In situ

摘要

Prodrug strategies use chemical modifications to improve the pharmacokinetic propertiesand therefore therapeutic effects of parent drugs. Traditional prodrug approaches useendogenous enzymes for activation. Bioorthogonal catalysis uses processes that endogenousenzymes cannot access, providing a complementary strategy for prodrug uncaging.Site-selective activation of prodrugs to drugs (uncaging) using synthetic catalysts is apromising strategy for localized drug activation. We discuss here recent studies thatincorporate metal catalysts into polymers and nanoparticle scaffolds to providebiocompatible “enzyme-like” catalysts that can penetrate bacterial biofilms and activateprodrug antibiotics in situ, affording a new strategy to treat bacterialbiofilm infections with the potential for reduced off-target effects.