scholarly journals Influence of microemulsion components on transdermal delivery of immunomodulator glucosaminylmuramyl dipeptide

Author(s):  
E. G. Kuznetsova ◽  
O. M. Kuryleva ◽  
L. A. Salomatina ◽  
S. V. Kursakov ◽  
S. V. Guryanova ◽  
...  

This paper demonstrates a chemical way of enhancing transdermal delivery using immunomodulator glucosaminylmuramyl dipeptide (GMDP) as an example. Objective: to study in vitro the effect of various components of the microemulsion composition on GMDP diffusion through the skin from a transdermal therapeutic system (TTS). Materials and methods. Medicinal substance – glucosaminylmuramyl dipeptide (Peptek, Russia). Excipients and raw materials: sodium chloride, purified water, sodium dodecyl sulfate, docusate sodium, oak bark, apricot kernel oil, alpha-tocopheryl acetate and Decaglyn PR-20 emulsifier. Equipment: Heidolph DIAX 900 mechanical disperser (Germany) and Hielscher UIS250V ultrasonic homogenizer (Germany). GMDP diffusion from TTS through unpreserved rabbit skin was studied on diffusion tester Copley (UK). GMDP in aqueous solutions was determined by reversed-phase high-performance liquid chromatography (RP-HPLC) on an Agilent 1200 chromatography system (Agilent Technologies, USA). Results. A microemulsion system composed of 20% docusate sodium in an oil phase and an oak bark decoction as an aqueous phase was developed. This made it possible to increase GMDP transdermal delivery by ~70% in comparison with the basic composition. Conclusion. The characteristic parameters of microemulsion components of GMDP contained in TTS, influencing GMDP diffusion through unpreserved rabbit skin in vitro, were determined. Introducing relative indicators would be advisable in order to correctly evaluate the results of different series of in vitro experiments with biological objects.

1985 ◽  
Vol 65 (2) ◽  
pp. 285-298 ◽  
Author(s):  
J. E. KRUGER ◽  
B. A. MARCHYLO

Chromatographic conditions were optimized and three commercially available columns were evaluated for separation of alcohol-soluble storage proteins of Neepawa wheat using reversed-phase high-performance liquid chromatography (RP-HPLC). Optimal separation was achieved using an extracting solution of 50% 1-propanol, 1% acetic acid, and 4% dithiothreitol and an HPLC elution time of 105 min at a flow rate of 1.0 mL/min. HPLC columns evaluated (SynChropak RP-P, Ultrapore RPSC and Aquapore RP-300) varied in selectivity and resolution. The column providing the greatest versatility was Aquapore RP-300 available in cartridge form. Sodium dodecyl sulfate gradient-gel electrophoresis analysis of protein peaks resolved by RP-HPLC indicated that many of the eluted peaks contained more than one protein species. Chromatographic protein patterns obtained for Neepawa wheat grown at different locations and in different years were qualitatively the same.Key words: Protein, high-performance liquid chromatography, wheat


Author(s):  
Z. N. Shchekoldina ◽  
A. A. Bogolyubov ◽  
A. Yu. Zakharov ◽  
B. A. Bulgakov ◽  
A. V. Babkin ◽  
...  

Objectives. Determination of target products and byproducts is necessary for the quality control of phthalonitrile monomer synthesis as well as production scaling and performing related kinetic studies. High-performance liquid chromatography (HPLC) is a simple and affordable method for quantitative chemical analysis, which also verifies the quality of raw materials. The objective of this study was to develop an HPLC technique for determining the composition of the reaction mixture in the synthesis of 1,3-bis(3,4-dicyanophenoxy)benzene (DPB).Methods. Reversed-phase HPLC was used to quantitatively analyze the reaction mixture.Results. A simple and rapid method for the quantitative HPLC analysis of phthalonitrile monomers and their mixtures with reagents was developed. Reaction times and the accumulation of byproducts were also studied.Conclusions. The successful performance of the developed technique allows us to recommend it for practical applications. The results obtained for reactors of different sizes have good convergence, and DPB synthesis was successfully scaled up to intermediate scale equipment.


2020 ◽  
Vol 11 (4) ◽  
pp. 5373-5381
Author(s):  
Iskandarsyah ◽  
Camelia Dwi Putri Masrijal ◽  
Harmita

A hormonal contraception progestin such as medroxyprogesterone acetate (MPA) is used to helps regulate ovulation thus as a part of contraception hormone therapy as a method of birth control. This study aimed to formulate, characterized, evaluated transfersomal gel containing medroxyprogesterone acetate and to increased subcutaneous penetration of medroxyprogesterone acetate. In this research, three transfersomes formulas were prepared and optimized, e.g. F1, F2 and F3 with phosphatidylcholine: tween 80 concentration were 90:10; 85:15; and 75:25, respectively. F2 was the best formula with the highest entrapment efficiency 81.20±0.42 %, Average 81.35 ±0.78 nm, morphology of vesicles were spheres, indeks polidispersity 0.198±0.012 and zeta potential was -34.83±0.64 mV. The transpersonal gel (FGT) containing F2, and non-transpersonal gel containing MPA in methanol(FG) were prepared. In vitro penetration test were conducted to both of them using Franz Diffusion cells. Analysis of medroxyprogesterone acetate used a high performance liquid chromatographic (HPLC) method with an ultraviolet detector on reversed-phase C18, 5µm; 150 x 4.6 mmcolumn; using acetonitrile-0.1% formic acid (60:40/v:v) and was detected at a wavelength of 240 nm with flow rate at 1.0 mL/min. Gel stability evaluation results showed that FGT was better than FG on pH stability, viscosity and rheological properties. Based on in vitro penetration study, cumulative subcutaneous penetration of medroxyprogesterone acetate from FGT was 2356.45 ± 197.73 ng.cm-2 and from FG 359.15 ± 13.60 ng.cm-2, respectively. Flux value for FGT and FG were 112.77 ± 6,47 ng.cm-2.hr-1and 17.99 ± 4.81 ng.cm-2.hr-1, respectively. It could be concluded that transfersomal gel medroxyprogesterone acetate for transdermal drug delivery increased cumulative transdermal penetration of medroxyprogesterone acetate by six times more than non-transfersomal gel dosage form.


2021 ◽  
pp. 301-308
Author(s):  
Olesya Nikolayevna Mazko ◽  
Lyudmila Ivanovna Tikhomirova ◽  
Lyudmila Vladimirovna Shcherbakova ◽  
Natal'ya Grigor'yevna Bazarnova ◽  
Dmitriy Alekseyevich Karpitsky

The aim of this study was to evaluate the effect of 6-benzylaminopurine (BAP) separately and in interaction with auxins on the change in the qualitative and quantitative composition of flavonoids in the raw materials of regenerating plants Iris sibirica L. Cambridge grade in comparison with aeroponic and intact raw materials using the method of high-performance liquid chromatography. Raw materials of I. sibirica Cambridge variety obtained in vitro culture had a richer qualitative composition of flavonoids than intact plants. The dependence of the accumulation of flavonoids on the concentration of 6-benzylaminopurine in nutrient media was noted. The presence of 13 compounds was observed in extracts of 70% ethyl alcohol from regenerating plants grown at the lowest concentration of BAP (1.0 µM) within the experiment. In quantitative terms, the flavonoid apigenin was maximally determined on a medium with BAP 1 µM, and kaempferol - on media with BAP 5.0 µM, supplemented with auxins. For a medium with 7.5 µM BAP, the lowest variety of compounds was observed (9) and the lowest kaempferol content. Auxins influenced the synthesis of flavonoids. The amount of flavonoids in all variants of the experiment increased by an average of 13% in the presence of auxins. The stages of the technological process of obtaining raw materials I. sibirica Cambridge variety on the basis of clonal micropropagation and cultivation in aeroponics conditions allowed to obtain raw materials that do not contain heavy and toxic metals, are not infected with pathogens and pests. With 1 m2 of useful area of aeroponics for 1 year, it is possible to collect 5 times more raw materials than with field cultivation. According to the qualitative composition of phenolic compounds, aeroponic raw materials are identical to intact plants.


2019 ◽  
Vol 55 (No. 2) ◽  
pp. 93-101 ◽  
Author(s):  
Francisco Teodoro Arroyo Cordero ◽  
Rocío Rodríguez-Arcos ◽  
Ana Jiménez-Araujo ◽  
Rafael Guillén-Bejarano ◽  
María José Basallote ◽  
...  

Glucosinolate extracts from sprouts of common Brassica nigra, B. juncea cv. Scala, B. carinata cv. Eleven, and Sinapis alba cv. Ludique were analysed by reversed phase high-performance liquid chromatography-diode array detection-mass spectrometry. The effect of the glucosinolate–myrosinase system on in vitro mycelial growth of Phytophthora cinnamomi Rands and Pythium spiculum B. Paul was assessed. Likewise, sinigrin and sinalbin monohydrate commercial standards were also tested. The extracts from B. carinata, which contained 159 mmol/g plant DW equivalent (85% sinigrin, 5% gluconapin, and 3% glucotropaeolin), were the most effective against Phytophthora and Pythium isolates used in this study. However, the extract from S. alba, which contained 1 180 mmol/g (100% sinalbin), did not inhibit the mycelial growth of the isolates tested. The use of the glucosinolate-myrosinase system provides important additional information to advance in the implementation of field application of brassicaceous amendments for the control of soil-borne pathogens.


Antioxidants ◽  
2019 ◽  
Vol 8 (4) ◽  
pp. 102 ◽  
Author(s):  
Emanuela Monteiro Coelho ◽  
Marcelo Eduardo Alves Olinda de Souza ◽  
Luiz Claudio Corrêa ◽  
Arão Cardoso Viana ◽  
Luciana Cavalcanti de Azevêdo ◽  
...  

The present work had the objective of producing liqueurs from mango peels (varieties “Haden” and “Tommy Atkins”) by processes of alcoholic maceration and maceration with pectinase, as well as to evaluate bioactive compounds by reversed-phase high-performance liquid chromatography coupled to diode array detection and fluorescence-detection (RP-HPLC/DAD/FD) and in vitro antioxidant activity (AOX), for by-product potential reuse. Alcoholic maceration in wine ethanol (65% v/v) produced liqueurs with higher phytochemical and AOX content. Maceration with pectinase resulted in liqueurs with higher quercetin-3-O-glucopyranoside content. In relation to mango varieties, Haden liqueurs presented higher bioactive content than Tommy Atkins liqueurs. The liqueurs presented high antioxidant activity. The main bioactive compounds found were flavanols (epicatechin-gallate, epigallocatechin-gallate), flavonols (quercetin-3-O-glucopyranoside and rutin), and phenolic acids (gallic acid, o-coumaric acid, and syringic acid). The present study showed that the production of liqueur enabled the recovering of an important part of the bioactive content of mango peels, suggesting an alternative for the recovery of antioxidant substances from this by-product.


Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3235
Author(s):  
Min Zuo ◽  
Xiao-xiao Liu ◽  
Di Liu ◽  
Hang-yun Zhao ◽  
Lu-lu Xuan ◽  
...  

Semen Allii Fistulosi (PSAF) is the seed of Allium fistulosum L. of the Liliaceae family. The purpose of this study was to extract, characterize, and evaluate the antioxidant activity in vitro of proteins. Using single factor and orthogonal design, the optimum conditions of extraction were determined to be as follows: extraction time 150 min, pH 8.5, temperature 60 °C, and ratio (v/w, mL/g) of extraction solvent to raw material 35. The isoelectric point of the pH was determined to be about 4.4 and 10.2, by measuring the protein content of PSAF solutions at different pH values. The amino acid composition of PSAF was determined by high performance liquid chromatography (HPLC), and the results suggested that the species of amino acids contained in the PSAF was complete. Sodium dodecyl sulphate polyacrylamide gel electrophoresis (SDS–PAGE) analysis showed the molecular weight was mainly between 40 and 55 kDa, and Fourier-transform infrared spectroscopy (FTIR) characterized prevalent protein absorption peaks. PSAF exhibited potent scavenging activities against DPPH assays, via targeting of hydroxyl and superoxide radicals, while chelating Fe2+ activity and demonstrating weak reducing power. This work revealed that PSAF possessed potential antioxidant activity in vitro, suggesting potential for use of PSAF as a natural antioxidant.


Proceedings ◽  
2019 ◽  
Vol 41 (1) ◽  
pp. 85
Author(s):  
Silvana Rodriguez ◽  
Rosa Ana Sueiro ◽  
Ana Paula Murray ◽  
José Manuel Leiro

The essential oils (EOs) from the leaves of Schinus areira and one of its components, globulol, were studied for their antioxidant, antimutagenic and antipromutagenic activities. The chemical composition of the EOs obtained using hydrodistillation was determined using gas chromatography-mass spectrometry (GC-MS), and fractionated using reversed phase high performance liquid chromatography (RP-HPLC). The active compound (16.61%) isolated was identified by comparison of its 1H and 13C NMR spectroscopy with those reported in the literature. The antioxidant activity of the EOs and globulol were determined using two methods: crocin bleaching inhibition (Trolox Equivalent Value, TEV Krel = 1.16 ± 0.11 vs. 1.24 ± 0.22) and scavenging of the DPPH radical (IC50 = 38.75 ± 2.5 μg/mL vs. 5.60 ± 0.9 μg/mL). The antimutagenic and antipromutagenic activities were evaluated in vitro and ex vivo, using the Ames assay with five strains of Salmonella typhimurium with and without exogenous metabolic activation (rat liver fraction S9), against different mutagens. The result determined that globulol and EOs of S. areira at the applied doses do not exhibit any mutagenic effect and showed the highest antioxidant activity.


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