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... B 3 is composed of nicotinic acid amide (niacinamide), nicotinic acid (niacin) and its esters ( Fig. 1). Niacinamide is a water-soluble compound of molecular weight 122.1 Da and melting point 130 O C, its pK a is 3.35 at 20 O C, partition coefficient octanol/water is -0.35. This substance is widely applied in cosmetic preparation at a concentration of 2-5%. Niacinamide is a well-tolerated and safe compound with a good bioavailability ...
Context 2
... B 3 is composed of nicotinic acid amide (niacinamide), nicotinic acid (niacin) and its esters ( Fig. 1). Niacinamide is a water-soluble compound of molecular weight 122.1 Da and melting point 130 O C, its pK a is 3.35 at 20 O C, partition coefficient octanol/water is -0.35. This substance is widely applied in cosmetic preparation at a concentration of 2-5%. Niacinamide is a well-tolerated and safe compound with a good bioavailability ...
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... In order to explore the effects of receiving solution type [13,14], receiving solution pH [15,16], skin type [17][18][19][20][21][22][23][24][25], receiving cell temperature [26], supply solution concentration, and supply solution application dose [14,27] on the transdermal absorption of nicotinamide, each factor was explored. For the effect of the solution in the receiving cell, the main body of the solution in the receiving cell was PBS buffer solution (pH 7.4), and the effects of 20% anhydrous ethanol, 2% PEG400, and 2% Tween 20 on the transdermal absorption results were investigated. ...
The goal of this research was to study the factors influencing the in vitro transdermal penetration of nicotinamide and to establish an evaluation method for the in vitro transdermal absorption of nicotinamide. The permeability of nicotinamide was investigated with Franz diffusion cell in vitro transcutaneous assays, and the effect of the receiving solution composition, receiving solution pH, skin type, diffusion cell temperature, active ingredient concentration, supply quantity, and product dosage form on its permeation was investigated separately by high-performance liquid chromatography. The best assay for the transdermal absorption of nicotinamide was established—there was a better transdermal absorption performance, more stable system, better applicability, and better reproducibility when the receiving solution was PBS (phosphate-buffered saline) solution, the pH was 7.4, the membrane was pig ear skin, the temperature was 37 °C, the concentration of nicotinamide was 3%, and the dose of the test substance was 2 g. In the three cosmetic dosage forms of toning lotion, milk lotion, and gel, the permeability of milk lotion was the highest, followed by toning lotion and gel.
... However, it is important to determine the degree of penetration through the skin of the active substances. The penetration degree of these substances may be different, depending on the compound's physical and chemical properties, such as lipophilicity, structure, and polarity [68,69]. To achieve the benefit action of phenolic acids in the skin, they should be released from the topical formulation and permeate the SC, which is the main skin barrier. ...
Epilobium angustifolium L. is a popular and well-known medicinal plant. In this study, an attempt to evaluate the possibility of using this plant in preparations for the care and treatment of skin diseases was made. The antioxidant, antiaging and anti-inflammatory properties of ethanolic extracts from Epilobium angustifolium (FEE) were assessed. Qualitative and quantitative evaluation of extracts chemically composition was performed by gas chromatography with mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC). The total polyphenol content (TPC) of biologically active compounds, such as the total content of polyphenols (TPC), flavonoids (TFC), and assimilation pigments, as well as selected phenolic acids, was assessed. FEE was evaluated for their anti-inflammatory and antiaging properties, achieving 68% inhibition of lipoxygenase activity, 60% of collagenase and 49% of elastase. FEE also showed high antioxidant activity, reaching to 87% of free radical scavenging using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 59% using 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). Additionally, in vitro penetration studies were performed using two vehicles, i.e., a hydrogel and an emulsion containing FEE. These studies showed that the active ingredients contained in FEE penetrate through human skin and accumulate in it. The obtained results indicate that E. angustifolium may be an interesting plant material to be applied as a component of cosmetic and dermatological preparations with antiaging and anti-inflammatory properties.
... Marti-Mesters et al. showed penetration of both CA and ChA (applied as pure compounds) through the pig skin [39]. As previously mentioned, the penetration of active substances through the skin also depends on the physicochemical properties, in particular molecular weight and lipophilicity of the compounds [56][57][58]. Higher lipophilicity increases whereas higher molecular weight decreases percutaneous absorption [54]. ...
Epilobium angustifolium L. is applied as an antiseptic agent in the treatment of skin diseases. However, there is a lack of information on human skin penetration of active ingredients with antioxidative potential. It seems crucial because bacterial infections of skin and subcutaneous tissue are common and partly depend on oxidative stress. Therefore, we evaluated in vitro human skin penetration of fireweed ethanol-water extracts (FEEs) by determining antioxidant activity of these extracts before and after penetration study using 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and Folin–Ciocalteu methods. Microbiological tests of extracts were done. The qualitative and quantitative evaluation was performed using gas chromatography-mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC-UV) methods. The in vitro human skin penetration using the Franz diffusion chamber was assessed. The high antioxidant activity of FEEs was found. Gallic acid (GA), chlorogenic acid (ChA), 3,4-dihydroxybenzoic acid (3,4-DHB), 4-hydroxybenzoic acid (4-HB), and caffeic acid (CA) were identified in the extracts. The antibacterial activities were found against Serratia lutea, S. marcescens, Bacillus subtilis, B. pseudomycoides, and B. thuringiensis and next Enterococcus faecalis, E. faecium, Streptococcus pneumoniae, Pseudomonas aeruginosa, and P. fluorescens strains. In vitro penetration studies showed the penetration of some phenolic acids and their accumulation in the skin. Our results confirm the importance of skin penetration studies to guarantee the efficacy of formulations containing E. angustifolium extracts.
The theoretical interpretation of the vaginal permeability phenomenon, the evaluation of the suitability of five artificial membranes, and the prediction of the behaviors of vaginal drugs were the main objectives of this study. Franz vertical diffusion cells and different validated HPLC methods were used to measure the permeability of six vaginally administered drugs (econazole, miconazole, metronidazole, clindamycin, lidocaine, and nonoxynol-9). This study was performed (in vitro) on different membranes of polyvinylidene fluoride (PVDF), plain cellulose or cellulose impregnated with isopropyl myristate (IPM), and cellulose combined with PVDF or IPM. The results were compared with those obtained from cow vaginal tissue (ex vivo), where cellulose was proven to be the best simulant. According to the permeability profiles (Papp), the water solubility of the drugs was considered a necessary criterion for their transport in the membranes or in the tissue, while the size was important for their penetration. Furthermore, it was found that polar compounds show clear superiority when penetrating cellulose or tissue, while non-polar ones show superiority when penetrating the lipophilic PVDF membrane. Finally, a successful attempt was made to predict the Papp values (|Papp-predPapp| < 0.005) of the six drugs under study based on a PLS (Partial Least Squares) in silico simulation model.
