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

Soleimanian, Yasamin; Goli, Sayed Amir Hossein; Varshosaz, Jaleh; Di Cesare Mannelli, Lorenzo; Ghelardini, Carla; Cirri, Marzia; Maestrelli, Francesca

doi:10.3390/pharmaceutics12040386

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

Yasamin Soleimanian

^1,2,

Sayed Amir Hossein Goli

Jaleh Varshosaz

Lorenzo Di Cesare Mannelli

⁴

Carla Ghelardini

⁴,

Marzia Cirri

and

Francesca Maestrelli

^2,*

Department of Food Science and Technology, College of Agriculture, Isfahan University of Technology, Isfahan 84156-83111, Iran

Department of Chemistry, University of Florence, via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy

Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan 81746-73461, Iran

⁴

Department of Neuroscience, Psychology, Drug Research and Child Health, University of Florence, via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy

Author to whom correspondence should be addressed.

Pharmaceutics 2020, 12(4), 386; https://doi.org/10.3390/pharmaceutics12040386

Received: 3 April 2020 / Revised: 16 April 2020 / Accepted: 20 April 2020 / Published: 22 April 2020

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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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. View Full-Text

Keywords: β-sitosterol; nanostructured lipid carrier; hypocholesterolemic activity; digestion; bioaccessibility; in vitro release

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Soleimanian, Y.; Goli, S.A.H.; Varshosaz, J.; Di Cesare Mannelli, L.; Ghelardini, C.; Cirri, M.; Maestrelli, F. β-Sitosterol Loaded Nanostructured Lipid Carrier: Physical and Oxidative Stability, In Vitro Simulated Digestion and Hypocholesterolemic Activity. Pharmaceutics 2020, 12, 386. https://doi.org/10.3390/pharmaceutics12040386

AMA Style

Soleimanian Y, Goli SAH, Varshosaz J, Di Cesare Mannelli L, Ghelardini C, Cirri M, Maestrelli F. β-Sitosterol Loaded Nanostructured Lipid Carrier: Physical and Oxidative Stability, In Vitro Simulated Digestion and Hypocholesterolemic Activity. Pharmaceutics. 2020; 12(4):386. https://doi.org/10.3390/pharmaceutics12040386

Chicago/Turabian Style

Soleimanian, Yasamin, Sayed Amir Hossein Goli, Jaleh Varshosaz, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Marzia Cirri, and Francesca Maestrelli. 2020. "β-Sitosterol Loaded Nanostructured Lipid Carrier: Physical and Oxidative Stability, In Vitro Simulated Digestion and Hypocholesterolemic Activity" Pharmaceutics 12, no. 4: 386. https://doi.org/10.3390/pharmaceutics12040386

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

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