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Liposomes coated with N-trimethyl chitosan to improve the absorption of harmine in vivo and in vitro
In this study, harmine liposomes (HM-lip) were prepared through the thin-film hydration–pH-gradient method and then coated with N-trimethyl chitosan (TMC). Particle size, zeta potential, entrapment efficiency, and in vitro release of HM-lip and TMC-coated harmine liposomes (TMC-HM-lip) were also det...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Dove Medical Press
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4725628/ https://www.ncbi.nlm.nih.gov/pubmed/26855571 http://dx.doi.org/10.2147/IJN.S95540 |
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author | Chen, Wei-liang Yuan, Zhi-Qiang Liu, Yang Yang, Shu-di Zhang, Chun-ge Li, Ji-zhao Zhu, Wen-jing Li, Fang Zhou, Xiao-feng Lin, Yi-mei Zhang, Xue-nong |
author_facet | Chen, Wei-liang Yuan, Zhi-Qiang Liu, Yang Yang, Shu-di Zhang, Chun-ge Li, Ji-zhao Zhu, Wen-jing Li, Fang Zhou, Xiao-feng Lin, Yi-mei Zhang, Xue-nong |
author_sort | Chen, Wei-liang |
collection | PubMed |
description | In this study, harmine liposomes (HM-lip) were prepared through the thin-film hydration–pH-gradient method and then coated with N-trimethyl chitosan (TMC). Particle size, zeta potential, entrapment efficiency, and in vitro release of HM-lip and TMC-coated harmine liposomes (TMC-HM-lip) were also determined. Sprague Dawley rats were further used to investigate the pharmacokinetics in vivo. Retention behavior in mouse gastrointestinal tract (GIT) was studied through high-performance liquid chromatography and near-infrared imaging. Degradation was further evaluated through incubation with Caco-2 cell homogenates, and a Caco-2 monolayer cell model was used to investigate the uptake and transport of drugs. HM-lip and TMC-HM-lip with particle size of 150–170 nm, an entrapment efficiency of about 81%, and a zeta potential of negative and positive, respectively, were prepared. The release of HM from HM-lip and TMC-HM-lip was slower than that from HM solution and was sensitive to pH. TMC-HM-lip exhibited higher oral bioavailability and had prolonged retention time in GIT. HM-lip and TMC-HM-lip could also protect HM against degradation in Caco-2 cell homogenates. The uptake amount of TMC-HM-lip was higher than that of HM and HM-lip. TMC-HM-lip further demonstrated higher apparent permeability coefficient (P(app)) from the apical to the basolateral side than HM and HM-lip because of its higher uptake and capability to open tight junctions in the cell monolayers. TMC-HM-lip can prolong the retention time in the GIT, protect HM against enzyme degradation, and improve transport across Caco-2 cell monolayers, thus enhancing the oral bioavailability of HM. |
format | Online Article Text |
id | pubmed-4725628 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-47256282016-02-05 Liposomes coated with N-trimethyl chitosan to improve the absorption of harmine in vivo and in vitro Chen, Wei-liang Yuan, Zhi-Qiang Liu, Yang Yang, Shu-di Zhang, Chun-ge Li, Ji-zhao Zhu, Wen-jing Li, Fang Zhou, Xiao-feng Lin, Yi-mei Zhang, Xue-nong Int J Nanomedicine Original Research In this study, harmine liposomes (HM-lip) were prepared through the thin-film hydration–pH-gradient method and then coated with N-trimethyl chitosan (TMC). Particle size, zeta potential, entrapment efficiency, and in vitro release of HM-lip and TMC-coated harmine liposomes (TMC-HM-lip) were also determined. Sprague Dawley rats were further used to investigate the pharmacokinetics in vivo. Retention behavior in mouse gastrointestinal tract (GIT) was studied through high-performance liquid chromatography and near-infrared imaging. Degradation was further evaluated through incubation with Caco-2 cell homogenates, and a Caco-2 monolayer cell model was used to investigate the uptake and transport of drugs. HM-lip and TMC-HM-lip with particle size of 150–170 nm, an entrapment efficiency of about 81%, and a zeta potential of negative and positive, respectively, were prepared. The release of HM from HM-lip and TMC-HM-lip was slower than that from HM solution and was sensitive to pH. TMC-HM-lip exhibited higher oral bioavailability and had prolonged retention time in GIT. HM-lip and TMC-HM-lip could also protect HM against degradation in Caco-2 cell homogenates. The uptake amount of TMC-HM-lip was higher than that of HM and HM-lip. TMC-HM-lip further demonstrated higher apparent permeability coefficient (P(app)) from the apical to the basolateral side than HM and HM-lip because of its higher uptake and capability to open tight junctions in the cell monolayers. TMC-HM-lip can prolong the retention time in the GIT, protect HM against enzyme degradation, and improve transport across Caco-2 cell monolayers, thus enhancing the oral bioavailability of HM. Dove Medical Press 2016-01-19 /pmc/articles/PMC4725628/ /pubmed/26855571 http://dx.doi.org/10.2147/IJN.S95540 Text en © 2016 Chen et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. |
spellingShingle | Original Research Chen, Wei-liang Yuan, Zhi-Qiang Liu, Yang Yang, Shu-di Zhang, Chun-ge Li, Ji-zhao Zhu, Wen-jing Li, Fang Zhou, Xiao-feng Lin, Yi-mei Zhang, Xue-nong Liposomes coated with N-trimethyl chitosan to improve the absorption of harmine in vivo and in vitro |
title | Liposomes coated with N-trimethyl chitosan to improve the absorption of harmine in vivo and in vitro |
title_full | Liposomes coated with N-trimethyl chitosan to improve the absorption of harmine in vivo and in vitro |
title_fullStr | Liposomes coated with N-trimethyl chitosan to improve the absorption of harmine in vivo and in vitro |
title_full_unstemmed | Liposomes coated with N-trimethyl chitosan to improve the absorption of harmine in vivo and in vitro |
title_short | Liposomes coated with N-trimethyl chitosan to improve the absorption of harmine in vivo and in vitro |
title_sort | liposomes coated with n-trimethyl chitosan to improve the absorption of harmine in vivo and in vitro |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4725628/ https://www.ncbi.nlm.nih.gov/pubmed/26855571 http://dx.doi.org/10.2147/IJN.S95540 |
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