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...

Descripción completa

Detalles Bibliográficos
Autores principales: Nimtrakul, Pataranapa, Sermsappasuk, Pakawadee, Tiyaboonchai, Waree
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