scholarly journals Control of the Transdermal Delivery Process of Active Substances of the Phytocomplex during Phonophoresis in Model Experiments

2019 ◽  
Vol 7 (13) ◽  
pp. 2079-2083
Author(s):  
Liudmila Ivanovna Babaskina ◽  
Tatiana Mikhailovna Litvinova ◽  
Dmitrii Vladimirovich Babaskin ◽  
Olga Valerevna Krylova

BACKGROUND: The scientific substantiation for the selection of therapeutically significant dosage of phytocomplex in the dosage form for phonophoresis, control over the delivery of active substances into the body, and what affects this process require the study of the kinetics of phytocomplex flavonoids delivery during phonophoresis. AIM: The aim was to study the possibilities of controlling the process of transdermal delivery of phytocomplex active substances (flavonoids) during phonophoresis in vitro model experiments. METHODS: Working compositions with different concentrations of phytocomplex for phonophoresis were used. The content of flavonoids in the compositions was determined using the spectrophotometric method and was calculated equivalent to quercetin, the flavonoid prevailing in the phytocomplex. The study of the kinetics of flavonoids delivery from working compositions was carried out using Franz diffusion cells and Carbosyl-P membranes. The authors determined the main parameters of the process and established the dependence of the delivery rate of flavonoids on their initial concentration in the working composition. The authors studied the effect of dimethyl sulfoxide and the base-forming substances of the working composition on the kinetics of phytocomplex flavonoid delivery during phonophoresis. RESULTS: The authors recorded an increase in the rate of delivery of the active substances from working compositions containing dimethyl sulfoxide into the model medium by almost 1.5-2 times during the first ten minutes of the experiment (approximate duration of the phonophoresis procedure). The authors proposed technological techniques for improvement of the phonophoresis method for the phytocomplex. The possibilities of control over the process of transdermal delivery of the phytocomplex active ingredients during phonophoresis in vitro model experiments were shown. CONCLUSION: The obtained results provide information for further pharmacological studies of the nature and mechanism of the effect of phytocomplex flavonoids during phonophoresis in the rehabilitation of patients with osteoarthrosis.

2021 ◽  
Vol 25 (3) ◽  
pp. 389-393
Author(s):  
O. P. Maidebura ◽  
V. V. Hnatyuk ◽  
A. S. Romaniv

Annotation. The use of nanotechnology in the medical, food, pharmaceutical, biotechnology industries today is an important scientific progress and valuable human heritage. Nanoemulsion technology is an ideal method for the manufacture of encapsulating systems for functional compounds, as it prevents their biotechnological biodegradation and improves their functional availability in the cells of the body. The aim of the article is a scientific-theoretical and practical review of the nutritional and valeological properties of nanoemulsions, their use for encapsulation of various nutraceuticals, namely fat-soluble vitamin D. The in vitro experiment was performed using Franz diffusion cells to study the release of bioactive compounds from nanocarriers. The cytotoxicity of nanoemulsions was investigated by analyzing the proliferation of thiazolyl blue tetrazolium bromide (TTB) cells and nasal epithelial cells as an “in vitro” model. The article provides to characterize the nutritional and valeological properties of nanoemulsions and to experimentally investigate hydrogels based on nanoemulsions as biocarriers of vitaminized compounds. During the study, low- and high-energy nanoemulsions were created, which were used for encapsulation of vitamin D3 and biologically active supplement - curcumin. Loaded nanoemulsions are added to homopolymer and copolymer hydrogels based on polysaccharides and their combinations. Both nanoemulsions and hydrogels are structurally characterized to evaluate the effect of the composition on the emulsification process by their properties. The cytotoxic effect of nanoemulsions "in vitro" on the epithelium of nasal cells, which had a positive therapeutic effect, was studied. In the future, further exploration and research will investigate the use of nanoemulsions as biocarriers for other vitamins and bioactive substances.


Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1507 ◽  
Author(s):  
Sylwia Borowska ◽  
Michał Tomczyk ◽  
Jakub W. Strawa ◽  
Małgorzata M. Brzóska

Previously, we have revealed that prolonged administration of a polyphenol-rich 0.1% extract from the berries of Aronia melanocarpa L. (chokeberries) alone and under chronic exposure to cadmium influences the body status of zinc (Zn) and copper (Cu). The aim of this study was to evaluate, in an in vitro model, the chelating properties of the extract (0.05% and 0.1%) and its main polyphenolic ingredients (cyanidin 3-O-β-galactoside, chlorogenic acid, neochlorogenic acid, (+)-catechin, (−)-epicatechin, quercetin, and kaempferol) regarding divalent ions of Zn (Zn2+) and Cu (Cu2+) at pH reflecting physiological conditions at the gastrointestinal tract such as 2 (empty stomach), 5.5 (full stomach), and 8 (duodenum). The study has revealed that the extract from Aronia berries, as well as cyanidin 3-O-β-galactoside and quercetin, can bind Zn2+ and Cu2+, but only at pH 5.5. Moreover, kaempferol was able to chelate Zn2+ at pH 5.5; however, this ability was weaker than those of cyanidin 3-O-β-galactoside and quercetin. The ability of the chokeberry extract to chelate Zn2+ and Cu2+ may be explained, at least partially, by the presence of polyphenols such as anthocyanin derivatives of cyanidin and quercetin. The findings seem to suggest that Aronia products, used as supplements of a diet, should be consumed before meals, and particular attention should be paid to adequate intake of Zn and Cu under prolonged consumption of these products to avoid deficiency of both bioelements in the body due to their complexation by chokeberry ingredients in the lumen of the gastrointestinal tract.


Molecules ◽  
2011 ◽  
Vol 16 (3) ◽  
pp. 2658-2671 ◽  
Author(s):  
Bojan D. Markovic ◽  
Vladimir D. Dobricic ◽  
Sote M. Vladimirov ◽  
Olivera A. Cudina ◽  
Vladimir M. Savic ◽  
...  

1983 ◽  
Vol 96 (5) ◽  
pp. 1241-1247 ◽  
Author(s):  
L C Milks ◽  
M J Brontoli ◽  
E B Cramer

Although polymorphonuclear leukocytes (PMN's) can migrate through every epithelium in the body regardless of its permeability, very little is known about the effect of epithelial permeability on PMN migration and the effect of emigrating PMN's on the permeability of the epithelium. In an in vitro model system of transepithelial migration, human PMN's were stimulated by 0.1 micrometer fMet-Leu-Phe to traverse confluent, polarized canine kidney epithelial monolayers of varying permeabilities. Epithelial permeability was determined by both conductance measurement and horseradish peroxidase (HRP) tracer studies. As epithelial permeability increased, the number of PMN invasion sites as well as the number of PMN's that traversed the monolayer increased. The effect of PMN migration on epithelial permeability was examined using the ultrastructural tracers HRP and lanthanum nitrate. PMN's traversing the monolayer made close cell-to-cell contacts with other invading PMNs and with adjacent epithelial cells. These close contacts appeared to prevent leakage of tracer across invasion sites. Following PMN emigration, epithelial junctional membranes reapproximated and were impermeable to the tracers. These results indicated that, in the absence of serum and connective tissue factors, (a) the number of PMN invasion sites and the number of PMN's that traversed an epithelium were a function of the conductance of the epithelium and (b) PMN's in the process of transepithelial migration maintained close cell-cell contacts and prevented the leakage of particles (greater than 5 nm in diameter) across the invasion site.


1987 ◽  
Vol 110 ◽  
Author(s):  
Raymond Connolly ◽  
Norman Shoenfeld ◽  
Karen Ramberg ◽  
Allan D. Callow

AbstractAn in vitro model for measuring platelet reactivity to a variety of biomaterial candidates for vascular grafts is described. A model consisting of a standard area of test material exposed to freshly labeled In platelets in plasma was evaluated. The platelets were isolated from ACD anticoagulated blood and resuspended in ACD plasma. It has been previously demonstrated that platelets so treated circulate in the body and will deposit on biomaterials exposed to the blood in vivo. The in vitro test consisted of an incubation of the platelets and materials at 37°C for one hour. At the end of the incubation, the platelet rich plasma was removed and the materials washed and removed for gamma counting. Platelet reactivity was normalized as a percentage of the counts on the material to counts in an aliquot of the platelet-plasma incubation media. The maximum uptake of platelets occurred within one hour. Platelets from three species, human, baboon, and dog were tested. Platelet uptake by Dacron and PTFE were in the range of 30–40% and 1–5% respectively. This is in accord with the known reactivity of these two vascular graft materials in vivo.A second series of studies were conducted with physically and pharmacologically inactivated platelets and inert particles. Those studies suggest that the initial results do not represent a biologic event but may reflect the porosity of the materials. This emphasizes the necessity of adequately defining an in vitro model against known in vivo activity.


2020 ◽  
Author(s):  
A.N. Goryachev ◽  
S.A. Kalantarov ◽  
A.G. Severova ◽  
A.S. Goryacheva

SummaryData on potential effectiveness and prospects of treatment of new coronavirus infection of COVID-19 caused by virus SARS-CoV-2 with the help of antisense oligonucleotides acting against RNA of virus on an in vitro model are given. The ability of antisense oligonucleotides to suppress viral replication in diseases caused by coronaviruses using the example of SARS and MERS is shown. The identity of the initial regulatory section of RNA of various coronaviruses was found within 50 - 100 nucleotides from the 5’-end, which allows using antisense suppression of this RNA fragment. A new RNA fragment of the virus present in all samples of coronovirus SARS-CoV-2 has been identified, the suppression of which with the help of an antisense oligonucleotide can be effective in the treatment of COVID-19. The study of the synthesized antisense oligonucleotide 5’ - AGCCGAGTGACAGCC ACACAG, complementary to the selected virus RNA sequence, was carried out. The low toxicity of the preparations of this group in the cell culture study and the ability to reduce viral load at high doses according to real time-PCR data are shown. The cytopathogenic dose exceeds 2 mg / ml. At a dosage of 1 mg / ml, viral replication is reduced by 5-13 times. Conclusions are made about the prospects of this direction and the feasibility of using the inhalation way of drug administration into the body.


1997 ◽  
Vol 82 (10) ◽  
pp. 3271-3277
Author(s):  
Rekha Bajoria ◽  
Nicholas M. Fisk ◽  
Soli F. Contractor

Abstract Drugs that cross the placenta sparingly are currently given directly to the fetus by invasive procedures. We investigated whether anionic small unilamellar (SUV) liposomes of different lipid compositions enhanced the transfer and uptake of T4 in an in vitro model of perfused human term placenta. T4-encapsulated anionic liposomes were prepared using lecithin (F-SUV) or distearoyl phosphatidylcholine (S-SUV) with cholesterol and dicetylcholine. The size distribution, encapsulation efficiency, and stability were determined in blood-based media. The transfer kinetics of free and liposomally encapsulated T4 were studied in a dually perfused isolated lobule of human term placenta, with creatinine and liposomal carboxyfluorescein as marker substances. Concentrations of T4 and rT3 were measured by RIA. T4 crossed the placenta sparingly (1.9 ± 0.5%) because it was metabolized to rT3 (9.2 ± 1.3%). Transplacental transfer of T4 was significantly increased by F-SUV (15.8 ± 2.1%; P < 0.001) and S-SUV liposomes (7.1 ± 1.2%; P < 0.001), with a concomitant decrease in fetal rT3 levels (P < 0.001). Placental uptake of F-SUV (13.5 ± 2.0%; P < 0.001) was greater than that of S-SUV liposomes (6.7 ± 0.8%; P < 0.001). Our data suggest that anionic liposomes increase transplacental transfer of T4. If confirmed in vivo, liposomes may provide an alternative noninvasive method of drug delivery to the fetus.


1998 ◽  
Vol 56 (1-3) ◽  
pp. 41-51 ◽  
Author(s):  
Regine Peschka ◽  
Cathi Dennehy ◽  
Francis C Szoka Jr

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