Pub Date : 2024-01-29DOI: 10.33380/2305-2066-2024-13-1-1510
E. Bakhrushina, A. Turaeva, D. Zhalyalova, D. A. Klimov, N. Demina, I. I. Krasnuk
Introduction. Emuxol-268 (JSC "NIOPIK", Russia) is a block copolymer produced in Russia with similar in physicochemical and biological properties to poloxamer Kolliphor® P 188 (Pluronic F68) manufactured by BASF, USA. However, a comparison of the properties of natural polymers to assess the prospects of their dosage forms has not been carried out before.Aim. The aim of the study was to demonstrate the interchangeability of auxiliary components using the example of the development of an ophthalmic drug insert by comparing the results of testing the dosage form in terms of such quality parameters as elasticity, thickness, mucoadhesion, pH, biodegradation time and irritation test (hen’s egg-chorioallantoic membrane test, HET-CAM test).Materials and methods. Poloxamers Emuxol 268 (JSC "NIOPIK", Russia) and Kolliphor® P 188 (BASF, Germany), hydroxyethyl cellulose (Natrosol™ 250 HHX, Ashland Global Holdings Inc., USA), and glycerol (LLC "Tulskaya Pharmfabrika", Russia) were used in the experiment. Elasticity, thickness, mucoadhesion, pH, biodegradation time, HET-CAM test were used as screening methods to identify the benefits of the composition.Results and discussion. Experiment results proved that the use of a domestic analogue makes it possible to create an ocular insert with improved quality parameters. The difference in the elasticity index of the inserts differs by 1.3 times, mucoadhesion – 1.7 times, biodegradation time – 2.5 times. In this connection, it can be assumed that an insert based on a domestic polymer contributes to an increase in the time of contact with the eye surface, thereby providing a prolonged effect of the drug and improving its bioavailability. The results obtained may be due to the difference in the average molecular weight of the hydrophobic polyoxypropylene part, which is 2600 Da for Emuxol 268 and 1800 Da for Kolliphor 188. The HET-CAM method showed the same results of the two compositions, both compositions do not have an irritating effect.Conclusion. Summing up, the only analogue of Kolliphor® P 188 available on the Russian pharmaceutical market – Emuxol-268 of JSC NIOPIK is a promising substance for replacement in the development of ophthalmic dosage forms. Despite the differences in physicochemical properties of the domestic block copolymer in comparison with the replaced poloxamer 188, its introduction into placebo inserts gave improved results in terms of quality indicators, which was revealed during a biopharmaceutical analysis.
{"title":"Development of Ocular Inserts Based on Import Substituted Poloxamer Emuxol 268","authors":"E. Bakhrushina, A. Turaeva, D. Zhalyalova, D. A. Klimov, N. Demina, I. I. Krasnuk","doi":"10.33380/2305-2066-2024-13-1-1510","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1510","url":null,"abstract":"Introduction. Emuxol-268 (JSC \"NIOPIK\", Russia) is a block copolymer produced in Russia with similar in physicochemical and biological properties to poloxamer Kolliphor® P 188 (Pluronic F68) manufactured by BASF, USA. However, a comparison of the properties of natural polymers to assess the prospects of their dosage forms has not been carried out before.Aim. The aim of the study was to demonstrate the interchangeability of auxiliary components using the example of the development of an ophthalmic drug insert by comparing the results of testing the dosage form in terms of such quality parameters as elasticity, thickness, mucoadhesion, pH, biodegradation time and irritation test (hen’s egg-chorioallantoic membrane test, HET-CAM test).Materials and methods. Poloxamers Emuxol 268 (JSC \"NIOPIK\", Russia) and Kolliphor® P 188 (BASF, Germany), hydroxyethyl cellulose (Natrosol™ 250 HHX, Ashland Global Holdings Inc., USA), and glycerol (LLC \"Tulskaya Pharmfabrika\", Russia) were used in the experiment. Elasticity, thickness, mucoadhesion, pH, biodegradation time, HET-CAM test were used as screening methods to identify the benefits of the composition.Results and discussion. Experiment results proved that the use of a domestic analogue makes it possible to create an ocular insert with improved quality parameters. The difference in the elasticity index of the inserts differs by 1.3 times, mucoadhesion – 1.7 times, biodegradation time – 2.5 times. In this connection, it can be assumed that an insert based on a domestic polymer contributes to an increase in the time of contact with the eye surface, thereby providing a prolonged effect of the drug and improving its bioavailability. The results obtained may be due to the difference in the average molecular weight of the hydrophobic polyoxypropylene part, which is 2600 Da for Emuxol 268 and 1800 Da for Kolliphor 188. The HET-CAM method showed the same results of the two compositions, both compositions do not have an irritating effect.Conclusion. Summing up, the only analogue of Kolliphor® P 188 available on the Russian pharmaceutical market – Emuxol-268 of JSC NIOPIK is a promising substance for replacement in the development of ophthalmic dosage forms. Despite the differences in physicochemical properties of the domestic block copolymer in comparison with the replaced poloxamer 188, its introduction into placebo inserts gave improved results in terms of quality indicators, which was revealed during a biopharmaceutical analysis.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"108 1-4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140490058","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}
Pub Date : 2024-01-29DOI: 10.33380/2305-2066-2024-13-1-1519
S. S. Gogina, E. A. Smirnova, Ya. M. Stanishevskii, A. M. Stoinova
Introduction. One of the most promising types of immunosensors is quartz crystal microbalance immunosensors (QCM immunosensors). Single-use biosensors are financially demanding, thus rendering the regeneration of the biosensor surface a pertinent issue for QCM immunosensors. Regeneration plays a pivotal role in sustaining the functionality of the sensor and enabling its reusability. In this article, "immunosensor" and "immunobiosensor" are interchangeable terms and are used to denote the same type of biosensors operating based on immunochemical interactions between antigens and antibodies.Text. This review discusses the features, operational principles, and applications of QCM immunosensors. Particular attention is directed toward the challenge of regenerating the biosensor surface as a key aspect ensuring their effective operation and the potential for multiple uses. Various regeneration methods and their advantages are examined. The reactivation of the biosensing layer on the QCM electrode secures its stability and functionality over extended periods, which is especially valuable in clinical and scientific research. The possibility of reusing the biosensor reduces material costs and waste production, aligning with ecological and economic concerns. Furthermore, the ability to analyze different analytes on the same surface fosters versatility in multiparametric investigations. It is essential to emphasize that the removal of residual analytes and the biosensor's regeneration process enhance reliability, selectivity, heightened sensitivity, and the potential for reproducible measurements.Conclusion. An analysis of scientific literature underscores the pivotal role of biosensor regeneration in maintaining functionality and reusability. The strength of the antigen-antibody interaction determines the conditions, which must be tailored individually for each antigen-antibody pair. The review thoroughly explores three primary approaches to the regeneration of piezoelectric transducers, including the use of a chemical method, oxygen plasma-based techniques, and the application of Piranha solution.
{"title":"Detection of Immunochemical Reactions Using Piezoquartz Immunosensor. Regeneration of the Electrode Bio-layer (Review)","authors":"S. S. Gogina, E. A. Smirnova, Ya. M. Stanishevskii, A. M. Stoinova","doi":"10.33380/2305-2066-2024-13-1-1519","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1519","url":null,"abstract":"Introduction. One of the most promising types of immunosensors is quartz crystal microbalance immunosensors (QCM immunosensors). Single-use biosensors are financially demanding, thus rendering the regeneration of the biosensor surface a pertinent issue for QCM immunosensors. Regeneration plays a pivotal role in sustaining the functionality of the sensor and enabling its reusability. In this article, \"immunosensor\" and \"immunobiosensor\" are interchangeable terms and are used to denote the same type of biosensors operating based on immunochemical interactions between antigens and antibodies.Text. This review discusses the features, operational principles, and applications of QCM immunosensors. Particular attention is directed toward the challenge of regenerating the biosensor surface as a key aspect ensuring their effective operation and the potential for multiple uses. Various regeneration methods and their advantages are examined. The reactivation of the biosensing layer on the QCM electrode secures its stability and functionality over extended periods, which is especially valuable in clinical and scientific research. The possibility of reusing the biosensor reduces material costs and waste production, aligning with ecological and economic concerns. Furthermore, the ability to analyze different analytes on the same surface fosters versatility in multiparametric investigations. It is essential to emphasize that the removal of residual analytes and the biosensor's regeneration process enhance reliability, selectivity, heightened sensitivity, and the potential for reproducible measurements.Conclusion. An analysis of scientific literature underscores the pivotal role of biosensor regeneration in maintaining functionality and reusability. The strength of the antigen-antibody interaction determines the conditions, which must be tailored individually for each antigen-antibody pair. The review thoroughly explores three primary approaches to the regeneration of piezoelectric transducers, including the use of a chemical method, oxygen plasma-based techniques, and the application of Piranha solution.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"80 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140486087","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}
Pub Date : 2024-01-29DOI: 10.33380/2305-2066-2024-13-1-1332
A. Gudkova, A. S. Chistyakova, A. I. Slivkin, A. S. Bolgov
Introduction. The issue of standardization and quality assessment of medicinal plant materials is currently one of the most important. To do this, a number of parameters are evaluated, the primary of which is the assessment of the authenticity of the analyzed plant object. The problem of identifying official species in the presence of closely related species is typical for plants belonging to the genus Persicaria Mill., among which only two species are used in medical practice and there is regulatory documentation for the herbs of these plants. The similarity of morphological and anatomical features of plant species acceptable for medical use and impurities interprets the need to use additional modern methods of analysis. One of such selective methods for diagnosing plant materials, along with the well-known and used in pharmaceutical analysis, is luminescence microscopy.Aim. The goal was to study the features of the luminescence of closely related species of the genus Persicaria Mill. to improve the process of their identification and standardization of official types of raw materials.Materials and methods. For work, 10 species of the genus Persicaria Mill. were used from families Polygonaceae Juss., most common in the Central Chernozem region: P. maculosa Gray, P. tomentósa Bicknell, P. lapathifólia Delarbre, P. nodósa Opiz, P. scábra Moldenke, P. brittingeri Opiz, P. hydropiper Delarbre, P. minor Opiz, P. amphibia Delarbre, P. amphibia var. terrestris Munshi & Javeid. The plants were cut at a height of about 15 cm from the soil during mass flowering in the summer of 2020 in the Voronezh region, dried in the shade. Previously, before the study, the plants were divided into morphological components (stems, leaves, petioles, bells, flowers, fruits), for which herbarium samples were used in dried form and individual parts were examined, straightened on a glass slide. To assess the luminescence of objects, a Micromed-3 Lum microscope (Russia) with a luminescent nozzle housing was used.Results and discussion. It was revealed that the intense fluorescence of large trichomes, the conducting system, guard cells of stomata, thickening of cell walls, and, in some species, the contents of receptacles and glands, is common to all studied species. A number of characteristic features of tissue luminescence for the studied species have been revealed: P. hydropiper has numerous brightly luminous receptacles and glands on all morphological parts. For P. maculosa, the presence of large receptacles along the veins was established for the first time. The perianth, glandules, and filiform hairs of the bell of P. brittingeri are clearly visible and have a yellowish-green luminescence. The leaf glands of P. tomentósa, unlike other species, do not have luminescence. The perianths of P. scábra and P. tomentósa have a yellowish-orange glow. The membranous trichomes are clearly visible in P. lapathifólia and stand out with a brownish tint. The largest number of long tuft
导言。药用植物材料的标准化和质量评估问题是当前最重要的问题之一。为此,需要对一系列参数进行评估,其中最主要的是对所分析植物对象真实性的评估。柿属(Persicaria Mill.)植物的典型问题是在存在近缘物种的情况下如何确定正式物种,其中只有两个物种被用于医疗实践,而且这些植物的药材都有规范性文件。可用于医疗用途的植物物种与杂质的形态和解剖特征相似,因此需要使用更多的现代分析方法。发光显微镜是诊断植物材料的选择性方法之一,也是众所周知的药物分析方法。目的是研究密切相关的柿属植物的发光特征,以改进其鉴定过程和官方原料类型的标准化。工作中使用了蓼科 Juss.中的 10 个柿属物种,它们在切尔诺泽姆中部地区最为常见:P. maculosa Gray、P. tomentósa Bicknell、P. lapathifólia Delarbre、P. nodósa Opiz、P. scábra Moldenke、P. brittingeri Opiz、P. hydropiper Delarbre、P. minor Opiz、P. amphibia Delarbre、P. amphibia var. terrestris Munshi & Javeid。2020 年夏天,在沃罗涅日地区大量开花时,在植株距土壤约 15 厘米处剪下,在阴凉处晾干。在研究之前,植物被分成不同的形态部分(茎、叶、叶柄、花铃、花、果),为此使用了标本馆的干燥样本,并在玻璃载玻片上拉直后对各个部分进行了检查。为了评估物体的发光情况,使用了带有发光喷嘴外壳的 Micromed-3 Lum 显微镜(俄罗斯)。结果表明,大毛状体、传导系统、气孔的保卫细胞、细胞壁的增厚以及某些物种的花托和腺体内容物的强烈荧光是所有研究物种的共同特征。所研究物种的组织发光有许多特征:P. hydropiper 的所有形态部位都有许多明亮发光的花托和腺体。对于 P. maculosa 而言,首次确定了沿叶脉存在大型花托。brittingeri 的花被、腺体和花铃丝状毛清晰可见,并发出黄绿色的荧光。Tomentósa 的叶腺体与其他物种不同,不发光。P. scábra 和 P. tomentósa 的花被呈黄橙色。P. lapathifólia的膜状毛状体清晰可见,呈褐色。在 P. amphibia var. terrestris 中,数量最多的长束毛状体发出明亮的绿色光芒。首次将发光显微镜方法应用于识别参数的分析和鉴定,建立了新的诊断特征并将其可视化,从而能够最准确地鉴定柿属物种。
{"title":"Luminescence Microscopy in the Identification of Closely related Species Using the Example of the Genus Persicaria Mill.","authors":"A. Gudkova, A. S. Chistyakova, A. I. Slivkin, A. S. Bolgov","doi":"10.33380/2305-2066-2024-13-1-1332","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1332","url":null,"abstract":"Introduction. The issue of standardization and quality assessment of medicinal plant materials is currently one of the most important. To do this, a number of parameters are evaluated, the primary of which is the assessment of the authenticity of the analyzed plant object. The problem of identifying official species in the presence of closely related species is typical for plants belonging to the genus Persicaria Mill., among which only two species are used in medical practice and there is regulatory documentation for the herbs of these plants. The similarity of morphological and anatomical features of plant species acceptable for medical use and impurities interprets the need to use additional modern methods of analysis. One of such selective methods for diagnosing plant materials, along with the well-known and used in pharmaceutical analysis, is luminescence microscopy.Aim. The goal was to study the features of the luminescence of closely related species of the genus Persicaria Mill. to improve the process of their identification and standardization of official types of raw materials.Materials and methods. For work, 10 species of the genus Persicaria Mill. were used from families Polygonaceae Juss., most common in the Central Chernozem region: P. maculosa Gray, P. tomentósa Bicknell, P. lapathifólia Delarbre, P. nodósa Opiz, P. scábra Moldenke, P. brittingeri Opiz, P. hydropiper Delarbre, P. minor Opiz, P. amphibia Delarbre, P. amphibia var. terrestris Munshi & Javeid. The plants were cut at a height of about 15 cm from the soil during mass flowering in the summer of 2020 in the Voronezh region, dried in the shade. Previously, before the study, the plants were divided into morphological components (stems, leaves, petioles, bells, flowers, fruits), for which herbarium samples were used in dried form and individual parts were examined, straightened on a glass slide. To assess the luminescence of objects, a Micromed-3 Lum microscope (Russia) with a luminescent nozzle housing was used.Results and discussion. It was revealed that the intense fluorescence of large trichomes, the conducting system, guard cells of stomata, thickening of cell walls, and, in some species, the contents of receptacles and glands, is common to all studied species. A number of characteristic features of tissue luminescence for the studied species have been revealed: P. hydropiper has numerous brightly luminous receptacles and glands on all morphological parts. For P. maculosa, the presence of large receptacles along the veins was established for the first time. The perianth, glandules, and filiform hairs of the bell of P. brittingeri are clearly visible and have a yellowish-green luminescence. The leaf glands of P. tomentósa, unlike other species, do not have luminescence. The perianths of P. scábra and P. tomentósa have a yellowish-orange glow. The membranous trichomes are clearly visible in P. lapathifólia and stand out with a brownish tint. The largest number of long tuft","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"49 20","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140487431","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}
Pub Date : 2024-01-29DOI: 10.33380/2305-2066-2024-13-1-1538
P. A. Mihajlova, A. A. Adamova, Y. Generalova, P. Snetkov, S. Morozkina
Introduction. The effectiveness of diflunisal in the treatment of cardiac amyloidosis has been clinically proven. Currently, only tablet forms of diflunisal are registered in the world, however, long-term use of NSAIDs leads to characteristic side effects. Therefore, delivery systems for diflunisal (including a form for external use) are now being actively developed to reduce side effects and improve its bioavailability.Aim. Research of the dynamics of release of the active substance diflunisal from the polymer matrix of hyaluronic acid.Materials and methods. The objects of the study are diflunisal gels in hyaluronic acid with a concentration of the main substance of 0.093, 0.14, 0.19 and 0.25 %. Quantitative determination was carried out by reverse-phase HPLC using a Prontosil C18, 120-5, 75 × 2 mm chromatographic column, thermostatically controlled at 40 °C. Eluent: phosphate buffer solution (PBS) with pH 3.0 and acetonitrile (30 : 70), flow rate 0.1 ml/min. Eluates were detected at wavelengths of 230, 270, 310 nm.Results and discussion. During the work, a method (HPLC) was selected and a method for determining diflunisal in a HA matrix was developed. The delivery system under study significantly increases the solubility of diflunisal in an aqueous solution compared to the dissolution of the substance. The release of the active substance from the matrices was carried out in a phosphate buffer solution with pH 7.6. The release rate for all samples exceeded 90 % after 3 hours after the start of the experiment, with most of the active substance released within an hour.Conclusion. The data obtained suggest that the release profile is characteristic of biodegradable matrices and diffusion-controlled delivery systems. Complete extraction of diflunisal from HA was achieved using PBS with pH 7.6 as a dissolution medium.
{"title":"Study of the Dynamics of Diflunisal Release from a Polymer Matrix","authors":"P. A. Mihajlova, A. A. Adamova, Y. Generalova, P. Snetkov, S. Morozkina","doi":"10.33380/2305-2066-2024-13-1-1538","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1538","url":null,"abstract":"Introduction. The effectiveness of diflunisal in the treatment of cardiac amyloidosis has been clinically proven. Currently, only tablet forms of diflunisal are registered in the world, however, long-term use of NSAIDs leads to characteristic side effects. Therefore, delivery systems for diflunisal (including a form for external use) are now being actively developed to reduce side effects and improve its bioavailability.Aim. Research of the dynamics of release of the active substance diflunisal from the polymer matrix of hyaluronic acid.Materials and methods. The objects of the study are diflunisal gels in hyaluronic acid with a concentration of the main substance of 0.093, 0.14, 0.19 and 0.25 %. Quantitative determination was carried out by reverse-phase HPLC using a Prontosil C18, 120-5, 75 × 2 mm chromatographic column, thermostatically controlled at 40 °C. Eluent: phosphate buffer solution (PBS) with pH 3.0 and acetonitrile (30 : 70), flow rate 0.1 ml/min. Eluates were detected at wavelengths of 230, 270, 310 nm.Results and discussion. During the work, a method (HPLC) was selected and a method for determining diflunisal in a HA matrix was developed. The delivery system under study significantly increases the solubility of diflunisal in an aqueous solution compared to the dissolution of the substance. The release of the active substance from the matrices was carried out in a phosphate buffer solution with pH 7.6. The release rate for all samples exceeded 90 % after 3 hours after the start of the experiment, with most of the active substance released within an hour.Conclusion. The data obtained suggest that the release profile is characteristic of biodegradable matrices and diffusion-controlled delivery systems. Complete extraction of diflunisal from HA was achieved using PBS with pH 7.6 as a dissolution medium.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"224 9","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140489935","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}
Pub Date : 2024-01-22DOI: 10.33380/2305-2066-2024-13-1-1468
S. V. Gribanova, I. Udyanskaya, V. Yankova, T. Slonskaya, N. B. Epshtein, A. A. Zhukova, O. Plakhotnaya, V. N. Kuzina
Introduction. In modern medicine, the requirements for the quality of used materials are getting stricter. There is serious concern about bacterial and fungal contamination related to the use of silicone polymeric products, especially those that are in direct contact with human tissues and body fluids. In this regard, the issue of impregnating silicone medical products with various biologically active substances (BAS), particularly with antimicrobial properties, appears relevant.Aim. The research studies the relevance of adding BAS into silicone medical devices to improve their quality and prevent negative consequences of their use. The authors of the article aimed at proving prolonged release of the chosen BAS from silicone products during their contact with skin and the bacteriostatic effect emerging as a result of the BAS release. That required verifying the existence of BAS in the washouts from silicone disks, which, in turn, proves the fact that BAS initially distributed evenly in the volume of a silicone disk are capable of diffusing to the surface and then releasing from it under mechanical action, as well as when treating it with alcohol or alcohol-containing solutions.Materials and methods. Symdiol and bisabolol were selected as the BAS for this study due to their proved antibacterial, anti-inflammatory and moisturizing properties. Bisabolol and symdiol were used in the form of Dragosantol 100 and SymDiol 68T preparations correspondingly. Silicone disks (SDs), impregnated with BAS (0,2 % of the volume) were used as a simulation model of silicone liners. The BAS release from silicone liner models was assessed using highly sensitive chromatographic methods of thin-layer and gas-liquid chromatography.Results and discussion. The method of impregnating SDs with BAS was worked out, the optimal concentration of these substances to add them into the silicone base was selected. The release of the impregnated additives, as well as prolonged stable releasing effect, were confirmed. The data obtained during the experiment allows saying with confidence that the impregnated preparation (symdiol and bisabolol) releases from a SD even upon short and low-intensity mechanical contact with skin, which produces stable bacteriostatic effect on a wide range of microorganisms. The process of BAS release from SDs is also facilitated when treating the product periodically with alcohol-containing solutions, which is necessary according to the operating rules. The obtained results of the chromatographic research quite correlate with the data of the previous microbiological experiments regarding the studied topic. Release of the studied BAS from polymer products during their contact with the skin within the period of not less than 3 months justifies feasibility of adding these BAS into the silicone base.Conclusions. The study confirmed the release of biologically active substances from silicone medical products. Adding BAS into silicone liners undoubtedly improves
简介现代医学对所用材料的质量要求越来越严格。人们严重关注与使用硅聚合物产品有关的细菌和真菌污染问题,尤其是那些与人体组织和体液直接接触的产品。因此,在硅胶医疗产品中浸渍各种生物活性物质(BAS),特别是具有抗菌特性的物质,似乎具有现实意义。该研究探讨了在硅胶医疗器械中添加 BAS 的相关性,以提高其质量并防止其使用过程中产生负面影响。文章作者的目的是证明硅胶产品在与皮肤接触的过程中,所选 BAS 的长期释放以及 BAS 释放所产生的抑菌效果。这就需要验证硅胶盘的冲洗液中是否存在 BAS,这反过来又证明了一个事实:最初均匀分布在硅胶盘体积中的 BAS 能够扩散到表面,然后在机械作用下以及用酒精或含酒精的溶液处理硅胶盘时从表面释放出来。由于 Symdiol 和 bisabolol 具有公认的抗菌、消炎和保湿特性,因此被选为本研究的 BAS。双羟萘酸和双羟萘酸分别以 Dragosantol 100 和 SymDiol 68T 制剂的形式使用。浸渍了 BAS(占体积的 0.2%)的硅胶盘(SD)被用作硅胶衬垫的模拟模型。结果和讨论。研究了用 BAS 对 SDs 进行浸渍的方法,并选择了将这些物质添加到硅胶基材中的最佳浓度。实验证实了浸渍添加剂的释放效果以及长期稳定的释放效果。根据实验中获得的数据,我们可以肯定地说,浸渍制剂(symdiol 和 bisabolol)即使在与皮肤进行短时间和低强度的机械接触时也会从 SD 中释放出来,从而对多种微生物产生稳定的抑菌作用。根据操作规定,定期用含酒精的溶液处理 SD 产品也有助于 BAS 的释放过程。色谱研究的结果与之前有关研究主题的微生物实验数据十分吻合。在不少于 3 个月的时间内,所研究的 BAS 会在聚合物产品与皮肤接触的过程中释放出来,这证明在硅酮基料中添加这些 BAS 是可行的。研究证实了硅胶医疗产品中生物活性物质的释放。在硅胶衬里中添加 BAS 无疑会提高这些医疗产品的质量,这些产品可用于假肢和矫形器。
{"title":"Release Control of Biologically Active Substances from Simulation Model of Silicone Liners","authors":"S. V. Gribanova, I. Udyanskaya, V. Yankova, T. Slonskaya, N. B. Epshtein, A. A. Zhukova, O. Plakhotnaya, V. N. Kuzina","doi":"10.33380/2305-2066-2024-13-1-1468","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1468","url":null,"abstract":"Introduction. In modern medicine, the requirements for the quality of used materials are getting stricter. There is serious concern about bacterial and fungal contamination related to the use of silicone polymeric products, especially those that are in direct contact with human tissues and body fluids. In this regard, the issue of impregnating silicone medical products with various biologically active substances (BAS), particularly with antimicrobial properties, appears relevant.Aim. The research studies the relevance of adding BAS into silicone medical devices to improve their quality and prevent negative consequences of their use. The authors of the article aimed at proving prolonged release of the chosen BAS from silicone products during their contact with skin and the bacteriostatic effect emerging as a result of the BAS release. That required verifying the existence of BAS in the washouts from silicone disks, which, in turn, proves the fact that BAS initially distributed evenly in the volume of a silicone disk are capable of diffusing to the surface and then releasing from it under mechanical action, as well as when treating it with alcohol or alcohol-containing solutions.Materials and methods. Symdiol and bisabolol were selected as the BAS for this study due to their proved antibacterial, anti-inflammatory and moisturizing properties. Bisabolol and symdiol were used in the form of Dragosantol 100 and SymDiol 68T preparations correspondingly. Silicone disks (SDs), impregnated with BAS (0,2 % of the volume) were used as a simulation model of silicone liners. The BAS release from silicone liner models was assessed using highly sensitive chromatographic methods of thin-layer and gas-liquid chromatography.Results and discussion. The method of impregnating SDs with BAS was worked out, the optimal concentration of these substances to add them into the silicone base was selected. The release of the impregnated additives, as well as prolonged stable releasing effect, were confirmed. The data obtained during the experiment allows saying with confidence that the impregnated preparation (symdiol and bisabolol) releases from a SD even upon short and low-intensity mechanical contact with skin, which produces stable bacteriostatic effect on a wide range of microorganisms. The process of BAS release from SDs is also facilitated when treating the product periodically with alcohol-containing solutions, which is necessary according to the operating rules. The obtained results of the chromatographic research quite correlate with the data of the previous microbiological experiments regarding the studied topic. Release of the studied BAS from polymer products during their contact with the skin within the period of not less than 3 months justifies feasibility of adding these BAS into the silicone base.Conclusions. The study confirmed the release of biologically active substances from silicone medical products. Adding BAS into silicone liners undoubtedly improves ","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"66 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139606543","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}
Pub Date : 2024-01-19DOI: 10.33380/2305-2066-2024-13-1-1508
D. A. Andreev, E. I. Balakin, A. S. Samoilov, V. I. Pustovoit
Introduction. Long-term use of anthracyclines during cancer chemotherapy has been associated with the development of potentially life-threatening cardiotoxicity. Despite researches ongoing since the middle of the last century, approaches to the choice of therapy remain limited.Text. Doxorubicin currently is the most widely used chemotherapy. The leading side effect mechanism of the drug is the formation of reactive oxygen species in mitochondria with the mediated development of oxidative stress, which contributes to myocardial damage. However, despite the huge number of scientific papers devoted to various aspects of doxorubicin cardiotoxicity, its prevention and treatment, this issue requires detailed investigation in order to develop more advanced methods for early diagnosis and timely cardioprotective therapy.Conclusion. The current review discusses the pathogenetic mechanisms of cardiotoxicity associated with the use of doxorubicin chemotherapy. The pathogenesis of the cardiomyocytes death mechanism will provide an opportunity to develop new diagnostic and therapeutic approaches in the clinical practice.
{"title":"The Role of Doxorubicin in the Formation of Cardiotoxicity – Generally Accepted Statement. Part I. Prevalence and Mechanisms of Formation (Review)","authors":"D. A. Andreev, E. I. Balakin, A. S. Samoilov, V. I. Pustovoit","doi":"10.33380/2305-2066-2024-13-1-1508","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1508","url":null,"abstract":"Introduction. Long-term use of anthracyclines during cancer chemotherapy has been associated with the development of potentially life-threatening cardiotoxicity. Despite researches ongoing since the middle of the last century, approaches to the choice of therapy remain limited.Text. Doxorubicin currently is the most widely used chemotherapy. The leading side effect mechanism of the drug is the formation of reactive oxygen species in mitochondria with the mediated development of oxidative stress, which contributes to myocardial damage. However, despite the huge number of scientific papers devoted to various aspects of doxorubicin cardiotoxicity, its prevention and treatment, this issue requires detailed investigation in order to develop more advanced methods for early diagnosis and timely cardioprotective therapy.Conclusion. The current review discusses the pathogenetic mechanisms of cardiotoxicity associated with the use of doxorubicin chemotherapy. The pathogenesis of the cardiomyocytes death mechanism will provide an opportunity to develop new diagnostic and therapeutic approaches in the clinical practice.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"80 5","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139612826","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}
Pub Date : 2024-01-19DOI: 10.33380/2305-2066-2024-13-1-1630
A. V. Bondarev, E. T. Zhilyakova, N. Avtina, N. Demina, K. K. Razmakhnin
Introduction. Medical clays are polymineral sorbents with a predominance of the underlying clay mineral, the concentration of which determines the quality of mineral raw materials and its adsorption activity. One of the methods of improving the quality of mineral raw materials is its activation by means of ultrasonic treatment.Aim. To study the effect of ultrasound on the activation and adsorption activity of mineral sorbents.Materials and methods. Clinoptilolite mineral raw materials of the Kholinsky deposit, montmorillonite mineral raw materials of the Belgorod deposit and kaolinite mineral raw materials of the Eleninsky deposit were used as objects of research. A high-frequency UZDN-1 unit was used for ultrasonic treatment. Determination of adsorption activity was carried out by methylene blue.Results and discussion. The effect of ultrasound on the activation of mineral sorbents at an ultrasonic wave frequency of 40 kHz for five minutes has been studied. It was found that the average content of Clinoptilolite, taking into account all fractions in the clay of the Kholinsky deposit, increases by 20 %, the average content of Montmorillonite, taking into account all fractions in the clay of the Belgorod deposit, increases by 14 %, the average content of Kaolinite, taking into account all fractions in the clay of the Eleninsky deposit, increases by 18 %. The effect of ultrasound on the adsorption activity of mineral sorbents has been investigated. The use of ultrasonic treatment increases the adsorption activity of mineral sorbents by 12–19 %.Conclusion. The developed method of activation of mineral sorbents by ultrasonic treatment can be used to activate mineral sorbents by increasing the concentration of the underlying mineral (Clinoptilolite, Montmorillonite, Kaolinite), as well as increasing their adsorption activity.
{"title":"Ultrasonic Activation of Mineral Sorbents","authors":"A. V. Bondarev, E. T. Zhilyakova, N. Avtina, N. Demina, K. K. Razmakhnin","doi":"10.33380/2305-2066-2024-13-1-1630","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1630","url":null,"abstract":"Introduction. Medical clays are polymineral sorbents with a predominance of the underlying clay mineral, the concentration of which determines the quality of mineral raw materials and its adsorption activity. One of the methods of improving the quality of mineral raw materials is its activation by means of ultrasonic treatment.Aim. To study the effect of ultrasound on the activation and adsorption activity of mineral sorbents.Materials and methods. Clinoptilolite mineral raw materials of the Kholinsky deposit, montmorillonite mineral raw materials of the Belgorod deposit and kaolinite mineral raw materials of the Eleninsky deposit were used as objects of research. A high-frequency UZDN-1 unit was used for ultrasonic treatment. Determination of adsorption activity was carried out by methylene blue.Results and discussion. The effect of ultrasound on the activation of mineral sorbents at an ultrasonic wave frequency of 40 kHz for five minutes has been studied. It was found that the average content of Clinoptilolite, taking into account all fractions in the clay of the Kholinsky deposit, increases by 20 %, the average content of Montmorillonite, taking into account all fractions in the clay of the Belgorod deposit, increases by 14 %, the average content of Kaolinite, taking into account all fractions in the clay of the Eleninsky deposit, increases by 18 %. The effect of ultrasound on the adsorption activity of mineral sorbents has been investigated. The use of ultrasonic treatment increases the adsorption activity of mineral sorbents by 12–19 %.Conclusion. The developed method of activation of mineral sorbents by ultrasonic treatment can be used to activate mineral sorbents by increasing the concentration of the underlying mineral (Clinoptilolite, Montmorillonite, Kaolinite), as well as increasing their adsorption activity.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"20 5","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139613618","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}
Pub Date : 2024-01-19DOI: 10.33380/2305-2066-2024-13-1-1478
A. Samoylov, E. I. Balakin, V. I. Pustovoit
Introduction. Strokes remain the second leading cause of death and the third leading cause of disability. Additional serum biomarker testing should be used to better diagnose transient ischemic attack (TIA), but most neurospecific biomarkers have low prognostic specificity and sensitivity. Timely identification of TIA and differential diagnosis of stroke in the first hour will ensure a shorter period of patient recovery and reduce the risk of mortality and disability. Serum biomarker studies should be included to overcome the difficulty of diagnosing TIA.Text. Neurospecific biomarkers such as S100B, GFAP, and NSE are used to diagnose acute ischemic damage to glial cells and neurons. S100B and GFAP are detected in astrocytes and NSE in neurons and cells of the neuroendocrine system. Elevated serum concentrations of these biomarkers are associated with various pathological conditions such as strokes and brain injuries and other central nervous system (CNS) lesions. Dynamic monitoring of biomarker concentrations makes it possible to evaluate the efficacy of the ongoing therapy and to identify predictors of patient deterioration for prompt correction of therapeutic procedures. To create a diagnostic panel it is necessary to study metabolic processes in ischemic tissue, taking into account concomitant diagnoses and results of neuroimaging, and to use breakthrough advances in machine learning and big data.Conclusion. The review showed that none of the assessed biomarkers can be recommended for the diagnosis of cerebral circulation disorders, but the combination of several neurospecific biomarkers can significantly improve diagnostic efficiency and find application in the differential diagnosis of stroke, intracranial hematoma, and other brain lesions for the purpose of early pharmacotherapy of CNS lesions and as surrogate endpoints during clinical trials.
导言。脑卒中仍然是导致死亡的第二大原因和导致残疾的第三大原因。为更好地诊断短暂性脑缺血发作(TIA),应使用额外的血清生物标志物检测,但大多数神经特异性生物标志物的预后特异性和敏感性较低。在第一时间及时发现 TIA 并鉴别诊断卒中可确保缩短患者的恢复期,降低死亡和残疾风险。应纳入血清生物标志物研究,以克服诊断 TIA 的困难。S100B、GFAP 和 NSE 等神经特异性生物标志物可用于诊断神经胶质细胞和神经元的急性缺血性损伤。S100B 和 GFAP 可在星形胶质细胞中检测到,NSE 可在神经元和神经内分泌系统细胞中检测到。这些生物标记物的血清浓度升高与中风、脑损伤和其他中枢神经系统(CNS)病变等各种病理情况有关。对生物标志物浓度进行动态监测,可以评估正在进行的治疗的疗效,并确定病人病情恶化的预测因素,以便及时纠正治疗程序。要建立一个诊断面板,就必须研究缺血组织的代谢过程,同时考虑到伴随的诊断和神经影像学结果,并利用机器学习和大数据方面的突破性进展。综述显示,没有一种评估的生物标志物可推荐用于诊断脑循环障碍,但几种神经特异性生物标志物的组合可显著提高诊断效率,并可应用于中风、颅内血肿和其他脑部病变的鉴别诊断,以便对中枢神经系统病变进行早期药物治疗,并在临床试验中作为替代终点。
{"title":"Biomarkers of Brain Ischemia (Review)","authors":"A. Samoylov, E. I. Balakin, V. I. Pustovoit","doi":"10.33380/2305-2066-2024-13-1-1478","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1478","url":null,"abstract":"Introduction. Strokes remain the second leading cause of death and the third leading cause of disability. Additional serum biomarker testing should be used to better diagnose transient ischemic attack (TIA), but most neurospecific biomarkers have low prognostic specificity and sensitivity. Timely identification of TIA and differential diagnosis of stroke in the first hour will ensure a shorter period of patient recovery and reduce the risk of mortality and disability. Serum biomarker studies should be included to overcome the difficulty of diagnosing TIA.Text. Neurospecific biomarkers such as S100B, GFAP, and NSE are used to diagnose acute ischemic damage to glial cells and neurons. S100B and GFAP are detected in astrocytes and NSE in neurons and cells of the neuroendocrine system. Elevated serum concentrations of these biomarkers are associated with various pathological conditions such as strokes and brain injuries and other central nervous system (CNS) lesions. Dynamic monitoring of biomarker concentrations makes it possible to evaluate the efficacy of the ongoing therapy and to identify predictors of patient deterioration for prompt correction of therapeutic procedures. To create a diagnostic panel it is necessary to study metabolic processes in ischemic tissue, taking into account concomitant diagnoses and results of neuroimaging, and to use breakthrough advances in machine learning and big data.Conclusion. The review showed that none of the assessed biomarkers can be recommended for the diagnosis of cerebral circulation disorders, but the combination of several neurospecific biomarkers can significantly improve diagnostic efficiency and find application in the differential diagnosis of stroke, intracranial hematoma, and other brain lesions for the purpose of early pharmacotherapy of CNS lesions and as surrogate endpoints during clinical trials.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"44 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139612024","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}
Pub Date : 2024-01-19DOI: 10.33380/2305-2066-2024-13-1-1400
E. Bakhrushina, V. S. Pyzhov, P. Sakharova, N. Demina, I. Krasnyuk
Introduction. Nowadays block copolymers of PEO and PPO (poloxamers, pluronics, proxanols) are among the most popular polymers in the pharmaceutical and biotechnological industries. They can be applied as effective nonionic surfactants, biological membrane stabilizers, elements of targeted delivery systems, solubilizers, as well as excipients in the technology of traditional dosage forms – gelling agents, lubricants, etc. For the past fifty years, the world's largest manufacturer of poloxamers has been the German chemical concern BASF. However, today in the Russian Federation there is a risk of defects, which defines the relevance of import substitution of this excipient.Text. The purpose of this review is to highlight the experience of production and implementation of PEO and PPO block copolymers into novel Russian scientists’ developments, comparing them with the experience of foreign research groups, which is necessary to assess the potential for import substitution. PEO and PPO block copolymers have been known in the Soviet Union since the late 60s as far as they are mentioned in textbooks of 1964 and 1973. Domestic block copolymers of PEO and PPO have been used in the oil refining industry, as well as in some branches of light industry and in the decontamination of radioactive waste. The unique domestic synthesis of PEO and PPO block copolymers was established in 1978 on the basis of the "Orgsintez" factory. Soviet poloxamers were produced under the brand name "proxanol" in a wide range of ratios of EO and PO units and molecular weights. It should be noted that today in the Russian Federation, industrial batches of the solubilizer Emuxol 268, which is close in its properties to the well-known poloxamer 188, are still produced, and block copolymers with other ratios of EO and PO units are synthesized to order.Conclusion. According to the retrospective analysis, the modern Russian industry has enough experience and resources to establish the synthesis of PEO and PPO block copolymers necessary to produce drugs and to develop innovative delivery systems and drugs. Based on the materials of the systematic review, the most complete register of known brands of PEO and PPO block copolymers synthesized over the past 50 years in our country and in the world was compiled for the first time, with a detailed description of their physicochemical properties.
{"title":"Retrospective Analysis of Polyethylene Oxide and Polypropylene Oxide Block Copolymers Production and Industrial Applications (Review)","authors":"E. Bakhrushina, V. S. Pyzhov, P. Sakharova, N. Demina, I. Krasnyuk","doi":"10.33380/2305-2066-2024-13-1-1400","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1400","url":null,"abstract":"Introduction. Nowadays block copolymers of PEO and PPO (poloxamers, pluronics, proxanols) are among the most popular polymers in the pharmaceutical and biotechnological industries. They can be applied as effective nonionic surfactants, biological membrane stabilizers, elements of targeted delivery systems, solubilizers, as well as excipients in the technology of traditional dosage forms – gelling agents, lubricants, etc. For the past fifty years, the world's largest manufacturer of poloxamers has been the German chemical concern BASF. However, today in the Russian Federation there is a risk of defects, which defines the relevance of import substitution of this excipient.Text. The purpose of this review is to highlight the experience of production and implementation of PEO and PPO block copolymers into novel Russian scientists’ developments, comparing them with the experience of foreign research groups, which is necessary to assess the potential for import substitution. PEO and PPO block copolymers have been known in the Soviet Union since the late 60s as far as they are mentioned in textbooks of 1964 and 1973. Domestic block copolymers of PEO and PPO have been used in the oil refining industry, as well as in some branches of light industry and in the decontamination of radioactive waste. The unique domestic synthesis of PEO and PPO block copolymers was established in 1978 on the basis of the \"Orgsintez\" factory. Soviet poloxamers were produced under the brand name \"proxanol\" in a wide range of ratios of EO and PO units and molecular weights. It should be noted that today in the Russian Federation, industrial batches of the solubilizer Emuxol 268, which is close in its properties to the well-known poloxamer 188, are still produced, and block copolymers with other ratios of EO and PO units are synthesized to order.Conclusion. According to the retrospective analysis, the modern Russian industry has enough experience and resources to establish the synthesis of PEO and PPO block copolymers necessary to produce drugs and to develop innovative delivery systems and drugs. Based on the materials of the systematic review, the most complete register of known brands of PEO and PPO block copolymers synthesized over the past 50 years in our country and in the world was compiled for the first time, with a detailed description of their physicochemical properties.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"99 44","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139612367","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}
Pub Date : 2024-01-12DOI: 10.33380/2305-2066-2024-13-1-1615
L. Nikolaeva, E. Sanarova, A. Lantsova
Introduction. The search for new methods of therapy for non-small cell lung cancer (NSCLC) is an urgent task of modern science. Gefitinib is a targeted drug widely used in the treatment of NSCLC in patients with a mutation in the epidermal growth factor receptor tyrosine kinase domain. However, using of gefitinib and other drugs from the group of tyrosine kinase inhibitors is to limited by rapidly developing resistance, for this reason finding of a ways overcome drug resistance is actual part of research interests.Text. The review is devoted to the use of gefitinib in modern developments: introduction to various targeted delivery systems (liposomes, micelles, microspheres, etc.), studying it in combination with other chemotherapeutic agents, as well as in combination with photo- or thermosensitive compounds in various micro- and nanostructured complexes.Conclusion. As a result of the analysis of literature data, it was shown that, despite the fact that gefitinib is a first-generation drug, foreign and Russian researchers consider it quite promising for further use in the treatment of NSCLC. At the same time, developments are being carried out both in the field of expanding combination therapy and in the field of creating complex structures of targeted action, into which, in addition to gefitinib, photosensitizers or other compounds with photo- or thermosensitive effects are introduced.
{"title":"Gefitinib: Combination Therapy and Complex Delivery Systems (Review)","authors":"L. Nikolaeva, E. Sanarova, A. Lantsova","doi":"10.33380/2305-2066-2024-13-1-1615","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1615","url":null,"abstract":"Introduction. The search for new methods of therapy for non-small cell lung cancer (NSCLC) is an urgent task of modern science. Gefitinib is a targeted drug widely used in the treatment of NSCLC in patients with a mutation in the epidermal growth factor receptor tyrosine kinase domain. However, using of gefitinib and other drugs from the group of tyrosine kinase inhibitors is to limited by rapidly developing resistance, for this reason finding of a ways overcome drug resistance is actual part of research interests.Text. The review is devoted to the use of gefitinib in modern developments: introduction to various targeted delivery systems (liposomes, micelles, microspheres, etc.), studying it in combination with other chemotherapeutic agents, as well as in combination with photo- or thermosensitive compounds in various micro- and nanostructured complexes.Conclusion. As a result of the analysis of literature data, it was shown that, despite the fact that gefitinib is a first-generation drug, foreign and Russian researchers consider it quite promising for further use in the treatment of NSCLC. At the same time, developments are being carried out both in the field of expanding combination therapy and in the field of creating complex structures of targeted action, into which, in addition to gefitinib, photosensitizers or other compounds with photo- or thermosensitive effects are introduced.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"3 5","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139532365","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}