CONTROL OF PHYSICO-CHEMICAL PROPERTIES OF A LIPID NANOCONTAINER FOR DELIVERY OF DRUGS WITH LOW BIOAVAILABILITY

2020 ◽  
pp. 153-154
Author(s):  
I. Yakimov ◽  
I. Le-Deygen ◽  
A. Skuredina ◽  
E. Kudryashova
Keyword(s):  
Targeted Delivery ◽  
Binding Sites ◽  
Chemical Properties ◽  
Anionic Phospholipid ◽  
Molecular Weights ◽  
Physico Chemical ◽  
Drug Incorporation ◽  
Mannose Derivatives ◽  
Derivatives Of ◽  
Selection Of

We have used two ways to control the physicochemical properties of liposomal nanocontainers for the delivery of fluoroquinolones: variation of the lipid composition of liposomes and selection of a functionalizing polymer based on chitosan mannose derivatives. The presence of anionic phospholipid cardiolipin in the liposome composition increases the loading efficiency by 5-20%. The mechanism of drug incorporation into membranes was studied, and the main binding sites were determined. The functionalization of the liposomal surface was carried out by chitosan mannose derivatives of various molecular weights, potentially providing targeted delivery to alveolar macrophages.

scholarly journals Synthesis and study of the properties of derivatives 4-phenyl-5-(1H-pyrrol-2-yl)-4H-1,2,4-triazole-3-thiols

2018 ◽  
pp. 59-66
Author(s):  
A. S. Gotsulya ◽  
D. P. Verba ◽  
O. I. Panasenko ◽  
Ye. G. Knysh
Keyword(s):  
Heterocyclic System ◽  
Chemical Properties ◽  
Physico Chemical ◽  
Methods Of Synthesis ◽  
Interesting Object ◽  
Physical And Chemical ◽  
Derivatives Of ◽  
Selection Of ◽  
Base Structure ◽  
And Chemical Properties

The successful use of drugs, derivatives of 1,2,4-triazole, creates the conditionsfor the production and investigation of properties of new derivatives of this heterocyclic system. The aim of this work was synthesis and study of physical and chemical properties of new derivatives of 1,2,4-triazole-3-thiol containing synthon of pyrrole. The object of the study was a 4-phenyl-5-(pyrrol-2-yl)-1,2,4-triazole-3-ylthio-R-carbothioamides. To achieve this goal it was necessary to solve following tasks: to conduct the selection of the optimum base structure to determine the most efficient way of chemical modification of the precursor of targeted synthesis, to carry out selection of necessary methods of synthesis, to investigate the physico-chemical properties and to set the structure of the obtained compounds. The synthesis of target products of the reaction was carried out using as starting material pyrrole, which with using the form non-catalytic form of reaction of the Fridel-Crafts was transformed into 2,2,2-trichloro-1-(pyrrol-2-yl), ethanol. The resulting material in the result of reaction of hydrazinolysis was converted into the pyrrol-2-carbohydrazide. The obtained intermediate product was used in the reaction of nucleophilic joining of phenylisothiocyanate with subsequent intramolecular alkaline heterocyclization. Synthesized thiol was used in the reaction of alkylation. The structure of the obtained substances are confirmed by using elemental analysis, 1H-NMR-spectroscopy, and their individuality – chromatographic methods of analysis. The resulting substances are an interesting object for further studies, especially biological activity.

scholarly journals Tryptic phosphopeptides from whole casein. II. Physicochemical properties related to the solubilization of calcium

1989 ◽  
Vol 56 (3) ◽  
pp. 335-341 ◽  
Author(s):  
Rafael Berrocal ◽  
Serge Chanton ◽  
Marcel A. Juillerat ◽  
Blaise Favillare ◽  
Jean-Claude Scherz ◽  
...  
Keyword(s):  
Binding Sites ◽  
Calcium Phosphates ◽  
Chemical Properties ◽  
Sodium Caseinate ◽  
Ph Values ◽  
Physico Chemical ◽  
Casein Phosphopeptides ◽  
Hydrolysis Of ◽  
Phosphate Solutions ◽  
Tryptic Hydrolysis

SummaryCasein phosphopeptides (GPP) were produced by tryptic hydrolysis of sodium caseinate and further purified by precipitation and chromatography on QAE-Sephadex A-25. Their physico-chemical properties were compared with the properties of an enzymically dephosphorylated equivalent preparation (DPP). Binding of Ca2+ to the peptides was measured using a Ca selective electrode and was found to increase with pH and to show 1/1 stoicheiometry Ca/Porg in CPP at pH 6·5 a.nd 7·6. Klotz plots indicated equivalent binding sites at these two pH values, but some heterogeneity was seen at pH 3·5. In contrast, DPP did not bind significant amounts of Ca2+.CPP effectively inhibited the formation of insoluble calcium phosphates at different Ca/P ratios. The effective CPP concentration was 10 mg/1 and complete stability of calcium phosphate solutions was obtained at about 100 mg/1. This stabilizing effect was dependent on the presence of organic P.

Combination of solid-state NMR and 1H NMR relaxometry for the study of intercalated saponite clays with the macrocyclic derivatives of Gd(iii) and Y(iii)

2020 ◽  
Vol 49 (20) ◽  
pp. 6566-6571 ◽  
Author(s):  
Daniela Lalli ◽  
Stefano Marchesi ◽  
Fabio Carniato ◽  
Chiara Bisio ◽  
Lorenzo Tei ◽  
...  
Keyword(s):  
Solid State ◽  
1H Nmr ◽  
Solid State Nmr ◽  
Chemical Properties ◽  
H Nmr ◽  
Nmr Relaxometry ◽  
Physico Chemical ◽  
Derivatives Of ◽  
1H Nmr Relaxometry ◽  
Synthetic Saponite

A combination of solid-state NMR and 1H-NMR relaxometric investigations has been employed to characterize the structure and physico-chemical properties of a novel synthetic saponite intercalated with Gd(iii) and Y(iii) chelates.

Working Fluids Used for Drilling Deep Boreholes

2014 ◽  
Vol 508 ◽  
pp. 150-155 ◽  
Author(s):  
Marian Šofranko ◽  
Erika Škvareková ◽  
Gabriel Wittenberger
Keyword(s):  
Chemical Composition ◽  
Drilling Fluid ◽  
Chemical Properties ◽  
Proper Function ◽  
Working Fluids ◽  
Physico Chemical ◽  
Geological Conditions ◽  
Deep Boreholes ◽  
Selection Of

Particularly important is the use of drilling fluid in carrying out drilling works to great depths and especially in difficult geological conditions. Proper function of the drilling fluid is governed by the selection of their physico-chemical properties. Drilling works of hydrogeological survey require circulation of borehole with such rinses, which at a minimum pollute water-bearing horizons and their chemical composition meets hygiene requirements.

Large molecular species of chorionic gonadotrophin from human placental tissues: biosynthesis and physico-chemical properties

1980 ◽  
Vol 94 (2) ◽  
pp. 259-267 ◽  
Author(s):  
Takeshi Maruo ◽  
Sheldon J. Segal ◽  
S. S. Koide
Keyword(s):  
Molecular Species ◽  
Sodium Dodecyl ◽  
Chemical Properties ◽  
First Trimester ◽  
Supernatant Fraction ◽  
Molecular Weights ◽  
Physico Chemical ◽  
Bovine Corpus Luteum ◽  
First Trimester Of Pregnancy ◽  
Α And Β Subunits

Abstract. Human placental tissues in the first trimester of pregnancy were maintained in organ culture and incubated with [3H]proline for 90 min at 37°C. The tissues were homogenized with a protease inhibitor in the buffered medium and separated into subcellular components. A large molecular protein which reacted with antiserum to hCG hCGα and hCGβ, and with the receptor membranes obtained from bovine corpus luteum, was detected in the microsomal component and post-microsomal supernatant fraction. This protein was purified by chromatography on Sephadex G-100, Sepharose-6B and DEAE-Sephadex A-50. The large molecular species of hCG contained high radioactivity and was immunoprecipitated with all three antisera. The purified large molecular hCG was analyzed by electrophoresis on sodium dodecyl sulphate (SDS) polyacrylamide gel. Its molecular weight was estimated to be 90000 daltons. When the large molecular hCG was treated with 8 m urea and mercaptoethanol in the presence of SDS, a major portion of the material dissociated into immunoreactive α and β subunits of rather high molecular weights compared to standard hCG subunits. Under similar conditions standard hCG dissociates completely into its subunits. The present results suggest that the large molecular species of hCG might be a complex composed of larger forms of α and β subunits. This complex might be an intermediary component in the biosynthetic pathway of hCG or a product of posttranslational modification.

scholarly journals Vegetation analysis, physico-chemical properties and economic potential of damar (Agathis dammara) in Mount Halimun Salak National Park,West Java, Indonesia

2020 ◽  
Vol 21 (3) ◽  
Author(s):  
Yelin Adalina ◽  
RENY SAWITRI
Keyword(s):  
National Park ◽  
Economic Status ◽  
Chemical Properties ◽  
Economic Potential ◽  
Vegetation Analysis ◽  
West Java ◽  
Physico Chemical ◽  
Important Value Index ◽  
Selection Of

Abstract. Adalina Y, Sawitri R. 2020. Vegetation analysis, physico-chemical properties and economic potential of damar (Agathis dammara) in Mount Halimun Salak National Park,West Java, Indonesia. Biodiversitas 21: 1122-1129. Analysing the potential of non-timber forest product (NTFP) plants in Mount Halimun Salak National Park (MHSNP) is one of the important aspects in supporting conservation and improving the economic status of communities around the forest. This study aims to determine the economic potential and benefits of damar plants (Agathis dammara) in MHSNP area of Kawah Ratu Resort, Sukabumi District, West Java, Indonesia along with analysis of damar plant forest and physico-chemical analysis of the copal/resin. The selection of research village was by purposive sampling and the selection of respondents was by random sampling. Forest vegetation in the Kawah Ratu Resort is entirely dominated by damar plants. The Important Value Index (IVI) of damar plant trees is 300% and the density is 582 trees/ha. The quality of copal from Kawah Ratu Resort meets SNI standards in parameters like ash content, soft point and melting point, while the saponification number is above SNI standard. Level of dung in copal chunks meet SNI standards and has better quality than copal in the form of powder. The present average income of farmers from resin tapping is Rp 624,000/person /month, which makes an average contribution of 63.08% to the total household income of farmers. But the actual economic potential of gum resin in Kawah Ratu Resort was estimated to be around Rp 596,920,000/month.

scholarly journals Synthesis, physico-chemical properties of 3-thio and 3-thio -4-amino derivatives of 1,2,4-triazole

2019 ◽  
pp. 28-44
Author(s):  
V. V. Parchenko
Keyword(s):  
Chemical Properties ◽  
Biological Properties ◽  
Modern Medicine ◽  
Toxic Substances ◽  
Triazole Derivatives ◽  
Synthetic Drugs ◽  
Physico Chemical ◽  
Methods Of Synthesis ◽  
Amino Derivatives ◽  
Derivatives Of

Modern medicine and pharmacy has at its disposal highly efficient synthetic drugs. Large extent of these drugs accounted for derivatives of 1,2,4-triazole. The purpose of the work was an attempt to summarize the literature in recent years related to the methods of synthesis and study of physico-chemical properties 3-thio- and 3-thio-4-amino derivatives of 1,2,4-triazole. Studies national scientists in recent years indicates prospects of the search in this direction, since this class of organic compounds is interest not only to scientists pharmaceutical, medical and veterinary field, but also among researchers of engineering, metallurgical and agricultural areas. 1,2,4-triazole derivatives are also widely used in practice for optical materials, photosensitizers are used as coloring agents, antioxidants, additives for fuels and oils, some of which are widely used as corrosion inhibitors for controlling various pests in agriculture. In addition, 1,2,4-triazole derivatives belong to the class low toxic or essentially non-toxic substances. The presence of a growing number of publications about methods of synthesis, reactions, physico-chemical and biological properties of 1,2,4-triazole, inspires scientists around the world search for perspective molecules of substituted 1,2,4-triazole. It should be noted that in spite of a sufficient amount of information about the derivatives of 1,2,4-triazole, some issues related to the generalization of data in the literature synthesis presented insufficient.

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