Karina Sommerfeld-Klatta, Magdalena Łukasik-Głębocka, Sylwia Kobyłka, B. Zielińska-Psuja
Valproic acid (VPA) is a broad-spectrum anticonvulsant drug. Its mechanism of action includes enhancing GABAergic transmission, blocking voltage-gated sodium channels, and affecting dopaminergic and serotonergic transmission (1). The mechanism of VPA toxicity, including its effects on the liver, is not fully known. It is assumed that oxidative stress and/or reactive products of drug biotransformation are responsible for its hepatotoxicity (2). The aim of the study was to verify the hypothesis concerning the influence of valproic acid and its metabolite, 2-propyl-4-pentenoic acid (4-en VPA) on the antioxidant status of patients treated with (VPA-T) and poisoned with valproic acid (VPA-P). The VPA-P group was divided into patients with (VPA-Ptox) and without (VPA-Pnon) toxic symptoms observed during the hospitalization. Oxidative stress was assessed using markers, such as antioxidant potential (FRAP) and reduced and oxidised glutathione (GSH/GSSG) ratio were measured in the plasma of the study patients. The obtained results showed statistically significant differences between the concentrations of the drug and its active metabolite levels in the VPA-T and VPA-P groups. In the VPA-P group, the increase of the level of 4-en VPA in the plasma correlated with the increase of the concentration of the drug. The influence of VPA on the antioxidant balance in both groups of patients was demonstrated. The plasma antioxidant potential of FRAP decreased with increasing valproic acid concentrations in the VPA-Ptox group. The lowest concentrations of GSH/GSSG ratio were found in the VPA-Pnon group, without symptoms of intoxication during hospitalization.
{"title":"The impact of valproic acid and 2-propyl-4-pentenoic acid on antioxidant status measured by GSH/GSSG ratio and FRAP levels in acute and chronic exposure","authors":"Karina Sommerfeld-Klatta, Magdalena Łukasik-Głębocka, Sylwia Kobyłka, B. Zielińska-Psuja","doi":"10.32383/appdr/168836","DOIUrl":"https://doi.org/10.32383/appdr/168836","url":null,"abstract":"Valproic acid (VPA) is a broad-spectrum anticonvulsant drug. Its mechanism of action includes enhancing GABAergic transmission, blocking voltage-gated sodium channels, and affecting dopaminergic and serotonergic transmission (1). The mechanism of VPA toxicity, including its effects on the liver, is not fully known. It is assumed that oxidative stress and/or reactive products of drug biotransformation are responsible for its hepatotoxicity (2). The aim of the study was to verify the hypothesis concerning the influence of valproic acid and its metabolite, 2-propyl-4-pentenoic acid (4-en VPA) on the antioxidant status of patients treated with (VPA-T) and poisoned with valproic acid (VPA-P). The VPA-P group was divided into patients with (VPA-Ptox) and without (VPA-Pnon) toxic symptoms observed during the hospitalization. Oxidative stress was assessed using markers, such as antioxidant potential (FRAP) and reduced and oxidised glutathione (GSH/GSSG) ratio were measured in the plasma of the study patients. The obtained results showed statistically significant differences between the concentrations of the drug and its active metabolite levels in the VPA-T and VPA-P groups. In the VPA-P group, the increase of the level of 4-en VPA in the plasma correlated with the increase of the concentration of the drug. The influence of VPA on the antioxidant balance in both groups of patients was demonstrated. The plasma antioxidant potential of FRAP decreased with increasing valproic acid concentrations in the VPA-Ptox group. The lowest concentrations of GSH/GSSG ratio were found in the VPA-Pnon group, without symptoms of intoxication during hospitalization.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41476084","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
In recent years, the scientific world has become more interested in genistein. It has been the subject of extensive research for its potential in treating various diseases and as a functional food. The medical benefits of genistein are well documented in the literature. Several studies have been performed to better understand the mechanisms of its beneficiary effects on health and to improve its pharmacokinetic and pharmacodynamic parameters. It has been approved for relieving menopausal symptoms and has received attention for its use in the treatment of inflammatory and age-related disorders, cancer, metabolic illnesses, genetic disorders, and skin care. Genistein shows considerable similarity to endogenous estradiol. It is classified in the group known as phytoestrogens which exhibit properties corresponding to estrogen in the human body. The estrogenic activity resulting from the aforementioned similarity in the appearance of genistein and estradiol molecules makes it possible for genistein to act as both an estrogen agonist and antagonist, depending on the number of endogenous hormones present in the environment in which it is found and the type of tissue. The similarity of the chemical structure of genistein and estradiol and interactions occurring between estradiol and genistein and the amino acid binding site of the estrogen receptors were analyzed. Further controlled trials are needed to determine the efficacy and safety of genistein. Future research will focus on enhancing its bioavailability through structural modification and innovative delivery methods and conducting human trials to confirm its biological and pharmacological effects.
{"title":"Genistein - characterization of the molecule, similarity to estradiol and pharmacological potential","authors":"Kacper Kossakowski, A. Pawełczyk, L. Zaprutko","doi":"10.32383/appdr/161915","DOIUrl":"https://doi.org/10.32383/appdr/161915","url":null,"abstract":"In recent years, the scientific world has become more interested in genistein. It has been the subject of extensive research for its potential in treating various diseases and as a functional food. The medical benefits of genistein are well documented in the literature. Several studies have been performed to better understand the mechanisms of its beneficiary effects on health and to improve its pharmacokinetic and pharmacodynamic parameters. It has been approved for relieving menopausal symptoms and has received attention for its use in the treatment of inflammatory and age-related disorders, cancer, metabolic illnesses, genetic disorders, and skin care. Genistein shows considerable similarity to endogenous estradiol. It is classified in the group known as phytoestrogens which exhibit properties corresponding to estrogen in the human body. The estrogenic activity resulting from the aforementioned similarity in the appearance of genistein and estradiol molecules makes it possible for genistein to act as both an estrogen agonist and antagonist, depending on the number of endogenous hormones present in the environment in which it is found and the type of tissue. The similarity of the chemical structure of genistein and estradiol and interactions occurring between estradiol and genistein and the amino acid binding site of the estrogen receptors were analyzed. Further controlled trials are needed to determine the efficacy and safety of genistein. Future research will focus on enhancing its bioavailability through structural modification and innovative delivery methods and conducting human trials to confirm its biological and pharmacological effects.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45600089","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
A. Rybarczyk, A. Majchrzak-Celińska, V. Krajka-Kuźniak
Glioblastoma multiforme (GBM), a high-grade astrocytoma, is an incurable brain tumor associated with genetic heterogeneity and dysregulated signaling pathways. As alternations of the endocannabinoid system have been demonstrated in GBM cells, the substances affecting its key elements may potentially inhibit tumor progression. Preclinical models indicate that CBD inhibits GBM tumor growth by inhibiting cellular proliferation, migration, and invasion but also promotes autophagy and apoptosis of tumor cells. Moreover, clinical trials indicate the safety and positive results regarding the survival of GBM patients upon cannabinoids treatment. Nevertheless, more human clinical trials with large sample sizes are urgently needed to implement cannabinoids, including CBD, into standard GBM treatment.
{"title":"The application of cannabidiol in the treatment of glioblastoma","authors":"A. Rybarczyk, A. Majchrzak-Celińska, V. Krajka-Kuźniak","doi":"10.32383/appdr/163414","DOIUrl":"https://doi.org/10.32383/appdr/163414","url":null,"abstract":"Glioblastoma multiforme (GBM), a high-grade astrocytoma, is an incurable brain tumor associated with genetic heterogeneity and dysregulated signaling pathways. As alternations of the endocannabinoid system have been demonstrated in GBM cells, the substances affecting its key elements may potentially inhibit tumor progression. Preclinical models indicate that CBD inhibits GBM tumor growth by inhibiting cellular proliferation, migration, and invasion but also promotes autophagy and apoptosis of tumor cells. Moreover, clinical trials indicate the safety and positive results regarding the survival of GBM patients upon cannabinoids treatment. Nevertheless, more human clinical trials with large sample sizes are urgently needed to implement cannabinoids, including CBD, into standard GBM treatment.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46339633","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Katarzyna Sowa-Kasprzak, Dorota Olender, J. Kujawski, L. Zaprutko, A. Pawełczyk
Synthesis and biological evaluation of hybrid molecules combining naturally occurring antioxidant active structures with anti-inflammatory agents has been a strong trend in medicinal chemistry. This study focuses on modulating the structure of curcumin derivatives or their analogues with the use of non-steroidal anti-inflammatory drugs (NSAIDs). The combinations of curcumin, its keto-blocked derivatives and monocarbonyl analogues with selected non-steroidal anti-inflammatory drugs (ibuprofen, naproxen) were obtained and characterized. The pyrazole, isoxazole, benzylidene derivatives as well as curcumin monocarbonyl analogues were used as substrates in the reactions with selected NSAIDs. As a result of the esterification of curcumin-type diphenol, the corresponding mono- and diester-type derivatives were also obtained and characterized. Moreover, the estimated values of binding affinities and the binding sites of docked derivatives were deduced from modeling studies were very favorable. Results obtained show the binding potential of curcumin and its analogs to the host-targeted proteins nucleocapsid phosphoprotein (PDB ID: 6VYO) structure. Additionally, with the use of selected methods of computational chemistry (Molinspiration Cheminformatics and Osiris Property Explorer) the molecular parameters of the relevant molecules were calculated.
{"title":"Synthesis of curcumin derivatives containing non-steroidal anti-inflammatory drugs","authors":"Katarzyna Sowa-Kasprzak, Dorota Olender, J. Kujawski, L. Zaprutko, A. Pawełczyk","doi":"10.32383/appdr/161972","DOIUrl":"https://doi.org/10.32383/appdr/161972","url":null,"abstract":"Synthesis and biological evaluation of hybrid molecules combining naturally occurring antioxidant active structures with anti-inflammatory agents has been a strong trend in medicinal chemistry. This study focuses on modulating the structure of curcumin derivatives or their analogues with the use of non-steroidal anti-inflammatory drugs (NSAIDs). The combinations of curcumin, its keto-blocked derivatives and monocarbonyl analogues with selected non-steroidal anti-inflammatory drugs (ibuprofen, naproxen) were obtained and characterized. The pyrazole, isoxazole, benzylidene derivatives as well as curcumin monocarbonyl analogues were used as substrates in the reactions with selected NSAIDs. As a result of the esterification of curcumin-type diphenol, the corresponding mono- and diester-type derivatives were also obtained and characterized. Moreover, the estimated values of binding affinities and the binding sites of docked derivatives were deduced from modeling studies were very favorable. Results obtained show the binding potential of curcumin and its analogs to the host-targeted proteins nucleocapsid phosphoprotein (PDB ID: 6VYO) structure. Additionally, with the use of selected methods of computational chemistry (Molinspiration Cheminformatics and Osiris Property Explorer) the molecular parameters of the relevant molecules were calculated.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46386871","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract: Intravenous lipid emulsion is a critical component of parenteral nutrition. Long-term administration of such therapy lead to liver dysfunction. As the cause of liver failure can be the size of lipid emulsion droplets, their reduction can positively affect the clinical condition of patients. This study aimed to develop and optimize the preparation process of intravenous lipid emulsions with reduced droplet size compared to commercially available formulations. The response surface methodology was applied to optimize the ultrasonic emulsification. The reduction of lipid droplet size was achieved by the use of a combination of 1.2% (w/w) soy phospholipids and various concentrations of Tween 80 (2, 3, and 4% (w/w)). The other variables were sonication amplitude and time of sonication. During the optimization process, fifteen soybeans oil-based intravenous lipid emulsions were developed. All formulations were characterized by the physicochemical properties appropriate for intravenous administration, i.e., MDD ranging from 119.1 ± 0.6 nm to 177.1 ± 2.1 nm, PdI below 0,219 ± 0,009. The pH and osmolarity ranged from 6.23 ± 0.01 to 6.58 ± 0 and from 328 ± 3 to 568 ± 8 mOsm/kg, respectively. The Box Behnken methodology allowed for optimizing the preparation of intravenous lipid emulsion using ultrasonic emulsification.
{"title":"Application of response surface methodology in the development of parenteral emulsion using ultrasonic emulsification","authors":"A. Gostyńska, J. Jańczak","doi":"10.32383/appdr/168239","DOIUrl":"https://doi.org/10.32383/appdr/168239","url":null,"abstract":"Abstract: Intravenous lipid emulsion is a critical component of parenteral nutrition. Long-term administration of such therapy lead to liver dysfunction. As the cause of liver failure can be the size of lipid emulsion droplets, their reduction can positively affect the clinical condition of patients. This study aimed to develop and optimize the preparation process of intravenous lipid emulsions with reduced droplet size compared to commercially available formulations. The response surface methodology was applied to optimize the ultrasonic emulsification. The reduction of lipid droplet size was achieved by the use of a combination of 1.2% (w/w) soy phospholipids and various concentrations of Tween 80 (2, 3, and 4% (w/w)). The other variables were sonication amplitude and time of sonication. During the optimization process, fifteen soybeans oil-based intravenous lipid emulsions were developed. All formulations were characterized by the physicochemical properties appropriate for intravenous administration, i.e., MDD ranging from 119.1 ± 0.6 nm to 177.1 ± 2.1 nm, PdI below 0,219 ± 0,009. The pH and osmolarity ranged from 6.23 ± 0.01 to 6.58 ± 0 and from 328 ± 3 to 568 ± 8 mOsm/kg, respectively. The Box Behnken methodology allowed for optimizing the preparation of intravenous lipid emulsion using ultrasonic emulsification.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45112620","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
This issue presents a collection of selected papers from the International Conference NEW TRENDS in Polish and global pharmacy: Science, business, and modern education, which took place on September 29-30, 2022, Poznań, Poland. The conference aimed to develop an effective communication platform between science and business. Prominent specialists in science, education, and business who deal with the issues of developing bridges between these three sectors participated in the event. Scientific achievements, the latest research results, and the potential of medical universities as an offer for the pharmaceutical industry were presented.
{"title":"In search of new trends","authors":"M. Stawny","doi":"10.32383/appdr/168232","DOIUrl":"https://doi.org/10.32383/appdr/168232","url":null,"abstract":"This issue presents a collection of selected papers from the International Conference NEW TRENDS in Polish and global pharmacy: Science, business, and modern education, which took place on September 29-30, 2022, Poznań, Poland.\u0000The conference aimed to develop an effective communication platform between science and business. Prominent specialists in science, education, and business who deal with the issues of developing bridges between these three sectors participated in the event. Scientific achievements, the latest research results, and the potential of medical universities as an offer for the pharmaceutical industry were presented.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45712755","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Sobczak-Kupiec Agnieszka, Beata Kaźmierska, P. Świątek, Izabela Muszalska-Kolos
Phenothiazine and its derivatives exhibit many properties. Hence they are the starting structures for many new potential drugs, biologically active compounds, dyes, etc. In this paper, we investigated a series of five fluphenazine analogs synthesized exhibiting inhibition of multidrug resistance (MDR) in tumor cells. During the drug discovery process, the determination of physicochemical properties of new compounds, such as dissociation constant values (pKa), is essential because it directly affects their pharmacokinetic profile. Thus, this study aimed to determine the pKa values of fluphenazine and its derivatives from the mobile phase pH dependence of the retention factor with the reverse phase liquid chromatographic method. Binary mixtures of phosphate buffer (pH 2.3-11.5) and acetonitrile (40-55%) in different percentages and the Gemini NX C18 column as the stationary phase were used in the tests. The pKa' values of fluphenazine derivatives at experimental concentrations of organic solvent were determined based on the obtained sigmoidal k curves as a function of pH. Then these values were extrapolated to 0% acetonitrile to obtain the actual pKa values. Moreover, a comparative evaluation of chromatographically obtained and computationally calculated pKa parameters was carried out.
{"title":"Determination of pKa values of fluphenazine analogs by reversed-phase high-performance liquid chromatography","authors":"Sobczak-Kupiec Agnieszka, Beata Kaźmierska, P. Świątek, Izabela Muszalska-Kolos","doi":"10.32383/appdr/165805","DOIUrl":"https://doi.org/10.32383/appdr/165805","url":null,"abstract":"Phenothiazine and its derivatives exhibit many properties. Hence they are the starting structures\u0000for many new potential drugs, biologically active compounds, dyes, etc. In this paper, we\u0000investigated a series of five fluphenazine analogs synthesized exhibiting inhibition of multidrug\u0000resistance (MDR) in tumor cells. During the drug discovery process, the determination of\u0000physicochemical properties of new compounds, such as dissociation constant values (pKa), is\u0000essential because it directly affects their pharmacokinetic profile. Thus, this study aimed to\u0000determine the pKa values of fluphenazine and its derivatives from the mobile phase pH\u0000dependence of the retention factor with the reverse phase liquid chromatographic method.\u0000Binary mixtures of phosphate buffer (pH 2.3-11.5) and acetonitrile (40-55%) in different\u0000percentages and the Gemini NX C18 column as the stationary phase were used in the tests. The\u0000pKa' values of fluphenazine derivatives at experimental concentrations of organic solvent were\u0000determined based on the obtained sigmoidal k curves as a function of pH. Then these values\u0000were extrapolated to 0% acetonitrile to obtain the actual pKa values. Moreover, a comparative\u0000evaluation of chromatographically obtained and computationally calculated pKa parameters\u0000was carried out.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46650552","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Joanna Kuźmińska, A. Sobczak, Izabela Muszalska-Kolos, A. Jelińska, Weronika Jankowska, T. Gośliński
Two novel fluorocurcumin adducts with a difluoroboryl group exhibited activity in vitro against two bladder cancer cell lines, namely 5637 and SCaBER. The stability was evaluated under physiologically relevant conditions to mimic both the digestive tract and the bladder environment. Therefore, experiments were performed in hydrochloric acid at pH 1.2, and in buffer solutions with pH from 4.5 to 6.8 at 37°C. A validated HPLC method, allowing the monitoring of changes in substrates and products concentrations over time, was applied. Notably, the main decomposition product was the fluorocurcumin derivative without the difluoroboryl group. The decomposition of the fluorocurcumin adducts to the major products undergoes the pseudo-first-order kinetics reaction.
{"title":"Kinetic studies of fluorocurcumin derivatives with anticancer activity","authors":"Joanna Kuźmińska, A. Sobczak, Izabela Muszalska-Kolos, A. Jelińska, Weronika Jankowska, T. Gośliński","doi":"10.32383/appdr/163486","DOIUrl":"https://doi.org/10.32383/appdr/163486","url":null,"abstract":"Two novel fluorocurcumin adducts with a difluoroboryl group exhibited activity in vitro against two bladder cancer cell lines, namely 5637 and SCaBER. The stability was evaluated under physiologically relevant conditions to mimic both the digestive tract and the bladder environment. Therefore, experiments were performed in hydrochloric acid at pH 1.2, and in buffer solutions with pH from 4.5 to 6.8 at 37°C. A validated HPLC method, allowing the monitoring of changes in substrates and products concentrations over time, was applied. Notably, the main decomposition product was the fluorocurcumin derivative without the difluoroboryl group. The decomposition of the fluorocurcumin adducts to the major products undergoes the pseudo-first-order kinetics reaction.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42303566","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M. Ogrodowczyk, A. Kaczmarek, A. Gostyńska, A. Jelińska
Radiation sterilization is a widely used method for ensuring the sterility of medical and pharmaceutical products. The process involves exposing the products to ionizing radiation, which destroys microorganisms such as bacteria, viruses, and fungi, rendering the products sterile. The most commonly used ionizing radiation sterilization methods are highly penetrating with low dose rate gamma-irradiation from isotopic sources and less penetrating but with high dose rate e-beam from accelerators. This review provides an overview of the principles and applications of radiation sterilization, including the types of radiation sources used, the differences between them that may affect the efficacy of the process, and the regulatory requirements for radiation sterilization of active pharmaceutical ingredients and drug dosage forms. This review focuses on the analytical methods used to evaluate the effect of irradiation on drug substances. Finally, it discusses studies on radiation sterilization of various groups of drugs, including anthracyclines, β-lactam antibiotics, chloramphenicol and its derivatives, sulphonamides, antifungal drugs, β-blockers, nonsteroidal anti-inflammatory drugs, steroids, and others, and drug dosage forms.
{"title":"The role of pharmaceutical analysis in ensuring the safety of drug radiation sterilization","authors":"M. Ogrodowczyk, A. Kaczmarek, A. Gostyńska, A. Jelińska","doi":"10.32383/appdr/163633","DOIUrl":"https://doi.org/10.32383/appdr/163633","url":null,"abstract":"Radiation sterilization is a widely used method for ensuring the sterility of medical and pharmaceutical products. The process involves exposing the products to ionizing radiation, which destroys microorganisms such as bacteria, viruses, and fungi, rendering the products sterile. The most commonly used ionizing radiation sterilization methods are highly penetrating with low dose rate gamma-irradiation from isotopic sources and less penetrating but with high dose rate e-beam from accelerators. This review provides an overview of the principles and applications of radiation sterilization, including the types of radiation sources used, the differences between them that may affect the efficacy of the process, and the regulatory requirements for radiation sterilization of active pharmaceutical ingredients and drug dosage forms. This review focuses on the analytical methods used to evaluate the effect of irradiation on drug substances. Finally, it discusses studies on radiation sterilization of various groups of drugs, including anthracyclines, β-lactam antibiotics, chloramphenicol and its derivatives, sulphonamides, antifungal drugs, β-blockers, nonsteroidal anti-inflammatory drugs, steroids, and others, and drug dosage forms.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45638367","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The purpose of the study was to evaluate the preparation of alginate-based microparticles with meloxicam (MLX). A poorly soluble substance classified to BCS class II, it was chosen as a model substance. The ionotropic gelation was the process used for the formation of microparticles. The impact of the carrier on the dissolution of MLX from this formulation was also investigated. Study was realized in few steps: preparation of polymer particles containing suspended MLX in their structure; drying them in various conditions (room temperature, freeze drying); morphology characterization and then assessment of impact of polymer on dissolution of the model substance. Also, DDSolver software was used for checking the similarity of release profiles. Validated UV-Vis spectrophotometric method was used for MLX determination on different steps of work. As it showed, calcium alginate particles were successfully prepared with ionotropic gelation. The drying method of prepared particles has a substantial impact on the release profiles of meloxicam, and these formulations significantly improve the MLX release from this form of the delivery system.
{"title":"Preliminary assessment of influence of calcium alginate beads on the dissolution of meloxicam","authors":"Barbara Jadach, Weronika Świetlik, Ł. Majchrzycki","doi":"10.32383/appdr/162533","DOIUrl":"https://doi.org/10.32383/appdr/162533","url":null,"abstract":"The purpose of the study was to evaluate the preparation of alginate-based microparticles with meloxicam (MLX). A poorly soluble substance classified to BCS class II, it was chosen as a model substance. The ionotropic gelation was the process used for the formation of microparticles. The impact of the carrier on the dissolution of MLX from this formulation was also investigated.\u0000Study was realized in few steps: preparation of polymer particles containing suspended MLX in their structure; drying them in various conditions (room temperature, freeze drying); morphology characterization and then assessment of impact of polymer on dissolution of the model substance. Also, DDSolver software was used for checking the similarity of release profiles. Validated UV-Vis spectrophotometric method was used for MLX determination on different steps of work. \u0000As it showed, calcium alginate particles were successfully prepared with ionotropic gelation. The drying method of prepared particles has a substantial impact on the release profiles of meloxicam, and these formulations significantly improve the MLX release from this form of the delivery system.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43800002","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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