Solubility In Water
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2022 ◽  
Vol 23 (2) ◽  
pp. 724
Agata Gurba ◽  
Przemysław Taciak ◽  
Mariusz Sacharczuk ◽  
Izabela Młynarczuk-Biały ◽  
Magdalena Bujalska-Zadrożny ◽  

Cancer is one of the leading causes of morbidity and mortality worldwide. Colorectal cancer (CRC) is the third most frequently diagnosed cancer in men and the second in women. Standard patterns of antitumor therapy, including cisplatin, are ineffective due to their lack of specificity for tumor cells, development of drug resistance, and severe side effects. For this reason, new methods and strategies for CRC treatment are urgently needed. Current research includes novel platinum (Pt)- and other metal-based drugs such as gold (Au), silver (Ag), iridium (Ir), or ruthenium (Ru). Au(III) compounds are promising drug candidates for CRC treatment due to their structural similarity to Pt(II). Their advantage is their relatively good solubility in water, but their disadvantage is an unsatisfactory stability under physiological conditions. Due to these limitations, work is still underway to improve the formula of Au(III) complexes by combining with various types of ligands capable of stabilizing the Au(III) cation and preventing its reduction under physiological conditions. This review summarizes the achievements in the field of stable Au(III) complexes with potential cytotoxic activity restricted to cancer cells. Moreover, it has been shown that not nucleic acids but various protein structures such as thioredoxin reductase (TrxR) mediate the antitumor effects of Au derivatives. The state of the art of the in vivo studies so far conducted is also described.

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 445
Aikaterini Sakellaropoulou ◽  
Angeliki Siamidi ◽  
Marilena Vlachou

Melatonin (MLT) is involved in many functions of the human body, mainly in sleeping-related disorders. It also has anti-oxidant potential and has been proven very effective in the treatment of seasonal affective disorders (SAD), which afflict some people during short winter days. Melatonin has been implicated in a range of other conditions, including Parkinson’s disease, Alzheimer’s and other neurological conditions, and in certain cancers. Its poor solubility in water leads to an insufficient absorption that led scientists to investigate MLT inclusion in cyclodextrins (CDs), as inclusion of drugs in CDs is a way of increasing the solubility of many lipophilic moieties with poor water solubility. The aim of this review is to gather all the key findings on MLT/CD complexes. The literature appraisal concluded that MLT inclusion leads to a 1:1 complex with the majority of CDs and increases the solubility of the hormone. The interactions of MLT with CDs can be studied by a variety of techniques, such as NMR, FT-IR, XRD and DCS. More importantly, the in vivo experiments showed an increase in the uptake of MLT when included in a CD.

2021 ◽  
pp. 088532822110504
Faiza Sajjad ◽  
Yiping Han ◽  
Leilei Bao ◽  
Yijia Yan ◽  
Donal O shea ◽  

Photodynamic therapy (PDT) is a promising new treatment for cancer; however, the hydrophobic interactions and poor solubility in water of photosensitizers limit the use in clinic. Nanoparticles especially carbon dots have attracted the attention of the world’s scientists because of their unique properties such as good solubility and biocompatibility. In this paper, we integrated carbon dots with different porphyrins to improve the properties of porphyrins and evaluated their efficacy as PDT drugs. The spectroscopic characteristics of porphyrins nano-conjugates were studied. Singlet oxygen generation rate and the light- and dark-induced toxicity of the conjugates were studied. Our results showed that the covalent interaction between CDs and porphyrins has improved the biocompatibility. The synthesized conjugates also inherit the pH sensitivity of the carbon dots, while the conjugation also decreases the hemolysis ratio making them a promising candidate for PDT. The incorporation of carbon dots into porphyrins improved their biocompatibility by reducing toxicity.

2021 ◽  
Vol 5 (6) ◽  
pp. 2160-2175
Sérgio Dantas de Oliveira Júnior ◽  
Paula Romenya Gouvea dos Santos ◽  
Lorena Bentolila de Aguiar ◽  
Larissa Batista Brito do Nascimento ◽  
Jocélia Pinheiro Santos ◽  

The functional properties of biofilms can vary according to the biopolymer used as the raw material; thus, in the search for alternative sources for preparation of biodegradable films, fruits and vegetables have been used to extract compounds of interest with applications in the food industry. The objective of this work was to obtain and characterize bioactive films based on pectin extracted from the epicarps (skin) of the fruit. The genipap (Genipa americana), red pitaya (Hylocereus polyrhizus) and star fruit (Averrhoa carambola) were collected, washed, pulped and dried at 50 °C for 24 h, and their epicarps were ground and subjected to pectin extraction using the casting method. The films were characterized as to their visual appearance, moisture, pH, water solubility and antioxidant activity. The pectin-based films of G. americana and H. polyrhizus showed a yellowish color, while A. carambola was dark brown. The highest pectin yield (29%) and moisture content (13.9%) were obtained from the H. polyrhizus film, while A. carambola showed the highest solubility in water (98.6%) and had the highest pH (3.9). Additionally, the film based on A. carambola showed greater antioxidant potential against ABTS (30.5%) and DPPH (34%), as well as greater reducing power (0.262 absorbance at 750 nm) and content of total phenolic compounds (553 mg GAE/100 g), whereas H. polyrhizus had a higher percentage of chelating ability (27%). The physicochemical characteristics and bioactive properties exhibited make the film formulation a viable alternative for the food industry.

2021 ◽  
Vol 10 (4) ◽  
pp. 166-170
D. V. Zayats ◽  
O. V. Buyklinskaya ◽  
Ju. R. Fedotova ◽  
N. S. Felenko

Introduction. Selenopyran is an organic selenium compound with sharply hydrophobic properties. An increase in solubility in water (and as a consequence – and bioavailability) is possible due to the formation of inclusion complexes with cyclodextrins.Aim. The aim of this work was to study the effect of a gel containing a clathrate complex of selenopyran with β-cyclodextrin on the rate of wound healing on a model of a conditionally aseptic full-thickness planar wound in rats.Materials and methods. The object of the study was a gel containing a clathrate complex of selenopyran with β-cyclodextrin (the content of selenopyran in the gel was 0.1 %). A model of a full-thickness planar wound in sexually mature male rats was used. 20 individuals were divided into 2 groups – intact (without treatment) and experimental (received gel treatment). Efficacy was assessed by the change in wound area at 3, 5, 7, 9, 11 and 14 days after application of wound.Results and discussion. The results of the study showed that the relative area of the wounds in the treated animals by the 3rd day of the experiment was less than in the intact ones. On the fifth day of the experiment, the differences were statistically significant (57.49 ± 12.51 % in treated animals versus 85.27 ± 26.61 % in intact animals). By the 14th day of the experiment, there were practically no differences in the groups of animals.Conclusion. The results obtained indicate that when using a gel containing selenopyran in combination with β-cyclodextrin, it accelerates the transition from the inflammation phase to the proliferation phase. This is most likely due to the antioxidant properties of selenopyran. Considering the lower concentration of selenopyran in comparison with the therapeutic concentrations of other antioxidants (taurine, allantoin), it can be considered as a promising wound healing agent for further study.

2021 ◽  
Vol 10 (4) ◽  
pp. 46-53
I. D. Kasymov ◽  
A. V. Basevich

Introduction. The article presents the results of studying the technological properties of individual excipients widely used in the compositions of existing orally dispersed tablets (ODT) for subsequent planning a multifactorial experiment. Samples of excipients were analyzed according to such pharmacopoeial indicators as description, flowability, bulk density, compressibility, fractional composition, solubility in water.Aim. The aim of the work is to create a list and study the technological properties of candidate substances for the role of auxiliary substances in the composition being developed by the ODT.Materials and methods. The technological properties of excipient samples were studied according to the methods of the State Pharmacopoeia of the XIV edition using the flowability tester GTL (ERWEKA, Germany), the bulk density tester SVM 221 (ERWEKA, Germany), the tablet press PGR-10 (LabTools, Russia) and the tablet hardness tester TBH 125 TDP (ERWEKA, Germany).Results and discussion. As a result of the study, experimental data on the technological properties of excipient samples were collected, and the selected samples were compared according to pharmaceutical and technological indicators.Conclusion. In the course of the study, a list of auxiliary substances for the development of the composition of ODT was formed and studies of their technological properties were carried out. The obtained experimental data will allow to develop an optimal matrix of a multifactorial experiment for the development of the composition of ODT and justify the choice of excipients.

2021 ◽  
Fabrizio Freni ◽  
Vincenzo Napolitano ◽  
Silvia Mancini ◽  
Roberto Buscaglia

Abstract In recent years, carbon neutrality has emerged as an important social and political focus globally, where carbon sequestration plays a key role. The present work is aimed at introducing ASCAPE (Aquifer Storage CAPacity Evaluation tool), a fast and flexible tool useful in case of CO2 aquifer sequestration to preliminarily evaluate the required storage capacity as a function of the maximum allowable pressure increment. ASCAPE is based on the volumetric method included in SPE "Guidelines for Applications of the CO2 Storage Resources Management System" (SPE, 2020) for aquifer sequestration. The analytical formula was integrated to include additional physical phenomena as CO2 solubility in water, pressure control through water production, effect of gas pools connected to aquifer. The tool, implemented in Excel/VBA environment, allows to easily obtain a theoretical Pressure increment vs. Aquifer Volume curve useful to estimate the required aquifer volume to store a given quantity of CO2. ASCAPE results were validated comparing to a simplified 3D model simulated by a compositional commercial dynamic simulator. The validation showed a very good alignment with the 3D dynamic simulation results under several conditions. Many tests were performed with and without the CO2 solubility model, demonstrating that this phenomenon acts as pressure increment reducer. The original volumetric model can be therefore considered slightly conservative, since it neglects this physical contribution, which allowed to improve the reliability of the proposed analytical model. The proposed methodology is a general-purpose application being not related to a specified candidate and, therefore, it can be tailored on the specific scenario to be evaluated. ASCAPE was developed for preliminary screening of CO2 sequestration concepts in greenfield development areas, where the absence of brown or exhausted fields makes the storage in aquifer the only viable solution. Different aquifers were compared under certain assumptions of carbon to be stored with and without water production, allowing a preliminary evaluation that will be used to rank the concepts in terms of technical/economic feasibility.

Processes ◽  
2021 ◽  
Vol 9 (12) ◽  
pp. 2185
Daliana Minda ◽  
Alexandra Mioc ◽  
Christian Banciu ◽  
Codruța Soica ◽  
Roxana Racoviceanu ◽  

Mebendazole and flubendazole are antihelmintic drugs that have re-entered the research spotlight due to their exhibited anticancer effects, thus making them strong candidates as repurposed drugs. However, these benzimidazole derivatives exhibit poor solubility in water and various organic solvents, which limits their bioavailability. With the aim of obtaining an improved drug solubility and increased biological effect, mebendazole and flubendazole were complexed with 2-hydroxypropyl-β-cyclodextrin (HPBCD). The binary 1:1 conjugates were physicochemically evaluated by X-ray diffraction, thermal analysis, and FTIR spectroscopy, revealing the formation of physical mixtures. The increased aqueous solubility of the binary 1:1 conjugates vs. pure benzimidazole compounds was demonstrated by performing dissolution tests. The in vitro antiproliferative activity of mebendazole and flubendazole, as well as their combination with HPBCD, was tested on two cancer cell lines, human melanoma—A375 and pulmonary adenocarcinoma—A549 by the MTT assay. The cytotoxic activity manifested in a dose-dependent manner while the presence of HPBCD increased the antiproliferative activity against the targeted cells. Treatment of A375 and A549 cell lines with the binary conjugates induced a significant inhibition of mitochondrial respiration, as revealed by high-resolution respirometry studies. Molecular docking analysis showed that one of the mechanisms related to MEB and FLU cytotoxic activity may be due to the inhibition of MEK/ERK proteins.

2021 ◽  
Vol 37 (6) ◽  
pp. 533-542
Florencia Anabel Mesas ◽  
María Cecilia Terrile ◽  
María Ximena Silveyra ◽  
Adriana Zuñiga ◽  
María Susana Rodriguez ◽  

Chitosan has been considered an environmental-friendly polymer. However, its use in agriculture has not been extended yet due to its relatively low solubility in water. N-Methylene phosphonic chitosan (NMPC) is a water-soluble derivative prepared by adding a phosphonic group to chitosan. This study demonstrates that NMPC has a fungicidal effect on the phytopathogenic fungus Fusarium solani f. sp. eumartii (F. eumartii) judged by the inhibition of F. eumartti mycelial growth and spore germination. NMPC affected fungal membrane permeability, reactive oxygen species production, and cell death. Also, this chitosan-derivative exerted antifungal effects against two other phytopathogens, Botrytis cinerea, and Phytophthora infestans. NMPC did not affect tomato cell viability at the same doses applied to these phytopathogens to exert fungicide action. In addition to water solubility, the selective biological cytotoxicity of NMPC adds value in its application as an antimicrobial agent in agriculture.

Nanomaterials ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 3204
Anna A. Antsiferova ◽  
Marina Yu. Kopaeva ◽  
Vyacheslav N. Kochkin ◽  
Pavel K. Kashkarov

Since ancient times, silver has been known for its pronounced bactericidal, antiviral and fungicidal properties. Currently, nanoparticles of this metal are widely used in the food, light and pharmaceutical industries, as well as in medicine. Silver in any form can have a toxic effect not only on pathogens, but also on healthy cells. The biological activity and bioavailability of silver preparations depend on the degree of their solubility in water. In addition, the maximum permissible concentration of soluble forms of silver is an order of magnitude lower than that of insoluble forms. This makes nanoparticles of silver with a hydrophilic coating that form stable colloidal solutions in aqueous media potentially unsafe objects. In this work, we studied the kinetics of the accumulation of silver nanoparticles with an average size of 34 ± 5 nm stabilized with polyvinylpyrrolidone in the organs of laboratory C57Bl/6 mice. The administration of nanoparticles was carried out orally for 30, 60, 120 and 180 days at the dose of 50 µg/day/animal. All the mice developed and gained weight normally during the experiment. No adverse effects were observed. Determination of the silver content in biological tissues of mammals was accomplished by neutron activation analysis. The masses and concentrations of silver in the brain and its different sections (hippocampus, cerebellum, cortex and remnants), as well as in the lungs, testes, liver, blood, kidneys, spleen and heart, were determined. The injection times at which the accumulation curves reached saturation were established. An extremely high accumulation of silver in the testes was shown at 120 days of administration, and a significant accumulation of silver in the lungs and brain was observed. The accumulation of silver in all parts of the brain except the cortex was significant, and its trend was similar to that in the whole brain.

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