Effects of PEGylation on the physicochemical properties and in vivo distribution of organic nanotubes

Effects of PEGylation on the physicochemical properties and in vivo distribution of organic nanotubes

Wuxiao Ding, Hiroyuki Minamikawa, Naohiro Kameta, Toshimi Shimizu, Mitsutoshi Masuda Nanosystem Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), Ibaraki, Japan Abstract: Application of organic nanotubes (ONTs) into drug nanocarriers ultimately requires...

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Autores principales: Ding W, Minamikawa H, Kameta N, Shimizu T, Masuda M
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2014
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Medicine (General)
R5-920
Acceso en línea:https://doaj.org/article/854ff55933c94a95a1697dabd58e3e64
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spelling oai:doaj.org-article:854ff55933c94a95a1697dabd58e3e642021-12-02T06:31:50ZEffects of PEGylation on the physicochemical properties and in vivo distribution of organic nanotubes1178-2013https://doaj.org/article/854ff55933c94a95a1697dabd58e3e642014-12-01T00:00:00Zhttp://www.dovepress.com/effects-of-pegylation-on-the-physicochemical-properties-and-in-vivo-di-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Wuxiao Ding, Hiroyuki Minamikawa, Naohiro Kameta, Toshimi Shimizu, Mitsutoshi Masuda Nanosystem Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), Ibaraki, Japan Abstract: Application of organic nanotubes (ONTs) into drug nanocarriers ultimately requires validation in live animals. For improving the dispersibility in biological media and in vivo distribution, the outer surface of an ONT was functionalized with polyethylene glycol (PEG) via the coassembly of an ONT-forming lipid with 5–20 mol% of a PEG-tethered lipid analogue (PEG-lipid). Firstly, the effect of PEGylation on the psysicochemical properties of ONTs, such as morphology and dispersibility, was investigated. PEGylation of ONTs slightly reduced the average length and effectively prevented the aggregation in phosphate-buffered saline (PBS). The PEGylated ONTs even showed high thermal stability in aqueous dispersion at least up to 95°C. Secondly, differential scanning calorimetry and powder X-ray diffraction indicated that ~10 mol% of PEG-lipid was completely incorporated into the ONTs, while 20 mol% of PEG-lipid encountered a partial phase separation during coassembly. In the heating differential scanning calorimetry runs, the resultant PEGylated ONTs with 5 mol% PEG-lipid showed no sign of phase separation up to 180°C under lyophilized condition, while those with 10 mol% and 20 mol% PEG-lipid showed some phase separation of the PEG-lipid above 120°C. Finally, PEGylation significantly affected the tissue distribution and prolonged the persistence time in the blood in mice. Non-PEGylated ONTs was quickly cleared from the circulation after intravenous infusion and preferentially accumulated in the lung, while PEGylated ONTs was mainly trapped in the liver and could circulate in the blood up to 24 hours. This study provided valuable information of physicochemical properties and the in vivo distribution behavior of PEGylated ONTs for their potential application into drug nanocarriers. Keywords: nanostructure, dispersibility, distributionDing WMinamikawa HKameta NShimizu TMasuda MDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 5811-5823 (2014)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Ding W
Minamikawa H
Kameta N
Shimizu T
Masuda M
Effects of PEGylation on the physicochemical properties and in vivo distribution of organic nanotubes
description Wuxiao Ding, Hiroyuki Minamikawa, Naohiro Kameta, Toshimi Shimizu, Mitsutoshi Masuda Nanosystem Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), Ibaraki, Japan Abstract: Application of organic nanotubes (ONTs) into drug nanocarriers ultimately requires validation in live animals. For improving the dispersibility in biological media and in vivo distribution, the outer surface of an ONT was functionalized with polyethylene glycol (PEG) via the coassembly of an ONT-forming lipid with 5–20 mol% of a PEG-tethered lipid analogue (PEG-lipid). Firstly, the effect of PEGylation on the psysicochemical properties of ONTs, such as morphology and dispersibility, was investigated. PEGylation of ONTs slightly reduced the average length and effectively prevented the aggregation in phosphate-buffered saline (PBS). The PEGylated ONTs even showed high thermal stability in aqueous dispersion at least up to 95°C. Secondly, differential scanning calorimetry and powder X-ray diffraction indicated that ~10 mol% of PEG-lipid was completely incorporated into the ONTs, while 20 mol% of PEG-lipid encountered a partial phase separation during coassembly. In the heating differential scanning calorimetry runs, the resultant PEGylated ONTs with 5 mol% PEG-lipid showed no sign of phase separation up to 180°C under lyophilized condition, while those with 10 mol% and 20 mol% PEG-lipid showed some phase separation of the PEG-lipid above 120°C. Finally, PEGylation significantly affected the tissue distribution and prolonged the persistence time in the blood in mice. Non-PEGylated ONTs was quickly cleared from the circulation after intravenous infusion and preferentially accumulated in the lung, while PEGylated ONTs was mainly trapped in the liver and could circulate in the blood up to 24 hours. This study provided valuable information of physicochemical properties and the in vivo distribution behavior of PEGylated ONTs for their potential application into drug nanocarriers. Keywords: nanostructure, dispersibility, distribution
format article
author Ding W
Minamikawa H
Kameta N
Shimizu T
Masuda M
author_facet Ding W
Minamikawa H
Kameta N
Shimizu T
Masuda M
author_sort Ding W
title Effects of PEGylation on the physicochemical properties and in vivo distribution of organic nanotubes
title_short Effects of PEGylation on the physicochemical properties and in vivo distribution of organic nanotubes
title_full Effects of PEGylation on the physicochemical properties and in vivo distribution of organic nanotubes
title_fullStr Effects of PEGylation on the physicochemical properties and in vivo distribution of organic nanotubes
title_full_unstemmed Effects of PEGylation on the physicochemical properties and in vivo distribution of organic nanotubes
title_sort effects of pegylation on the physicochemical properties and in vivo distribution of organic nanotubes
publisher Dove Medical Press
publishDate 2014
url https://doaj.org/article/854ff55933c94a95a1697dabd58e3e64
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AT minamikawah effectsofpegylationonthephysicochemicalpropertiesandinvivodistributionoforganicnbspnanotubes
AT kametan effectsofpegylationonthephysicochemicalpropertiesandinvivodistributionoforganicnbspnanotubes
AT shimizut effectsofpegylationonthephysicochemicalpropertiesandinvivodistributionoforganicnbspnanotubes
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