland
Suzie H. Pun
Suzie H.
Pun
Boronic Acid Copolymers for Direct Loading and Acid-Triggered
Release of Bis-T-23 in Cultured Podocytes
American Chemical Society
2018
acid-reversible
phenylboronic acid-containing polymers
kidney disease treatment
covalent boronate ester bond
solubilize Bis-T -23.
Bis-T -23
boronic ester bond
podocyte
2018-11-23 00:00:00
Journal contribution
https://acs.figshare.com/articles/journal_contribution/Boronic_Acid_Copolymers_for_Direct_Loading_and_Acid-Triggered_Release_of_Bis-T-23_in_Cultured_Podocytes/7396739
We
report an acid-reversible linker for triggered release of Bis-T-23,
an experimental small molecule drug for kidney disease treatment that
restores podocyte morphology during disease. Bis-T-23 contains catechols,
which form an acid-reversible, covalent boronate ester bond with boronic
acids. We synthesized phenylboronic acid-containing polymers using
reversible addition–fragmentation chain transfer polymerization
that were able to directly load and solubilize Bis-T-23. Because of
the reversibility of the boronic ester bond, drug was released in
its native form in a pH-dependent manner. The polymers rapidly trafficked
into acidic compartments and did not exhibit cytotoxicity, and polymer-drug
conjugates successfully delivered Bis-T-23 into cultured podocytes.