Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine

The purpose of this study was to investigate the loading properties of the non-psychoactive cannabidiol (CBD) in a new nanostructured lipid carrier (NLC), evaluating its bioaccessibility in gastric and intestinal simulated physiological media. CBD has a low water solubility, as well as high instabil...

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Main Authors: Lucia Grifoni, Giulia Vanti, Anna Rita Bilia
Format: Article
Language:English
Published: MDPI AG 2023-04-01
Series:Nutraceuticals
Subjects:
Online Access:https://www.mdpi.com/1661-3821/3/2/16
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author Lucia Grifoni
Giulia Vanti
Anna Rita Bilia
author_facet Lucia Grifoni
Giulia Vanti
Anna Rita Bilia
author_sort Lucia Grifoni
collection DOAJ
description The purpose of this study was to investigate the loading properties of the non-psychoactive cannabidiol (CBD) in a new nanostructured lipid carrier (NLC), evaluating its bioaccessibility in gastric and intestinal simulated physiological media. CBD has a low water solubility, as well as high instability in simulated physiological conditions and in the acidic media, which results in a very low bioavailability—less than 6%. NLCs containing CBD (10 mg/mL), Compritol 888 ATO, Lauroglycol 90, Labrafil 2125, Tween 20, and Poloxamer 188 were formulated. This resulted in them being suitable for oral administration because the size was less than 200 nm, polydispersity index 0.152, and ζ-potential −39.21 ± 1.89 mV. Recovery and encapsulation efficiency were 100% and 93%, respectively. After two hours of incubation in simulated gastric fluid (SGF), NLCs remained unchanged, protecting CBD from acidic medium. Indeed, CBD is also reported to be not stable in media with pH = 7.4 at 37 °C, but our studies evidenced that in the presence of the intestinal fluid, the NLC was digested and formed an emulsion, which can protect and preserve the CBD chemical structure, as confirmed by the 100% recovery found after six hours. Accordingly, CBD-loaded NLCs are a promising oral formulation that optimize bioaccessibility in the small intestine.
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spelling doaj.art-f91fa2178e324b7ab67715f95380dcde2023-11-18T11:55:24ZengMDPI AGNutraceuticals1661-38212023-04-013221022110.3390/nutraceuticals3020016Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small IntestineLucia Grifoni0Giulia Vanti1Anna Rita Bilia2Department of Chemistry, University of Florence, Via U. Schiff 6, Sesto Fiorentino, 50019 Florence, ItalyDepartment of Chemistry, University of Florence, Via U. Schiff 6, Sesto Fiorentino, 50019 Florence, ItalyDepartment of Chemistry, University of Florence, Via U. Schiff 6, Sesto Fiorentino, 50019 Florence, ItalyThe purpose of this study was to investigate the loading properties of the non-psychoactive cannabidiol (CBD) in a new nanostructured lipid carrier (NLC), evaluating its bioaccessibility in gastric and intestinal simulated physiological media. CBD has a low water solubility, as well as high instability in simulated physiological conditions and in the acidic media, which results in a very low bioavailability—less than 6%. NLCs containing CBD (10 mg/mL), Compritol 888 ATO, Lauroglycol 90, Labrafil 2125, Tween 20, and Poloxamer 188 were formulated. This resulted in them being suitable for oral administration because the size was less than 200 nm, polydispersity index 0.152, and ζ-potential −39.21 ± 1.89 mV. Recovery and encapsulation efficiency were 100% and 93%, respectively. After two hours of incubation in simulated gastric fluid (SGF), NLCs remained unchanged, protecting CBD from acidic medium. Indeed, CBD is also reported to be not stable in media with pH = 7.4 at 37 °C, but our studies evidenced that in the presence of the intestinal fluid, the NLC was digested and formed an emulsion, which can protect and preserve the CBD chemical structure, as confirmed by the 100% recovery found after six hours. Accordingly, CBD-loaded NLCs are a promising oral formulation that optimize bioaccessibility in the small intestine.https://www.mdpi.com/1661-3821/3/2/16cannabidiolnutraceuticallow bioavailabilitynanostructured lipid carriershigh loadingdigestion in the small intestine
spellingShingle Lucia Grifoni
Giulia Vanti
Anna Rita Bilia
Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine
Nutraceuticals
cannabidiol
nutraceutical
low bioavailability
nanostructured lipid carriers
high loading
digestion in the small intestine
title Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine
title_full Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine
title_fullStr Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine
title_full_unstemmed Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine
title_short Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine
title_sort nanostructured lipid carriers loaded with cannabidiol enhance its bioaccessibility to the small intestine
topic cannabidiol
nutraceutical
low bioavailability
nanostructured lipid carriers
high loading
digestion in the small intestine
url https://www.mdpi.com/1661-3821/3/2/16
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