O. Poshyvak, O. Pinyazhko, L. Godlevsky, M. Pervak, O. Yehorenko, Z. Doğanyiğit, A. Okan, E. Akyuz, S. N. A. Hathal, A. Liashenko
{"title":"Immunohistochemical neuroinflammatory markers in the hippocampus of PTZ-kindled rats under conditions of rapamycin and axitinib treatment","authors":"O. Poshyvak, O. Pinyazhko, L. Godlevsky, M. Pervak, O. Yehorenko, Z. Doğanyiğit, A. Okan, E. Akyuz, S. N. A. Hathal, A. Liashenko","doi":"10.15587/2519-4852.2023.274703","DOIUrl":"https://doi.org/10.15587/2519-4852.2023.274703","url":null,"abstract":"The aim of the study is to determine the level of HIF-1α, TNF-α, and NF-kB in the hippocampus of kindled rats treated with rapamycin and axitinib. \u0000Materials and methods. Kindling was produced in 29 rats by administration of three-week pentylenetetrazole (PTZ, 35.0 mg/kg, i.p.). Treatment with rapamycin (0.5 mg/kg, i.p.) and axitinib (2.5 mg/kg, i.p.) was performed for ten days in fully kindled rats. The avidin-biotin-peroxidase method was used for hippocampal slice staining. For negative control, staining was performed using only secondary antibodies. \u0000Results. The HIF-1α expression increased in kindled rats raised by 1.77 times compared to the control (p<0.001). Axitinib treatment resulted in of HIF-1α level of 16.7 % (p<0.05) compared with kindled animals, while combined treatment with rapamycin and axitinib reduced HIF-1α by 33.8 % (p<0.01). In kindled rats, TNF-α expression was 3.74 times greater than in control (p<0.001). Rapamycin treatment reduced TNF-α by 31.0 % (p<0.01). Axitinib treatment caused a reduction of TNF-α by 21.1 % (p<0.05). Combined treatment with rapamycin and axitinib reduced TNF-α by 48.0 % (p<0.001) but still exceeded the TNF-α in control by 1.95 times (p<0.01). NF-kB level in kindled rats exceeded the control by three times (p<0.001). Rapamycin caused a reduction of 19.3 % (p>0.05), while axitinib – by 26.5 % (p<0.05) compared with kindled rats. Combined treatment with rapamycin and axitinib resulted in NF-kB reduction by 56.7 % compared with kindled rats (p<0.001). \u0000Conclusions. PTZ-kindling resulted in an increase in the immunoreactivity of HIF-1α, TNF-α, and NF-kB in the hippocampus. Combined treatment with rapamycin and axitinib engendered prevention of generalized seizures and normalized the level of HIF-1α and NF-kB with a significant reduction of TNF-α. Effects of treatment favours of synergy action of rapamycin and axitinib","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"43 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78911963","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M. Horyn, M. Piponski, Tetiana Zaremba, T. Kucher, Svetlana Krstevska Balkanov, Tanja Bakovska Stoimenova, D. Korobko, Nataliia Potikha, Liubomyr Kryskiw, L. Logoyda
{"title":"Application of salts of chaotropic anions in the development of hplc methods for the determination of meldonium in dosage forms","authors":"M. Horyn, M. Piponski, Tetiana Zaremba, T. Kucher, Svetlana Krstevska Balkanov, Tanja Bakovska Stoimenova, D. Korobko, Nataliia Potikha, Liubomyr Kryskiw, L. Logoyda","doi":"10.15587/2519-4852.2023.274469","DOIUrl":"https://doi.org/10.15587/2519-4852.2023.274469","url":null,"abstract":"The aim of the work was to create an approach for the development of HPLC methods for the determination of meldonium in dosage forms with the usage of salts of chaotropic anions in mobile phases. \u0000Material and methods. Analytical equipment: Shimadzu UPLC system LC-40 PDA; Shimadzu Nexera-i LC-2040C 3D-Plus, controlled by software Lab Solution version 5.97, electronic laboratory balance RAD WAG AS 200/C, pH-meter I-160MI. Meldonium dihydrate (purity 99.3 %) was purchased from Sigma-Aldrich (Switzerland), and Vasopro capsules 500 mg were purchased from a local pharmacy. Chromatographic conditions: Agilent Zorbax C-18 SB 150 mm x 4.6 mm 3.5 μm column was used (Agilent Technologies, USA). Mobile phases: 1) 0.25 % KPF6 w/v – 0.1 % v/v 85 %H3PO4 95 % – 5 % ACN, 2) 0.3 % bis-(trifluoromethane)sulfonimide lithium salt 97 % w/v – 0.1 %v/v 85 % H3PO4 80 % – 20 % acetonitrile. Flow rate - 1mL/min, T=32 °C, detection UV=at 4 channels - 190 nm, 195 nm, 200 nm, 205 nm. \u0000Results and discussion. We have proposed two approaches using two different salts of chaotropic anions - potassium hexafluorophosphate and bis-(trifluoromethane)sulfonimide lithium salt – for the HPLC method development. The chaotropic effects of these anions toward meldonium strongly influenced the analyte migratory behaviour. Both mobile phases involved, in addition to the use of a chaotrope, also the use of acetonitrile and pH adjustment with 0.1 % v/v 85 % H3PO4 solution. The detection wavelength (190 nm, 195 nm, 200 nm, 205 nm) was selected experimentally. The results were obtained for 8 concepts. Parameters of the chromatographic system confirm the conclusions and results of this investigation for the influence of chaotropic salts on N-containing molecules in an acidic pH medium, by increasing their retentivity and improving peak shape and uniformity homogeneity, even on the column without end-capping and base-deactivating. Validation of the analytical method was carried out following the requirements of SPhU. Conclusions. HPLC methods for the determination of meldonium in dosage forms have been developed, using positive impacts of chaotropic salts on the molecules containing N-atoms in their molecule on their retentions and peak symmetries on the chromatogram. The validation of the analytical methods showed their suitability for pharmaceutical analysis","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"7 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81898981","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Almat G. Rustemkulov, T. Gontova, B. Makhatova, Aisana E. Rustemkulova, N. Gemedzhieva, Aizhamal Shormanova, G. Starchenko, A. Raal, U. Datkhaev, O. Koshovyi
{"title":"Macro and microscopic analysis of Alfredia nivea KAR. & KIR herb","authors":"Almat G. Rustemkulov, T. Gontova, B. Makhatova, Aisana E. Rustemkulova, N. Gemedzhieva, Aizhamal Shormanova, G. Starchenko, A. Raal, U. Datkhaev, O. Koshovyi","doi":"10.15587/2519-4852.2023.274766","DOIUrl":"https://doi.org/10.15587/2519-4852.2023.274766","url":null,"abstract":"Kazakhstan flora is rich in promising little-studied plants that are used in folk medicine, but additional deep research is required for their introduction into medical practice with the help of modern scientific techniques. An interesting object for introduction into the official medical and pharmaceutical practice is the Alfredia Nivea Kar. & Kir, family Asteraceae, whose extracts have a neurotropic effect. \u0000The aim. Regarding mentioned above, in order to create new medicines based on the grass of the Alfredia nivea, it is necessary to develop methods of its macro and microscopic identification. \u0000Materials and methods. Macro- and microscopic studies of the grass of Alfredia nivea were carried out in accordance with the methodology of SPhU 2.8.23 \"Microscopic examination of medicinal vegetable raw materials\". Macroscopic studies were performed using magnifying glass and binocular microscope MBS-9, microscopic-using MS Microscopes 10 (eyepiece X5, X10, X15, lenses x10, x40), micromed XS-4130 (WF15X, Opera, lens X40/0, 65, x10/0,25) with microphoto addon (China). \u0000Results. The morphological and anatomical features of the Alfredia nivea grass. Diagnostic features of the structure of stems, leaves and flowers of this species were revealed. \u0000Conclusions. The macroscopic and anatomical identification parameters of the grass of the Alfredia of Snow. The study of the morphological and anatomical features of the stems, leaves and flowers of Alfredia nivea, considering the requirements of European pharmacopoeia. Diagnostic features of the structure of stems, leaves and flowers of the species were found, which were used as key quality indicators for standardization and identification of raw materials","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83952867","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
E. Bezuglaya, A. Krasnopyorova, A. Liapunova, I. Zinchenko, N. Lyapunov, O. Sytnik
{"title":"Influence of physicochemical properties and structure of mixed solvents propylene glycol – macrogol 400 on their in vitro release","authors":"E. Bezuglaya, A. Krasnopyorova, A. Liapunova, I. Zinchenko, N. Lyapunov, O. Sytnik","doi":"10.15587/2519-4852.2023.274468","DOIUrl":"https://doi.org/10.15587/2519-4852.2023.274468","url":null,"abstract":"Aim. To study the density and dynamic viscosity of the mixed solvents propylene glycol (PG) – macrogol 400 (M400), to calculate their excess values and excess activation parameters of viscous flow, to evaluate the features of the structure of the mixed solvents and its influence on the in vitro release of PG and M400. \u0000Materials and methods. The mixed solvents PG - M400 were studied over the entire concentration range at temperatures from 293.15 to 313.15 K. The density and dynamic viscosity were determined, and the excess density, excess dynamic viscosity, activation parameters of viscous flow, and excess activation parameters of viscous flow were calculated. The in vitro release of PG and M400 from the mixed solvents was studied using vertical diffusion cells. The content of PG and M400 in the receptor medium was determined by gas chromatography using validated analytical procedures. The release rate, cumulative content, percentage of released PG or M400, coefficients of correlation and coefficients of determination were calculated. \u0000Results. The isotherms of excess density and excess dynamic viscosity of the mixed solvents PG-M400 pass through a maximum. The enthalpy makes the main contribution to the free activation energy of the viscous flow. The excess free energy is positive and has small values; the values of the excess entropy and excess enthalpy are negative, and the isotherms have the minimum at PG concentrations of 70‑75mol %. The release parameters of M400 are greater in binary mixtures where the M400 structure predominates. At PG content of ~75 mol %, the release parameters for PG and M400 are identical. With the increase in PG content above 75 mol %, when the PG structure predominates in the system, the release parameters of PG increase dramatically, and the release parameters of M400 decrease sharply. \u0000Conclusions. The structure of the binary system PG – M400 depends on its composition. Based on the isotherms of excess activation of viscous flow, it is possible to differentiate the areas where the structure of PG or the structure of M400 dominates, or the mixed structure of the binary solvent prevails. The in vitro release parameters for PG and M400 depend on the structure of the mixed solvents. The greatest difference in the release parameters of PG and M400 was observed in the area where the structure of PG dominates","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"53 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81276819","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Optimization of the isolation of biologically active complexes from buds and shoots of birch and poplar buds for their further use in cosmeceutical compositions","authors":"Alyona Yanevich, D. Mokshin, V. Polyakov","doi":"10.15587/2519-4852.2023.273394","DOIUrl":"https://doi.org/10.15587/2519-4852.2023.273394","url":null,"abstract":"The aim is to optimize the isolation of biologically active birch and poplar complexes based on woodworking industry waste to study their biological activity to create cosmeceutical compositions that have cosmetic and pharmaceutical effects. \u0000Materials and methods. The object of research is the vegetative organs of birch (buds and shoots) and poplar (buds). In the process of work, experimental studies were carried out on the extraction and separation of natural compounds, development of biological complexes of vegetative organs of birch and poplar, study of the chemical composition and standardization of biologically active complexes of birch and preparations based on them. \u0000Results. The optimal methods for extracting natural complexes were determined. Created as a semi-industrial installation for producing biologically active complexes by barothermal method, combining two processes - high pressure and hydrodistillation. The optimal operating cycle and plant parameters were determined. The optimal solvents for the extraction of biologically active complexes from the vegetative organs of birch and poplar have been determined. Petroleum ether (33.60 %) extracted the most compounds from birch buds, in birch shoots - ethanol (8.34 %). Qualitative and quantitative indicators of biologically active complexes are determined, and projects for examining the obtained biologically active complexes are proposed. We determined the yield of essential oil depending on the time of collection of raw materials and determined that the largest amount of essential oil is contained in spring buds (0.21 % of dry raw materials) and shoots (0.08 %). \u0000Conclusions. Biological complexes created from timber processing waste with high activity are the basis for the creation of cosmetic products. The created semi-industrial plant will provide the basis for creating new original products in industrial volumes.","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"37 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84852192","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
N. Sydora, V. Yakovenko, O. Ochkur, A. Rudnyk, O. Honcharov, Svetlana Zuikina, K. Romas, M. Marchenko
{"title":"Technology of obtaining and chemical profiles of dry extracts from leaves of prospective species of the hawthorn genus","authors":"N. Sydora, V. Yakovenko, O. Ochkur, A. Rudnyk, O. Honcharov, Svetlana Zuikina, K. Romas, M. Marchenko","doi":"10.15587/2519-4852.2023.274772","DOIUrl":"https://doi.org/10.15587/2519-4852.2023.274772","url":null,"abstract":"The aim of the work was to develop a technology for obtaining dry extracts from leaves of non-pharmacopoeia species of hawthorn and establishing their chemical profiles.\u0000Materials and methods. Leaves of Crataegus mollis Sarg., Crataegus submollis Sarg. and Crataegus arnoldiana Sarg., used to obtain the dry extracts, were harvested in the Botanical Garden of the National University named after M. N. Karazina in August 2021. To determine the chemical profiles of the obtained dry extracts, the spectrophotometric method and the high-performance liquid chromatography (HPLC) method were used.\u0000Results. A technological scheme for obtaining dry extracts of hawthorn leaves has been developed. The content of flavonoids and hydroxycinnamic acids in dry extracts of the leaves of C. mollis Sarg., C. submollis Sarg. and C. arnoldiana Sarg. was determined. The content of free amino acids in extracts ranges from 0.70 % to 0.99 %. The content of flavonoids ranged from 7.25 %±0.04 to 8.43 %±0.01, of hydroxycinnamic acids - from 2.35 %±0.02 to 2.85 %±0.03. Rutin, kaempferol-3-O-glycoside, epicatechin and chlorogenic acid were identified in all extracts by the HPLC method. In dry leaf extracts of C. arnoldiana Sarg. and C. mollis identified p-coumaric acid; C. arnoldiana Sarg. – quercetin; C. arnoldiana Sarg. and C. submollis Sarg. – ferulic acid; C. submollis Sarg. and C. mollis Sarg. – quercetin-3-O-rhamnoside.\u0000Conclusions. Dry leaf extracts of C. mollis Sarg., C. submollis Sarg. and C. arnoldiana Sarg. were obtained. For the first time, the content of flavonoids and hydroxycinnamic acids in the extracts was determined by HPLC. It was established that the chemical profile of the obtained extracts is formed by rutin, chlorogenic acid and kaempferol-3-O-glycoside, which can be used in further standardization of these substances. In addition, a comparative study of the amino acid composition of the obtained extracts was carried out for the first time","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"41 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84501669","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Study of hypoglycemic properties of «Glyphasonorm» tablets and «Glyphasolin» capsules on the streptozotocin-induced diabetic rat model","authors":"V. Rybak, Alexander Honcharov, Viktoriia Korol","doi":"10.15587/2519-4852.2022.271034","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.271034","url":null,"abstract":"The risk of developing any complications of diabetes is significantly reduced by monitoring and correcting blood glucose levels and blood pressure, as well as by observing healthy lifestyle rules. Early detection and treatment of type 2 diabetes contribute to the prevention of disease progression and the development of complications. \u0000The aim is to study the hypoglycemic effect of «Glyphasonorm» tablets and «Glyphasolin» capsules in a rat model of streptozotocin-induced diabetes. \u0000Materials and methods. The studies were carried out on Wistar rats injected intraperitoneally with nicotinamide at a dose of 230 mg/kg 15 minutes before intravenous injection of streptozotocin at a dose of 65 mg/kg. The dynamics of body weight of rats, glucose and glycosylated haemoglobin levels under the impact of long-term administration of metformin, «Glyphasonorm» tablets and «Glyphasolin» capsules were investigated. \u0000Results and discussion. The studies on a streptozotocin-induced diabetic model have established that under the action of «Glyphasonorm» tablets and «Glyphasolin» capsules, the level of glycosylated haemoglobin, which decreased along with the level of glucose in the blood of animals, was significantly reduced in comparison with diabetic control. After 14 days of research, the \"Glyphasolin\" capsules showed more pronounced hypoglycemic activity (4.4 % and 8.0 % more) than the \"Glyphasonorm\" tablets and the reference drug metformin. The «Glyphasolin» capsules on the 12th day of the study showed a marked decrease in glycosylated haemoglobin in the blood of animals (3.1 % and 5.6 % more) than the «Glyphasonorm» tablets and metformin. \u0000Conclusions. In the experimental model of streptozotocin diabetes in rats, \"Gliphasolin\" capsules showed a more pronounced hypoglycemic effect, which was manifested by a decrease in the content of glycosylated haemoglobin in the blood and prevailed over the effect of the comparative drug metformin and \"Gliphasonorm\" tablets. \u0000«Glyphasolin» capsules and «Glyphasonorm» tablets based on bioflavonoid complex from bean show promise in the treatment of type 2 diabetes on the background of obesity and reducing the risk of micro- and macroangiopathy","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81875824","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Raissa Fitri, H. Syahputra, N. Nasri, V. E. Kaban, Zulmai Rani
{"title":"Formulation of a biocellulose mask containing the essence of Aloe vera (L.) Burm.f combination with vitamin E as anti-aging","authors":"Raissa Fitri, H. Syahputra, N. Nasri, V. E. Kaban, Zulmai Rani","doi":"10.15587/2519-4852.2022.268987","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.268987","url":null,"abstract":"Most ageing processes are accelerated due to an increasing amount of endogenic stress from outdoor or indoor activity overload. The essence of aloe vera is formulated in the form of a biocellulose mask. It is one of the solutions to deliver essence within polymeric substances, obtained through the fermentation process with the help of Acetobacter xyllinum. \u0000The aim of this study is to enhance anti-ageing activity derived from Aloe vera (L) essence combined with vitamin E, thus in the form of a biocellulose mask that will prolong skin contact and reduce the main cotton sheet mask problem of deforestation, hence its eco-friendly benefit. \u0000Material and methods: Twelve volunteers around 25 to 45 years old are subjected to a biocellulose mask containing Aloe vera essence combined with vitamin E for at least 4 weeks to achieve a balanced skin criterion including wrinkles, spots, facial pores, and moisture. Aloe vera and vitamin E constituents within F0; F1, F2; F3, [0%, 0%]; [0%, 1%]; [5%, 0 %] and [5 %, 1 %] as per the following. \u0000Results: Results showed that bio-cellulose masks containing 5 % Aloe vera with 1 % of vitamin E essence in F3 provide a beneficial anti-ageing activity rather than other biocellulose mask preparations. \u0000Conclusion: Biocellulose mask through the fermentation process can improve skin conditions, the formula combined with the well-known activity of aloe vera as an exfoliating agent and antioxidant vitamin E, it can not only provide skin rejuvenation but also provide anti-ageing activity","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"11 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81890794","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
O. Bezugla, A. Liapunova, I. Zinchenko, Oleksii Liapunov, N. Lyapunov, Yu. M. Stolper
{"title":"Study of factors affecting the in vitro release of ketoprofen from carbomers-based gels","authors":"O. Bezugla, A. Liapunova, I. Zinchenko, Oleksii Liapunov, N. Lyapunov, Yu. M. Stolper","doi":"10.15587/2519-4852.2022.268933","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.268933","url":null,"abstract":"The aim. To identify some factors affecting the in vitro release of ketoprofen from carbomer-based gels. \u0000Materials and methods. Carbomer-based gels containing ketoprofen as well as a Newtonian liquid without carbomer, which was the dispersion medium of the gel, were studied by rotational viscometry and spin probe method. The flow behaviour and rheological parameters were determined using the rheograms, and the rotational correlation times of the two dissolved spin probes, the molecules of which contain a carboxyl group or an amino group, were determined by EPR spectra. In vitro release tests were performed using vertical diffusion chambers using a validated method. The quantitative determination of ketoprofen in gels, liquid and receptor medium was performed by liquid chromatography, and ethanol was quantified by gas chromatography according to validated procedures. Gels with different brands of carbomers, neutralised with trolamine or trometamol, with different contents of ketoprofen and ethanol, and with pH from 6.0 to 7.0 were studied. \u0000Results. The sol → gel transition due to the neutralisation of the carbomer did not affect the shape and parameters of the EPR spectrum of the spin probe containing a carboxyl group in the molecule (like a carbomer and ketoprofen) in contrast to the probe with an amino group. If the substance dissolved in the gels does not interact with the carbomer, then its molecules/ions rotate rapidly in the liquid medium. This facilitates the release of a such substance from carbomer-based gels. The medicinal product Nobi Gel® gel 2.5 % and Newtonian liquid were equivalent in relation to the in vitro release parameters of ketoprofen from these objects. Сarbomer-based gels, which differed significantly in terms of rheological parameters, were also found to be equivalent in terms of ketoprofen release parameters. The in vitro release of ketoprofen was affected by its concentration and ethanol content in the gel. A change in pH from 6.0 to 7.0 practically did not affect the parameters of in vitro release of ketoprofen from gels. \u0000Conclusions. The formation of a carbomer-based gel did not affect the rotational correlation time of the probe, which did not interact with the carbomer. Parameters of in vitro release of ketoprofen from the gel and Newtonian liquid differed little; these parameters were also little affected by the difference in apparent viscosity of the gels. The in vitro release of ketoprofen depended on its concentration and ethanol content","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"47 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74675376","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
J. Awe, O. Osukoya, O. Adewale, T. Obafemi, O. B. Afolabi, A. Kuku
{"title":"Antinociceptive effects of Treculia africana decne (african breadfruit) seed lectin in Wistar rats","authors":"J. Awe, O. Osukoya, O. Adewale, T. Obafemi, O. B. Afolabi, A. Kuku","doi":"10.15587/2519-4852.2022.270312","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.270312","url":null,"abstract":"The aim: The use of synthetic compounds to treat many diseases must be strictly controlled due to their potential health hazards. Hence, there is a need to search for natural products to serve as safe alternatives to synthetic products. This study investigated the antinociceptive effects and anti-inflammatory activities of Treculia africana seed lectin. \u0000Materials and methods: Lectins were purified from Treculia africana seeds using ion exchange and size-exclusion chromatography. The antinociceptive activity of the lectin was assessed in Wistar rats using abdominal writhing and paw-licking tests induced by acetic acid and formalin, respectively. Anti-inflammatory activity was assessed using carrageenan-induced paw oedema. \u0000Results: Treculia africana seed lectins at 10 mg/kg (p.o.) produced sedation, reduced ambulation, reduced response to touch, analgesia, and decreased defecation in experimental animals. Administration of Treculia africana seed lectin (1 mg/kg and 10 mg/kg) in experimental animals significantly reduced (P < 0.05) acetic acid-induced muscular writhing in a dose-dependent manner with 23.88 and 36.80 per cent inhibition, respectively. Both early and late phases of formalin-induced nociception were significantly inhibited (P < 0.001) by the lectin at all doses (0.1, 1.0 and 10.0 mg/kg), comparably with the standard drug, diclofenac sodium. At 10 mg/kg, T. africana lectin caused a 69.12 % and 65.55 % reduction in both early and late phases of formalin-induced paw licking. Treculia africana lectin also significantly brought about a reduction (P < 0.05) in inflammation induced by sub-plantar injection of carrageenan as measured by a decrease in paw swollenness. \u0000Conclusion: The study showed that Treculia africana lectin possesses antinociceptive and anti-inflammatory properties and can potentially be employed therapeutics to ameliorate pain and inflammation","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"88 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89627364","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}