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新型脂质体的制备与表征。头孢吡肟包封于阳离子脂质体中的杀菌活性。

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

作者信息

Moyá Maria Luisa, López-López Manuel, Lebrón José Antonio, Ostos Francisco José, Pérez David, Camacho Vanesa, Beck Irene, Merino-Bohórquez Vicente, Camean Manuel, Madinabeitia Nuria, López-Cornejo Pilar

机构信息

Department of Physical Chemistry, University of Seville, 41012 Seville, Spain.

Departament of Chemical Engineering, Physical Chemistry and Material Science. Faculty of Experimental Sciences, University of Huelva, Campus El Carmen, E-21071 Huelva, Spain.

出版信息

Pharmaceutics. 2019 Feb 6;11(2):69. doi: 10.3390/pharmaceutics11020069.

DOI:10.3390/pharmaceutics11020069
PMID:30736367
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6410124/
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, ,,-triethyl--(12-naphthoxydodecyl)ammonium. Results showed a better encapsulation-efficiency percentage (EE%) of cefepime in liposomes with phosphatidylcholine and cholesterol than with 1,2-dioleoyl--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 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 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 with high inhibitory activity.

摘要

头孢吡肟是一种具有广谱抗菌活性的抗生素。然而，这种抗生素有几种副作用且降解率高。因此，制备能够包封这种抗生素的新型脂质体并对其进行表征似乎是制药行业的一个重要研究方向。制备并表征了阴离子脂质体和阳离子脂质体。所有阳离子结构都含有相同的阳离子表面活性剂，即，，，-三乙基--(12-萘氧基十二烷基)铵。结果表明，与1,2-二油酰基--甘油-3-磷酸乙醇胺（DOPE）相比，头孢吡肟在含有磷脂酰胆碱和胆固醇的脂质体中的包封效率百分比（EE%）更高。胆固醇的存在和脂质体中蛋黄磷脂的量增加了包封百分比。测定了负载在含有磷脂酰胆碱的脂质体中的头孢吡肟对的杀菌活性。琼脂平板上游离头孢吡肟的抑菌圈与负载头孢吡肟的抑菌圈相似。还在工作条件下测量了培养物的生长速率常数。不含任何抗生素的脂质体对该速率常数没有影响。所有获得的结果表明，PC:CH:12NBr脂质体是头孢吡肟的生物相容性纳米载体，可用于对具有高抑制活性的细菌感染。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/578906fd72c0/pharmaceutics-11-00069-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/8aeaff32a3f9/pharmaceutics-11-00069-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/75eb74f53c7b/pharmaceutics-11-00069-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/197d79e29f78/pharmaceutics-11-00069-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/5c73992cab27/pharmaceutics-11-00069-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/42da5ac82bd1/pharmaceutics-11-00069-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/c763ab862bf8/pharmaceutics-11-00069-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/a1fd3b3ec477/pharmaceutics-11-00069-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/7f0210128801/pharmaceutics-11-00069-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/578906fd72c0/pharmaceutics-11-00069-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/8aeaff32a3f9/pharmaceutics-11-00069-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/75eb74f53c7b/pharmaceutics-11-00069-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/197d79e29f78/pharmaceutics-11-00069-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/5c73992cab27/pharmaceutics-11-00069-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/42da5ac82bd1/pharmaceutics-11-00069-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/c763ab862bf8/pharmaceutics-11-00069-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/a1fd3b3ec477/pharmaceutics-11-00069-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/7f0210128801/pharmaceutics-11-00069-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb5/6410124/578906fd72c0/pharmaceutics-11-00069-g009.jpg

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