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Pharmaceutics. 2019 Feb 6;11(2). pii: E69. doi: 10.3390/pharmaceutics11020069.

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

Author information

1
Department of Physical Chemistry, University of Seville, 41012 Seville, Spain. moya@us.es.
2
Departament of Chemical Engineering, Physical Chemistry and Material Science. Faculty of Experimental Sciences, University of Huelva, Campus El Carmen, E-21071 Huelva, Spain. manuel.lopez@diq.uhu.es.
3
Department of Physical Chemistry, University of Seville, 41012 Seville, Spain. lebronjunior@hotmail.com.
4
Department of Physical Chemistry, University of Seville, 41012 Seville, Spain. fraostmar@alum.us.es.
5
Department of Physical Chemistry, University of Seville, 41012 Seville, Spain. david_perezalf@hotmail.com.
6
Department of Physical Chemistry, University of Seville, 41012 Seville, Spain. vane_farma@hotmail.com.
7
Department of Physical Chemistry, University of Seville, 41012 Seville, Spain. irenebeckdiaz93@gmail.com.
8
Departament of Microbiology, Faculty of Biology, University of Sevilla, 41012 Seville, Spain. vicenmb@hotmail.com.
9
Departament of Microbiology, Faculty of Biology, University of Sevilla, 41012 Seville, Spain. manuel.camean.sspa@juntadeandalucia.es.
10
Hospital Pharmacy Area, University Hospital Virgen Macarena, 41009 Seville, Spain. nuria@us.es.
11
Department of Physical Chemistry, University of Seville, 41012 Seville, Spain. pcornejo@us.es.

Abstract

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, N,N,N-triethyl-N-(12-naphthoxydodecyl)ammonium. Results showed a better encapsulation-efficiency percentage (EE%) of cefepime in liposomes with phosphatidylcholine and cholesterol than with 1,2-dioleoyl-sn-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 Escherichia coli 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 E. coli 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 Escherichia coli with high inhibitory activity.

KEYWORDS:

bactericidal activity; cefepime; encapsulation; liposome; surfactant.; zeta potential

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