scholarly journals Annatto Oil Loaded Nanostructured Lipid Carriers: A Potential New Treatment for Cutaneous Leishmaniasis

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1912
Author(s):  
Marianna Araújo Ferreira ◽  
Renato Ferreira de Almeida Júnior ◽  
Thiago Souza Onofre ◽  
Bruna Renata Casadei ◽  
Kleber Juvenal Silva Farias ◽  
...  
Keyword(s):  
Leishmania Major ◽  
Pure Water ◽  
Thermal Analyses ◽  
Antioxidant Properties ◽  
Average Diameter ◽  
Nanostructured Lipid Carrier ◽  
Bixa Orellana ◽  
Paramagnetic Resonance ◽  
3T3 Fibroblasts

Annatto (Bixa orellana L.) is extensively used as food pigment worldwide. Recently, several studies have found it to have healing and antioxidant properties, as well as effective action against leishmaniasis. Therefore, the purpose of this study was to incorporate the oil obtained from annatto seeds into a nanostructured lipid carrier (NLC) and evaluate its physicochemical properties and biological activity against Leishmania major. Nanoparticles were prepared by the fusion-emulsification and ultrasonication method, with the components Synperonic™ PE (PL) as the surfactant, cetyl palmitate (CP) or myristyl myristate (MM) as solid lipids, annatto oil (AO) (2% and 4%, w/w) as liquid lipid and active ingredient, and ultra-pure water. Physicochemical and biological characterizations were carried out to describe the NLCs, including particle size, polydispersity index (PDI), and zeta potential (ZP) by dynamic light scattering (DLS), encapsulation efficiency (EE%), thermal behavior, X-ray diffraction (XRD), transmission electron microscopy (TEM), Electron Paramagnetic Resonance (EPR), cytotoxicity on BALB/c 3T3 fibroblasts and immortalized human keratinocyte cells, and anti-leishmaniasis activity in vitro. Nanoparticles presented an average diameter of ~200 nm (confirmed by TEM results), a PDI of less than 0.30, ZP between −12.6 and −31.2 mV, and more than 50% of AO encapsulated in NLCs. Thermal analyses demonstrated that the systems were stable at high temperatures with a decrease in crystalline structure due to the presence of AOs (confirmed by XRD). In vitro, the anti-leishmania test displayed good activity in encapsulating AO against L. major. The results indicate that the oily fraction of Bixa orellana L. in NLC systems should be evaluated as a potential therapeutic agent against leishmaniasis.

scholarly journals Formulation of Nanomicelles to Improve the Solubility and the Oral Absorption of Silymarin

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1688 ◽  
Author(s):  
Vieri Piazzini ◽  
Mario D’Ambrosio ◽  
Cristina Luceri ◽  
Lorenzo Cinci ◽  
Elisa Landucci ◽  
...  
Keyword(s):  
Encapsulation Efficiency ◽  
Oral Absorption ◽  
Drug Loading ◽  
Antioxidant Properties ◽  
Aqueous Solubility ◽  
Average Diameter ◽  
Critical Micellar Concentration ◽  
Polydispersity Index ◽  
Vitamin E Tpgs

Two novel nanomicellar formulations were developed to improve the poor aqueous solubility and the oral absorption of silymarin. Polymeric nanomicelles made of Soluplus and mixed nanomicelles combining Soluplus with d-α-tocopherol polyethylene glycol 1000 succinate (vitamin E TPGS) were prepared using the thin film method. Physicochemical parameters were investigated, in particular the average diameter, the homogeneity (expressed as polydispersity index), the zeta potential, the morphology, the encapsulation efficiency, the drug loading, the critical micellar concentration and the cloud point. The sizes of ~60 nm, the narrow size distribution (polydispersity index ≤0.1) and the encapsulation efficiency >92% indicated the high affinity between silymarin and the core of the nanomicelles. Solubility studies demonstrated that the solubility of silymarin increased by ~6-fold when loaded into nanomicelles. Furthermore, the physical and chemical parameters of SLM-loaded formulations stored at room temperature and in refrigerated conditions (4 °C) were monitored over three months. In vitro stability and release studies in media miming the physiological conditions were also performed. In addition, both formulations did not alter the antioxidant properties of silymarin as evidenced by the 1,1-Diphenyl-2-picrylhydrazyl radical (DPPH) assay. The potential of the nanomicelles to increase the intestinal absorption of silymarin was firstly investigated by the parallel artificial membrane permeability assay. Subsequently, transport studies employing Caco-2 cell line demonstrated that mixed nanomicelles statistically enhanced the permeability of silymarin compared to polymeric nanomicelles and unformulated extract. Finally, the uptake studies indicated that both nanomicellar formulations entered into Caco-2 cells via energy-dependent mechanisms.

scholarly journals Fucoxanthin for Topical Administration, a Phototoxic vs. Photoprotective Potential in a Tiered Strategy Assessed by In Vitro Methods

Antioxidants ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 328 ◽  
Author(s):  
Renata Spagolla Napoleão Tavares ◽  
Camila Martins Kawakami ◽  
Karina de Castro Pereira ◽  
Gabriela Timotheo do Amaral ◽  
Carolina Gomes Benevenuto ◽  
...  
Keyword(s):  
Human Skin ◽  
Scientific Information ◽  
Antioxidant Properties ◽  
Topical Administration ◽  
Significant Inhibition ◽  
Mouse Fibroblast ◽  
3T3 Fibroblasts ◽  
Photo Effect

Fucoxanthin possesses a well-described antioxidant activity that might be useful for human skin photoprotection. However, there is a lack of scientific information regarding its properties when applied onto human skin. Thus, the objective of the present study was to assess the photoprotective and phototoxicity potential of fucoxanthin based on its ultraviolet (UVB 280–320 nm; UVA 320–400 nm) and visible (VIS 400–700 nm) absorption, photostability, phototoxicity in 3T3 mouse fibroblast culture vs. full-thickness reconstructed human skin (RHS), and its ability to inhibit reactive oxygen species formation that is induced by UVA on HaCaT keratinocytes. Later, we evaluated the antioxidant properties of the sunscreen formulation plus 0.5% fucoxanthin onto RHS to confirm its bioavailability and antioxidant potential through the skin layers. The compound was isolated from the alga Desmarestia anceps. Fucoxanthin, despite presenting chemical photo-instability (dose 6 J/cm2: 35% UVA and 21% VIS absorbance reduction), showed acceptable photodegradation (dose 27.5 J/cm2: 5.8% UVB and 12.5% UVA absorbance reduction) when it was added to a sunscreen at 0.5% (w/v). In addition, it increased by 72% of the total sunscreen UV absorption spectra, presenting UV-booster properties. Fucoxanthin presented phototoxic potential in 3T3 fibroblasts (mean photo effect 0.917), but it was non-phototoxic in the RHS model due to barrier function that was provided by the stratum corneum. In addition, it showed a significant inhibition of ROS formation at 0.01% (p < 0.001), in HaCat, and in a sunscreen at 0.5% (w/v) (p < 0.001), in RHS. In conclusion, in vitro results showed fucoxanthin protective potential to the skin that might contribute to improving the photoprotective potential of sunscreens in vivo.

scholarly journals An EGF- and Curcumin-Co-Encapsulated Nanostructured Lipid Carrier Accelerates Chronic-Wound Healing in Diabetic Rats

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4610
Author(s):  
Hye-Jin Lee ◽  
Moses Jeong ◽  
Young-Guk Na ◽  
Sung-Jin Kim ◽  
Hong-Ki Lee ◽  
...  
Keyword(s):  
Wound Healing ◽  
Chronic Wounds ◽  
Chronic Wound ◽  
Healing Process ◽  
Double Emulsion ◽  
Average Diameter ◽  
Diabetic Rats ◽  
Wound Healing Process ◽  
Nanostructured Lipid Carrier

Nanostructured lipid carriers (NLC) are capable of encapsulating hydrophilic and lipophilic drugs. The present study developed an NLC containing epidermal growth factor (EGF) and curcumin (EGF–Cur-NLC). EGF–Cur-NLC was prepared by a modified water-in-oil-in-water (w/o/w) double-emulsion method. The EGF–Cur-NLC particles showed an average diameter of 331.8 nm and a high encapsulation efficiency (81.1% and 99.4% for EGF and curcumin, respectively). In vitro cell studies were performed using two cell types, NIH 3T3 fibroblasts and HaCaT keratinocytes. The results showed no loss of bioactivity of EGF in the NLC formulation. In addition, EGF–Cur-NLC improved in vitro cell migration, which mimics the wound healing process. Finally, EGF–Cur-NLC was evaluated in a chronic wound model in diabetic rats. We found that EGF–Cur-NLC accelerated wound closure and increased the activity of antioxidant enzymes. Overall, these results reveal the potential of the NLC formulation containing EGF and curcumin to promote healing of chronic wounds.

scholarly journals A Tara Gum/Olive Mill Wastewaters Phytochemicals Conjugate as a New Ingredient for the Formulation of an Antioxidant-Enriched Pudding

Foods ◽  
2022 ◽  
Vol 11 (2) ◽  
pp. 158
Author(s):  
Umile Gianfranco Spizzirri ◽  
Paolino Caputo ◽  
Cesare Oliviero Rossi ◽  
Pasquale Crupi ◽  
Marilena Muraglia ◽  
...  
Keyword(s):  
High Performance ◽  
Antioxidant Properties ◽  
Quinic Acid ◽  
Oral Toxicity ◽  
Main Compound ◽  
3T3 Fibroblasts ◽  
Olive Mill Wastewaters ◽  
Polymeric Conjugate ◽  
Olive Mill

Olive mill wastewater, a high polyphenols agro-food by-product, was successfully exploited in an eco-friendly radical process to synthesize an antioxidant macromolecule, usefully engaged as a functional ingredient to prepare functional puddings. The chemical composition of lyophilized olive mill wastewaters (LOMW) was investigated by HPLC-MS/MS and 1H-NMR analyses, while antioxidant profile was in vitro evaluated by colorimetric assays. Oleuropein aglycone (5.8 μg mL−1) appeared as the main compound, although relevant amounts of an isomer of the 3-hydroxytyrosol glucoside (4.3 μg mL−1) and quinic acid (4.1 μg mL−1) were also detected. LOMW was able to greatly inhibit ABTS radical (IC50 equal to 0.019 mg mL−1), displaying, in the aqueous medium, an increase in its scavenger properties by almost one order of magnitude compared to the organic one. LOMW reactive species and tara gum chains were involved in an eco-friendly grafting reaction to synthesize a polymeric conjugate that was characterized by spectroscopic, calorimetric and toxicity studies. In vitro acute oral toxicity was tested against 3T3 fibroblasts and Caco-2 cells, confirming that the polymers do not have any effect on cell viability at the dietary use concentrations. Antioxidant properties of the polymeric conjugate were also evaluated, suggesting its employment as a thickening agent, in the preparation of pear puree-based pudding. High performance of consistency and relevant antioxidants features over time (28 days) were detected in the milk-based foodstuff, in comparison with its non-functional counterparts, confirming LOWM as an attractive source to achieve high performing functional foods.

scholarly journals In vitro antioxidant properties of golden grass (Syngonanthus nitens) by electron paramagnetic resonance

2019 ◽  
Vol 7 (4) ◽  
pp. 1353-1360
Author(s):  
Rafael P. Barroso ◽  
Leonardo S. Berlim ◽  
Amando S. Ito ◽  
Antonio J. Costa‐Filho
Keyword(s):  
Electron Paramagnetic Resonance ◽  
Antioxidant Properties ◽  
Paramagnetic Resonance ◽  
Golden Grass ◽  
Syngonanthus Nitens ◽  
Electron Paramagnetic

QUALITATIVE AND QUANTITATIVE PHYTOCHEMICAL SCREENING AND IN VITRO ANTIOXIDANT EVALUATION OF PERGULARIA DAEMIA

2018 ◽  
Vol 24 (2) ◽  
Author(s):  
GITA MISHRA ◽  
HEMESHWER KUMAR CHANDRA ◽  
NISHA SAHU ◽  
SATENDRA KUMAR NIRALA ◽  
MONIKA BHADAURIA
Keyword(s):  
Reducing Sugars ◽  
Antioxidant Properties ◽  
Phytochemical Analysis ◽  
Phytochemical Screening ◽  
Qualitative And Quantitative ◽  
The Family ◽  
Ethanolic Extracts ◽  
Antioxidant Evaluation ◽  
In Vitro Antioxidant Activity

Pergularia daemia belongs to the family Asclepiadaceae, known to have anticancer, anti-inflammatory activity. Aim of the present study was to evaluate qualitative and quantitative phytochemical and antioxidant properties of ethanolic extracts of leaf, stem and root parts of P. daemia . Preliminary phytochemical analysis and in vitro antioxidant properties were evaluated by standard methods. The qualitative phytochemical analysis of P. daemia showed presence of flavonoids, tannins, alkaloid, phytosterol, carbohydrate, phenol, saponin, glycosides, terpenoids, steroids proteins and reducing sugars. Quantitative analysis showed polyphenol, flavonoid, flavonone, flavone and flavonol in P. daemia leaves, stem and root in considerable quantity. The in vitro antioxidant activity of P. daemia clearly demonstrated that leaf, stem and root parts have prominent antioxidant properties and was effective in scavenging free radicals.

ДИНИТРОЗИЛЬНЫЕ КОМПЛЕКСЫ ЖЕЛЕЗА C ТИОЛСОДЕРЖАЩИМИ ЛИГАНДАМИ ПРЕДСТАВЛЕНЫ В ЖИВЫХ ОРГАНИЗМАХ В ОСНОВНОМ ИХ БИЯДЕРНОЙ ФОРМОЙ

2020 ◽  
Vol 65 (6) ◽  
pp. 1142-1153
Author(s):  
В.Д. Микоян ◽  
◽  
Е.Н. Бургова ◽  
Р.Р. Бородулин ◽  
А.Ф. Ванин ◽  
...  
Keyword(s):  
Electron Paramagnetic Resonance ◽  
Sodium Nitrite ◽  
Iron Complexes ◽  
Paramagnetic Resonance ◽  
First Case ◽  
Dinitrosyl Iron ◽  
Electron Paramagnetic ◽  
Dinitrosyl Complexes

The number of mononitrosyl iron complexes with diethyldithiocarbamate, formed in the liver of mice in vivo and in vitro after intraperitoneal injection of binuclear dinitrosyl iron complexes with N-acetyl-L-cysteine or glutathione, S-nitrosoglutathione, sodium nitrite or the vasodilating drug Isoket® was assessed by electron paramagnetic resonance (EPR). The number of the said complexes, in contrast to the complexes, formed after nitrite or Isoket administration, the level of which sharply increased after treatment of liver preparations with a strong reducing agent - dithionite, did not change in the presence of dithionite. It was concluded that, in the first case, EPR-detectable mononitrosyl iron complexes with diethyldithiocarbamate in the absence and presence of dithionite appeared as a result of the reaction of NO formed from nitrite with Fe2+-dieth- yldithiocarbamate and Fe3+-diethyldithiocarbamate complexes, respectively. In the second case, mononitrosyl iron complexes with diethyldithiocarbamate appeared as a result of the transition of iron-mononitosyl fragments from ready-made iron-dinitrosyl groups of binuclear dinitrosyl complexes, which is three to four times higher than the content of the mononuclear form of these complexes in the tissue...

Utilizing ICG Spectroscopical Properties for Real-Time Nanoparticle Release Quantification In vitro and In vivo in Imaging Setups

2020 ◽  
Vol 26 (31) ◽  
pp. 3828-3833 ◽  
Author(s):  
Tuula Peñate-Medina ◽  
Eike Kraas ◽  
Kunliang Luo ◽  
Jana Humbert ◽  
Hanwen Zhu ◽  
...  
Keyword(s):  
Release Kinetics ◽  
Pure Water ◽  
Squamous Carcinoma ◽  
Peak Shift ◽  
Intensity Increase ◽  
Nude Mouse Model ◽  
Absorption And Emission ◽  
Squamous Carcinoma Cells

Background: Nanoparticle imaging and tracking the release of the loaded material from the nanoparticle system have attracted significant attention in recent years. If the release of the loaded molecules could be monitored reliably in vivo, it would speed up the development of drug delivery systems remarkably. Methods: Here, we test a system that uses indocyanine green (ICG) as a fluorescent agent for studying release kinetics in vitro and in vivo from the lipid iron nanoparticle delivery system. The ICG spectral properties like its concentration dependence, sensitivity and the fluctuation of the absorption and emission wavelengths can be utilized for gathering information about the change of the ICG surrounding. Results: We have found that the absorption, fluorescence, and photoacoustic spectra of ICG in lipid iron nanoparticles differ from the spectra of ICG in pure water and plasma. We followed the ICG containing liposomal nanoparticle uptake into squamous carcinoma cells (SCC) by fluorescence microscopy and the in vivo uptake into SCC tumors in an orthotopic xenograft nude mouse model under a surgical microscope. Conclusion: Absorption and emission properties of ICG in the different solvent environment, like in plasma and human serum albumin, differ from those in aqueous solution. Photoacoustic spectral imaging confirmed a peak shift towards longer wavelengths and an intensity increase of ICG when bound to the lipids. The SCC cells showed that the ICG containing liposomes bind to the cell surface but are not internalized in the SCC-9 cells after 60 minutes of incubation. We also showed here that ICG containing liposomal nanoparticles can be traced under a surgical camera in vivo in orthotopic SCC xenografts in mice.

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