Abstract

Naringenin (4′,5,7-trihydroxyflavanone-7-rhamnoglucosideor naringenin-7-rhamnoglucoside), a flavonoid present in large quantities in citrus, has different beneficial effects on human health as an antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator. Different studies have shown that this substance also has a hypoglycemic and antihypertensive effect, reduces cholesterol and triglycerides, and plays an important protective role in the heart tissue; moreover, it provides neuroprotection against various neurological disorders such as Parkinson’s disease and unpredictable chronic stress-induced depression. Despite these advantages, Naringenin is poorly absorbed, and the small percentage absorbed is rapidly degraded by the liver, as a result losing its activity. Several approaches have been attempted to overcome these obstacles, among them, nanotechnology, with the use of Drug Delivery Systems (DDS) as Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC). DDS can, in fact, improve the drug bioavailability. The aim of this study was to develop and characterize SLN and NLC containing Naringenin and to evaluate the ability of these nanoparticles to release Naringenin at the cell level using biomembrane models represented by Multilamellar Vesicles (MLV). These studies were performed using Differential Scanning Calorimetry, a powerful technique to detect the interaction of drugs and delivery systems with MLV. It was shown that Naringenin could be better incorporated into NLC with respect to SLN and that Naringenin could be released by NLC into the biomembrane model. Therefore, suggesting the administration of Naringenin loaded into nanoparticles could help avoid the disadvantages associated with the use of the free molecule.

Highlights

  • Naringenin (4,5,7-trihydroxyflavanone-7-rhamnoglucosideor naringenin-7-rhamnoglucoside, NAR) is a flavonoid present in large quantities in citrus

  • It was shown that Naringenin could be better incorporated into Nanostructured Lipid Carriers (NLC) with respect to Solid Lipid Nanoparticles (SLN) and that Naringenin could be released by NLC into the biomembrane model

  • Naringenin might seem to be the cure for different ills, but some problems have to be considered: the first relates to studies on animals which use doses that cannot be administered to humans; second, this substance is poorly absorbed, and the small percentage absorbed, around 15%, is rapidly degraded by the liver, losing its activity as a result [6]; the third and most significant negative aspect is the inhibitory effect of the activity of some cytochrome P450 isoforms [7], an enzymatic complex that has a fundamental role in the degradation and elimination of different drugs

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Summary

Introduction

Naringenin (4 ,5,7-trihydroxyflavanone-7-rhamnoglucosideor naringenin-7-rhamnoglucoside, NAR) is a flavonoid present in large quantities in citrus. SLN and NLC have been introduced as potential delivery systems due to their high encapsulation ability, control release, and targeting delivery properties that allow a reduction of the total dose of the drug and its side effects [14,15,16] They can protect the drugs against enzymes and can slow down drug degradation and elimination, thereby enhancing the bioavailability of drugs [17]. It was shown that NLC could better incorporate Naringenin with respect to SLN and that Naringenin could be released by NLC into the biomembrane model These studies suggest that the administration of Naringenin-loaded nanoparticles could prevent the disadvantages associated with the use of the free molecule

Materials
SLN and NLC Preparation
Characterization of Nanoparticles
Stability Tests
Preparation of MLV
DSC Analysis
Naringenin and MLV Contact Kinetic
Nanoparticle Characterization
DSC Analysis of Nanoparticles
Full Text
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