Abstract

The aim of the present study was the encapsulation of cedar (Juniperus phoenicea) essential oil (CEO) of Greek origin in β-cyclodextrin (β-CD) through the formation of inclusion complexes (ICs) using the co-precipitation method with different β-CD-to-CEO weight ratios (90:10, 85:15, 80:20, 70:30 (w/w)). The encapsulation of CEO in β-CD through host–guest interactions was confirmed by Nuclear Magnetic Resonance (NMR) spectroscopy, FT-IR spectroscopy, Differential Scanning Calorimetry (DSC) and Thermogravimetric Analysis (TGA). The obtained ICs exhibited nanoscale size (315.9 nm to 769.6 nm),Polydispersity Index from 0.326 to 0.604 and satisfactory stability in suspension (−37.0 mV to −17.0 mV). The process yield was satisfactory, ranging between 65% and 78%, while the inclusion efficiency ranged from 10% to 27%. The in vitro release study conducted for the IC with the optimal characteristics (β-CD:CEO 80:20 (w/w)) exhibited a sustained release profile, with an initial burst effect in the first 5 h. The release profile could be well expressed by the Higuchi equation: Q = 18.893 t1/2 + 9.5919, R2 = 0.8491. The cedar EO presented significant acetylcholinesterase inhibition (IC50 37 μg/mL), which was prolonged by its encapsulation into the β-CD cavity.

Highlights

  • Over the last few decades, there has been a growing interest in the therapeutic potential of natural products, such as essential oils (EOs), which present a wide range of biological properties, including antimicrobial [1], antioxidant [2], antivirus [3], anticancer [4]and neuroprotective [5] activities

  • Cedar (Juniperus phoenicea) essential oil of food-grade quality, obtained by steam distillation from the berries of J. phoenicea, which were collected from Viotia, Greece, during the summer of 2017, was kindly provided by the Laboratory of Nutritional Physiology and Feeding, Animal Sciences and Aquaculture Faculty, Agricultural University of Athens (A.U.A., Athens, Greece). β-Cyclodextrin (β-CD) of >99% purity was purchased from Fluka (Gillingham, England), while ethanol of analytical reagent grade, ethyl acetate, hexane, K2 HPO4 and KH2 PO4 of ACS grade and anhydrous sodium sulfate were purchased from

  • The results reveal that β-CD–Cedar Essential Oil (CEO) inclusion complexes (ICs) dispersed in Dimethyl sulfoxide (DMSO) presented IC50 65.4 μg/mL

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Summary

Introduction

Over the last few decades, there has been a growing interest in the therapeutic potential of natural products, such as essential oils (EOs), which present a wide range of biological properties, including antimicrobial [1], antioxidant [2], antivirus [3], anticancer [4]and neuroprotective [5] activities. Over the last few decades, there has been a growing interest in the therapeutic potential of natural products, such as essential oils (EOs), which present a wide range of biological properties, including antimicrobial [1], antioxidant [2], antivirus [3], anticancer [4]. Thereafter, EOs have found a considerable range of applications as naturally occurring bioactive agents in the field of medicine, food and cosmetic preservation [6]. The biological activities of EOs are assigned to several small molecules, including terpenoids, phenolic and aliphatic constituents. Essential oils are well known for their ability to scavenge free radicals [8], as well as to inhibit acetylcholinesterase activity [9] and suppress Aβ peptide deposits [10]. AChE inhibitors are a constantly developing research field since they comprise the main therapeutic strategy for

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