Abstract

Background: The nanoincorporation of the extract of Citrus limon (L.) Osbeck var. pompia into liposomes was aimed at improving its antioxidant and antibacterial effects. Methods: The extract of the rind of Citrus limon (L.) Osbeck var. pompia was obtained by maceration in ethanol, evaporation, and freeze-drying. The extract phytochemical fingerprint was obtained by HPLC and mass spectrometry, and it was determined that gallic acid, neohesperidin, eriocitrin, and neoeriocitrin were the most abundant components. The freeze-dried extract was loaded in liposomes, glycerosomes, and penetration-enhancer-containing vesicles prepared with propylene glycol (PG-PEVs). Results: Capability of the vesicles of improving efficacy of the extract in counteracting oxidative stress was studied in vitro in keratinocytes, along with antimicrobial activity against planktonic cultures of Streptococcus mutans, Lactobacillus acidophilus, and Streptococcus sanguinis. Conclusion: Results showed that the vesicles, especially glycerosomes and PG-PEVs, prevented oxidative damage and cell death, and inhibited bacterial proliferation.

Highlights

  • Citrus fruits have been receiving a growing interest, mainly because their use appears to be associated with reduced risk for gastro-intestinal and esophageal cancer, and cardiovascular diseases [1]

  • Medicines 2018, 5, 0108 fruit rind was used to obtain an extract with antioxidant activity, which was incorporated in liposomes, glycerosomes, and hyalurosomes

  • The non-dialysed and dialysed vesicles were diluted with a DPPH (2,2-diphenyl-1-picrylhydrazyl; 40 μg/mL) methanolic solution, and the antioxidant activity was assayed as a function of the discoloration of the free radical at 517 nm [11]

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Summary

Introduction

Citrus fruits have been receiving a growing interest, mainly because their use appears to be associated with reduced risk for gastro-intestinal and esophageal cancer, and cardiovascular diseases [1]. Though the citrus rind is an important source of bioactive compounds, it is commonly considered organic waste This part of the fruit is rich in phenolic compounds that have been demonstrated to possess several valuable properties, in particular anti-inflammatory, antioxidant, and antimicrobial activities [2]. Medicines 2018, 5, 0108 fruit rind was used to obtain an extract with antioxidant activity, which was incorporated in liposomes, glycerosomes, and hyalurosomes. The extract was found to have protective and regenerative properties in vitro, which were enhanced by the incorporation in phospholipid vesicles [8] Keeping in mind these results, in the present study, the pompia rind was used to produce an extract rich in phenolics by maceration in ethanol. The antibacterial activity of the formulations against cariogenic bacteria Streptococcus mutans and Lactobacillus acidophilus, and towards commensal Streptococcus sanguinis, were assessed

Materials
Fruit Harvest and Extract Preparation
HPLC-DAD Analysis
Vesicle Preparation
Vesicle Characterization
In Vitro Antioxidant Effect of the Extract
Determination of Antibacterial Activity
Statistical Analysis of Data
Extract Characterization
Vesicle
In Vitro Antioxidant Activity of the Formulations
Viability
Conclusions
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