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Research Project
From soil to skin: Eco-friendly extract from kiwiberry leaves for prevention of skin aging process
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Influence of temperature on the subcritical water extraction of Actinidia arguta leaves: A screening of pro-healthy compounds
Publication . Silva, Ana Margarida; Luís, Ana Sofia; Moreira, Manuela M.; Ferraz, Ricardo; Brezo-Borjan, Tanja; Švarc-Gajić, Jaroslava; Costa, Paulo C.; Delerue-Matos, Cristina; Rodrigues, Francisca
Actinidia arguta is a species disseminated in Europe and classified by the Chinese Herbal Medicine as a medicinal plant. The fruit (kiwiberry) has been extensively exploited for multiple purposes, while leaves where discarded. The objective of this study was to evaluate the optimal Subcritical Water Extraction (SWE) temperature (110 °C - 160 °C) of antioxidants and polyphenols from A. arguta leaves. The optimal temperature of extraction was 123 °C, revealing the highest phenolic and flavonoid contents and good scavenging efficiencies against HOCl (IC50 = 17.06 μg/mL) and O2●- (IC50 = 335.2 μg/mL), without toxicity on intestinal cells. The phenolic profile was characterized by high amounts of phenolic acids (e.g., gallic acids), flavanols (catechin) and flavonols (e.g., quercetin-3-O-galactoside). This work allows to conclude that SWE can be a useful extraction technique for the recovery of polyphenolics from A. arguta leaves
Development and Optimization of a Topical Formulation with Castanea sativa Shells Extract Based on the Concept “Quality by Design”
Publication . Oliveira, Nágilla; Cádiz-Gurrea, María de La Luz; Silva, Ana Margarida; Macedo, Catarina; Rodrigues, Francisca; Costa, Paulo
The proposed study aims to develop and optimize a topical formulation with Castanea sativa shells extract considering the concept of Quality by Design, focusing on a planned development that consider the vulnerabilities of the entire process through risk analysis tools and design of experiments (DoE). A Box–Behnken design with three factors and three levels was used as a statistical tool for the execution of the DoE and the analysis of the response surface methodology responses. The independent variables studied were the quantity of sodium lauryl sulfate (%) (X1), beeswax (%) (X2) and macadamia oil (%) (X3); the dependent variables were pH (Y1), viscosity (Y2) and adhesiveness (Y3). According to the mathematical model, the optimal formulation contains 0.93% of sodium lauryl sulfate, 5.00% of beeswax and 10.00% of macadamia oil. The optimal formulation with the extract was prepared and characterized over the time, regarding organoleptic and technological characteristics, allowing conclusions to be reached regarding its stability. The formulation presented a pleasant odor and was light brown in color, it also demonstrated pseudoplastic-thixotropic behavior and a small reduction in the formulation consistency after 30 days of storage. This study demonstrated the efficiency of the Quality by Design methodology to understand the product variability, supporting that this approach favors a better understanding of the whole process and enables to design a robust development stage, reducing costs and generating high-quality products
New Perspectives on the Sustainable Employment of Chestnut Shells as Active Ingredient against Oral Mucositis: A First Screening
Publication . Ferreira, Ana Sofia; Silva, Ana Margarida; Pinto, Diana; Moreira, Manuela M.; Ferraz, Ricardo; Švarc-Gajić, Jaroslava; Costa, Paulo C.; Delerue-Matos, Cristina; Rodrigues, Francisca
Oral mucositis (OM), a common side effect of oncological treatment, is an oral mucosal disorder characterized by painful ulcerations and increased risk of infection. The use of natural antioxidants to suppress the redox imbalance responsible for the OM condition has emerged as an interesting approach to prevent/treat OM. This study aims to explore the chestnut (Castana sativa) shells as potential active ingredient against OM. Therefore, chestnut shells were extracted at different temperatures (110–180 °C) by Subcritical Water Extraction (SWE), aiming to recover antioxidants. The extracts were also evaluated against microorganisms present in the oral cavity as well as on human oral cell lines (TR146 and HSC3). The highest phenolic content was obtained with the extraction temperature of 110 °C, exhibiting the best antioxidant/antiradical activities and scavenging efficiencies against HOCl (IC50 = 4.47 μg/mL) and ROO• (0.73 μmol TE/mg DW). High concentrations of phenolic acids (e.g., gallic and protocatechuic acids) and flavanoids (catechin, epicatechin and rutin) characterized the phenolic profile. The antimicrobial activity against several oral microorganisms present in the oral cavity during OM, such as Streptococcus, Staphylococcus, Enterococcus, and Escherichia, was demonstrated. Finally, the effects on HSC3 and TR146 cell lines revealed that the extract prepared at 110 °C had the lowest IC50 (1325.03 and 468.15 µg/mL, respectively). This study highlights the potential effects of chestnut shells on OM
Formulation, Characterization, and Cytotoxicity Evaluation of Lactoferrin Functionalized Lipid Nanoparticles for Riluzole Delivery to the Brain
Publication . Teixeira, Maria Inês; Lopes, Carla Martins; Gonçalves, Hugo; Catita, José; Silva, Ana Margarida; Rodrigues, Francisca; Amaral, Maria Helena; Costa, Paulo C.
Amyotrophic lateral sclerosis (ALS) is a neurodegenerative disease with a very poor prognosis. Its treatment is hindered by a lack of new therapeutic alternatives and the existence of the blood–brain barrier (BBB), which restricts the access of drugs commonly used in ALS, such as riluzole, to the brain. To overcome these limitations and increase brain targeting, riluzole-loaded nanostructured lipid carriers (NLC) were prepared and functionalized with lactoferrin (Lf), facilitating transport across the BBB by interacting with Lf receptors expressed in the brain endothelium. NLC were characterized with respect to their physicochemical properties (size, zeta potential, polydispersity index) as well as their stability, encapsulation efficiency, morphology, in vitro release profile, and biocompatibility. Moreover, crystallinity and melting behavior were assessed by DSC and PXRD. Nanoparticles exhibited initial mean diameters between 180 and 220 nm and a polydispersity index below 0.3, indicating a narrow size distribution. NLC remained stable over at least 3 months. Riluzole encapsulation efficiency was very high, around 94–98%. FTIR and protein quantification studies confirmed the conjugation of Lf on the surface of the nanocarriers, with TEM images showing that the functionalized NLC presented a smooth surface and uniform spherical shape. An MTT assay revealed that the nanocarriers developed in this study did not cause a substantial reduction in the viability of NSC-34 and hCMEC/D3 cells at a riluzole concentration up to 10 μM, being therefore biocompatible. The results suggest that Lf-functionalized NLC are a suitable and promising delivery system to target riluzole to the brain
Insights into the 3D In Vitro Permeability and In Vivo Antioxidant Protective Effects of Kiwiberry Leaf Extract: A Step Forward to Human Nutraceutical Use
Publication . Silva, Ana Margarida; Almeida, Andreia; Dall’Acqua, Stefano; Loschi, Francesca; Sarmento, Bruno; Costa, Paulo C.; Delerue-Matos, Cristina; Rodrigues, Francisca
Actinidia arguta (Siebold & Zucc.) Planch. ex Miq. (kiwiberry) leaves are a source of phenolic compounds with pro-health biological effects, such as antioxidant and anti-inflammatory activities. Despite the huge number of studies reporting the composition of A. arguta leaves, no in vitro or in vivo studies explore its potential use as nutraceutical ingredient based on these activities. Therefore, this study aims to characterize the safety profile of kiwiberry leaf extracts using in vitro and in vivo approaches through the assessment of intestinal cell viability (Caco-2 and HT29-MTX), 3D intestinal permeation, and, most important, the redox markers, biochemical profile and liver and kidney function effects after the animal assays. Briefly, wistar rats were orally treated for 7 days with kiwiberry leaf extracts (50 and 75 mg/kg bw), water (negative control), or vitamin C (positive control). The cell viability was above 90% at 1000 μg/mL for both cells. Coumaroyl quinic acid and rutin achieved a permeation higher than 25% in the 3D intestinal model. The animal studies confirmed the extracts’ ability to increase superoxide dismutase, glutathione peroxidase, and catalase content in animals’ livers and kidneys while simultaneously decreasing the triglycerides content. This study highlighted the antioxidant capacity of kiwiberry leaf extracts, ensuring their efficacy and safety as a nutraceutical ingredient
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Funding agency
Fundação para a Ciência e a Tecnologia
Funding programme
POR_NORTE
Funding Award Number
SFRH/BD/144994/2019