Surface-modified gatifloxacin nanoparticles with potential for treating central nervous system tuberculosis
Patricia Marcianes,1 Sofia Negro,1,2 Luis García-García,3 Consuelo Montejo,4 Emilia Barcia,1,2 Ana Fernández-Carballido1,2 1Department of Pharmaceutics, School of Pharmacy, University Complutense of Madrid, Madrid, Spain; 2Institute of Pharmaceutical Technology, Uni...
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| Format: | Article |
| Language: | English |
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Dove Medical Press
2017-03-01
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| Series: | International Journal of Nanomedicine |
| Subjects: | |
| Online Access: | https://www.dovepress.com/surface-modified-gatifloxacin-nanoparticles-with-potential-for-treatin-peer-reviewed-article-IJN |
| _version_ | 1818925995771559936 |
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| author | Marcianes P Negro S García-García L Montejo C Barcia E Fernández-Carballido A |
| author_facet | Marcianes P Negro S García-García L Montejo C Barcia E Fernández-Carballido A |
| author_sort | Marcianes P |
| collection | DOAJ |
| description | Patricia Marcianes,1 Sofia Negro,1,2 Luis García-García,3 Consuelo Montejo,4 Emilia Barcia,1,2 Ana Fernández-Carballido1,2 1Department of Pharmaceutics, School of Pharmacy, University Complutense of Madrid, Madrid, Spain; 2Institute of Pharmaceutical Technology, University Complutense of Madrid, Madrid, Spain; 3Multidisciplinary Institute of Cerebral Cartography, University Complutense of Madrid, Madrid, Spain; 4Department of Pharmaceutical and Health Sciences, School of Pharmacy, University CEU-San Pablo, Spain Abstract: A new nanocarrier is developed for the passage of gatifloxacin through the blood–brain barrier to treat central nervous system tuberculosis. Gatifloxacin nanoparticles were prepared by nanoprecipitation using poly(lactic-co-glycolic acid) (PLGA) 502 and polysorbate 80 or Labrafil as surface modifiers. The evaluation of in vivo blood–brain barrier transport was carried out in male Wistar rats using rhodamine-loaded PLGA nanoparticles prepared with and without the surface modifiers. At 30 and 60 minutes after administration, nanoparticle biodistribution into the brain (hippocampus and cortex), lungs, and liver was studied. The results obtained from the cerebral cortex and hippocampus showed that functionalization of rhodamine nanoparticles significantly increased their passage into the central nervous system. At 60 minutes, rhodamine concentrations decreased in both the lungs and the liver but were still high in the cerebral cortex. To distinguish the effect between the surfactants, gatifloxacin-loaded PLGA nanoparticles were prepared. The best results corresponded to the formulation prepared with polysorbate 80 with regard to encapsulation efficiency (28.2%), particle size (176.5 nm), and ζ-potential (-20.1 mV), thereby resulting in a promising drug delivery system to treat cerebral tuberculosis. Keywords: polysorbate 80, Labrafil, gatifloxacin, nanoparticles, targeting, blood–brain barrier, brain delivery |
| first_indexed | 2024-12-20T02:50:05Z |
| format | Article |
| id | doaj.art-da8a6987a11445bebf783069b7dd4127 |
| institution | Directory Open Access Journal |
| issn | 1178-2013 |
| language | English |
| last_indexed | 2024-12-20T02:50:05Z |
| publishDate | 2017-03-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | International Journal of Nanomedicine |
| spelling | doaj.art-da8a6987a11445bebf783069b7dd41272022-12-21T19:56:03ZengDove Medical PressInternational Journal of Nanomedicine1178-20132017-03-01Volume 121959196831823Surface-modified gatifloxacin nanoparticles with potential for treating central nervous system tuberculosisMarcianes PNegro SGarcía-García LMontejo CBarcia EFernández-Carballido APatricia Marcianes,1 Sofia Negro,1,2 Luis García-García,3 Consuelo Montejo,4 Emilia Barcia,1,2 Ana Fernández-Carballido1,2 1Department of Pharmaceutics, School of Pharmacy, University Complutense of Madrid, Madrid, Spain; 2Institute of Pharmaceutical Technology, University Complutense of Madrid, Madrid, Spain; 3Multidisciplinary Institute of Cerebral Cartography, University Complutense of Madrid, Madrid, Spain; 4Department of Pharmaceutical and Health Sciences, School of Pharmacy, University CEU-San Pablo, Spain Abstract: A new nanocarrier is developed for the passage of gatifloxacin through the blood–brain barrier to treat central nervous system tuberculosis. Gatifloxacin nanoparticles were prepared by nanoprecipitation using poly(lactic-co-glycolic acid) (PLGA) 502 and polysorbate 80 or Labrafil as surface modifiers. The evaluation of in vivo blood–brain barrier transport was carried out in male Wistar rats using rhodamine-loaded PLGA nanoparticles prepared with and without the surface modifiers. At 30 and 60 minutes after administration, nanoparticle biodistribution into the brain (hippocampus and cortex), lungs, and liver was studied. The results obtained from the cerebral cortex and hippocampus showed that functionalization of rhodamine nanoparticles significantly increased their passage into the central nervous system. At 60 minutes, rhodamine concentrations decreased in both the lungs and the liver but were still high in the cerebral cortex. To distinguish the effect between the surfactants, gatifloxacin-loaded PLGA nanoparticles were prepared. The best results corresponded to the formulation prepared with polysorbate 80 with regard to encapsulation efficiency (28.2%), particle size (176.5 nm), and ζ-potential (-20.1 mV), thereby resulting in a promising drug delivery system to treat cerebral tuberculosis. Keywords: polysorbate 80, Labrafil, gatifloxacin, nanoparticles, targeting, blood–brain barrier, brain deliveryhttps://www.dovepress.com/surface-modified-gatifloxacin-nanoparticles-with-potential-for-treatin-peer-reviewed-article-IJNPolysorbate 80LabrafilGatifloxacinNanoparticlesTargetingBlood-Brain BarrierBrain delivery |
| spellingShingle | Marcianes P Negro S García-García L Montejo C Barcia E Fernández-Carballido A Surface-modified gatifloxacin nanoparticles with potential for treating central nervous system tuberculosis International Journal of Nanomedicine Polysorbate 80 Labrafil Gatifloxacin Nanoparticles Targeting Blood-Brain Barrier Brain delivery |
| title | Surface-modified gatifloxacin nanoparticles with potential for treating central nervous system tuberculosis |
| title_full | Surface-modified gatifloxacin nanoparticles with potential for treating central nervous system tuberculosis |
| title_fullStr | Surface-modified gatifloxacin nanoparticles with potential for treating central nervous system tuberculosis |
| title_full_unstemmed | Surface-modified gatifloxacin nanoparticles with potential for treating central nervous system tuberculosis |
| title_short | Surface-modified gatifloxacin nanoparticles with potential for treating central nervous system tuberculosis |
| title_sort | surface modified gatifloxacin nanoparticles with potential for treating central nervous system tuberculosis |
| topic | Polysorbate 80 Labrafil Gatifloxacin Nanoparticles Targeting Blood-Brain Barrier Brain delivery |
| url | https://www.dovepress.com/surface-modified-gatifloxacin-nanoparticles-with-potential-for-treatin-peer-reviewed-article-IJN |
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