Synthesis and Characterization of Polymer-Drug Conjugates by Strain-Promoted Azide-Alkyne Cycloaddition-Mediated Polymerization.

ABSTRACT: Polymer-drug conjugates (PDCs) modify the biodistribution of small-molecule anticancer agents to prevent undesired off-target adverse effects. Here, we report the preparation of two PDCs by strain-promoted [3 + 2] azide-alkyne cycloaddition-mediated step-growth polymerization. This method does not require the use of a catalyst or high temperatures and it allows the rapid synthesis of high molecular-weight PDCs containing gemcitabine (M_w ~ 40.18 kDa) and doxorubicin (M_w ~ 1800 kDa) with narrow molecular weight distribution and high drug loading (29.2 %wt. gemcitabine and 10.3 %wt. doxorubicin). α-ω-bis-azide-terminated bifunctional gemcitabine-coupled and doxorubicin-coupled monomers, with drug linkage via Gly-Phe-Leu-Gly (GFLG), a cathepsin B-sensitive peptide

SUBMITTER: Gbadegesin OD 

PROVIDER: S-EPMC12233213 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature