scholarly journals The Effect of Cream and Gel Vehicles on the Percutaneous Absorption and Skin Retention of a New Eugenol Derivative With Antioxidant Activity

2021 ◽  
Vol 12 ◽  
Author(s):  
Edyta Makuch ◽  
Anna Nowak ◽  
Andrzej Günther ◽  
Robert Pełech ◽  
Łukasz Kucharski ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Steam Distillation ◽  
Skin Permeation ◽  
Biologically Active ◽  
Skin Permeability ◽  
Skin Accumulation ◽  
Radical Reduction ◽  
Skin Retention

The effect of cream and gel vehicles containing clove water on skin permeability was compared for a new eugenol derivative (eugenyl dichloroacetate—EDChA) with antioxidant activity. In vitro permeation experiments were conducted in a Franz cell with porcine skin. The cumulative mass and skin accumulation of EDChA were investigated and compared. The antioxidative capacity of the studied vehicles was determined by using the diphenylpicrylhydrazyl (DPPH) free radical reduction method. The antioxidant activity (evaluated with DPPH, ABTS, and the Folin–Ciocalteu methods) of the fluid that penetrated through the pig skin and of the fluid obtained after the skin extraction, were also determined. For comparison, eugenol was also tested. The results of this work could contribute to the development of vehicles with antioxidant potential estimated after 24 h of conducting the experiment, which indicates long-term protection against reactive oxygen species (ROS) in the deeper layers of the skin. The waste water from the clove buds steam distillation -contains several valuable biologically active compounds, and its use is environmentally friendly. We observed that gel vehicles were the best enhancer of skin permeation for both eugenol and its derivative. In most cases, -similar cumulative masses of eugenol and its ester were found in the acceptor fluid. The accumulation of EDChA was higher for cream vehicles in relation to the parent eugenol when applied onto the skin. The greatest amounts of eugenol were accumulated in the skin when these compounds were used in gel vehicles.

scholarly journals An Advanced Mode of Antioxidants Delivery System Effective in the Treatment of ROS and Skin Permeation of The Cosmetic Formulations - The Possible Application of Clove Oil, Eugenol and New Eugenol Derivative

2020 ◽  
Author(s):  
Edyta Makuch ◽  
Anna Nowak ◽  
Andrzej Günther ◽  
Robert Pełech ◽  
Łukasz Kucharski ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Delivery System ◽  
Steam Distillation ◽  
Skin Permeation ◽  
Dichloroacetic Acid ◽  
Biologically Active ◽  
Clove Oil ◽  
Pig Skin ◽  
Cosmetic Formulations

The main focus of this work is to extend the knowledge about the complexity of issues of oxidative stress. Natural compounds play a serious role in multiple aspects of both human, leading to clear health-promoting effects. This work is focused on the potential application cosmetic formulations containing including but not limited to of clove water and isolated clove oils on their aid in the control of the diseases. The aim of our work was to prepare to evaluate cosmetic formulations containing clove oil, eugenol or new eugenol ester derivative (eugenyl dichloroacetate - EDChA) but also cosmetic formulations containing the aqueous phase obtained after separation of essential oil following the clove buds steam distillation. To evaluate the antioxidants transdermal delivery system, in vitro permeation experiments in a Franz diffusion cell were performed using pig skin. The antioxidative capacity of the cosmetic formulations obtained was determined by the DPPH free radical reduction method. In the next stage, the antioxidant activity (DPPH, ABTS, and Folin–Ciocalteu methods) of the fluid that penetrated through pig skin and of the fluid obtained after skin extraction, were also evaluated. For comparison, studies of cosmetic formulation containing alone dichloroacetic acid (DChAA) were as well carried out. The obtained cosmetic formulations were characterized by of antioxidant activity estimated after 24 hours of conducting the experiment, which indicates long-term protection against reactive oxygen species (ROS) in the deeper layers of the skin. The results of this work contribute to the development of cosmetic formulations with antioxidant potential, emphasizing that the water phases are waste from the process of cloves steam distillation and are not used to prepare cosmetic formulations. The use of waste water from the clove buds steam distillation process is environmentally friendly and not allows us to waste, containing however valuable biologically active compounds (furfural, methyl salicylate, 4-allilofenol, eugenol, α- and β-caryophyllene, eugenyl acetate, β-caryophyllene oxide). Together, these results suggest that cosmetic formulations may be potential drug candidates for chemopreventive, antineoplastic and antimutagenic therapy.

scholarly journals Effect of Different Durations of Solid-Phase Fermentation for Fireweed (Chamerion angustifolium (L.) Holub) Leaves on the Content of Polyphenols and Antioxidant Activity In Vitro

Molecules ◽  
2020 ◽  
Vol 25 (4) ◽  
pp. 1011 ◽  
Author(s):  
Marius Lasinskas ◽  
Elvyra Jariene ◽  
Nijole Vaitkeviciene ◽  
Ewelina Hallmann ◽  
Katarzyna Najman
Keyword(s):  
Antioxidant Activity ◽  
High Performance ◽  
Solid Phase ◽  
Principal Component ◽  
Biologically Active ◽  
Chamerion Angustifolium ◽  
Oenothein B ◽  
And Control

Fireweed has recently been recognized as a plant with high antioxidant potential and phenolic content. Its leaves can be fermented to prepare an infusion with ideal antioxidant activity. The aim of this study was to investigate and to determine the influence of solid-phase fermentation of different durations on the variation of polyphenols in the leaves of fireweed. Laboratory experiments were conducted in 2017–2018. The leaves of fireweed, naturally growing, were fermented for different periods of time: not fermented (control) and fermented for 24 and 48 h. The evaluation of polyphenols and antioxidant activity in leaves was performed using high- performance liquid chromatography (HPLC). Additionally, principal component analysis was used to characterize differences in bioactive compounds between fireweed samples fermented at different durations. Solid-phase fermented leaves were characterized by higher contents of oenothein B, quercetin and benzoic acid but had lower contents of quercetin-3-O-rutinoside, luteolin and chlorogenic and gallic acids. Antioxidant activity in short- (24 h) and long-term (48 h) fermentation (compared to control) gave the highest level of regression in 2017, but in 2018 the effect was observed only with short-term fermentation and control. In conclusion, solid-phase fermentation can be used to modulate biologically active compounds in fireweed leaves.

scholarly journals Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3579
Author(s):  
Svetlana A. Popova ◽  
Evgenia V. Pavlova ◽  
Oksana G. Shevchenko ◽  
Irina Yu. Chukicheva ◽  
Aleksandr V. Kutchin
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
High Reactivity ◽  
Biologically Active ◽  
Brain Lipids ◽  
Wide Range ◽  
Privileged Structure ◽  
Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

Aktywność przeciwutleniająca ekstraktów z wybranych roślin należących do rodziny Rosaceae

2018 ◽  
Vol 19 (3) ◽  
Author(s):  
Anna Muzykiewicz ◽  
Joanna Zielonka-Brzezicka ◽  
Adam Klimowicz
Keyword(s):  
Antioxidant Activity ◽  
Extraction Method ◽  
Extraction Methods ◽  
Biologically Active ◽  
Sorbus Aucuparia ◽  
Cydonia Oblonga ◽  
Leaf Extracts ◽  
Soxhlet Apparatus ◽  
Rosaceae Family

Introduction. Plants are a valuable source of biologically active compounds, including antioxidants, which could prevent the development of oxidative stress. The members of Rosaceae family such as Sorbus aucuparia L. and Cydonia oblonga Mill. are the examples of plants contained antioxidants. Aim. The aim of the study was to evaluate the antioxidant potential of leaves and fruits extracts of rowan and quince, taking into account influence of the extrahent as well as extraction method on this activity. Material and methods. The extracts were obtained by classic extraction methods – shaking and extraction in Soxhlet apparatus. Methanol, acetone as well as 70 and 96% (v/v) ethanol were used as solvents. Antioxidant activity was estimated by DPPH, FRAP, Folin-Ciocalteu (F-C) and ABTS methods. Results. The highest antioxidant activity was found in leaf extracts of both plants. In most cases, rowan extracts showed higher potential than appropriate extracts of quince. The most effective extraction method was extraction in Soxhlet apparatus using methanol (in case of rowan and quince) as well as 96% (v/v) ethanol (quince) and 70% (v/v) ethanol (rowan). The highest results were obtained with FRAP method, whereas the lowest – with DPPH. Conclusions. The presented in vitro results confirmed, that the leaves and fruits extracts of selected plants belonging to the Rosaceae family showed antioxidant activity and could be applied in various industry branches.

Investigating the potential of Quercetin enthused nano lipoidal system for the management of dermatitis

2021 ◽  
pp. 6516-6526
Author(s):  
Deepti Dwivedi ◽  
Shubham Pandey ◽  
Shafaque Asif ◽  
Vineet Awasthi ◽  
Gurjeet Kaur ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Skin Permeation ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Laser Scanning Microscopy ◽  
Polydispersity Index ◽  
In Vivo Studies ◽  
Confocal Laser ◽  
Skin Retention

Objective: The present research work was undertaken to develop quercetin enthused nanolipoidal systems and its characterization. The objective was to investigate potential of prepared system in the management of DNCB induced dermatitis. Method: Nanolipoidal system was prepared in different combinations with quercetin, L-α phosphatidylcholine (SPC) and ethanol and characterized for particle size, polydispersity index (PDI), zeta potential, drug entrapment efficiency, percentage drug release, skin retention and skin permeation. Selected batches were further incorporated into Carbopol 934 base gel. The vesicles were in size range 324.19-359 nm while polydispersity index (PDI) ranges from 0.241-0.554 and for zeta potential, it was from -26.33 to -39.3 nm. Entrapment efficiency was from 23.77-94.68 %. Confocal laser scanning microscopy showed penetration depth of rhodamine enthused ethosome across rat skin up to 45.23 µm which was significantly higher than the rhodamine solution (10 µm). In dinitrochlorobenzene (DNCB) induced mice dermatitis model histopathology study showed a marked decrease in amount of inflammatory cell nucleus in mice treated with quercetin loaded ethosomal gel followed by 76.13% decrease in-ear swelling and ear mass respectively in morphology study. The conventional marketed formulation showed a nominal decrease in epidermal thickness. Further Primary irritation index was less than 0.4 indicating negligible irritation in all the groups. Results: The optimized formulation F6 with SPC and ethanol in the ratio of 20:80 displayed the highest drug content and entrapment efficiency of 94.68±1.14%. PDI was 0.241±0.11 and skin retention 7.7%. Batch F6 with vesicle size and zeta potential of 324.9±19 nm and -26.33 mV, respectively, was incorporated in Carbopol 934 base gel and the prepared gel was evaluated for morphology, spreadability, in vitro, ex vivo release study, and kinetics study and in vivo studies. Conclusion: The present study revealed that the developed ethosomal gel can be used for enhanced delivery of Quercetin via skin. The in vitro studies indicated that the gel serves as an efficient carrier for Quercetin. It showed its effectiveness in the management of dermatitis. Further, Quercetin loaded nanoethosomal gel formulation can be viewed as a promising drug delivery system for the management of dermatitis.

scholarly journals Transcutol® P Containing SLNs for Improving 8-Methoxypsoralen Skin Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 973
Author(s):  
Giulia Pitzanti ◽  
Antonella Rosa ◽  
Mariella Nieddu ◽  
Donatella Valenti ◽  
Rosa Pireddu ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Skin Layer ◽  
Skin Permeability ◽  
Puva Therapy ◽  
Ultraviolet A ◽  
3T3 Fibroblasts ◽  
Skin Delivery

Topical psoralens plus ultraviolet A radiation (PUVA) therapy consists in the topical application of 8-methoxypsoralen (8-MOP) followed by the skin irradiation with ultraviolet A radiation. The employment of classical 8-MOP vehicles in topical PUVA therapy is associated with poor skin deposition and weak skin permeability of psoralens, thus requiring frequent drug administration. The aim of the present work was to formulate solid lipid nanoparticles (SLNs) able to increase the skin permeation of 8-MOP. For this purpose, the penetration enhancer Transcutol® P (TRC) was added to the SLN formulation. SLNs were characterized with respect to size, polydispersity index, zeta potential, entrapment efficiency, morphology, stability, and biocompatibility. Finally, 8-MOP skin diffusion and distribution within the skin layers was investigated using Franz cells and newborn pig skin. Freshly prepared nanoparticles showed spherical shape, mean diameters ranging between 120 and 133 nm, a fairly narrow size distribution, highly negative ζ potential values, and high entrapment efficiency. Empty and loaded formulations were almost stable over 30 days. In vitro penetration and permeation studies demonstrated a greater 8-MOP accumulation in each skin layer after SLN TRC 2% and TRC 4% application than that after SLN TRC 0% application. Finally, the results of experiments on 3T3 fibroblasts showed that the incorporation of TRC into SLNs could enhance the cellular uptake of nanoparticles, but it did not increase their cytotoxicity.

scholarly journals An Investigation of the Influence of PEG 400 and PEG-6-Caprylic/Capric Glycerides on Dermal Delivery of Niacinamide

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2907
Author(s):  
Yanling Zhang ◽  
Majella E. Lane ◽  
David J. Moore
Keyword(s):  
Skin Permeation ◽  
Ternary Systems ◽  
Pharmaceutical Products ◽  
Porcine Skin ◽  
Peg 400 ◽  
Skin Delivery ◽  
Dermal Delivery ◽  
Binary And Ternary Systems ◽  
Skin Retention

Polyethylene glycols (PEGs) and PEG derivatives are used in a range of cosmetic and pharmaceutical products. However, few studies have investigated the influence of PEGs and their related derivatives on skin permeation, especially when combined with other solvents. Previously, we reported niacinamide (NIA) skin permeation from a range of neat solvents including propylene glycol (PG), Transcutol® P (TC), dimethyl isosorbide (DMI), PEG 400 and PEG 600. In the present work, binary and ternary systems composed of PEGs or PEG derivatives combined with other solvents were investigated for skin delivery of NIA. In vitro finite dose studies were conducted (5 μL/cm2) in porcine skin over 24 h. Higher skin permeation of NIA was observed for all vehicles compared to PEG 400. However, overall permeation for the binary and ternary systems was comparatively low compared with results for PG, TC and DMI. Interestingly, values for percentage skin retention of NIA for PEG 400:DMI and PEG 400:TC were significantly higher than values for DMI, TC and PG (p < 0.05). The findings suggest that PEG 400 may be a useful component of formulations for the delivery of actives to the skin rather than through the skin. Future studies will expand the range of vehicles investigated and also look at skin absorption and residence time of PEG 400 compared to other solvents.

scholarly journals EFFECT OF MENTHOL ON THE TRANSDERMAL PERMEATION OF ACECLOFENAC FROM MICROEMULSION FORMULATION

2019 ◽  
pp. 117-122
Author(s):  
Abdul Baquee Ahmed ◽  
Gouranga Das
Keyword(s):  
Droplet Size ◽  
Skin Permeation ◽  
Peak Height ◽  
Skin Permeability ◽  
Permeability Barrier ◽  
Microemulsion Formulation ◽  
Transdermal Permeation ◽  
Ir Studies ◽  
Ft Ir

Objective: The aim of this investigation was to enhance the transdermal permeation of aceclofenac (ACF) from microemulsion formulation using menthol as a natural permeation enhancer. Methods: Microemulsion containing 2% w/v of ACF was prepared by a titration method with different concentration of oil, surfactant and co-surfactant. The prepared microemulsion was evaluated for droplet size, viscosity, pH and in vitro skin permeation studies. Menthol at 3-8% w/w was added to the selected microemulsion formulation and their effect on skin permeation was evaluated across rat epidermis using modified Keshary-Chien diffusion cell. The Fourier transform infrared spectroscopy (FT-IR) was performed to understand the regulation action of menthol in the skin permeability barrier. Results: The average droplet size of the microemulsion was found to be 89.4±2.12 to 175.2±3.10 nm. The transdermal flux of the microemulsion containing 8% w/w menthol showed 2.9 fold increases in transdermal flux of ACF compared with the formulation without menthol. Result of FT-IR studies showed decrease in peak height of the symmetric and asymmetric C-H stretching vibrations may be because of the extraction of the stratum corneum (SC) lipids and the alteration of the skin permeability barrier. Conclusion: This result suggests that menthol significantly enhanced the transdermal permeation of ACF and may be an effective natural penetration enhancer for transdermal delivery of the drug.

scholarly journals The Nutritional Value of Non-Traditional Gluten-Free Flakes and Their Antioxidant Activity

Antioxidants ◽  
2019 ◽  
Vol 8 (11) ◽  
pp. 565
Author(s):  
Kristýna Šťastná ◽  
Martina Mrázková ◽  
Daniela Sumczynski ◽  
Betül Cındık ◽  
Erkan Yalçın
Keyword(s):  
Antioxidant Activity ◽  
High Performance ◽  
Sugar Content ◽  
Chenopodium Quinoa ◽  
Biologically Active ◽  
Eragrostis Tef ◽  
Total Phenolic ◽  
Phenolic Antioxidants ◽  
In Vitro Digestibility

Nowadays, there is a growing interest for foods with a lower sugar content and rich in fiber and biologically active substances. The main purpose of this study was to prepare flakes from non-traditional pigmented cereals (Oryza sativa, Chenopodium quinoa, and Eragrostis tef) and to analyze their fibre, sugar, and in vitro digestibility values. Regarding phenolic antioxidants (soluble, soluble conjugated, and insoluble bound fractions), their content and antioxidant activity were measured using spectrophotometry and high performance liquid chromatography (HPLC) methods. Hydrothermally treated grains resulted in flakes with higher total dietary fibre contents (11.1–24.4%), quinoa and teff flakes were rich in maltose (up to 42.0 mg/g). Non-traditional flakes had lower in vitro digestibility, but conversely, they exhibited the highest phenolic contents corresponding with the highest antioxidant activity values (up to 2.33 mg Gallic acid equivalent/g of total phenolic content and 1.59 mg Trolox equivalent/g for 2,2-diphenyl-1-picrylhydrazyl (DPPH) in case of brown teff). Among free phenolics, the main contributors to an antioxidant activity were p-coumaric, o-coumaric, and gallic acids (r > 0.8186); among the soluble conjugated fractions, they were epigallocatechin, epicatechin, caffeic, and vanillic acids (r > 0.5935); while caffeic, protocatechuic, and ferulic acids (r > 0.5751) were the main contributors among the insoluble bound phenolics.

Comparison of immunomodulatory properties of purified lactoferrin, lactoperoxidase and β-casein in sheep

1998 ◽  
Vol 65 (4) ◽  
pp. 697-701 ◽  
Author(s):  
CHUN W. WONG ◽  
DENNIS L. WATSON ◽  
GEOFFREY O. REGESTER ◽  
GEOFFREY W. SMITHERS
Keyword(s):  
Biomedical Applications ◽  
Bovine Milk ◽  
Milk Proteins ◽  
Biologically Active ◽  
Immunological Effects ◽  
Bovine Milk Proteins ◽  
Proteins And Peptides

Bovine milk contains a variety of proteins and peptides that are biologically active (Ogra & Ogra, 1978; Duncan & McArthur, 1981; Newby et al. 1982; Juto, 1985; Stoeck et al. 1989; Mincheva-Nilsson et al. 1990; Watson, 1990; Barta et al. 1991; Politis et al. 1991; Fiat et al. 1993). Our laboratory has a long-term interest in some purified milk proteins, particularly lactoferrin (LF), lactoperoxidase (LP) and β-casein (β-CN), which have been shown to be immunologically significant. Some of our recent studies on these bovine milk proteins, particularly β-CN, indicated that their in vitro immunological effects did not always parallel their in vivo activities (Wong et al. 1996a, b; 1997a, b). This study was designed to investigate and compare the capacity of these purified bovine milk proteins to modulate a range of components that are vital to in vivo immune responses in sheep, with a view to providing further information on their potential in biomedical applications. To achieve this objective, a sensitive lymphatic cannulation model was employed that allows in vivo immune components and their functions to be measured in lymph collected under physiological conditions.

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