Abstract

In order to improve the membrane lipophilicity and the affinity towards the environment of lipid bilayers, squalene (SQ) could be conjugated to phospholipids in the formation of liposomes. The effect of membrane composition and concentrations on the degradation of liposomes prepared via the extrusion method was investigated. Liposomes were prepared using a mixture of SQ, cholesterol (CH) and Tween80 (TW80). Based on the optimal conditions, liposome batches were prepared in the absence and presence of SQ. Their physicochemical and stability behavior were evaluated as a function of liposome constituent. From the optimization study, the liposomal formulation containing 5% (w/w) mixed soy lecithin (ML), 0.5% (w/w) SQ, 0.3% (w/w) CH and 0.75% (w/w) TW80 had optimal physicochemical properties and displayed a unilamellar structure. Liposome prepared using the optimal formulation had a low particle size (158.31 ± 2.96 nm) and acceptable %increase in the particle size (15.09% ± 3.76%) and %trolox equivalent antioxidant capacity (%TEAC) loss (35.69% ± 0.72%) against UV light treatment (280–320 nm) for 6 h. The interesting outcome of this research was the association of naturally occurring substance SQ for size reduction without the extra input of energy or mechanical procedures, and improvement of vesicle stability and antioxidant activity of ML-based liposome. This study also demonstrated that the presence of SQ in the membrane might increase the acyl chain dynamics and decrease the viscosity of the dispersion, thereby limiting long-term stability of the liposome.

Highlights

  • When carrier complexes are applied as oral delivery systems in the food and nutraceutical industries, it is imperative that they must be stable in food formulations and are non-toxic and Molecules 2020, 25, 5873; doi:10.3390/molecules25245873 www.mdpi.com/journal/moleculesMolecules 2020, 25, 5873 biodegradable

  • mixed soy lecithin (ML) is known to degrade upon exposure to air and light [4], and this restricts its application in food and nutraceutical products

  • This study indicated the importance of choosing the correct composition to obtain a qualitative functionalization of liposomes

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Summary

Introduction

When carrier complexes are applied as oral delivery systems in the food and nutraceutical industries, it is imperative that they must be stable in food formulations and are non-toxic and Molecules 2020, 25, 5873; doi:10.3390/molecules25245873 www.mdpi.com/journal/moleculesMolecules 2020, 25, 5873 biodegradable. Liposomes resemble the structure of biomembranes and are suitable for use as a delivery system in food to ensure good cellular uptake [1]. They are known to be unstable against external and internal stresses including physical (e.g., temperature, light), chemical (e.g., redox, pH) and biological (e.g., enzymes) [2,3]. For an efficient application of liposomal carriers as food and nutraceutical delivery systems, it is necessary to obtain deeper insights into the impact of incorporated materials on membrane integrity and vesicle stability by modulating the composition of the lipid bilayer. The lipids which are very susceptible to this step include those with a double bond, as the unsaturation permits the delocalization of the rest of the unpaired electrons, which further decreases the energy in this state

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