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Ciprofloxacin-Loaded Mixed Polymeric Micelles as Antibiofilm Agents
In this work, mixed polymeric micelles (MPMs) based on a cationic poly(2-(dimethylamino)ethyl methacrylate)-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA(29)-b-PCL(70)-b-PDMAEMA(29)) and a non-ionic poly(ethylene oxide)–b-poly(propylene oxide)–b-poly(ethylene oxide) (PE...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10145464/ https://www.ncbi.nlm.nih.gov/pubmed/37111633 http://dx.doi.org/10.3390/pharmaceutics15041147 |
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author | Stancheva, Rumena Paunova-Krasteva, Tsvetelina Topouzova-Hristova, Tanya Stoitsova, Stoyanka Petrov, Petar Haladjova, Emi |
author_facet | Stancheva, Rumena Paunova-Krasteva, Tsvetelina Topouzova-Hristova, Tanya Stoitsova, Stoyanka Petrov, Petar Haladjova, Emi |
author_sort | Stancheva, Rumena |
collection | PubMed |
description | In this work, mixed polymeric micelles (MPMs) based on a cationic poly(2-(dimethylamino)ethyl methacrylate)-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA(29)-b-PCL(70)-b-PDMAEMA(29)) and a non-ionic poly(ethylene oxide)–b-poly(propylene oxide)–b-poly(ethylene oxide) (PEO(99)-b-PPO(67)-b-PEO(99)) triblock copolymers, blended at different molar ratios, were developed. The key physicochemical parameters of MPMs, including size, size distribution, and critical micellar concentration (CMC), were evaluated. The resulting MPMs are nanoscopic with a hydrodynamic diameter of around 35 nm, and the ζ-potential and CMC values strongly depend on the MPM’s composition. Ciprofloxacin (CF) was solubilized by the micelles via hydrophobic interaction with the micellar core and electrostatic interaction between the polycationic blocks, and the drug localized it, to some extent, in the micellar corona. The effect of a polymer-to-drug mass ratio on the drug-loading content (DLC) and encapsulation efficiency (EE) of MPMs was assessed. MPMs prepared at a polymer-to-drug mass ratio of 10:1 exhibited very high EE and a prolonged release profile. All micellar systems demonstrated their capability to detach pre-formed Gram-positive and Gram-negative bacterial biofilms and significantly reduced their biomass. The metabolic activity of the biofilm was strongly suppressed by the CF-loaded MPMs indicating the successful drug delivery and release. The cytotoxicity of empty and CF-loaded MPMs was evaluated. The test reveals composition-dependent cell viability without cell destruction or morphological signs of cell death. |
format | Online Article Text |
id | pubmed-10145464 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-101454642023-04-29 Ciprofloxacin-Loaded Mixed Polymeric Micelles as Antibiofilm Agents Stancheva, Rumena Paunova-Krasteva, Tsvetelina Topouzova-Hristova, Tanya Stoitsova, Stoyanka Petrov, Petar Haladjova, Emi Pharmaceutics Article In this work, mixed polymeric micelles (MPMs) based on a cationic poly(2-(dimethylamino)ethyl methacrylate)-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA(29)-b-PCL(70)-b-PDMAEMA(29)) and a non-ionic poly(ethylene oxide)–b-poly(propylene oxide)–b-poly(ethylene oxide) (PEO(99)-b-PPO(67)-b-PEO(99)) triblock copolymers, blended at different molar ratios, were developed. The key physicochemical parameters of MPMs, including size, size distribution, and critical micellar concentration (CMC), were evaluated. The resulting MPMs are nanoscopic with a hydrodynamic diameter of around 35 nm, and the ζ-potential and CMC values strongly depend on the MPM’s composition. Ciprofloxacin (CF) was solubilized by the micelles via hydrophobic interaction with the micellar core and electrostatic interaction between the polycationic blocks, and the drug localized it, to some extent, in the micellar corona. The effect of a polymer-to-drug mass ratio on the drug-loading content (DLC) and encapsulation efficiency (EE) of MPMs was assessed. MPMs prepared at a polymer-to-drug mass ratio of 10:1 exhibited very high EE and a prolonged release profile. All micellar systems demonstrated their capability to detach pre-formed Gram-positive and Gram-negative bacterial biofilms and significantly reduced their biomass. The metabolic activity of the biofilm was strongly suppressed by the CF-loaded MPMs indicating the successful drug delivery and release. The cytotoxicity of empty and CF-loaded MPMs was evaluated. The test reveals composition-dependent cell viability without cell destruction or morphological signs of cell death. MDPI 2023-04-04 /pmc/articles/PMC10145464/ /pubmed/37111633 http://dx.doi.org/10.3390/pharmaceutics15041147 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Stancheva, Rumena Paunova-Krasteva, Tsvetelina Topouzova-Hristova, Tanya Stoitsova, Stoyanka Petrov, Petar Haladjova, Emi Ciprofloxacin-Loaded Mixed Polymeric Micelles as Antibiofilm Agents |
title | Ciprofloxacin-Loaded Mixed Polymeric Micelles as Antibiofilm Agents |
title_full | Ciprofloxacin-Loaded Mixed Polymeric Micelles as Antibiofilm Agents |
title_fullStr | Ciprofloxacin-Loaded Mixed Polymeric Micelles as Antibiofilm Agents |
title_full_unstemmed | Ciprofloxacin-Loaded Mixed Polymeric Micelles as Antibiofilm Agents |
title_short | Ciprofloxacin-Loaded Mixed Polymeric Micelles as Antibiofilm Agents |
title_sort | ciprofloxacin-loaded mixed polymeric micelles as antibiofilm agents |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10145464/ https://www.ncbi.nlm.nih.gov/pubmed/37111633 http://dx.doi.org/10.3390/pharmaceutics15041147 |
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