Nanoparticules muco-pénétrantes: véhicules pour l’administration orale du paclitaxel
Paclitaxel is an anticancer drug used as solution for perfusion for the treatment of certain types of cancers. In the last years, a number of strategies have been proposed for the development of an oral formulation of this drug. However, this task is quite complicated due to the poor aqueous solubil...
| Autores: | , , , , , , |
|---|---|
| Formato: | artículo |
| Fecha de publicación: | 2013 |
| País: | España |
| Recursos: | Universidad de Navarra |
| Repositorio: | Dadun. Depósito Académico Digital de la Universidad de Navarra |
| Idioma: | francés |
| OAI Identifier: | oai:dadun.unav.edu:10171/29211 |
| Acesso em linha: | https://hdl.handle.net/10171/29211 |
| Access Level: | acceso abierto |
| Palavra-chave: | Nanoparticles Paclitaxel Oral Poly(ethylene glycol) Controlled release |
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Nanoparticules muco-pénétrantes: véhicules pour l’administration orale du paclitaxelMuco-penetrating nanoparticles: vehicles for the oral administration of paclitaxelZabaleta, V. (Virginia)|||/items/a9d12878-8a6c-445c-91a8-8ab784e9b343Calleja, P. (Patricia)|||/items/ace0469f-1278-4224-ae64-5620cc933addEspuelas, S. (Socorro)|||/items/b57c05de-0bc4-4fcf-ae1e-c9b2fb92964cCorrales, L. (Leticia)|||/items/25c2d48d-8ffb-42b9-adab-dd66b9660e88Pio, R. (Rubén)|||/items/d5c409b3-dbed-4f0c-8bad-94c31e0e5a95Agüeros, M. (Maite)|||/items/a9af1dc6-4b7f-4957-a249-8787aead4212Irache-Garreta, J.M. (Juan Manuel)|||/items/c7cbbe9e-faeb-47e1-b7e8-2d956ca50173NanoparticlesPaclitaxelOralPoly(ethylene glycol)Controlled releasePaclitaxel is an anticancer drug used as solution for perfusion for the treatment of certain types of cancers. In the last years, a number of strategies have been proposed for the development of an oral formulation of this drug. However, this task is quite complicated due to the poor aqueous solubility of paclitaxel as well as the fact that this compound is substrate of the intestinal P-glycoprotein and the cytochrome P450 enzymatic complex. In this work, we have developed pegylated nanoparticles with mucopenetrating properties in order to conduct paclitaxel onto the surface of the enterocyte. These nanoparticles displayed a size of about 180 nm and a drug loading close to 15% by weight. The pharmacokinetic study in mice has shown that these nanoparticles were capable to offer therapeutic plasma levels of paclitaxel up to 72 hours. In addition, the oral relative bioavailability of paclitaxel when loaded in nanoparticles pegylated with poly(ethylene glycol) 2000 (PEG) was found to be 85%. In a subcutaneous model of tumour in mice, these pegylated nanoparticles administered orally every 3 days have demonstrated a similar efficacy than Taxol® administered intravenously every day during 9 days. All of these results suggested that these pegylated nanoparticles were capable to cross the mucus layer of the gut and, then, reach the surface of the enterocytes. The PEG molecules would facilitate the adhesion of nanoparticles to this epithelial surface, minimise the pre-systemic metabolism of paclitaxel and, thus, promote its absorption.Académie Nationale de PharmacieDadun. Depósito Académico Digital Universidad de Navarra20132013-05-2720132013-01-0120132013-01-01journal articlehttp://purl.org/coar/resource_type/c_6501info:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/10171/29211reponame:Dadun. Depósito Académico Digital de la Universidad de Navarrainstname:Universidad de NavarraFrancésfraopen accesshttp://purl.org/coar/access_right/c_abf2info:eu-repo/semantics/openAccessoai:dadun.unav.edu:10171/292112026-06-21T12:47:57Z |
| dc.title.none.fl_str_mv |
Nanoparticules muco-pénétrantes: véhicules pour l’administration orale du paclitaxel Muco-penetrating nanoparticles: vehicles for the oral administration of paclitaxel |
| title |
Nanoparticules muco-pénétrantes: véhicules pour l’administration orale du paclitaxel |
| spellingShingle |
Nanoparticules muco-pénétrantes: véhicules pour l’administration orale du paclitaxel Zabaleta, V. (Virginia)|||/items/a9d12878-8a6c-445c-91a8-8ab784e9b343 Nanoparticles Paclitaxel Oral Poly(ethylene glycol) Controlled release |
| title_short |
Nanoparticules muco-pénétrantes: véhicules pour l’administration orale du paclitaxel |
| title_full |
Nanoparticules muco-pénétrantes: véhicules pour l’administration orale du paclitaxel |
| title_fullStr |
Nanoparticules muco-pénétrantes: véhicules pour l’administration orale du paclitaxel |
| title_full_unstemmed |
Nanoparticules muco-pénétrantes: véhicules pour l’administration orale du paclitaxel |
| title_sort |
Nanoparticules muco-pénétrantes: véhicules pour l’administration orale du paclitaxel |
| dc.creator.none.fl_str_mv |
Zabaleta, V. (Virginia)|||/items/a9d12878-8a6c-445c-91a8-8ab784e9b343 Calleja, P. (Patricia)|||/items/ace0469f-1278-4224-ae64-5620cc933add Espuelas, S. (Socorro)|||/items/b57c05de-0bc4-4fcf-ae1e-c9b2fb92964c Corrales, L. (Leticia)|||/items/25c2d48d-8ffb-42b9-adab-dd66b9660e88 Pio, R. (Rubén)|||/items/d5c409b3-dbed-4f0c-8bad-94c31e0e5a95 Agüeros, M. (Maite)|||/items/a9af1dc6-4b7f-4957-a249-8787aead4212 Irache-Garreta, J.M. (Juan Manuel)|||/items/c7cbbe9e-faeb-47e1-b7e8-2d956ca50173 |
| author |
Zabaleta, V. (Virginia)|||/items/a9d12878-8a6c-445c-91a8-8ab784e9b343 |
| author_facet |
Zabaleta, V. (Virginia)|||/items/a9d12878-8a6c-445c-91a8-8ab784e9b343 Calleja, P. (Patricia)|||/items/ace0469f-1278-4224-ae64-5620cc933add Espuelas, S. (Socorro)|||/items/b57c05de-0bc4-4fcf-ae1e-c9b2fb92964c Corrales, L. (Leticia)|||/items/25c2d48d-8ffb-42b9-adab-dd66b9660e88 Pio, R. (Rubén)|||/items/d5c409b3-dbed-4f0c-8bad-94c31e0e5a95 Agüeros, M. (Maite)|||/items/a9af1dc6-4b7f-4957-a249-8787aead4212 Irache-Garreta, J.M. (Juan Manuel)|||/items/c7cbbe9e-faeb-47e1-b7e8-2d956ca50173 |
| author_role |
author |
| author2 |
Calleja, P. (Patricia)|||/items/ace0469f-1278-4224-ae64-5620cc933add Espuelas, S. (Socorro)|||/items/b57c05de-0bc4-4fcf-ae1e-c9b2fb92964c Corrales, L. (Leticia)|||/items/25c2d48d-8ffb-42b9-adab-dd66b9660e88 Pio, R. (Rubén)|||/items/d5c409b3-dbed-4f0c-8bad-94c31e0e5a95 Agüeros, M. (Maite)|||/items/a9af1dc6-4b7f-4957-a249-8787aead4212 Irache-Garreta, J.M. (Juan Manuel)|||/items/c7cbbe9e-faeb-47e1-b7e8-2d956ca50173 |
| author2_role |
author author author author author author |
| dc.contributor.none.fl_str_mv |
Dadun. Depósito Académico Digital Universidad de Navarra |
| dc.subject.none.fl_str_mv |
Nanoparticles Paclitaxel Oral Poly(ethylene glycol) Controlled release |
| topic |
Nanoparticles Paclitaxel Oral Poly(ethylene glycol) Controlled release |
| description |
Paclitaxel is an anticancer drug used as solution for perfusion for the treatment of certain types of cancers. In the last years, a number of strategies have been proposed for the development of an oral formulation of this drug. However, this task is quite complicated due to the poor aqueous solubility of paclitaxel as well as the fact that this compound is substrate of the intestinal P-glycoprotein and the cytochrome P450 enzymatic complex. In this work, we have developed pegylated nanoparticles with mucopenetrating properties in order to conduct paclitaxel onto the surface of the enterocyte. These nanoparticles displayed a size of about 180 nm and a drug loading close to 15% by weight. The pharmacokinetic study in mice has shown that these nanoparticles were capable to offer therapeutic plasma levels of paclitaxel up to 72 hours. In addition, the oral relative bioavailability of paclitaxel when loaded in nanoparticles pegylated with poly(ethylene glycol) 2000 (PEG) was found to be 85%. In a subcutaneous model of tumour in mice, these pegylated nanoparticles administered orally every 3 days have demonstrated a similar efficacy than Taxol® administered intravenously every day during 9 days. All of these results suggested that these pegylated nanoparticles were capable to cross the mucus layer of the gut and, then, reach the surface of the enterocytes. The PEG molecules would facilitate the adhesion of nanoparticles to this epithelial surface, minimise the pre-systemic metabolism of paclitaxel and, thus, promote its absorption. |
| publishDate |
2013 |
| dc.date.none.fl_str_mv |
2013 2013-05-27 2013 2013-01-01 2013 2013-01-01 |
| dc.type.none.fl_str_mv |
journal article http://purl.org/coar/resource_type/c_6501 |
| dc.type.openaire.fl_str_mv |
info:eu-repo/semantics/article |
| format |
article |
| dc.identifier.none.fl_str_mv |
https://hdl.handle.net/10171/29211 |
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https://hdl.handle.net/10171/29211 |
| dc.language.none.fl_str_mv |
Francés fra |
| language_invalid_str_mv |
Francés |
| language |
fra |
| dc.rights.none.fl_str_mv |
open access http://purl.org/coar/access_right/c_abf2 |
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info:eu-repo/semantics/openAccess |
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open access http://purl.org/coar/access_right/c_abf2 |
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openAccess |
| dc.format.none.fl_str_mv |
application/pdf |
| dc.publisher.none.fl_str_mv |
Académie Nationale de Pharmacie |
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Académie Nationale de Pharmacie |
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reponame:Dadun. Depósito Académico Digital de la Universidad de Navarra instname:Universidad de Navarra |
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Universidad de Navarra |
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Dadun. Depósito Académico Digital de la Universidad de Navarra |
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Dadun. Depósito Académico Digital de la Universidad de Navarra |
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15.301603 |