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Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration
Intravenously administered for the treatment of rectum cancer, irinotecan produces severe side effects due to very high plasma concentrations. A novel irinotecan-encapsulated double reverse thermosensitive nanocarrier system (DRTN) for rectal administration was developed as an alternative. The DRTN...
Autores principales: | , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8241086/ https://www.ncbi.nlm.nih.gov/pubmed/28181835 http://dx.doi.org/10.1080/10717544.2016.1272651 |
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author | Din, Fakhar ud Choi, Ju Yeon Kim, Dong Wuk Mustapha, Omer Kim, Dong Shik Thapa, Raj Kumar Ku, Sae Kwang Youn, Yu Seok Oh, Kyung Taek Yong, Chul Soon Kim, Jong Oh Choi, Han-Gon |
author_facet | Din, Fakhar ud Choi, Ju Yeon Kim, Dong Wuk Mustapha, Omer Kim, Dong Shik Thapa, Raj Kumar Ku, Sae Kwang Youn, Yu Seok Oh, Kyung Taek Yong, Chul Soon Kim, Jong Oh Choi, Han-Gon |
author_sort | Din, Fakhar ud |
collection | PubMed |
description | Intravenously administered for the treatment of rectum cancer, irinotecan produces severe side effects due to very high plasma concentrations. A novel irinotecan-encapsulated double reverse thermosensitive nanocarrier system (DRTN) for rectal administration was developed as an alternative. The DRTN was fabricated by dispersing the thermosensitive irinotecan-encapsulated solid lipid nanoparticles (SLN) in the thermosensitive poloxamer solution. Its gel properties, pharmacokinetics, morphology, anticancer activity and immunohistopathology were assessed after its rectal administration to rats and tumor-bearing mice. In the DRTN, the solid form of the SLN and the liquid form of the poloxamer solution persisted at 25 °C; the former melted to liquid, and the latter altered to gel at 36.5 °C. The DRTN was easily administered to the anus, gelling rapidly and strongly after rectal administration. Compared to the conventional hydrogel and intravenously administered solution, it retarded dissolution and initial plasma concentration. The DRTN gave sustained release and nearly constant plasma concentrations of irinotecan at 1–3 h in rats, resulting in improved anticancer activity. It induced no damage to the rat rectum and no body weight loss in tumor-bearing mice. Thus, this irinotecan-encapsulated DRTN associated with a reduced burst effect, lack of toxicity and excellent antitumor efficacy would be strongly recommended as a rectal pharmaceutical product alternative to commercial intravenous injection in the treatment of rectum and colon cancer. |
format | Online Article Text |
id | pubmed-8241086 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
spelling | pubmed-82410862021-07-08 Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration Din, Fakhar ud Choi, Ju Yeon Kim, Dong Wuk Mustapha, Omer Kim, Dong Shik Thapa, Raj Kumar Ku, Sae Kwang Youn, Yu Seok Oh, Kyung Taek Yong, Chul Soon Kim, Jong Oh Choi, Han-Gon Drug Deliv Research Article Intravenously administered for the treatment of rectum cancer, irinotecan produces severe side effects due to very high plasma concentrations. A novel irinotecan-encapsulated double reverse thermosensitive nanocarrier system (DRTN) for rectal administration was developed as an alternative. The DRTN was fabricated by dispersing the thermosensitive irinotecan-encapsulated solid lipid nanoparticles (SLN) in the thermosensitive poloxamer solution. Its gel properties, pharmacokinetics, morphology, anticancer activity and immunohistopathology were assessed after its rectal administration to rats and tumor-bearing mice. In the DRTN, the solid form of the SLN and the liquid form of the poloxamer solution persisted at 25 °C; the former melted to liquid, and the latter altered to gel at 36.5 °C. The DRTN was easily administered to the anus, gelling rapidly and strongly after rectal administration. Compared to the conventional hydrogel and intravenously administered solution, it retarded dissolution and initial plasma concentration. The DRTN gave sustained release and nearly constant plasma concentrations of irinotecan at 1–3 h in rats, resulting in improved anticancer activity. It induced no damage to the rat rectum and no body weight loss in tumor-bearing mice. Thus, this irinotecan-encapsulated DRTN associated with a reduced burst effect, lack of toxicity and excellent antitumor efficacy would be strongly recommended as a rectal pharmaceutical product alternative to commercial intravenous injection in the treatment of rectum and colon cancer. Taylor & Francis 2017-02-09 /pmc/articles/PMC8241086/ /pubmed/28181835 http://dx.doi.org/10.1080/10717544.2016.1272651 Text en © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Din, Fakhar ud Choi, Ju Yeon Kim, Dong Wuk Mustapha, Omer Kim, Dong Shik Thapa, Raj Kumar Ku, Sae Kwang Youn, Yu Seok Oh, Kyung Taek Yong, Chul Soon Kim, Jong Oh Choi, Han-Gon Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration |
title | Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration |
title_full | Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration |
title_fullStr | Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration |
title_full_unstemmed | Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration |
title_short | Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration |
title_sort | irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8241086/ https://www.ncbi.nlm.nih.gov/pubmed/28181835 http://dx.doi.org/10.1080/10717544.2016.1272651 |
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