Preparation and Characterization of New Liposomes. Bactericidal Activity of Cefepime Encapsulated into Cationic Liposomes

Cefepime is an antibiotic with a broad spectrum of antimicrobial activity. However, this antibiotic has several side effects and a high degradation rate. For this reason, the preparation and characterization of new liposomes that are able to encapsulate this antibiotic seem to be an important resear...

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Main Authors: Maria Luisa Moyá, Manuel López-López, José Antonio Lebrón, Francisco José Ostos, David Pérez, Vanesa Camacho, Irene Beck, Vicente Merino-Bohórquez, Manuel Camean, Nuria Madinabeitia, Pilar López-Cornejo
Format: Article
Language:English
Published: MDPI AG 2019-02-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/11/2/69
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author Maria Luisa Moyá
Manuel López-López
José Antonio Lebrón
Francisco José Ostos
David Pérez
Vanesa Camacho
Irene Beck
Vicente Merino-Bohórquez
Manuel Camean
Nuria Madinabeitia
Pilar López-Cornejo
author_facet Maria Luisa Moyá
Manuel López-López
José Antonio Lebrón
Francisco José Ostos
David Pérez
Vanesa Camacho
Irene Beck
Vicente Merino-Bohórquez
Manuel Camean
Nuria Madinabeitia
Pilar López-Cornejo
author_sort Maria Luisa Moyá
collection DOAJ
description Cefepime is an antibiotic with a broad spectrum of antimicrobial activity. However, this antibiotic has several side effects and a high degradation rate. For this reason, the preparation and characterization of new liposomes that are able to encapsulate this antibiotic seem to be an important research line in the pharmaceutical industry. Anionic and cationic liposomes were prepared and characterized. All cationic structures contained the same cationic surfactant, <i>N</i>,<i>N</i>,<i>N</i>-triethyl-<i>N</i>-(12-naphthoxydodecyl)ammonium. Results showed a better encapsulation-efficiency percentage (EE%) of cefepime in liposomes with phosphatidylcholine and cholesterol than with 1,2-dioleoyl-<i>sn</i>-glycero-3-phosphoethanolamine (DOPE). The presence of cholesterol and the quantity of egg-yolk phospholipid in the liposome increased the encapsulation percentage. The bactericidal activity against <i>Escherichia coli</i> of cefepime loaded into liposomes with phosphatidylcholine was measured. The inhibitory zone in an agar plate for free cefepime was similar to that obtained for loaded cefepime. The growth-rate constant of <i>E. coli</i> culture was also measured in working conditions. The liposome without any antibiotic exerted no influence in such a rate constant. All obtained results suggest that PC:CH:12NBr liposomes are biocompatible nanocarriers of cefepime that can be used in bacterial infections against <i>Escherichia coli</i> with high inhibitory activity.
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spelling doaj.art-20a0bb76c5bd4e37a2a29e31ffe65ea62022-12-22T04:25:19ZengMDPI AGPharmaceutics1999-49232019-02-011126910.3390/pharmaceutics11020069pharmaceutics11020069Preparation and Characterization of New Liposomes. Bactericidal Activity of Cefepime Encapsulated into Cationic LiposomesMaria Luisa Moyá0Manuel López-López1José Antonio Lebrón2Francisco José Ostos3David Pérez4Vanesa Camacho5Irene Beck6Vicente Merino-Bohórquez7Manuel Camean8Nuria Madinabeitia9Pilar López-Cornejo10Department of Physical Chemistry, University of Seville, 41012 Seville, SpainDepartament of Chemical Engineering, Physical Chemistry and Material Science. Faculty of Experimental Sciences, University of Huelva, Campus El Carmen, E-21071 Huelva, SpainDepartment of Physical Chemistry, University of Seville, 41012 Seville, SpainDepartment of Physical Chemistry, University of Seville, 41012 Seville, SpainDepartment of Physical Chemistry, University of Seville, 41012 Seville, SpainDepartment of Physical Chemistry, University of Seville, 41012 Seville, SpainDepartment of Physical Chemistry, University of Seville, 41012 Seville, SpainDepartament of Microbiology, Faculty of Biology, University of Sevilla, 41012 Seville, SpainDepartament of Microbiology, Faculty of Biology, University of Sevilla, 41012 Seville, SpainHospital Pharmacy Area, University Hospital Virgen Macarena, 41009 Seville, SpainDepartment of Physical Chemistry, University of Seville, 41012 Seville, SpainCefepime is an antibiotic with a broad spectrum of antimicrobial activity. However, this antibiotic has several side effects and a high degradation rate. For this reason, the preparation and characterization of new liposomes that are able to encapsulate this antibiotic seem to be an important research line in the pharmaceutical industry. Anionic and cationic liposomes were prepared and characterized. All cationic structures contained the same cationic surfactant, <i>N</i>,<i>N</i>,<i>N</i>-triethyl-<i>N</i>-(12-naphthoxydodecyl)ammonium. Results showed a better encapsulation-efficiency percentage (EE%) of cefepime in liposomes with phosphatidylcholine and cholesterol than with 1,2-dioleoyl-<i>sn</i>-glycero-3-phosphoethanolamine (DOPE). The presence of cholesterol and the quantity of egg-yolk phospholipid in the liposome increased the encapsulation percentage. The bactericidal activity against <i>Escherichia coli</i> of cefepime loaded into liposomes with phosphatidylcholine was measured. The inhibitory zone in an agar plate for free cefepime was similar to that obtained for loaded cefepime. The growth-rate constant of <i>E. coli</i> culture was also measured in working conditions. The liposome without any antibiotic exerted no influence in such a rate constant. All obtained results suggest that PC:CH:12NBr liposomes are biocompatible nanocarriers of cefepime that can be used in bacterial infections against <i>Escherichia coli</i> with high inhibitory activity.https://www.mdpi.com/1999-4923/11/2/69cefepimeliposomebactericidal activityzeta potentialencapsulationsurfactant.
spellingShingle Maria Luisa Moyá
Manuel López-López
José Antonio Lebrón
Francisco José Ostos
David Pérez
Vanesa Camacho
Irene Beck
Vicente Merino-Bohórquez
Manuel Camean
Nuria Madinabeitia
Pilar López-Cornejo
Preparation and Characterization of New Liposomes. Bactericidal Activity of Cefepime Encapsulated into Cationic Liposomes
Pharmaceutics
cefepime
liposome
bactericidal activity
zeta potential
encapsulation
surfactant.
title Preparation and Characterization of New Liposomes. Bactericidal Activity of Cefepime Encapsulated into Cationic Liposomes
title_full Preparation and Characterization of New Liposomes. Bactericidal Activity of Cefepime Encapsulated into Cationic Liposomes
title_fullStr Preparation and Characterization of New Liposomes. Bactericidal Activity of Cefepime Encapsulated into Cationic Liposomes
title_full_unstemmed Preparation and Characterization of New Liposomes. Bactericidal Activity of Cefepime Encapsulated into Cationic Liposomes
title_short Preparation and Characterization of New Liposomes. Bactericidal Activity of Cefepime Encapsulated into Cationic Liposomes
title_sort preparation and characterization of new liposomes bactericidal activity of cefepime encapsulated into cationic liposomes
topic cefepime
liposome
bactericidal activity
zeta potential
encapsulation
surfactant.
url https://www.mdpi.com/1999-4923/11/2/69
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