Cargando…
Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers
The oral delivery of amphotericin B (AmB) has remained a challenge due to its low solubility, permeability, and instability in gastric acidic pH. To solve these issues, herein, we reported a novel approach of using nanostructured lipid carriers (NLCs) and NLCs coating with Eudragit(®)L100-55 (Eu-NLC...
Autores principales: | , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2020
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7470155/ https://www.ncbi.nlm.nih.gov/pubmed/32633144 http://dx.doi.org/10.1080/10717544.2020.1785050 |
_version_ | 1783578530993405952 |
---|---|
author | Nimtrakul, Pataranapa Sermsappasuk, Pakawadee Tiyaboonchai, Waree |
author_facet | Nimtrakul, Pataranapa Sermsappasuk, Pakawadee Tiyaboonchai, Waree |
author_sort | Nimtrakul, Pataranapa |
collection | PubMed |
description | The oral delivery of amphotericin B (AmB) has remained a challenge due to its low solubility, permeability, and instability in gastric acidic pH. To solve these issues, herein, we reported a novel approach of using nanostructured lipid carriers (NLCs) and NLCs coating with Eudragit(®)L100-55 (Eu-NLCs) for the oral delivery of AmB. This study aimed to compare their ability in protecting the drug from degradation in gastrointestinal fluids and permeation enhancement in Caco-2 cells. Uncoated NLCs and Eu-NLCs possessed a mean particle size of ∼180 and ∼550 nm, with a zeta potential of ∼−30 and ∼−50 mV, respectively. Both NLCs demonstrated an AmB entrapment efficiency up to ∼75%. They possessed significantly greater AmB water solubility than the free drug by up to 10-fold. In fasted state simulated gastric fluid, Eu-NLCs provided significantly greater AmB protection from acidic degradation than uncoated NLCs. In fasted state simulated intestinal fluid, both uncoated and Eu-NLCs showed a fast release characteristic. Caco-2 cells permeation studies revealed that uncoated NLCs provided significantly higher apparent permeation coefficient (P(app)) value than Eu-NLCs. Moreover, after 6 months of storage at 4 °C in the absence of light, the physicochemical stabilities of the lyophilized uncoated and Eu-NLCs could be maintained. In conclusion, the developed NLCs and Eu-NLCs could be a potential drug delivery system in improving the oral bioavailability of AmB. |
format | Online Article Text |
id | pubmed-7470155 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
spelling | pubmed-74701552020-09-15 Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers Nimtrakul, Pataranapa Sermsappasuk, Pakawadee Tiyaboonchai, Waree Drug Deliv Research Article The oral delivery of amphotericin B (AmB) has remained a challenge due to its low solubility, permeability, and instability in gastric acidic pH. To solve these issues, herein, we reported a novel approach of using nanostructured lipid carriers (NLCs) and NLCs coating with Eudragit(®)L100-55 (Eu-NLCs) for the oral delivery of AmB. This study aimed to compare their ability in protecting the drug from degradation in gastrointestinal fluids and permeation enhancement in Caco-2 cells. Uncoated NLCs and Eu-NLCs possessed a mean particle size of ∼180 and ∼550 nm, with a zeta potential of ∼−30 and ∼−50 mV, respectively. Both NLCs demonstrated an AmB entrapment efficiency up to ∼75%. They possessed significantly greater AmB water solubility than the free drug by up to 10-fold. In fasted state simulated gastric fluid, Eu-NLCs provided significantly greater AmB protection from acidic degradation than uncoated NLCs. In fasted state simulated intestinal fluid, both uncoated and Eu-NLCs showed a fast release characteristic. Caco-2 cells permeation studies revealed that uncoated NLCs provided significantly higher apparent permeation coefficient (P(app)) value than Eu-NLCs. Moreover, after 6 months of storage at 4 °C in the absence of light, the physicochemical stabilities of the lyophilized uncoated and Eu-NLCs could be maintained. In conclusion, the developed NLCs and Eu-NLCs could be a potential drug delivery system in improving the oral bioavailability of AmB. Taylor & Francis 2020-07-07 /pmc/articles/PMC7470155/ /pubmed/32633144 http://dx.doi.org/10.1080/10717544.2020.1785050 Text en © 2020 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by-nc/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial License (http://creativecommons.org/licenses/by-nc/4.0/ (https://creativecommons.org/licenses/by-nc/4.0/) ), which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Nimtrakul, Pataranapa Sermsappasuk, Pakawadee Tiyaboonchai, Waree Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers |
title | Strategies to enhance oral delivery of amphotericin B: a comparison of
uncoated and enteric-coated nanostructured lipid carriers |
title_full | Strategies to enhance oral delivery of amphotericin B: a comparison of
uncoated and enteric-coated nanostructured lipid carriers |
title_fullStr | Strategies to enhance oral delivery of amphotericin B: a comparison of
uncoated and enteric-coated nanostructured lipid carriers |
title_full_unstemmed | Strategies to enhance oral delivery of amphotericin B: a comparison of
uncoated and enteric-coated nanostructured lipid carriers |
title_short | Strategies to enhance oral delivery of amphotericin B: a comparison of
uncoated and enteric-coated nanostructured lipid carriers |
title_sort | strategies to enhance oral delivery of amphotericin b: a comparison of
uncoated and enteric-coated nanostructured lipid carriers |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7470155/ https://www.ncbi.nlm.nih.gov/pubmed/32633144 http://dx.doi.org/10.1080/10717544.2020.1785050 |
work_keys_str_mv | AT nimtrakulpataranapa strategiestoenhanceoraldeliveryofamphotericinbacomparisonofuncoatedandentericcoatednanostructuredlipidcarriers AT sermsappasukpakawadee strategiestoenhanceoraldeliveryofamphotericinbacomparisonofuncoatedandentericcoatednanostructuredlipidcarriers AT tiyaboonchaiwaree strategiestoenhanceoraldeliveryofamphotericinbacomparisonofuncoatedandentericcoatednanostructuredlipidcarriers |