scholarly journals Development of Novel Oral Formulations of Disulfide Antioxidants Based on Porous Silica for Controlled Release of the Drugs

Materials ◽  
2021 ◽  
Vol 14 (4) ◽  
pp. 963
Author(s):  
Ekaterina S. Dolinina ◽  
Elena V. Parfenyuk

Powerful antioxidant α-lipoic acid (LA) exhibits limited therapeutic efficiency due to its pharmacokinetic properties. Therefore, the purpose of this work was to evaluate the ability of silica-based composites of LA as well as its amide (lipoamide, LM), as new oral drug formulations, to control their release and maintain their therapeutic concentration and antioxidant activity in the body over a long time. The composites synthesized at different sol–gel synthesis pH and based on silica matrixes with various surface chemistry were investigated. The release behavior of the composites in media mimicking pH of digestive fluids (pH 1.6, 6.8, and 7.4) was revealed. The effects of chemical structure of the antioxidants, synthesis pH, surface chemistry of the silica matrixes in the composites as well as the pH of release medium on kinetic parameters of the drug release and mechanisms of the process were discussed. The comparative analysis of the obtained data allowed the determination of the most promising composites. Using these composites, modeling of the release process of the antioxidants in accordance with transit conditions of the drugs in stomach, proximal, and distal parts of small intestine and colon was carried out. The composites exhibited the release close to the zero order kinetics and maintained the therapeutic concentration of the drugs and antioxidant effect in all parts of the intestine for up to 24 h. The obtained results showed that encapsulation of LA and LM in the silica matrixes is a promising way to improve their bioavailability and antioxidant activity.

Author(s):  
Khvorova L.S. ◽  
Byzov V.A.

The article is devoted to the creation of a carbohydrate product with rosehip extract in the form of sweets (glucose Fudge) with a therapeutic and preventive effect aimed at restoring the body of people exposed to intense physical and mental stress and the effects of damaging environmental factors. As carbohydrates in the recipe, simple carbohydrates (glucose) and complex carbohydrates in the form of starch molasses containing (maltose, tri - Tetra - sugars, dextrins) are used. Glucose in the formulation is the main energy ingredient, sweetener and structure-forming component that gives the product a solid consistency due to crystallization. The medicinal effect of the product is provided by rosehip extract. Numerous published studies have established its vitamin, immunostimulating and antioxidant activity, inhibition of uric acid formation and obesity, which are associated with flavonoids, other phenolic compounds, and vitamins. The list of medicinal properties of rosehip extract shows the feasibility of using it in additional nutrition of people in order to prevent diseases. For the formulation of our sweets, the extraction of crushed rosehip fruits was carried out three times with hot water at a temperature of 65-700C, followed by concentration of the extract under vacuum to 25-30% SV. The resulting extract-concentrate was introduced into the formulation in a dosage of 5.5% SV per 100 g of SV glucose Fudge, which provided the necessary dosage for the product when used from 3 (for children) to 10 sweets a day (for adults) for the prevention of colds.


2017 ◽  
Vol 59 (1) ◽  
pp. 81-85
Author(s):  
Jianjun Zhang ◽  
Hao Zeng ◽  
Chun Liu ◽  
Chao Li ◽  
Sude Ma ◽  
...  

Planta Medica ◽  
2021 ◽  
Author(s):  
Sandra Alves de Sousa Garcia ◽  
Priscila Bianca Rodrigues da Rocha ◽  
Bruno dos Santos Souza ◽  
Andressa Tuane Santana Paz ◽  
Ana Luiza Caetano Negris ◽  
...  

AbstractPunicalagin, the principal ellagitannin of Lafoensia pacari leaves, has proven antioxidant activity, and standardized extracts of L. pacari can be topically used for skin aging management. We hypothesized that Pluronic nanomicelles or vesicles could solubilize sufficiently large amounts of the standardized extracts of L. pacari and provide chemical stability to punicalagin. The standardized extracts of L. pacari were obtained with an optimized extraction procedure, and the antioxidant activity was characterized. Formulations containing Pluronic at 25% and 35% were obtained with or without Span 80. They were characterized by average diameter, polydispersity index, punicalagin content, physicochemical stability, and rheology. A release and skin permeation study was carried out in vertical diffusion cells. The extraction procedure allowed quantifying high punicalagin content (i.e., 141.61 ± 3.87 mg/g). The standardized extracts of L. pacari showed antioxidant activity for all evaluated methods. Pluronic at 25 and Pluronic at 35 with standardized extracts of L. pacari showed an average diameter of about 25 nm. The addition of Span 80 significantly increased the mean diameter by 15-fold (p < 0.05), indicating the spontaneous formation of vesicles. Pluronic formulations significantly protected punicalagin from chemical degradation (p < 0.05). Pluronic at 25 formulations presented as free-flowing liquid-like systems, while Pluronic at 35 resulted in an increase of about 44-fold in |ƞ*|. The addition of Span 80 significantly reduced the Pluronic sol-gel transition temperature (p < 0.05), indicating the formation of vesicles. Formulations with Span 80 significantly enhanced punicalagin skin permeation compared to formulations without Span 80 (p < 0.05). Formulations with Span 80 were demonstrated to be the most promising formulations, as they allowed significant permeation of punicalagin (about 80 to 315 µg/cm2), which has been shown to have antioxidant activity.


Coatings ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 420
Author(s):  
Giuseppina Raffaini

TiO2 is widely used in biomaterial implants. The topography, chemical and structural properties of titania surfaces are an important aspect to study. The size of TiO2 nanoparticles synthetized by sol–gel method can influence the responses in the biological environment, and by using appropriate heat treatments different contents of different polymorphs can be formed. Protein adsorption is a crucial step for the biological responses, involving, in particular, albumin, the most abundant blood protein. In this theoretical work, using molecular mechanics and molecular dynamics methods, the adsorption process of an albumin subdomain is reported both onto specific different crystallographic faces of TiO2 anatase and also on its ideal three-dimensional nanosized crystal, using the simulation protocol proposed in my previous theoretical studies about the adsorption process on hydrophobic ordered graphene-like or hydrophilic amorphous polymeric surfaces. The different surface chemistry of anatase crystalline faces and the nanocrystal topography influence the adsorption process, in particular the interaction strength and protein fragment conformation, then its biological activity. This theoretical study can be a useful tool to better understand how the surface chemistry, crystal structure, size and topography play a key role in protein adsorption process onto anatase surface so widely used as biomaterial.


Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1487
Author(s):  
Joanna Klepacka ◽  
Elżbieta Tońska ◽  
Ryszard Rafałowski ◽  
Marta Czarnowska-Kujawska ◽  
Barbara Opara

Due to the different levels of bioactive compounds in tea reported in the literature, the aim of this study was to determine whether commercially available leaf teas could be an important source of phenolics and selected minerals (copper, manganese, iron, zinc, magnesium, calcium, sodium, potassium) and if the differences in the content of these components between various types of tea are significant. It was found that both the amount of these compounds in tea and the antioxidant activity of tea infusions were largely determined by the origin of tea leaves as well as the processing method, which can modify the content of the studied components up to several hundred-fold. The group of green teas was the best source of phenolic compounds (110.73 mg/100 mL) and magnesium (1885 µg/100 mL) and was also characterised by the highest antioxidant activity (59.02%). This type of tea is a great contributor to the daily intake of the studied components. The average consumption of green tea infusions, assumed to be 3–4 cups (1 L) a day, provides the body with health-promoting polyphenol levels significantly exceeding the recommended daily dose. Moreover, drinking one litre of an unfermented tea infusion provides more than three times the recommended daily intake of manganese. Tea infusions can be a fairly adequate, but only a supplementary, source of potassium, zinc, magnesium, and copper in the diet. Moreover, it could be concluded that the antioxidant activity of all the analysed types of tea infusions results not only from the high content of phenolic compounds and manganese but is also related to the presence of magnesium and potassium.


Biomolecules ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 79
Author(s):  
Svetlana N. Morozkina ◽  
Thi Hong Nhung Vu ◽  
Yuliya E. Generalova ◽  
Petr P. Snetkov ◽  
Mayya V. Uspenskaya

For a long time, the pharmaceutical industry focused on natural biologically active molecules due to their unique properties, availability and significantly less side-effects. Mangiferin is a naturally occurring C-glucosylxantone that has substantial potential for the treatment of various diseases thanks to its numerous biological activities. Many research studies have proven that mangiferin possesses antioxidant, anti-infection, anti-cancer, anti-diabetic, cardiovascular, neuroprotective properties and it also increases immunity. It is especially important that it has no toxicity. However, mangiferin is not being currently applied to clinical use because its oral bioavailability as well as its absorption in the body are too low. To improve the solubility, enhance the biological action and bioavailability, mangiferin integrated polymer systems have been developed. In this paper, we review molecular mechanisms of anti-cancer action as well as a number of designed polymer-mangiferin systems. Taking together, mangiferin is a very promising anti-cancer molecule with excellent properties and the absence of toxicity.


1998 ◽  
Vol 519 ◽  
Author(s):  
L. Bergogne ◽  
S. Fennouh ◽  
J. Livage ◽  
C. Roux

AbstractBioencapsulation in sol-gel materials has been widely studied during the past decade. Trapped species appear to retain their bioactivity in the porous silica matrix. Small analytes can diffuse through the pores allowing bioreactions to be performed in-situ, inside the sol-gel glass. A wide range of biomolecules and micro-organisms have been encapsulated. The catalytic activity of enzymes is used for the realization of biosensors or bioreactors. Antibody-antigen recognition has been shown to be feasible within sol-gel matrices. Trapped antibodies bind specifically the corresponding haptens and can be used for the detection of traces of chemicals. Even whole cells are now encapsulated without any alteration of their cellular organization. They can be used for the production of chemicals or as antigens for immunoassays.


1894 ◽  
Vol 54 (326-330) ◽  
pp. 53-57 ◽  

For a long time I have adopted a process for separating the glycogen of the liver consisting in boiling with potash, pouring into alcohol, and collecting the precipitate. For the purpose of estimation, the precipitated glycogen was converted by means of sulphuric acid into glucose, the determination of which gave the information required. I afterwards applied the process to blood, and the various organs and tissues of the body, with the result that a more or less notable amount of cupric oxide reducing product was obtained, which I at the time looked upon as taking origin, as in the case of the liver, from glycogen.


2000 ◽  
Vol 612 ◽  
Author(s):  
Sylvie Acosta ◽  
André Ayral ◽  
Christian Guizard ◽  
Charles Lecornec ◽  
Gérard Passemard ◽  
...  

AbstractPorous silica exhibits attractive dielectric properties, which make it a potential candidate for use as insulator into interconnect structures. A new way of preparation of highly porous silica layers by the sol-gel route was investigated and is presented. The synthesis strategy was based on the use of common and low toxicity reagents and on the development of a simple process without gaseous ammonia post-treatment or supercritical drying step. Defect free layers were deposited by spin coating on 200 mm silicon wafers and characterized. Thin layers with a total porosity larger than 70% and an average pore size of 5 nm were produced. The dielectric constant measured under nitrogen flow on these highly porous layers is equal to ∼ 2.5, which can be compared to the value calculated from the measured porosity, ∼ 1.9. This difference is explained by the presence of water adsorbed on the hydrophilic surface of the unmodified silica.


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