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

Sony Chandi Shrestha,1,2 Kebreab Ghebremeskel,1 Kenneth White,1 Caterina Minelli,2 Ihab Tewfik,3 Panna Thapa,4 Sundus Tewfik5 1School of Human Sciences, London Metropolitan University, London, UK; 2Surface Technology, National Physical Laboratory, London, UK; 3Life Sciences, University of Westminste...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Shrestha SC, Ghebremeskel K, White K, Minelli C, Tewfik I, Thapa P, Tewfik S
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2021
Materias:	cardiovascular diseases cholesterol phytostanol ester (pse) solid lipid nanoparticles (slnps) hypercholesterolemia Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/ee3ce9c7e47246d28b69cf6ded2eb7e1
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:ee3ce9c7e47246d28b69cf6ded2eb7e1
record_format	dspace
spelling	oai:doaj.org-article:ee3ce9c7e47246d28b69cf6ded2eb7e12021-12-02T13:58:32ZFormulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study1178-2013https://doaj.org/article/ee3ce9c7e47246d28b69cf6ded2eb7e12021-03-01T00:00:00Zhttps://www.dovepress.com/formulation-and-characterization-of-phytostanol-ester-solid-lipid-nano-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Sony Chandi Shrestha,1,2 Kebreab Ghebremeskel,1 Kenneth White,1 Caterina Minelli,2 Ihab Tewfik,3 Panna Thapa,4 Sundus Tewfik5 1School of Human Sciences, London Metropolitan University, London, UK; 2Surface Technology, National Physical Laboratory, London, UK; 3Life Sciences, University of Westminster, London, UK; 4Department of Pharmacy, Kathmandu University, Dhulikhel, Nepal; 5Department of Applied Nanomolecules, Bloomsnano Limited, London, UKCorrespondence: Sony Chandi Shrestha Email soneem@gmail.comBackground: 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.Keywords: cardiovascular diseases, cholesterol, phytostanol ester, PSE, solid lipid nanoparticles, SLNPs, hypercholesterolemiaShrestha SCGhebremeskel KWhite KMinelli CTewfik IThapa PTewfik SDove Medical Pressarticlecardiovascular diseasescholesterolphytostanol ester (pse)solid lipid nanoparticles (slnps)hypercholesterolemiaMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 16, Pp 1977-1992 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	cardiovascular diseases cholesterol phytostanol ester (pse) solid lipid nanoparticles (slnps) hypercholesterolemia Medicine (General) R5-920
spellingShingle	cardiovascular diseases cholesterol phytostanol ester (pse) solid lipid nanoparticles (slnps) hypercholesterolemia Medicine (General) R5-920 Shrestha SC Ghebremeskel K White K Minelli C Tewfik I Thapa P Tewfik S Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study
description	Sony Chandi Shrestha,1,2 Kebreab Ghebremeskel,1 Kenneth White,1 Caterina Minelli,2 Ihab Tewfik,3 Panna Thapa,4 Sundus Tewfik5 1School of Human Sciences, London Metropolitan University, London, UK; 2Surface Technology, National Physical Laboratory, London, UK; 3Life Sciences, University of Westminster, London, UK; 4Department of Pharmacy, Kathmandu University, Dhulikhel, Nepal; 5Department of Applied Nanomolecules, Bloomsnano Limited, London, UKCorrespondence: Sony Chandi Shrestha Email soneem@gmail.comBackground: 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.Keywords: cardiovascular diseases, cholesterol, phytostanol ester, PSE, solid lipid nanoparticles, SLNPs, hypercholesterolemia
format	article
author	Shrestha SC Ghebremeskel K White K Minelli C Tewfik I Thapa P Tewfik S
author_facet	Shrestha SC Ghebremeskel K White K Minelli C Tewfik I Thapa P Tewfik S
author_sort	Shrestha SC
title	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_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_sort	formulation and characterization of phytostanol ester solid lipid nanoparticles for the management of hypercholesterolemia: an ex vivo study
publisher	Dove Medical Press
publishDate	2021
url	https://doaj.org/article/ee3ce9c7e47246d28b69cf6ded2eb7e1
work_keys_str_mv	AT shresthasc formulationandcharacterizationofphytostanolestersolidlipidnanoparticlesforthemanagementofhypercholesterolemiaanexvivostudy AT ghebremeskelk formulationandcharacterizationofphytostanolestersolidlipidnanoparticlesforthemanagementofhypercholesterolemiaanexvivostudy AT whitek formulationandcharacterizationofphytostanolestersolidlipidnanoparticlesforthemanagementofhypercholesterolemiaanexvivostudy AT minellic formulationandcharacterizationofphytostanolestersolidlipidnanoparticlesforthemanagementofhypercholesterolemiaanexvivostudy AT tewfiki formulationandcharacterizationofphytostanolestersolidlipidnanoparticlesforthemanagementofhypercholesterolemiaanexvivostudy AT thapap formulationandcharacterizationofphytostanolestersolidlipidnanoparticlesforthemanagementofhypercholesterolemiaanexvivostudy AT tewfiks formulationandcharacterizationofphytostanolestersolidlipidnanoparticlesforthemanagementofhypercholesterolemiaanexvivostudy
_version_	1718392235828969472

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

Ejemplares similares