β-Sitosterol Loaded Nanostructured Lipid Carrier: Physical and Oxidative Stability, In Vitro Simulated Digestion and Hypocholesterolemic Activity

Abstract

The objective of the present study was to explore the potential of nanostructured lipid carriers (NLCs) for improving the oral delivery of β-sitosterol, a poorly water-soluble bioactive component with hypocholesterolemic activity. Two β-sitosterol formulations with different solid lipid compositions were prepared by melt emulsification, followed by the sonication technique, and the effect of storage conditions and simulated digestion on the physical, chemical and oxidative stability, bioaccessibility and release were extensively studied. Both NLC preparations remained relatively stable during the four weeks of storage at different conditions (4, 25 and 40 °C), with more superior stability at lower temperatures. The in vitro digestion experiment indicated a high physical stability after exposure to the simulated mouth and stomach stages and an improved overall β-sitosterol bioaccessibility at the end of the digestion. The NLCs presented an increased solubility and gradual release which could be justified by the remarkable affinity of β-sitosterol to the complex lipid mixture. An in vivo study demonstrated an improved reduction in the total cholesterol and low-density lipoprotein cholesterol plasma levels in mice compared with the drug suspension. These investigations evidenced the potential of the developed NLC formulations for the enhancement of solubility and in vivo performance of β-sitosterol.

Chemical composition and antioxidant activities of essential oils and extracts from cones of Tetraclinis articulata (Vahl) Masters

“…According to the results of Table 4, β-sitosterol constitutes the majority sterol with a percentage of 77.74%, followed by 10.55% of compesterol; brassicasterol (4.06%); stigmasterol (2.56%); cholesterol (0.48%); Δ-5-Avenosterol (0.37%); Δ-7-Avenosterol (0.27%) and Δ-7-stigmasterol (0.09%). Among these, the most abundant phytosterols is β-sitosterol, which has a broad range of in vivo biological functions including antitumor, anti-inflammatory, antidiabetic, and gallstonereducing activities (Soleimanian et al, 2020).To our knowledge, this study is the first carried out on the composition of phytosterols, no study has been mentioned in the literature on the composition of phytosterols in T. articulata cones.…”

Anti-depressant effect of Naringenin-loaded hybridized nanoparticles in diabetic rats via PPARγ/NLRP3 pathway

“…The impact of one month storage on both physical and chemical properties was examined 46 , 47 , to test the stability of the optimized formulation. NAR-HNPs was kept in screw-capped vials in the dark and stored at 4 °C, 25 °C, and 40 °C 48 . Every 10 days, samples were taken, evaluated for EE%, PS, ZP, and PDI, and then compared to freshly made formulation.…”

Development of a Nanostructured Lipid Carrier (NLC) by a Low-Energy Method, Comparison of Release Kinetics and Molecular Dynamics Simulation

“…Regarding FDA guidelines, ƒ2 values Drug release from nanoparticles has different mechanisms depending on their composition, including matrix erosion, diffusion, or swallowing. In lipid nanoparticles, the drug release process is mainly governed by matrix diffusion and erosion [69]. Specifically, in NLC, the incorporation of a liquid lipid component in the formulation results in a less-ordered structure that prevents drug expulsion [70].…”