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Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study

BACKGROUND: Phytostanols are naturally occurring compounds that reduce blood cholesterol levels significantly. However, their aqueous insolubility poses formulation challenges. AIM: To formulate and characterize solid lipid nanoparticle carriers for phytostanol esters to enhance the bioavailability...

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Autores principales: Shrestha, Sony Chandi, Ghebremeskel, Kebreab, White, Kenneth, Minelli, Caterina, Tewfik, Ihab, Thapa, Panna, Tewfik, Sundus
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7955784/
https://www.ncbi.nlm.nih.gov/pubmed/33727810
http://dx.doi.org/10.2147/IJN.S276301
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author Shrestha, Sony Chandi
Ghebremeskel, Kebreab
White, Kenneth
Minelli, Caterina
Tewfik, Ihab
Thapa, Panna
Tewfik, Sundus
author_facet Shrestha, Sony Chandi
Ghebremeskel, Kebreab
White, Kenneth
Minelli, Caterina
Tewfik, Ihab
Thapa, Panna
Tewfik, Sundus
author_sort Shrestha, Sony Chandi
collection PubMed
description BACKGROUND: Phytostanols are naturally occurring compounds that reduce blood cholesterol levels significantly. However, their aqueous insolubility poses formulation challenges. AIM: To formulate and characterize solid lipid nanoparticle carriers for phytostanol esters to enhance the bioavailability of phytostanols. METHODS: Phytostanol ester solid lipid nanoparticles were formulated by the microemulsion method. They were characterized for particle size distribution, polydispersity index, shape, surface charge, entrapment efficiency, stability, chemical structure, and thermal properties. The uptake of the formulation by cell lines, HepG2 and HT-29, and its effect on cell viability were evaluated. RESULTS: The formulation of solid lipid nanoparticles was successfully optimised by varying the type of lipids and their concentration relative to that of surfactants in the present study. The optimised formulation had an average diameter of (171 ± 9) nm, a negative surface charge of (−23.0 ± 0.8) mV and was generally spherical in shape. We report high levels of drug entrapment at (89 ± 5)% in amorphous form, drug loading of (9.1 ± 0.5)%, nanoparticle yield of (67 ± 4)% and drug excipient compatibility. The biological safety and uptake of the formulations were demonstrated on hepatic and intestinal cell lines. CONCLUSION: Phytostanol ester solid lipid nanoparticles were successfully formulated and characterized. The formulation has the potential to provide an innovative drug delivery system for phytostanols which reduce cholesterol and have a potentially ideal safety profile. This can contribute to better management of one of the main risk factors of cardiovascular diseases.
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spelling pubmed-79557842021-03-15 Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study Shrestha, Sony Chandi Ghebremeskel, Kebreab White, Kenneth Minelli, Caterina Tewfik, Ihab Thapa, Panna Tewfik, Sundus Int J Nanomedicine Original Research BACKGROUND: Phytostanols are naturally occurring compounds that reduce blood cholesterol levels significantly. However, their aqueous insolubility poses formulation challenges. AIM: To formulate and characterize solid lipid nanoparticle carriers for phytostanol esters to enhance the bioavailability of phytostanols. METHODS: Phytostanol ester solid lipid nanoparticles were formulated by the microemulsion method. They were characterized for particle size distribution, polydispersity index, shape, surface charge, entrapment efficiency, stability, chemical structure, and thermal properties. The uptake of the formulation by cell lines, HepG2 and HT-29, and its effect on cell viability were evaluated. RESULTS: The formulation of solid lipid nanoparticles was successfully optimised by varying the type of lipids and their concentration relative to that of surfactants in the present study. The optimised formulation had an average diameter of (171 ± 9) nm, a negative surface charge of (−23.0 ± 0.8) mV and was generally spherical in shape. We report high levels of drug entrapment at (89 ± 5)% in amorphous form, drug loading of (9.1 ± 0.5)%, nanoparticle yield of (67 ± 4)% and drug excipient compatibility. The biological safety and uptake of the formulations were demonstrated on hepatic and intestinal cell lines. CONCLUSION: Phytostanol ester solid lipid nanoparticles were successfully formulated and characterized. The formulation has the potential to provide an innovative drug delivery system for phytostanols which reduce cholesterol and have a potentially ideal safety profile. This can contribute to better management of one of the main risk factors of cardiovascular diseases. Dove 2021-03-09 /pmc/articles/PMC7955784/ /pubmed/33727810 http://dx.doi.org/10.2147/IJN.S276301 Text en © 2021 Shrestha et al. http://creativecommons.org/licenses/by-nc/3.0/ This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms (https://www.dovepress.com/terms.php).
spellingShingle Original Research
Shrestha, Sony Chandi
Ghebremeskel, Kebreab
White, Kenneth
Minelli, Caterina
Tewfik, Ihab
Thapa, Panna
Tewfik, Sundus
Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study
title Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study
title_full Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study
title_fullStr Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study
title_full_unstemmed Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study
title_short Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study
title_sort formulation and characterization of phytostanol ester solid lipid nanoparticles for the management of hypercholesterolemia: an ex vivo study
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7955784/
https://www.ncbi.nlm.nih.gov/pubmed/33727810
http://dx.doi.org/10.2147/IJN.S276301
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