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

Authors Shrestha SC, Ghebremeskel K, White K, Minelli C, Tewfik I, Thapa P, Tewfik S

Received 14 August 2020

Accepted for publication 4 December 2020

Published 9 March 2021 Volume 2021:16 Pages 1977—1992


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 3

Editor who approved publication: Prof. Dr. Thomas J. Webster

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, UK

Correspondence: Sony Chandi Shrestha Email [email protected]

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.

Keywords: cardiovascular diseases, cholesterol, phytostanol ester, PSE, solid lipid nanoparticles, SLNPs, hypercholesterolemia

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