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 Enhancement of the Antioxidant and Skin Permeation Properties of Eugenol by the Esterification of Eugenol to New Derivatives

2020 ◽  
Author(s):  
EDYTA MAKUCH ◽  
Anna Nowak ◽  
Andrzej Günther ◽  
Robert Pełech ◽  
Łukasz Kucharski ◽  
...  
Keyword(s):  
Gas Chromatography ◽  
Antioxidant Activity ◽  
Free Radical ◽  
Skin Permeation ◽  
Radical Scavenging ◽  
Skin Penetration ◽  
Dichloroacetic Acid ◽  
Pig Skin ◽  
High Level

Abstract The aim of the study was to determine the antioxidant activity and assess the lipophilicity and skin penetration of eugenyl chloroacetate (EChA), eugenyl dichloroacetate (EDChA), and eugenyl trichloroacetate (ETChA). Identification of the obtained products was based on gas chromatography (GC), infrared spectroscopy (FTIR/ATR), gas chromatography coupled with mass spectrometry (GC-MS), and the analysis of 13C-NMR and 1H-NMR spectra. The antioxidative capacity of the derivatives obtained was determined by the DPPH free radical reduction method, while the octanol/water partition coefficient (shake-flask method) was tested to determine the lipophilicity of these compounds. In the next stage of testing EDChA and ETChA–(compounds characterized by the highest degree of free radical scavenging), the penetration of DPPH through pig skin and its accumulation in the skin were evaluated. For comparison, penetration studies of eugenol alone as well as dichloroacetic acid (DChAA) and trichloroacetic acid (TChAA) were also carried out. The antioxidant activity (DPPH, ABTS, and Folin–Ciocalteu methods) of the fluid that penetrated through pig skin was also evaluated. The in vitro pig skin penetration study showed that eugenol derivatives are particularly relevant for topical application. The obtained derivatives were characterized by a high level 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.

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 Enhancement of the antioxidant and skin permeation properties of eugenol by the esterification of eugenol to new derivatives

AMB Express ◽  
2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Edyta Makuch ◽  
Anna Nowak ◽  
Andrzej Günther ◽  
Robert Pełech ◽  
Łukasz Kucharski ◽  
...  
Keyword(s):  
Gas Chromatography ◽  
Antioxidant Activity ◽  
Free Radical ◽  
Skin Permeation ◽  
Radical Scavenging ◽  
Skin Penetration ◽  
Dichloroacetic Acid ◽  
Pig Skin ◽  
High Level

Abstract The aim of the study was to determine the antioxidant activity and assess the lipophilicity and skin penetration of eugenyl chloroacetate (EChA), eugenyl dichloroacetate (EDChA), and eugenyl trichloroacetate (ETChA). Identification of the obtained products was based on gas chromatography (GC), infrared spectroscopy (FTIR/ATR), gas chromatography coupled with mass spectrometry (GC-MS), and the analysis of 13C-NMR and 1H-NMR spectra. The antioxidative capacity of the derivatives obtained was determined by the DPPH free radical reduction method, while the octanol/water partition coefficient (shake-flask method) was tested to determine the lipophilicity of these compounds. In the next stage of testing EDChA and ETChA–(compounds characterized by the highest degree of free radical scavenging), the penetration of DPPH through pig skin and its accumulation in the skin were evaluated. For comparison, penetration studies of eugenol alone as well as dichloroacetic acid (DChAA) and trichloroacetic acid (TChAA) were also carried out. The antioxidant activity (DPPH, ABTS, and Folin–Ciocalteu methods) of the fluid that penetrated through pig skin was also evaluated. The in vitro pig skin penetration study showed that eugenol derivatives are particularly relevant for topical application. The obtained derivatives were characterized by a high level of antioxidant activity 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.

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.

TOPICAL DELIVERY OF DRUGS USING ETHOSOMES: A REVIEW

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (08) ◽  
pp. 7-20
Author(s):  
V Sankar ◽  
V. Wilson ◽  
K. Siram ◽  
A. Karuppaiah ◽  
S Hariharan ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Skin Permeation ◽  
Protective Layer ◽  
Systemic Circulation ◽  
Healing Time ◽  
Androgenic Alopecia ◽  
Recurrent Herpes

The skin is the largest organ of the human body that restricts the movement of drug to the systemic circulation. Topical drug delivery system is a system where the drug reaches the systemic circulation through the protective layer i.e. skin. The main disadvantage of this route is the low diffusion rate of the drugs which is across the stratum corneum layer of the skin. To overcome this problem to a certain extent, ethosomal delivery for drugs and herbal compounds has been recently introduced. Literature studies indicate that ethosomal formulation of acyclovir shows high therapeutic efficiency with shorter healing time in the treatment of recurrent herpes labialis than conventional Zovirax. Also, the ethosomes of minoxidil enhanced the skin permeation of minoxidil in vitro in comparison to its ethanolic or phospholipid ethanolic micellar solution or hydroethanolic solution. T he advantages of this system include increased drug permeation, increased drug entrapment and improved drug delivery. Ethosomal drug delivery system opens up doors for the development of new and novel therapies for treating male pattern baldness, as it is an easier way to prepare, in addition to its safety and efficacy. In this review article, we have focused on methods of preparation of ethosomes, characterization techniques, applications, details about the various research trials for the management of androgenic alopecia and various ethosomal products in market.

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.

scholarly journals FORMULATION AND DEVELOPMENT OF TRANSDERMAL DRUG DELIVERY SYSTEM OF ETHINYLESTRADIOL AND TESTOSTERONE: IN VITRO EVALUATION

2019 ◽  
Vol 11 (1) ◽  
pp. 55
Author(s):  
Shikha Baghel Chauhan ◽  
Tanveer Naved ◽  
Nayyar Parvez
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
Physical Parameters ◽  
Transdermal Patch ◽  
Transdermal Drug Delivery System ◽  
In Vitro Skin Permeation

Objective: The combination therapy of ethinylestradiol and testosterone in post-menopausal females has shown improved sexual response and libido. The present studies were designed to develop a suitable matrix-type transdermal drug delivery system (TDDS) of ethinylestradiol and testosterone using the polymer chitosan.Methods: Five formulations (ET1 to ET5) were developed by varying the concentration of polymer and keeping the drug load constant. Physical parameters and drug excipient interaction studies were evaluated in all the formulations. In vitro skin permeation profiles of ethinylestradiol and testosterone from various formulations were simultaneously characterized in a thermostatically controlled modified Franz Diffusion cell using HPLC. Based on the physical parameters and in vitro skin permeation profile formulation ET3 containing 30 mg/ml of chitosan was found to be the best and chosen for further studies. Optimized formulation was subjected to in vivo pharmacokinetic analysis in rats using ELISA.Results: Stability profile of patch formulation ET3 depicted stability up to 3 mo. One week skin irritation evaluation in rats indicated that formulation ET3 was nonirritating. Combination transdermal patch across rat skin showed a maximum release of 92.936 and 95.03 % in 60 h with a flux of 2.088 and 21.398 µg/cm2h for ethinylestradiol and testosterone respectively.Conclusion: The net result of this study is the formulation of a stable, non-irritating transdermal patch of ethinylestradiol and testosterone, with good bioavailability and can be used as Estrogen Replacement Therapy (ERT) in postmenopausal women.

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.

scholarly journals BIOMIMETIC APPROACHES TO STUDY OF PROPERTIES OF MEDICINAL SUBSTANCES

2019 ◽  
Vol 62 (10) ◽  
pp. 4-29
Author(s):  
Nina B. Melnikova ◽  
Olga N. Solovyova ◽  
Evgeni N. Evgeni N. Kochetkov
Keyword(s):  
Antioxidant Activity ◽  
Superoxide Dismutase ◽  
Lipid Bilayers ◽  
Superoxide Anion ◽  
Molecular Form ◽  
Biologically Active ◽  
New Drugs ◽  
In Vitro Experiments ◽  
Medicinal Substances

The review is devoted to an assessment of the current level of use of biomimetic approaches to the study of the properties of known drugs and the development of new drugs. In this review, we consider the main biological functions of superoxide dismutase, namely the catalytic decomposition of toxic superoxide anion of oxygen to the molecular form of oxygen and protection against induced apoptosis. The biomimetic enzymes-Mn- and TEMPO-containing equivalents of superoxide dismutase SOD with antitumor and antioxidant activity were discussed more detail. The relationship between the properties and activity of SOD mimetics with their structure among them the nature of the anion and ligands, the coordination number, the geometry of the presence of conjugated bonds, and other parameters of the molecules. The study of the properties of Mn-SOD mimetics makes it possible to develop a new class of drugs successfully tested by in vivo and in vitro experiments and which are at the stages of clinical trials. Stable TEMPO radicals containing compounds are able to perform SOD functions, exhibiting antioxidant activity in relation not only to superoxide-anion, but also to peroxynitrile, and moreover to act as a spin label. The biomimetic membrane systems (monolayers, planar lipid bilayers, liposomes and other nano-sized objects) are discussed too for studying properties in in vitro experiments and for delivering potent and medicinal substances. The biomimetic approach combination allows to create the new promising drugs, including those based on SOD mimetics, and to develop the synthetic analogues of biologically active substances and methods of their delivery. The advantages of such dosage forms are lower toxicity of the preparations, lack of immunogenicity and a decrease in the dose of potent drugs.

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