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Nonionic Microemulsions as Solubilizers of Hydrophobic Drugs: Solubilization of Paclitaxel

The strategy using nonionic microemulsion as a solubilizer for hydrophobic drugs was studied and is demonstrated in this work. The aqueous phase behaviors of mixed nonionic surfactants with various oils at 37 °C are firstly constructed to give the optimal formulations of nonionic microemulsions with...

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Autores principales: Lo, Jen-Ting, Lee, Tzer-Min, Chen, Bing-Hung
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5457098/
https://www.ncbi.nlm.nih.gov/pubmed/28773882
http://dx.doi.org/10.3390/ma9090761
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author Lo, Jen-Ting
Lee, Tzer-Min
Chen, Bing-Hung
author_facet Lo, Jen-Ting
Lee, Tzer-Min
Chen, Bing-Hung
author_sort Lo, Jen-Ting
collection PubMed
description The strategy using nonionic microemulsion as a solubilizer for hydrophobic drugs was studied and is demonstrated in this work. The aqueous phase behaviors of mixed nonionic surfactants with various oils at 37 °C are firstly constructed to give the optimal formulations of nonionic microemulsions with applications in the enhanced solubilization of the model hydrophobic drug, paclitaxel, at 37 °C. Briefly, the suitable oil phase with paclitaxel significantly dissolved is microemulsified with appropriate surfactants. Surfactants utilized include Tween 80, Cremophor EL, and polyethylene glycol (4.3) cocoyl ether, while various kinds of edible oils and fatty esters are used as the oil phase. On average, the apparent solubility of paclitaxel is increased to ca. 70–100 ppm in the prepared microemulsions at 37 °C using tributyrin or ethyl caproate as the oil phases. The sizes of the microemulsions attained are mostly from ca. 60 nm to ca. 200 nm. The cytotoxicity of the microemulsion formulations is assessed with the cellular viability of 3T3 cells. In general, the cell viability is above 55% after 24 h of cultivation in media containing these microemulsion formulations diluted to a concentration of total surfactants equal to 50 ppm and 200 ppm.
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spelling pubmed-54570982017-07-28 Nonionic Microemulsions as Solubilizers of Hydrophobic Drugs: Solubilization of Paclitaxel Lo, Jen-Ting Lee, Tzer-Min Chen, Bing-Hung Materials (Basel) Article The strategy using nonionic microemulsion as a solubilizer for hydrophobic drugs was studied and is demonstrated in this work. The aqueous phase behaviors of mixed nonionic surfactants with various oils at 37 °C are firstly constructed to give the optimal formulations of nonionic microemulsions with applications in the enhanced solubilization of the model hydrophobic drug, paclitaxel, at 37 °C. Briefly, the suitable oil phase with paclitaxel significantly dissolved is microemulsified with appropriate surfactants. Surfactants utilized include Tween 80, Cremophor EL, and polyethylene glycol (4.3) cocoyl ether, while various kinds of edible oils and fatty esters are used as the oil phase. On average, the apparent solubility of paclitaxel is increased to ca. 70–100 ppm in the prepared microemulsions at 37 °C using tributyrin or ethyl caproate as the oil phases. The sizes of the microemulsions attained are mostly from ca. 60 nm to ca. 200 nm. The cytotoxicity of the microemulsion formulations is assessed with the cellular viability of 3T3 cells. In general, the cell viability is above 55% after 24 h of cultivation in media containing these microemulsion formulations diluted to a concentration of total surfactants equal to 50 ppm and 200 ppm. MDPI 2016-09-07 /pmc/articles/PMC5457098/ /pubmed/28773882 http://dx.doi.org/10.3390/ma9090761 Text en © 2016 by the authors; Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Lo, Jen-Ting
Lee, Tzer-Min
Chen, Bing-Hung
Nonionic Microemulsions as Solubilizers of Hydrophobic Drugs: Solubilization of Paclitaxel
title Nonionic Microemulsions as Solubilizers of Hydrophobic Drugs: Solubilization of Paclitaxel
title_full Nonionic Microemulsions as Solubilizers of Hydrophobic Drugs: Solubilization of Paclitaxel
title_fullStr Nonionic Microemulsions as Solubilizers of Hydrophobic Drugs: Solubilization of Paclitaxel
title_full_unstemmed Nonionic Microemulsions as Solubilizers of Hydrophobic Drugs: Solubilization of Paclitaxel
title_short Nonionic Microemulsions as Solubilizers of Hydrophobic Drugs: Solubilization of Paclitaxel
title_sort nonionic microemulsions as solubilizers of hydrophobic drugs: solubilization of paclitaxel
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5457098/
https://www.ncbi.nlm.nih.gov/pubmed/28773882
http://dx.doi.org/10.3390/ma9090761
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