In vitro evaluation of gentamicin released from microparticles
Gentamicin (GEN) is an aminoglycoside antibiotic with a potent antibacterial activity against a wide variety of bacteria. However, its poor cellular penetration limits its use in the treatment of infections caused by intracellular pathogens. One potential strategy to overcome this problem is the use...
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| Format: | info:eu-repo/semantics/article |
| Language: | eng |
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Elsevier
2012
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| Online Access: | https://hdl.handle.net/10171/22383 |
| _version_ | 1793400099029647360 |
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| author | Blanco-Prieto, M.J. (María José) Lecaroz, M.C. (María Concepción) Renedo, M.J. (María Jesús) Kunkova, J. (J.) Gamazo, C. (Carlos) |
| author_facet | Blanco-Prieto, M.J. (María José) Lecaroz, M.C. (María Concepción) Renedo, M.J. (María Jesús) Kunkova, J. (J.) Gamazo, C. (Carlos) |
| author_sort | Blanco-Prieto, M.J. (María José) |
| collection | DSpace |
| description | Gentamicin (GEN) is an aminoglycoside antibiotic with a potent antibacterial activity against a wide variety of bacteria. However, its poor cellular penetration limits its use in the treatment of infections caused by intracellular pathogens. One potential strategy to overcome this problem is the use of particulate carriers that can target the intracellular sites of infection. In this study GEN was ion-paired with the anionic AOT surfactant to obtain a hydrophobic complex (GEN–AOT) that was formulated as a particulated material either by the precipitation with a compressed antisolvent (PCA) method or by encapsulation into poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs). The micronization of GEN–AOT by PCA yielded a particulated material with a higher surface area than the non-precipitated complex, while PLGA NPs within a size range of 250–330 nm and a sustained release of the drug over 70 days were obtained by preparing the NPs using the emulsion solvent evaporation method. For the first time, GEN encapsulation efficiency values of ∼100% were achieved for the different NP formulations with no signs of interaction between the drug and the polymer. Finally, in vitro studies against the intracellular bacteria Brucella melitensis, used as a model of intracellular pathogen, demonstrated that the bactericidal activity of GEN was unmodified after ion-pairing, precipitation or encapsulation into NPs. These results encourage their use for treatment for infections caused by GEN-sensitive intracellular bacteria. |
| format | info:eu-repo/semantics/article |
| id | oai:dadun.unav.edu:10171-22383 |
| institution | Universidad de Navarra |
| language | eng |
| publishDate | 2012 |
| publisher | Elsevier |
| record_format | dspace |
| spelling | oai:dadun.unav.edu:10171-223832020-03-23T17:31:39Z In vitro evaluation of gentamicin released from microparticles Blanco-Prieto, M.J. (María José) Lecaroz, M.C. (María Concepción) Renedo, M.J. (María Jesús) Kunkova, J. (J.) Gamazo, C. (Carlos) Gentamicin Hydrophobic ion pairing Supercritical fluids Drug delivery systems Intracellular pathogens Gentamicin (GEN) is an aminoglycoside antibiotic with a potent antibacterial activity against a wide variety of bacteria. However, its poor cellular penetration limits its use in the treatment of infections caused by intracellular pathogens. One potential strategy to overcome this problem is the use of particulate carriers that can target the intracellular sites of infection. In this study GEN was ion-paired with the anionic AOT surfactant to obtain a hydrophobic complex (GEN–AOT) that was formulated as a particulated material either by the precipitation with a compressed antisolvent (PCA) method or by encapsulation into poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs). The micronization of GEN–AOT by PCA yielded a particulated material with a higher surface area than the non-precipitated complex, while PLGA NPs within a size range of 250–330 nm and a sustained release of the drug over 70 days were obtained by preparing the NPs using the emulsion solvent evaporation method. For the first time, GEN encapsulation efficiency values of ∼100% were achieved for the different NP formulations with no signs of interaction between the drug and the polymer. Finally, in vitro studies against the intracellular bacteria Brucella melitensis, used as a model of intracellular pathogen, demonstrated that the bactericidal activity of GEN was unmodified after ion-pairing, precipitation or encapsulation into NPs. These results encourage their use for treatment for infections caused by GEN-sensitive intracellular bacteria. 2012-05-31T11:46:11Z 2012-05-31T11:46:11Z 2002-08 info:eu-repo/semantics/article https://hdl.handle.net/10171/22383 eng info:eu-repo/semantics/openAccess application/pdf Elsevier |
| spellingShingle | Gentamicin Hydrophobic ion pairing Supercritical fluids Drug delivery systems Intracellular pathogens Blanco-Prieto, M.J. (María José) Lecaroz, M.C. (María Concepción) Renedo, M.J. (María Jesús) Kunkova, J. (J.) Gamazo, C. (Carlos) In vitro evaluation of gentamicin released from microparticles |
| title | In vitro evaluation of gentamicin released from microparticles |
| title_full | In vitro evaluation of gentamicin released from microparticles |
| title_fullStr | In vitro evaluation of gentamicin released from microparticles |
| title_full_unstemmed | In vitro evaluation of gentamicin released from microparticles |
| title_short | In vitro evaluation of gentamicin released from microparticles |
| title_sort | in vitro evaluation of gentamicin released from microparticles |
| topic | Gentamicin Hydrophobic ion pairing Supercritical fluids Drug delivery systems Intracellular pathogens |
| url | https://hdl.handle.net/10171/22383 |
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