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Shrestha, Sony C., Ghebremeskel, Kebreab, White, Kenneth, Minelli, Caterina, Tewfik, Ihab, Thapa, Panna and Tewfik, Sundus (2021) Formulation and characterization of phytostanol ester solid lipid nanoparticles for the management of hypercholesterolemia: an ex vivo study. International Journal of Nanomedicine, 16. pp. 1977-1992. ISSN 1178-2013
Background:
Phytostanols are naturally occurring compounds which reduce blood cholesterol levels significantly. However, their aqueous insolubility poses formulation challenges.
Aim:
To formulate and characterize solid lipid nanoparticles 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 were 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.
Conclusions:
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.
Available under License Creative Commons Attribution Non-commercial 4.0.
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