Microemulsions based on polyglycerol polyricinoleate as drug delivery systems

2020 ◽  
pp. 24-33
Author(s):  
Natalya Sedyakina ◽  
Nataliya Feldman ◽  
Sergey Lutsenko
Keyword(s):  
Methylene Blue ◽  
Small Intestine ◽  
Active Substance ◽  
Tween 80 ◽  
Water Soluble ◽  
Biologically Active ◽  
Reverse Microemulsion ◽  
Biologically Active Substance ◽  
Paraffin Oil ◽  
System Water

The aim of the work is to develop composition of reverse microemulsion stabilized by the surfactant from a number of polyglycerol polyricinoleates for encapsulating water-soluble biologically active substance (BAS) and studying the kinetics of its release into the medium simulating the medium of the small intestine. Materials and methods. Possible stable (equilibrium) phases of the reverse microemulsion in the pseudoternary system water–PG-3-PR/Tween 80–paraffin oil were determined by titration of surfactant/co-surfactant mixtures–oil in water with hydrophilic-lipophilic balance (HLB) values of the surfactant mixture ranging from 4.0 to 7.0. Stability of a number of compositions during storage at 20 °C for 6 months was studied. Based on the obtained data, a composition was selected for encapsulating methylene blue (MS) dye as a model of a water-soluble biologically active substance. Microemulsion was obtained by mixing paraffin oil and surfactants with selected mass ratio followed by the addition of an aqueous phase. Reverse microemulsion morphology was evaluated with transmission electron microscopy (TEM). To evaluate the in vitro drug release rate, aliquots of an aqueous dye solution (control sample) and MB-containing microemulsions were placed in dialysis bags and immersed in 0.01 M phosphate-buffered saline (PBS) (pH 7.4) in a thermostatic shaking incubator at 180 rpm and 37 °C. Aliquots of the release medium were selected at predetermined time intervals and the concentration of MB dye was determined using a UV spectrophotometer at 660 nm. Results. Composition containing 13.5 wt% paraffin oil, 76.5 wt% mixture of PG3-PR/Tween 80 (HLB 5.5) and 10 wt% water was chosen to encapsulate the biologically active agents. Number average droplet diameter in the dispersed phase of the obtained microemulsion was 55 nm. Dye-loaded microemulsion sample showed a prolonged release of biologically active substances within 48 hours of the experiment (15.2%) and low initial release rate. Conclusion. Possible stable phases of reverse microemulsion in the pseudoternary system water–PG-3-PR/Twin 80–paraffin oil were determined in the course of the work and optimal microemulsion composition for encapsulating medicinal substances was found. It was shown that the resulting microemulsion system provides a sustained release of methylene blue as a model of a water-soluble biologically active substance in a medium simulating medium of the small intestine. The obtained data allow to consider this composition as a potential nanoscale system for the sustained delivery of water-soluble drugs.

scholarly journals Development of UV-spectrophotometry Method of the Quantitative Determination of a New Substance Quinazoline-4(3h)-on Derivate

2020 ◽  
Vol 9 (1) ◽  
pp. 30-34
Author(s):  
E. S. Mishchenko ◽  
A. D. Lazaryan ◽  
T. T. Lihota
Keyword(s):  
Quantitative Determination ◽  
Active Substance ◽  
Research Work ◽  
Biologically Active ◽  
Uv Spectrophotometry ◽  
Pharmacological Effects ◽  
Specific Absorption ◽  
Biologically Active Substance ◽  
Effective Remedy

Introduction. The aim idea of this research article is a development of the quantitative determination of a biologically active substance quinazolin4(3H)-on derivate with laboratory cypher «VMA-10-182, by UV-spectrophotometry with followed validation. The substance is an effective remedy that combines several pharmacological effects, like an antidepressant, anxiolytic and nootropic. As a result of preclinical trials, the research compound has proven to be an effective remedy in the fight and prevention of acute cerebrovascular accident (stroke). The substance realized pharmacological effects by stimulating the production of nitric oxide by the endothelial cells of the brain. As aresult of stimulating is a vasodilation of the vessels and improvement of blood flow in the ischemic part of the vessels occur. Therefore, for introducing the biologically active substance into medical practice we need to develop ways to control the quality of substance.Aim. The objective of this research work is to develop a method of the quantitative determination of a biologically active substance, derivative quinazolin-4(3H)-on (laboratory sypher – VMA-10-18), by method of UV spectrophotometry. The results of the research work were validated.Materials and methods. In this research we used a substance VMA-10-18 wich was previously purified from the initial and intermediate products of the synthesis. This substance is a white crystalline powder, odorless, hygroscopic.Results and discussion. The quantitative content of the active substance derived quinazolin-4(3H)-on has been determined. The specific absorption rate was calculated, followed by statistical processing of the results. The validation was carried out according to the «Specificity», «Linearity», «Accuracy», «Repeatability». The results indicate the effectiveness of the developed methodology and experimental reproducibility.Conclusion. Researches of physicochemical properties show al us use 95 % ethanol as a solvent. As a result we developed a method for the quantitative determination of the substance which can be proposed for inclusion in the normative documents. The quantitative determination of the active substance in the test substance was established, and the specific absorption index was calculated. All information are statistically processed and meet the requirements of regulatory documentation.

scholarly journals Immunohistochemical and morphometric study of hepatocyte proliferation in 18-days old infant rats after a mechanical trauma being administered «Suvar» biologically active substance

2015 ◽  
Vol 96 (4) ◽  
pp. 554-557
Author(s):  
L P Romanova ◽  
I I Malyshev ◽  
O V Vorob’eva
Keyword(s):  
Active Substance ◽  
Proliferative Activity ◽  
Biologically Active ◽  
Hepatocyte Proliferation ◽  
Morphometric Study ◽  
Mechanical Trauma ◽  
Ki 67 ◽  
Control Infant ◽  
Biologically Active Substance ◽  
Infant Rats

Aim. Morphometric and immunohistochemical study of hepatocyte proliferative activity in 18-days-old infant rates after a mechanical trauma of the liver. Methods. After an artificial mechanical injury of the liver with a steel needle in 18-days old infant rats, a biologically active substance «Suvar» in a dose of 50 mg/kg (n=36) was administered to animals. After animals were withdrawn from the experiment, a morphometric study (where the number of mitoses of hepatocytes for every 7000 cells were calculated) and immunohistochemistry of liver tissue were performed. For the immunohistochemistry, two commercially available monoclonal antibodies kits (manufactured by «Santa Cruz») were used: (1) proliferative activity marker Ki-67; (2) apoptosis marker bcl-2. Immunohistochemistry was performed according to standard protocol. Thirty-six operated infant rats, in whom the biologically active substance was not administered, were analyzed as the controls. Results. The number of ki-67 positive hepatocytes in experimental animals on the 3rd, 5th,7th and the 9th day after the operation was significantly higher compared to controls. This was in accordance with the changes of the number of mitoses in hepatocytes, where the greatest number of mitoses was also registered on 3rd, 5th,7th and the 9th day. Both in experimental and in control infant rats, only single cells marked bcl-2 antibodies were found. The gained results support the opinion of the majority of the researchers that the liver regenerates mainly due to hepatocyte proliferation. Conclusion. Morphometric study and immunohistochemistry confirmed that biologically active substance «Suvar» stimulates hepatocyte proliferation of hepatic cells, allowing better healing of liver injury compared to control animals.

scholarly journals Ethological and biological features of the organism of the black-and-white bulls when using natural feed additives in the diets

2020 ◽  
Vol 17 ◽  
pp. 00237
Author(s):  
Oksana Krasnova ◽  
Ekaterina Hardina ◽  
Sergei Hramov ◽  
Michail Kudrin ◽  
Nina Konik
Keyword(s):  
Active Substance ◽  
Feed Additives ◽  
Biologically Active ◽  
Feed Additive ◽  
Biologically Active Substance ◽  
Black And White ◽  
Scientific Experiment ◽  
Biological Features ◽  
Livestock Feed ◽  
Meat Productivity

The authors studied the natural feed additive effect to the behaviour and biochemical blood composition of the black-and-white bulls. As results of the scientific experiment we came to the conclusion that using of the biologically active substance dihydroquercetin as a part of a natural feed additive in livestock feed for the metabolic processes intensity stimulation, the nutrient synthesis intensity and higher rates meat productivity formation.

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