Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy

Chong Li, Xiaolin Zhang, Xinliang Huang, Xiaoying Wang, Guojian Liao, Zhangbao ChenCollege of Pharmaceutical Sciences, Southwest University, Chongqing, People’s Republic of ChinaAbstract: The purpose of this study was to investigate flexible nanoliposomes for mediating topical delivery of...

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Autores principales: Li C, Zhang X, Huang X, Wang X, Liao G, Chen Z
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Publicado: Dove Medical Press 2013
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spelling oai:doaj.org-article:7d1b171a32324954a90c60b7376499df2021-12-02T02:16:45ZPreparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy1176-91141178-2013https://doaj.org/article/7d1b171a32324954a90c60b7376499df2013-03-01T00:00:00Zhttp://www.dovepress.com/preparation-and-characterization-of-flexible-nanoliposomes-loaded-with-a12554https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Chong Li, Xiaolin Zhang, Xinliang Huang, Xiaoying Wang, Guojian Liao, Zhangbao ChenCollege of Pharmaceutical Sciences, Southwest University, Chongqing, People’s Republic of ChinaAbstract: The purpose of this study was to investigate flexible nanoliposomes for mediating topical delivery of daptomycin, and to document permeation rates and bacteriostatic activity towards skin infections. Response surface methodology was used to optimize the daptomycin-loaded flexible nanoliposomes (DAP-FL), and the amount of drug loaded into the particles was evaluated as the investigation index. The optimal lipid ratio was lecithin to sodium cholate 17:1 (w/w) and the lipid to drug ratio was 14:1 (w/w). The hydration temperature was set at 37°C and the duration of treatment with ultrasound was 20 minutes. The DAP-FL obtained had a small mean particle size (55.4 nm) with a narrow size distribution (polydispersity index 0.15). The mean entrapment efficiency was 87.85% ± 2.15% and the mean percent drug loading was 5.61% ± 0.14%. Using skin mounted between the donor and receptor compartments of a modified Franz diffusion cell, the percentage and quantity of cumulative daptomycin permeation from DAP-FL within 12 hours were measured at 96.28% ± 0.70% and (132.23 ± 17.73) µg/cm2 *5 = 661.15 ± 88.65 µg/cm2, directly, showing rapid and efficient antibacterial activity against Staphylococcus aureus. Following local administration of DAP-FL, daptomycin was detected in multilayer tissues within the skin and underlying structures in the dorsal skin of the mouse. Effective therapeutic concentrations were maintained for several hours, and significantly inhibited bacterial growth and injury-induced biofilms. These results demonstrate that the DAP-FL can enhance the ability of daptomycin to permeate the skin efficiently, where it has a powerful antibacterial action and activity against biofilms. This novel formulation of daptomycin has potential as a new approach in the clinical application of daptomycin.Keywords: daptomycin, liposomes, response surface methodology, biofilmLi CZhang XHuang XWang XLiao GChen ZDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 1285-1292 (2013)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Li C
Zhang X
Huang X
Wang X
Liao G
Chen Z
Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy
description Chong Li, Xiaolin Zhang, Xinliang Huang, Xiaoying Wang, Guojian Liao, Zhangbao ChenCollege of Pharmaceutical Sciences, Southwest University, Chongqing, People’s Republic of ChinaAbstract: The purpose of this study was to investigate flexible nanoliposomes for mediating topical delivery of daptomycin, and to document permeation rates and bacteriostatic activity towards skin infections. Response surface methodology was used to optimize the daptomycin-loaded flexible nanoliposomes (DAP-FL), and the amount of drug loaded into the particles was evaluated as the investigation index. The optimal lipid ratio was lecithin to sodium cholate 17:1 (w/w) and the lipid to drug ratio was 14:1 (w/w). The hydration temperature was set at 37°C and the duration of treatment with ultrasound was 20 minutes. The DAP-FL obtained had a small mean particle size (55.4 nm) with a narrow size distribution (polydispersity index 0.15). The mean entrapment efficiency was 87.85% ± 2.15% and the mean percent drug loading was 5.61% ± 0.14%. Using skin mounted between the donor and receptor compartments of a modified Franz diffusion cell, the percentage and quantity of cumulative daptomycin permeation from DAP-FL within 12 hours were measured at 96.28% ± 0.70% and (132.23 ± 17.73) µg/cm2 *5 = 661.15 ± 88.65 µg/cm2, directly, showing rapid and efficient antibacterial activity against Staphylococcus aureus. Following local administration of DAP-FL, daptomycin was detected in multilayer tissues within the skin and underlying structures in the dorsal skin of the mouse. Effective therapeutic concentrations were maintained for several hours, and significantly inhibited bacterial growth and injury-induced biofilms. These results demonstrate that the DAP-FL can enhance the ability of daptomycin to permeate the skin efficiently, where it has a powerful antibacterial action and activity against biofilms. This novel formulation of daptomycin has potential as a new approach in the clinical application of daptomycin.Keywords: daptomycin, liposomes, response surface methodology, biofilm
format article
author Li C
Zhang X
Huang X
Wang X
Liao G
Chen Z
author_facet Li C
Zhang X
Huang X
Wang X
Liao G
Chen Z
author_sort Li C
title Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy
title_short Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy
title_full Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy
title_fullStr Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy
title_full_unstemmed Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy
title_sort preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy
publisher Dove Medical Press
publishDate 2013
url https://doaj.org/article/7d1b171a32324954a90c60b7376499df
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