Pub Date : 2023-09-01DOI: 10.33320/maced.pharm.bull.2023.69.03.142
Sanja Dukovska, Elizabeta Atanaskova, Maja Simonoska Crcarevska, Marija Glavas Dodov, Katerina Goracinova, Nikola Geskovski
Film coating of solid dosage forms in pharmaceutical manufacturing is carried out using range of equipment, process parameters and coating formulations to achieve the quality target profile of the dosage form. Besides for aesthetic reasons, film coatings are mostly applied to modify the dissolution behaviour of active pharmaceutical ingredients. Currently, a number of coater types are used in pharmaceutical industry, including drum, fluid bed, rotary and continuous coaters. The end-point of coating process is usually defined by the amount of applied coating dispersion or weight gain of coated dosage forms. However, these measurements provide little information on coating quality attributes such as coating thickness, uniformity etc. Other monitoring techniques are scanning electron microscopy, Near infrared (NIR) or Fourier transform infrared spectroscopy (FTIR) (Hasar et al., 2013). The aim of this research was to examine the suitability of Wurster-Fluid bed technique for functional Eudragit L100 coating on tablet cores by monitoring critical attributes during the process.
{"title":"Suitability of Wurster-Fluid Bed technique for functional Eudragit L-100 coating on tablet cores","authors":"Sanja Dukovska, Elizabeta Atanaskova, Maja Simonoska Crcarevska, Marija Glavas Dodov, Katerina Goracinova, Nikola Geskovski","doi":"10.33320/maced.pharm.bull.2023.69.03.142","DOIUrl":"https://doi.org/10.33320/maced.pharm.bull.2023.69.03.142","url":null,"abstract":"Film coating of solid dosage forms in pharmaceutical manufacturing is carried out using range of equipment, process parameters and coating formulations to achieve the quality target profile of the dosage form. Besides for aesthetic reasons, film coatings are mostly applied to modify the dissolution behaviour of active pharmaceutical ingredients. Currently, a number of coater types are used in pharmaceutical industry, including drum, fluid bed, rotary and continuous coaters. The end-point of coating process is usually defined by the amount of applied coating dispersion or weight gain of coated dosage forms. However, these measurements provide little information on coating quality attributes such as coating thickness, uniformity etc. Other monitoring techniques are scanning electron microscopy, Near infrared (NIR) or Fourier transform infrared spectroscopy (FTIR) (Hasar et al., 2013). The aim of this research was to examine the suitability of Wurster-Fluid bed technique for functional Eudragit L100 coating on tablet cores by monitoring critical attributes during the process.","PeriodicalId":30550,"journal":{"name":"Makedonsko Farmacevtski Bilten","volume":"28 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135637645","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 : 2023-09-01DOI: 10.33320/maced.pharm.bull.2023.69.03.148
Ivana Stojanovska, Toshe Rafajlov, Beti Djurdjic, Lina Livrinska, Maja Simonoska Crcarevska, Katerina Goracinova, Selestina Gorgieva, Vineta Vuksanovich, Nikola Geskovski
Microbial infections are one of the prime causes of morbidity and mortality and have become a significant issue within the medical field. A considerable number of infections are currently linked to antibiotic-resistant bacteria, primarily due to the inappropriate and excessive utilization of antibiotics. Nanotechnology, employing materials at the nanoscale, is progressively finding applications in clinical settings, particularly as a novel approach for addressing infectious diseases. Among these nanoscale materials, nanoparticles (NPs) have exhibited extensive antibacterial capabilities, effectively targeting both Gram-positive and Gram-negative bacteria. The main rationale behind considering NPs as an alternative to antibiotics lies in their ability to combat microbial drug resistance, presenting a promising solution in certain cases. Over the last twenty years, researchers have been drawn to the beneficial characteristics of chitosan (CS). This compound is non-toxic, biocompatible, and edible, making it highly appealing for various applications. Moreover, CS exhibits antimicrobial properties. In particular, nanoparticles based on CS have displayed favorable antibacterial effectiveness and their full potential is not yet achieved (Al-Zahrani et al., 2021). The aim of our study was to prepare Gentamycin sulphate loaded CS nanoparticles and screen the main effects of the formulation and process parameters on their physical properties (particle size, zeta potential), in a One Factor At a Time (OFAT) study.
{"title":"Screening the effects of process and formulation factors upon the physical properties of Chitosan-TPP nanoparticles as drug delivery carriers for Gentamycin sulphate","authors":"Ivana Stojanovska, Toshe Rafajlov, Beti Djurdjic, Lina Livrinska, Maja Simonoska Crcarevska, Katerina Goracinova, Selestina Gorgieva, Vineta Vuksanovich, Nikola Geskovski","doi":"10.33320/maced.pharm.bull.2023.69.03.148","DOIUrl":"https://doi.org/10.33320/maced.pharm.bull.2023.69.03.148","url":null,"abstract":"Microbial infections are one of the prime causes of morbidity and mortality and have become a significant issue within the medical field. A considerable number of infections are currently linked to antibiotic-resistant bacteria, primarily due to the inappropriate and excessive utilization of antibiotics. Nanotechnology, employing materials at the nanoscale, is progressively finding applications in clinical settings, particularly as a novel approach for addressing infectious diseases. Among these nanoscale materials, nanoparticles (NPs) have exhibited extensive antibacterial capabilities, effectively targeting both Gram-positive and Gram-negative bacteria. The main rationale behind considering NPs as an alternative to antibiotics lies in their ability to combat microbial drug resistance, presenting a promising solution in certain cases. Over the last twenty years, researchers have been drawn to the beneficial characteristics of chitosan (CS). This compound is non-toxic, biocompatible, and edible, making it highly appealing for various applications. Moreover, CS exhibits antimicrobial properties. In particular, nanoparticles based on CS have displayed favorable antibacterial effectiveness and their full potential is not yet achieved (Al-Zahrani et al., 2021). The aim of our study was to prepare Gentamycin sulphate loaded CS nanoparticles and screen the main effects of the formulation and process parameters on their physical properties (particle size, zeta potential), in a One Factor At a Time (OFAT) study.","PeriodicalId":30550,"journal":{"name":"Makedonsko Farmacevtski Bilten","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135639676","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 : 2023-09-01DOI: 10.33320/maced.pharm.bull.2023.69.03.145
Amina Tucak-Smajić, Ivana Ruseska, Edina Vranić, Andreas Zimmer
MicroRNAs (miRNAs) are important regulators of gene expression in cells. However, their application in gene therapy is limited by obstacles such as poor cellular uptake and instability (Mendonça et al., 2023). To overcome these limitations, cationic nanostructured lipid carriers (cNLCs) as delivery systems for miRNAs are developed. cNLCs protect and stabilize miRNAs, and also enhance cellular uptake, which results in effective nucleic acid-based therapy. Another approach, found in literature, to enhance cellular uptake is coating particles with human serum albumin (HSA) (Liu et al., 2012). Therefore, the effect of functionalization of miRNA-cNLC complexes with HSA was investigated. The physicochemical properties of uncoated and HSA-coated complexes were compared in terms of particle size, size distribution, surface charge, topography, and cellular uptake in 3T3-L1 mouse embryonic fibroblasts and MCF-7 human breast cancer cells.
{"title":"Functionalization of miRNA—cNLC complexes","authors":"Amina Tucak-Smajić, Ivana Ruseska, Edina Vranić, Andreas Zimmer","doi":"10.33320/maced.pharm.bull.2023.69.03.145","DOIUrl":"https://doi.org/10.33320/maced.pharm.bull.2023.69.03.145","url":null,"abstract":"MicroRNAs (miRNAs) are important regulators of gene expression in cells. However, their application in gene therapy is limited by obstacles such as poor cellular uptake and instability (Mendonça et al., 2023). To overcome these limitations, cationic nanostructured lipid carriers (cNLCs) as delivery systems for miRNAs are developed. cNLCs protect and stabilize miRNAs, and also enhance cellular uptake, which results in effective nucleic acid-based therapy. Another approach, found in literature, to enhance cellular uptake is coating particles with human serum albumin (HSA) (Liu et al., 2012). Therefore, the effect of functionalization of miRNA-cNLC complexes with HSA was investigated. The physicochemical properties of uncoated and HSA-coated complexes were compared in terms of particle size, size distribution, surface charge, topography, and cellular uptake in 3T3-L1 mouse embryonic fibroblasts and MCF-7 human breast cancer cells.","PeriodicalId":30550,"journal":{"name":"Makedonsko Farmacevtski Bilten","volume":"59 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135637637","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 : 2023-09-01DOI: 10.33320/maced.pharm.bull.2023.69.03.119
Jindra Valentová, Andrea Baránková, Desana Matušová
Salidroside (SAL), a phenylpropanoid glycoside extracted from the root of Rhodiola rosea, is known for its pharmacological properties such as antioxidation, antiinflammation, neuroprotective, anti-cancer, and cardioprotective properties (Ching et al., 2015; Zhao et al., 2021). Salidroside is effective in suppressing solar ultraviolet-induced skin inflammation (Wu et al., 2016) and prevents skin carcinogenesis (Kong and Xu, 2016). The hydrophilicity of SAL leads to poor skin permeability, therefore different liposomal nanocarriers for SAL were tested (Zhang, 2015). To improve the SAL transdermal delivery, the transdermal patches containing the dry extract from Rhodiola rosea were formulated. The patch adhesion and dissolution of SAL were tested. The most promising formulations were matrix systems containing two different combinations: gelatine with chitosan or pectin with polyethylene oxide (Haršányová et al., 2018). Based on previous results, the aim of our work was the evaluation of transdermal permeation of SAL from Rhodiola rosea extract
{"title":"In vitro transdermal delivery and skin metabolism of salidroside from Rhodiola rosea extract","authors":"Jindra Valentová, Andrea Baránková, Desana Matušová","doi":"10.33320/maced.pharm.bull.2023.69.03.119","DOIUrl":"https://doi.org/10.33320/maced.pharm.bull.2023.69.03.119","url":null,"abstract":"Salidroside (SAL), a phenylpropanoid glycoside extracted from the root of Rhodiola rosea, is known for its pharmacological properties such as antioxidation, antiinflammation, neuroprotective, anti-cancer, and cardioprotective properties (Ching et al., 2015; Zhao et al., 2021). Salidroside is effective in suppressing solar ultraviolet-induced skin inflammation (Wu et al., 2016) and prevents skin carcinogenesis (Kong and Xu, 2016). The hydrophilicity of SAL leads to poor skin permeability, therefore different liposomal nanocarriers for SAL were tested (Zhang, 2015). To improve the SAL transdermal delivery, the transdermal patches containing the dry extract from Rhodiola rosea were formulated. The patch adhesion and dissolution of SAL were tested. The most promising formulations were matrix systems containing two different combinations: gelatine with chitosan or pectin with polyethylene oxide (Haršányová et al., 2018). Based on previous results, the aim of our work was the evaluation of transdermal permeation of SAL from Rhodiola rosea extract","PeriodicalId":30550,"journal":{"name":"Makedonsko Farmacevtski Bilten","volume":"85 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135200761","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 : 2023-09-01DOI: 10.33320/maced.pharm.bull.2023.69.03.117
Marjan Velkovski, Damjan Shushleski, Irena Slaveska Spirevska
Ciprofloxacin belongs to the group of fluoroquinolone antibiotics, used to treat a number of bacterial infections. This includes bone and joint infections, intra-abdominal infections, certain types of infectious diarrhea, respiratory tract infections, skin infections, typhoid fever, and urinary tract infections, among others (Solomkin et al. 2010). Ciprofloxacin occupies an important role in treatment guidelines issued by major medical societies for the treatment of serious infections, especially those likely to be caused by Gramnegative bacteria, including Pseudomonas aeruginosa. For example, ciprofloxacin in combination with metronidazole is one of several first-line antibiotic regimens recommended by the Infectious Diseases Society of America for the treatment of communityacquired abdominal infections in adults (Solomkin et al., 2010). It also features prominently in treatment guidelines for acute pyelonephritis, complicated or hospital-acquired urinary tract infection, acute or chronic prostatitis (Grabe et al., 2013). All pharmaceutical forms are subject to chemical and microbiological quality control. A microbiological quality control method that will be used in routine for determination of product microbiological purity must be subject of validation. Microbiological quality control parameters for Ciprofloxacin 500 mg film-coated tablet as non-aqueous pharmaceutical preparation for oral use are: Total Aerobic Microbial Count (TAMC), Total Yeasts and Molds Count (TYMC) and Absence of Escherichia coli (Ph.Eur. 10.0, 2019). Мaterials and methods
{"title":"Method suitability validation for determination of microbiological purity of Ciprofloxacin film-coated tablet","authors":"Marjan Velkovski, Damjan Shushleski, Irena Slaveska Spirevska","doi":"10.33320/maced.pharm.bull.2023.69.03.117","DOIUrl":"https://doi.org/10.33320/maced.pharm.bull.2023.69.03.117","url":null,"abstract":"Ciprofloxacin belongs to the group of fluoroquinolone antibiotics, used to treat a number of bacterial infections. This includes bone and joint infections, intra-abdominal infections, certain types of infectious diarrhea, respiratory tract infections, skin infections, typhoid fever, and urinary tract infections, among others (Solomkin et al. 2010). Ciprofloxacin occupies an important role in treatment guidelines issued by major medical societies for the treatment of serious infections, especially those likely to be caused by Gramnegative bacteria, including Pseudomonas aeruginosa. For example, ciprofloxacin in combination with metronidazole is one of several first-line antibiotic regimens recommended by the Infectious Diseases Society of America for the treatment of communityacquired abdominal infections in adults (Solomkin et al., 2010). It also features prominently in treatment guidelines for acute pyelonephritis, complicated or hospital-acquired urinary tract infection, acute or chronic prostatitis (Grabe et al., 2013). All pharmaceutical forms are subject to chemical and microbiological quality control. A microbiological quality control method that will be used in routine for determination of product microbiological purity must be subject of validation. Microbiological quality control parameters for Ciprofloxacin 500 mg film-coated tablet as non-aqueous pharmaceutical preparation for oral use are: Total Aerobic Microbial Count (TAMC), Total Yeasts and Molds Count (TYMC) and Absence of Escherichia coli (Ph.Eur. 10.0, 2019). Мaterials and methods","PeriodicalId":30550,"journal":{"name":"Makedonsko Farmacevtski Bilten","volume":"194 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135249536","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 : 2023-09-01DOI: 10.33320/maced.pharm.bull.2023.69.03.132
Filip Djokoski, Marija Hiljadnikova-Bajro
It is now well known that the human microbiome significantly impacts the development and support of fundamental physiological elements such as metabolism and immunity, influencing even one’s behavior. Dysbiotic microbiota is significantly involved in the etiopathogenesis of many diseases including neoplasia, affecting the processes of tumor initiation and progression, either by direct action on the tumor cells or indirect influence via the individual's immune system, This paper addresses the current knowledge about the impact of the human microbiome on the efficacy of cancer immunotherapy (CI) based on immune checkpoint inhibitors-(ICI) and the possible application of the microbiota as a novel therapy for cancer.
{"title":"The Impact of the Human Microbiome on Cancer Immunotherapy","authors":"Filip Djokoski, Marija Hiljadnikova-Bajro","doi":"10.33320/maced.pharm.bull.2023.69.03.132","DOIUrl":"https://doi.org/10.33320/maced.pharm.bull.2023.69.03.132","url":null,"abstract":"It is now well known that the human microbiome significantly impacts the development and support of fundamental physiological elements such as metabolism and immunity, influencing even one’s behavior. Dysbiotic microbiota is significantly involved in the etiopathogenesis of many diseases including neoplasia, affecting the processes of tumor initiation and progression, either by direct action on the tumor cells or indirect influence via the individual's immune system, This paper addresses the current knowledge about the impact of the human microbiome on the efficacy of cancer immunotherapy (CI) based on immune checkpoint inhibitors-(ICI) and the possible application of the microbiota as a novel therapy for cancer.","PeriodicalId":30550,"journal":{"name":"Makedonsko Farmacevtski Bilten","volume":"3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134918136","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 : 2023-09-01DOI: 10.33320/maced.pharm.bull.2023.69.03.111
Olivera Blažeska, Natasa Anevska-Sojanovska, Jelena Lazova
The purpose of this study is to explain why and how to give an understandable concept for the implementation of a trustworthy GC-FID-HS method which will be used for the determination of residual ethanol in solid dosage form (tablets). The tablets drug product belongs to a class of medications benzodiazepines which are used to treat panic attacks with or without agoraphobia, anxiety states of different severity, including those associated with depression, agitation, restlessness and tension accompanied with or without psychosomatic symptoms as well as anxiety which accompanies depressive disorder. As a central nervous system depressant, ethanol is one of the most commonly consumed psychoactive drugs. Ethanol serves many purposes in medicines, as a solvent, preservative, or cutaneous penetration enhancer. Although, ethanol can impair cognitive and psychomotor functions so exposure to ethanol when used as an excipient in medicines is usually limited. Exposure is affected by the dose volume and weight of the patient. This solvent was evaluated for its possible risk to human health. Therefore, the analysis of ethanol is a necessary tool for the standard management of prescribed drugs (Umamheswari et al., 2021). The concentration of residual ethanol should not exceed the limit prescribed in the ICH guidelines for Class 3 residual solvents (ICH Q3C (R6), 2018; ICH Q3C (R8), 2020). Ethanol anhydrous was used for the preparation of binder solution during the manufacturing process of tablets but it cannot be completely removed by common manufacturing techniques so it was necessary to validate sensitive and accurate method for estimation of ethanol. Some methods according to several literary data, have been established for the analysis of ethanol, using a mix of several diluents as dissolving solutions (Alahmad et al., 2013) or solid phase microextraction headspace method (Hanwar et al., 2022). However, it is taking too much time and money. This GCFID-HS method is considered to be a less expensive and fast method for the estimation of ethanol in tablets and it has been widely employed in the analysis. The method was validated according to ICH guidelines Q2 (R2), following various parameters such as specificity, linearity, precision, accuracy, robustness, the limit of quantification (LOQ) and the limit of detection (LOD). The objective of the development and validation of an analytical procedure is to show that it is suitable for the intended purpose (ICH, 2022).
{"title":"GC-FID-HS method development and validation for quantitative estimation of ethanol as residual in tablets drug product from the class of benzodiazepine","authors":"Olivera Blažeska, Natasa Anevska-Sojanovska, Jelena Lazova","doi":"10.33320/maced.pharm.bull.2023.69.03.111","DOIUrl":"https://doi.org/10.33320/maced.pharm.bull.2023.69.03.111","url":null,"abstract":"The purpose of this study is to explain why and how to give an understandable concept for the implementation of a trustworthy GC-FID-HS method which will be used for the determination of residual ethanol in solid dosage form (tablets). The tablets drug product belongs to a class of medications benzodiazepines which are used to treat panic attacks with or without agoraphobia, anxiety states of different severity, including those associated with depression, agitation, restlessness and tension accompanied with or without psychosomatic symptoms as well as anxiety which accompanies depressive disorder. As a central nervous system depressant, ethanol is one of the most commonly consumed psychoactive drugs. Ethanol serves many purposes in medicines, as a solvent, preservative, or cutaneous penetration enhancer. Although, ethanol can impair cognitive and psychomotor functions so exposure to ethanol when used as an excipient in medicines is usually limited. Exposure is affected by the dose volume and weight of the patient. This solvent was evaluated for its possible risk to human health. Therefore, the analysis of ethanol is a necessary tool for the standard management of prescribed drugs (Umamheswari et al., 2021). The concentration of residual ethanol should not exceed the limit prescribed in the ICH guidelines for Class 3 residual solvents (ICH Q3C (R6), 2018; ICH Q3C (R8), 2020). Ethanol anhydrous was used for the preparation of binder solution during the manufacturing process of tablets but it cannot be completely removed by common manufacturing techniques so it was necessary to validate sensitive and accurate method for estimation of ethanol. Some methods according to several literary data, have been established for the analysis of ethanol, using a mix of several diluents as dissolving solutions (Alahmad et al., 2013) or solid phase microextraction headspace method (Hanwar et al., 2022). However, it is taking too much time and money. This GCFID-HS method is considered to be a less expensive and fast method for the estimation of ethanol in tablets and it has been widely employed in the analysis. The method was validated according to ICH guidelines Q2 (R2), following various parameters such as specificity, linearity, precision, accuracy, robustness, the limit of quantification (LOQ) and the limit of detection (LOD). The objective of the development and validation of an analytical procedure is to show that it is suitable for the intended purpose (ICH, 2022).","PeriodicalId":30550,"journal":{"name":"Makedonsko Farmacevtski Bilten","volume":"307 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135200752","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 : 2023-09-01DOI: 10.33320/maced.pharm.bull.2023.69.03.130
Valentina Gocić, Ana Marković, Jelena Lazarević, Andrija Šmelcerović
Chalcones represent a class of bioactive, naturally occurring compounds, consisting of two aromatic rings (ring A and ring B) linked by α,β-unsaturated three-carbon chain (Table 1). In nature, chalcones are abundant in fruits, vegetables and various plants, many of which have found their place in traditional herbal medicine for the therapy of various medical conditions (Orlikova et al., 2011). Chalcone derivatives, either from natural sources or synthetically obtained, have demonstrated numerous bioactivities, and are considered as privileged scaffolds in medicinal chemistry. It has been shown that this group of compounds exerts antioxidant, antineoplastic, antiangiogenic, hypolipidemic, antimicrobial, antiinflammatory, tyrosine inhibitory, vasorelaxant and other activities. Chalcones have also been reported to possess enzyme inhibitory activities towards numerous pharmacologically significant enzymes including cholinesterases, xanthine oxidase, cyclooxygenase, lipoxygenase, etc. (Zhuang et al., 2017). Deoxyribonuclease I (DNase I) is one of the most important enzymes in the human body which catalyzes DNA hydrolysis forming 5'-oligonucleotides. This enzyme is one of the main nucleases responsible for DNA fragmentation during programmed cell death (apoptosis) (Oliveri et al., 2001; Samejima and Earnshaw, 2005). Elevated levels of DNase I can lead to increased DNA fragmentation and excessive cell death, thus contributing to the development of numerous pathological conditions (cardiovascular, autoimmune, neurodegenerative) (Oliveri et al., 2001). Having in mind the pathophysiological importance of DNase I, the relatively small number of known organic inhibitors of this enzyme, as well as the fact that there is no inhibitor defined as a "gold standard", there is a need for finding new efficient DNase I inhibitors. To the best of our knowledge, there is no information of chalcones as DNase I inhibitors, therefore this experiment represents an entry into an unexplored field which will hopefully result in increased interest for further research on this topic and discovery of new active chalcone structures.
{"title":"Evaluation of DNase I inhibitory activity on synthetic halogenated chalcone derivatives","authors":"Valentina Gocić, Ana Marković, Jelena Lazarević, Andrija Šmelcerović","doi":"10.33320/maced.pharm.bull.2023.69.03.130","DOIUrl":"https://doi.org/10.33320/maced.pharm.bull.2023.69.03.130","url":null,"abstract":"Chalcones represent a class of bioactive, naturally occurring compounds, consisting of two aromatic rings (ring A and ring B) linked by α,β-unsaturated three-carbon chain (Table 1). In nature, chalcones are abundant in fruits, vegetables and various plants, many of which have found their place in traditional herbal medicine for the therapy of various medical conditions (Orlikova et al., 2011). Chalcone derivatives, either from natural sources or synthetically obtained, have demonstrated numerous bioactivities, and are considered as privileged scaffolds in medicinal chemistry. It has been shown that this group of compounds exerts antioxidant, antineoplastic, antiangiogenic, hypolipidemic, antimicrobial, antiinflammatory, tyrosine inhibitory, vasorelaxant and other activities. Chalcones have also been reported to possess enzyme inhibitory activities towards numerous pharmacologically significant enzymes including cholinesterases, xanthine oxidase, cyclooxygenase, lipoxygenase, etc. (Zhuang et al., 2017). Deoxyribonuclease I (DNase I) is one of the most important enzymes in the human body which catalyzes DNA hydrolysis forming 5'-oligonucleotides. This enzyme is one of the main nucleases responsible for DNA fragmentation during programmed cell death (apoptosis) (Oliveri et al., 2001; Samejima and Earnshaw, 2005). Elevated levels of DNase I can lead to increased DNA fragmentation and excessive cell death, thus contributing to the development of numerous pathological conditions (cardiovascular, autoimmune, neurodegenerative) (Oliveri et al., 2001). Having in mind the pathophysiological importance of DNase I, the relatively small number of known organic inhibitors of this enzyme, as well as the fact that there is no inhibitor defined as a \"gold standard\", there is a need for finding new efficient DNase I inhibitors. To the best of our knowledge, there is no information of chalcones as DNase I inhibitors, therefore this experiment represents an entry into an unexplored field which will hopefully result in increased interest for further research on this topic and discovery of new active chalcone structures.","PeriodicalId":30550,"journal":{"name":"Makedonsko Farmacevtski Bilten","volume":"76 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134964092","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}
Essential oils are widely targeted for their properties, such as antimicrobial, antiparasitic, insecticidal and repellent actions, among other therapeutic applications on which studies have been based (Tidori Miura et al., 2021) Allelopathy is defined as the effect(s) of one plant on other plant (s) through the release of chemical compounds (allelochemicals) in the environment by leaching, exudation, volatilization (release of essential oils), or decomposition (El Sawia et al., 2019) For this study were used the commercial essential oils of Origanum Vulgaris and Thymus Vulgaris. The purpose of this study was the evaluation of the ecotoxicological activity of these essential oils.
{"title":"Allelopathy, cardiotoxicity and lethality bioassays of essential oils","authors":"Enkelejda Goci, Entela Haloci, Claudio Ferrante, Bleona Pasha","doi":"10.33320/maced.pharm.bull.2023.69.03.123","DOIUrl":"https://doi.org/10.33320/maced.pharm.bull.2023.69.03.123","url":null,"abstract":"Essential oils are widely targeted for their properties, such as antimicrobial, antiparasitic, insecticidal and repellent actions, among other therapeutic applications on which studies have been based (Tidori Miura et al., 2021) Allelopathy is defined as the effect(s) of one plant on other plant (s) through the release of chemical compounds (allelochemicals) in the environment by leaching, exudation, volatilization (release of essential oils), or decomposition (El Sawia et al., 2019) For this study were used the commercial essential oils of Origanum Vulgaris and Thymus Vulgaris. The purpose of this study was the evaluation of the ecotoxicological activity of these essential oils.","PeriodicalId":30550,"journal":{"name":"Makedonsko Farmacevtski Bilten","volume":"22 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135200759","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 : 2023-09-01DOI: 10.33320/maced.pharm.bull.2023.69.03.121
Bisera Jurišić Dukovski, Josip Ljubica, Petra Kocbek, Luka Bočkor, Ivan Pepić, Anita Hafner, Jasmina Lovrić
In the development of topical ophthalmic formulations, an important aspect of characterization is the study of the effect of the formulation on the corneal epithelium. The most extensively characterized human cell line used in corneal biocompatibility studies is the immortalized human corneal epithelial cell line (HCE-T) (Juretić et al., 2017). Most in vitro biocompatibility studies are currently performed with cells cultured in a twodimensional (2D) environment (Fitzgerald et al., 2015), which does not accurately reflect the structure of the corneal epithelium in vivo. The use of such inappropriate experimental tools may lead to misleading conclusions about the biocompatibility of investigated formulations. The objective of this research was to develop a threedimensional (3D) HCE-T cell model grown on 96-well insert plates. Such model simulates 3D structure of corneal epithelium and would enable an improved in vitro biocompatibility screening in terms of throughput and robustness in the development of topical ophthalmic formulations.
{"title":"Development of a 3D corneal epithelial model for early biocompatibility screening of topical ophthalmic formulations","authors":"Bisera Jurišić Dukovski, Josip Ljubica, Petra Kocbek, Luka Bočkor, Ivan Pepić, Anita Hafner, Jasmina Lovrić","doi":"10.33320/maced.pharm.bull.2023.69.03.121","DOIUrl":"https://doi.org/10.33320/maced.pharm.bull.2023.69.03.121","url":null,"abstract":"In the development of topical ophthalmic formulations, an important aspect of characterization is the study of the effect of the formulation on the corneal epithelium. The most extensively characterized human cell line used in corneal biocompatibility studies is the immortalized human corneal epithelial cell line (HCE-T) (Juretić et al., 2017). Most in vitro biocompatibility studies are currently performed with cells cultured in a twodimensional (2D) environment (Fitzgerald et al., 2015), which does not accurately reflect the structure of the corneal epithelium in vivo. The use of such inappropriate experimental tools may lead to misleading conclusions about the biocompatibility of investigated formulations. The objective of this research was to develop a threedimensional (3D) HCE-T cell model grown on 96-well insert plates. Such model simulates 3D structure of corneal epithelium and would enable an improved in vitro biocompatibility screening in terms of throughput and robustness in the development of topical ophthalmic formulations.","PeriodicalId":30550,"journal":{"name":"Makedonsko Farmacevtski Bilten","volume":"77 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135200765","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}