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J Control Release ; 369: 39-52, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38508523

RESUMEN

The emergence of multidrug-resistant bacteria along with their resilient biofilms necessitates the development of creative antimicrobial remedies. We designed versatile fluorinated polymer micelles with surface-charge-switchable properties, demonstrating enhanced efficacy against Methicillin-Resistant Staphylococcus Aureus (MRSA) in planktonic and biofilm states. Polymethacrylate diblock copolymers with pendant fluorocarbon chains and carboxyl betaine groups were prepared using reversible addition-fragmentation chain transfer polymerization. Amphiphilic fluorinated copolymers self-assembled into micelles, encapsulating ciprofloxacin in their cores (CIP@FCBMs) for antibacterial and antibiofilm applications. As a control, fluorine-free copolymer micelles loaded with ciprofloxacin (CIP@BCBMs) were prepared. Although both CIP@FCBMs and CIP@BCBMs exhibited pH-responsive surface charges and lipase-triggered drug release, CIP@FCBMs exhibited powerful antimicrobial and antibiofilm activities in vitro and in vivo, attributed to superior serum stability, higher drug loading, enhanced fluorination-facilitated cellular uptake, and lipase-triggered drug release. Collectively, reversing surface charge, on-demand antibiotic release, and fluorination-mediated nanoparticles hold promise for treating bacterial infections and biofilms.


Asunto(s)
Antibacterianos , Betaína , Biopelículas , Ciprofloxacina , Lipasa , Staphylococcus aureus Resistente a Meticilina , Infecciones Estafilocócicas , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Antibacterianos/farmacología , Antibacterianos/administración & dosificación , Antibacterianos/química , Biopelículas/efectos de los fármacos , Lipasa/metabolismo , Concentración de Iones de Hidrógeno , Animales , Betaína/química , Betaína/administración & dosificación , Betaína/análogos & derivados , Infecciones Estafilocócicas/tratamiento farmacológico , Ciprofloxacina/farmacología , Ciprofloxacina/administración & dosificación , Ciprofloxacina/química , Fluorocarburos/química , Fluorocarburos/farmacología , Micelas , Liberación de Fármacos , Polímeros/química , Humanos , Ácidos Polimetacrílicos/química
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