Pub Date : 2023-05-15DOI: 10.1590/s2175-97902023e22430
Elton Max Nascimento do Egito, Isaac Aaron Morales Frias, Maria D. L. Oliveira, César Augusto Souza de Andrade
Lipoprotein monitoring is desirable in the management of medical conditions such as atherosclerotic cardiovascular disease and coronary artery disease, in which controlling the concentration of these chylomicrons is crucial. Current clinical methods are complex and present poor reproducibility between laboratories. For these reasons, recent guidelines discard the assessment of low-density lipoprotein cholesterol (LDL-C) as a routine analysis during lipid-lowering therapies. Concerning the importance of monitoring this parameter, the authors present an electrochemical immunosensor constructed from a simple and easy-to-reproduce platform that allows detecting and quantifying LDL nanoparticles directly from human serum samples. The performance of the biosensor was studied by scanning electron microscopy, cyclic voltammetry, and electrochemical impedance spectroscopy. The biosensing platform displays good stability and linearity between 30 mg dL -1 and 135 mg dL -1 with a detection limit of 20 mg dL -1 . The proposed biosensor can be easily employed for monitoring LDL concentration in clinical treatments.
{"title":"Electrochemical immunosensing of low-density lipoprotein based on sol-gel encapsulation","authors":"Elton Max Nascimento do Egito, Isaac Aaron Morales Frias, Maria D. L. Oliveira, César Augusto Souza de Andrade","doi":"10.1590/s2175-97902023e22430","DOIUrl":"https://doi.org/10.1590/s2175-97902023e22430","url":null,"abstract":"Lipoprotein monitoring is desirable in the management of medical conditions such as atherosclerotic cardiovascular disease and coronary artery disease, in which controlling the concentration of these chylomicrons is crucial. Current clinical methods are complex and present poor reproducibility between laboratories. For these reasons, recent guidelines discard the assessment of low-density lipoprotein cholesterol (LDL-C) as a routine analysis during lipid-lowering therapies. Concerning the importance of monitoring this parameter, the authors present an electrochemical immunosensor constructed from a simple and easy-to-reproduce platform that allows detecting and quantifying LDL nanoparticles directly from human serum samples. The performance of the biosensor was studied by scanning electron microscopy, cyclic voltammetry, and electrochemical impedance spectroscopy. The biosensing platform displays good stability and linearity between 30 mg dL -1 and 135 mg dL -1 with a detection limit of 20 mg dL -1 . The proposed biosensor can be easily employed for monitoring LDL concentration in clinical treatments.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67742271","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}
Pub Date : 2023-05-15DOI: 10.1590/s2175-97902023e22106
Anna Kelly Moura-Silva, B. Mano-Sousa, Lays Pedrosa Santos, R. R. D. Costa, F. P. D. Andrade, J. M. Duarte-Almeida, D. Gonçalves
Guarana
{"title":"Development and validation of an analytical method by HPLC-DAD for determination of caffeine in products based on guarana extracts (Paullinia cupana)","authors":"Anna Kelly Moura-Silva, B. Mano-Sousa, Lays Pedrosa Santos, R. R. D. Costa, F. P. D. Andrade, J. M. Duarte-Almeida, D. Gonçalves","doi":"10.1590/s2175-97902023e22106","DOIUrl":"https://doi.org/10.1590/s2175-97902023e22106","url":null,"abstract":"Guarana","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67741858","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}
Pub Date : 2023-05-15DOI: 10.1590/s2175-97902023e211019
Fabio Tamanini, Beatriz Sakakibara Moraes, C. Amaral, A. Carvalho, E. Trovatti
The form of drug administration affects the success of treatment, since it can influence adherence of the patient to the therapy. The use of orodispersible films has emerged as a way to overcome some drawbacks of conventional methods of drug delivery, especially for patients experiencing difficulty in swallowing. These films are prepared using a matrix that incorporates the drug and contains other substances that confer the properties of the system. The present work describes the use of thermoplastic starch as a carrier for the model drug diclofenac, including film preparation and testing of its orodispersible potential. Preparation of the film employed a microwave oven to gelatinize and plasticize corn starch, with incorporation of the model drug, followed by solvent-casting. The samples were characterized using mechanical tests, analyses of water uptake and water content, and Fourier transform infrared spectroscopy. The results indicated that the film presented promising properties as an alternative system for oral drug administration, with good incorporation and distribution of the drug in the matrix. The material displayed satisfactory mechanical properties, which are crucial for this type of material, due to the need for oral administration and handling before use.
{"title":"Starch-based orodispersible film for diclofenac release","authors":"Fabio Tamanini, Beatriz Sakakibara Moraes, C. Amaral, A. Carvalho, E. Trovatti","doi":"10.1590/s2175-97902023e211019","DOIUrl":"https://doi.org/10.1590/s2175-97902023e211019","url":null,"abstract":"The form of drug administration affects the success of treatment, since it can influence adherence of the patient to the therapy. The use of orodispersible films has emerged as a way to overcome some drawbacks of conventional methods of drug delivery, especially for patients experiencing difficulty in swallowing. These films are prepared using a matrix that incorporates the drug and contains other substances that confer the properties of the system. The present work describes the use of thermoplastic starch as a carrier for the model drug diclofenac, including film preparation and testing of its orodispersible potential. Preparation of the film employed a microwave oven to gelatinize and plasticize corn starch, with incorporation of the model drug, followed by solvent-casting. The samples were characterized using mechanical tests, analyses of water uptake and water content, and Fourier transform infrared spectroscopy. The results indicated that the film presented promising properties as an alternative system for oral drug administration, with good incorporation and distribution of the drug in the matrix. The material displayed satisfactory mechanical properties, which are crucial for this type of material, due to the need for oral administration and handling before use.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67738600","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}
Pub Date : 2023-05-15DOI: 10.1590/s2175-97902023e22643
Chetna Modi, P. Bharadia
Transfersomes
{"title":"In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate","authors":"Chetna Modi, P. Bharadia","doi":"10.1590/s2175-97902023e22643","DOIUrl":"https://doi.org/10.1590/s2175-97902023e22643","url":null,"abstract":"Transfersomes","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67742673","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}
Pub Date : 2023-05-08DOI: 10.1590/s2175-97902023e201178
Mohd Basheeruddin, V. Lavanya, Neesar Ahmed, Shazia Jamal
Abstract Diclofenac sodium (DF) is a non-steroidal anti-inflammatory drug (NSAID) that possesses antipyretic, analgesic, antinociceptive and anti-inflammatory activities. Like other NSAIDs, DF is known to be associated with renal, cardiovascular, and gastrointestinal complications. The present study was carried out to evaluate the adverse effects of DF in vivo in wistar albino rats and to assess if oral administration of the organic osmolyte betaine mitigates the adverse effect of DF. Eighteen male Wistar rats were divided into three groups, one group of animals was fed orally with 20 mg/kg of DF once/day, and the other group received a combination of 20 mg/kg of DF and 30 mg/kg of betaine, once/day. Apart from the hematological and biochemical parameters, histopathological changes in the liver, lungs, brain, heart and kidney were also investigated. Histopathological alterations that were found in the liver, kidney, and lungs of DF-treated animals were found to be minimal or absent in DF + betaine-treated animals, as compared to untreated control. The results showed that betaine mitigates the adverse effects associated with DF treatment.
{"title":"Organic osmolyte betaine mitigates the deleterious effects of Diclofenac in vivo in wistar albino rats","authors":"Mohd Basheeruddin, V. Lavanya, Neesar Ahmed, Shazia Jamal","doi":"10.1590/s2175-97902023e201178","DOIUrl":"https://doi.org/10.1590/s2175-97902023e201178","url":null,"abstract":"Abstract Diclofenac sodium (DF) is a non-steroidal anti-inflammatory drug (NSAID) that possesses antipyretic, analgesic, antinociceptive and anti-inflammatory activities. Like other NSAIDs, DF is known to be associated with renal, cardiovascular, and gastrointestinal complications. The present study was carried out to evaluate the adverse effects of DF in vivo in wistar albino rats and to assess if oral administration of the organic osmolyte betaine mitigates the adverse effect of DF. Eighteen male Wistar rats were divided into three groups, one group of animals was fed orally with 20 mg/kg of DF once/day, and the other group received a combination of 20 mg/kg of DF and 30 mg/kg of betaine, once/day. Apart from the hematological and biochemical parameters, histopathological changes in the liver, lungs, brain, heart and kidney were also investigated. Histopathological alterations that were found in the liver, kidney, and lungs of DF-treated animals were found to be minimal or absent in DF + betaine-treated animals, as compared to untreated control. The results showed that betaine mitigates the adverse effects associated with DF treatment.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67737044","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 Voriconazole increases tacrolimus blood concentration significantly when coadministrated. The recommendation of reducing tacrolimus to 1/3 in voriconazole package insert seems not to be satisfactory in clinical practice. In vitro studies demonstrated that the magnitude of inhibition depends on the concentration of voriconazole, while voriconazole exposure is determined by the genotype status of CYP2C19. CYP2C19 gene polymorphism challenges the management of drug-drug interactions(DDIs) between voriconazole and tacrolimus. This work aimed to predict the impact of CYP2C19 polymorphism on the DDIs by using physiologically based pharmacokinetics (PBPK) models. The precision of the developed voriconazole and tacrolimus models was reasonable by evaluating the pharmacokinetic parameters fold error, such as AUC0-24, Cmax and tmax. Voriconazole increased tacrolimus concentration immediately in all population. The simulated duration of DDIs disappearance after voriconazole withdrawal were 146h, 90h and 66h in poor metabolizers (PMs), intermediate metabolizers (IMs) and extensive metabolizers(EMs), respectively. The developed and optimized PBPK models in this study can be applied to assit the dose adjustment for tacrolimus with and without voriconazole.
{"title":"Prediction of the Impact of CYP2C19 Polymorphism on Drug-Drug Interaction between Voriconazole and Tacrolimus Using Physiologically-Based Pharmacokinetic Modelling","authors":"Zhi-Ping Jin, M. Yan, Si-Ze Li, Bao-Qing Wang, Qing-fang Xu, Wei Wu, Xiaoyang Li, Qian-zhou Lv, Xiao-Qiang Xiang","doi":"10.1590/s2175-97902023e21343","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21343","url":null,"abstract":"Abstract Voriconazole increases tacrolimus blood concentration significantly when coadministrated. The recommendation of reducing tacrolimus to 1/3 in voriconazole package insert seems not to be satisfactory in clinical practice. In vitro studies demonstrated that the magnitude of inhibition depends on the concentration of voriconazole, while voriconazole exposure is determined by the genotype status of CYP2C19. CYP2C19 gene polymorphism challenges the management of drug-drug interactions(DDIs) between voriconazole and tacrolimus. This work aimed to predict the impact of CYP2C19 polymorphism on the DDIs by using physiologically based pharmacokinetics (PBPK) models. The precision of the developed voriconazole and tacrolimus models was reasonable by evaluating the pharmacokinetic parameters fold error, such as AUC0-24, Cmax and tmax. Voriconazole increased tacrolimus concentration immediately in all population. The simulated duration of DDIs disappearance after voriconazole withdrawal were 146h, 90h and 66h in poor metabolizers (PMs), intermediate metabolizers (IMs) and extensive metabolizers(EMs), respectively. The developed and optimized PBPK models in this study can be applied to assit the dose adjustment for tacrolimus with and without voriconazole.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67739723","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}
Pub Date : 2023-05-08DOI: 10.1590/s2175-97902023e21415
E. Costa, T. Castro, C. Gonçalves-de-Albuquerque, H. C. F. Faria Neto, J. Gonçalves, R. Estrela
Dasatinib, a potent oral multi-targeted kinase inhibitor against Src and Bcr-Abl, can decrease inflammatory response in sepsis. A simple and cost-effective method for determination of an effective dose dasatinib was established. This method was validated in human plasma, with the aim of reducing the number of animals used, thus, avoiding ethical problems. Dasatinib and internal standard lopinavir were extracted from 180 uL of plasma using liquid-liquid extraction with methyl tert-butil ether, followed by liquid chromatography coupled to triple quadrupole mass spectrometry in multiple reaction monitoring mode. For the pharmacokinetic study, 1 mg/kg of dasatinib was administered to mice with and without sepsis. The method was linear over the concentration range of 1-98 ng/mL for DAS in mice and human plasma, with r 2 >0.99 and presented intra-and interday precision within the range of 2.3 – 6.2 and 4.3 – 7.0%, respectively. Further intra-and interday accuracy was within the range of 88.2 – 105.8 and 90.6 – 101.7%, respectively. The mice with sepsis showed AUC0-t = 2076.06 h*ng/mL and Cmax = 102.73 ng/mL and mice without sepsis presented AUC0-t = 2128.46 h*ng/mL. Cmax = 164.5 ng/mL. The described analytical method was successfully employed in pharmacokinetic study of DAS in mice.
{"title":"Development and validation of liquid chromatography-tandem mass spectrometry method to quantify dasatinib in plasma and its application to a pharmacokinetic study","authors":"E. Costa, T. Castro, C. Gonçalves-de-Albuquerque, H. C. F. Faria Neto, J. Gonçalves, R. Estrela","doi":"10.1590/s2175-97902023e21415","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21415","url":null,"abstract":"Dasatinib, a potent oral multi-targeted kinase inhibitor against Src and Bcr-Abl, can decrease inflammatory response in sepsis. A simple and cost-effective method for determination of an effective dose dasatinib was established. This method was validated in human plasma, with the aim of reducing the number of animals used, thus, avoiding ethical problems. Dasatinib and internal standard lopinavir were extracted from 180 uL of plasma using liquid-liquid extraction with methyl tert-butil ether, followed by liquid chromatography coupled to triple quadrupole mass spectrometry in multiple reaction monitoring mode. For the pharmacokinetic study, 1 mg/kg of dasatinib was administered to mice with and without sepsis. The method was linear over the concentration range of 1-98 ng/mL for DAS in mice and human plasma, with r 2 >0.99 and presented intra-and interday precision within the range of 2.3 – 6.2 and 4.3 – 7.0%, respectively. Further intra-and interday accuracy was within the range of 88.2 – 105.8 and 90.6 – 101.7%, respectively. The mice with sepsis showed AUC0-t = 2076.06 h*ng/mL and Cmax = 102.73 ng/mL and mice without sepsis presented AUC0-t = 2128.46 h*ng/mL. Cmax = 164.5 ng/mL. The described analytical method was successfully employed in pharmacokinetic study of DAS in mice.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67739746","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}
Pub Date : 2023-05-08DOI: 10.1590/s2175-97902023e21414
Jiahong Wang
The aim of the present study was to investigate the usefulness of multidrug resistance protein 1 (MDR1) and neuropeptide Y (NPY) levels in predicting the efficacy of levetiracetam (LEV) plus oxcarbazepine (OXC) treatment administered to children with epilepsy and to determine their prognosis. Overall, 193 children with epilepsy admitted to the hospital were enrolled and randomly divided into two groups according to different treatment methods: group A (n = 106, treated with LEV plus OXC combination) and group B (n = 87, treated with OXC only). After treatment, compared with group B, group A exhibited a remarkably higher total effective rate and a significantly lower total adverse reaction rate. Areas under the curve for MDR1 and NPY for predicting ineffective treatment were 0.867 and 0.834, whereas those for predicting epilepsy recurrence were 0.916 and 0.829, respectively. Electroencephalography abnormalities, intracranial hemorrhage, neonatal convulsion, premature delivery, and MDR1 and NPY levels were independent risk factors for poor prognosis in children with epilepsy. Serum MDR1 and NPY levels exhibited a high predictive value for early epilepsy diagnosis, treatment efficacy assessment, and prognostication in children with epilepsy treated with LEV plus OXC combination.
{"title":"Levetiracetam plus Oxcarbazepine Combination Treatment Downregulates Serum Multidrug Resistance Protein 1 Levels and Upregulates Neuropeptide Y Levels in Children with Epilepsy","authors":"Jiahong Wang","doi":"10.1590/s2175-97902023e21414","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21414","url":null,"abstract":"The aim of the present study was to investigate the usefulness of multidrug resistance protein 1 (MDR1) and neuropeptide Y (NPY) levels in predicting the efficacy of levetiracetam (LEV) plus oxcarbazepine (OXC) treatment administered to children with epilepsy and to determine their prognosis. Overall, 193 children with epilepsy admitted to the hospital were enrolled and randomly divided into two groups according to different treatment methods: group A (n = 106, treated with LEV plus OXC combination) and group B (n = 87, treated with OXC only). After treatment, compared with group B, group A exhibited a remarkably higher total effective rate and a significantly lower total adverse reaction rate. Areas under the curve for MDR1 and NPY for predicting ineffective treatment were 0.867 and 0.834, whereas those for predicting epilepsy recurrence were 0.916 and 0.829, respectively. Electroencephalography abnormalities, intracranial hemorrhage, neonatal convulsion, premature delivery, and MDR1 and NPY levels were independent risk factors for poor prognosis in children with epilepsy. Serum MDR1 and NPY levels exhibited a high predictive value for early epilepsy diagnosis, treatment efficacy assessment, and prognostication in children with epilepsy treated with LEV plus OXC combination.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67739525","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}
Pub Date : 2023-05-08DOI: 10.1590/s2175-97902023e21525
Giulia de Souza Castro, E. L. C. Cruz-Cazarim, M. Silvério, A. Mendonça, M. S. Cazarim
The incorrect disposal of medicines and their environmental impact has been related to the health medicalization and the improper use of medication by society. In this sense, it is very important to know the profile of drug disposal for foster health policies. The aim was to identify the profile of disposal of medicines by the population, including the cost perspective. This is an inquiry descriptive study that began in September 2019. Medicine disposal health education program was carried out over six months in two University pharmacies. A questionnaire for sociodemographic and discarded medicines data collection was applied. Logistic regression analysis for variables association of correct disposal and the chi-square and t-student analysis for comparison between disposal programs were performed for a level of 5% and test power of 80%. Medicines weighed 23.3 kg and 28.5 kg, with the cost variation from US$ 13.5 to US$ 16.1 until the final treatment. The correct disposal was strongly associated with the disposal reason (p=0.013), source of information (p=0.006), prescription (p=0.03), form of use (p=0.01), acquisition source (p=0.001), cost with medication (p=0.0001), education (p=0.028) and age (p=0.05). The correct medicine disposal was associated with important features of the community related to education health.
{"title":"Health education can save the environment from medicine residues","authors":"Giulia de Souza Castro, E. L. C. Cruz-Cazarim, M. Silvério, A. Mendonça, M. S. Cazarim","doi":"10.1590/s2175-97902023e21525","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21525","url":null,"abstract":"The incorrect disposal of medicines and their environmental impact has been related to the health medicalization and the improper use of medication by society. In this sense, it is very important to know the profile of drug disposal for foster health policies. The aim was to identify the profile of disposal of medicines by the population, including the cost perspective. This is an inquiry descriptive study that began in September 2019. Medicine disposal health education program was carried out over six months in two University pharmacies. A questionnaire for sociodemographic and discarded medicines data collection was applied. Logistic regression analysis for variables association of correct disposal and the chi-square and t-student analysis for comparison between disposal programs were performed for a level of 5% and test power of 80%. Medicines weighed 23.3 kg and 28.5 kg, with the cost variation from US$ 13.5 to US$ 16.1 until the final treatment. The correct disposal was strongly associated with the disposal reason (p=0.013), source of information (p=0.006), prescription (p=0.03), form of use (p=0.01), acquisition source (p=0.001), cost with medication (p=0.0001), education (p=0.028) and age (p=0.05). The correct medicine disposal was associated with important features of the community related to education health.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67740580","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}
Pub Date : 2023-05-08DOI: 10.1590/s2175-97902023e22540
A. Scherbakov, Y. Kuznetsov, M. Yastrebova, A. Khamidullina, D. Sorokin, M. Tserfas, I. Levina
This study aimed to investigate the activities of novel 20( R )-3,20-dihydroxy-19-norpregn-1,3,5(10)- trienes ( kuz7 and kuz8b) of natural 13β-and epimeric 13α-series against triple-negative MDA-MB-231 breast cancer cells. High antiproliferative activity of synthesized compounds kuz8b and kuz7 against MDA-MB-231 triple-negative cancer cells was revealed. The steroid kuz7 of natural 13β-configuration was more active against MDA-MB-231 cells than the 13α-steroid kuz8b . Cell cycle analysis revealed common patterns for the action of both tested compounds. The number of cells in the subG1 phase increased in a dose-dependent manner, indicating induction of apoptosis, which was also verified by PARP cleavage. In contrast, the number of cells in the G0/G1 phase decreases with increasing compound concentration. Steroid kuz7 at micromolar concentrations reduced the expression of GLUT1, a glucose transporter. High efficacy of the combination of kuz7 with biguanide metformin was shown, and synergistic effects on MDA-MB-231 cell growth and expression of the anti-apoptotic protein Bcl-2 were revealed. According to the obtained results, including the high activity of kuz7 against triple-negative cancer cells, the detected induction of apoptosis, and the decrease in GLUT1 expression, 13β-steroid kuz7 is of interest for further preclinical studies both alone and in combination with the metabolic drug metformin.
{"title":"Antiproliferative effects of 13α/β-steroids on triple-negative MDA-MB-231 breast cancer cells: unraveling intracellular signaling without ERα","authors":"A. Scherbakov, Y. Kuznetsov, M. Yastrebova, A. Khamidullina, D. Sorokin, M. Tserfas, I. Levina","doi":"10.1590/s2175-97902023e22540","DOIUrl":"https://doi.org/10.1590/s2175-97902023e22540","url":null,"abstract":"This study aimed to investigate the activities of novel 20( R )-3,20-dihydroxy-19-norpregn-1,3,5(10)- trienes ( kuz7 and kuz8b) of natural 13β-and epimeric 13α-series against triple-negative MDA-MB-231 breast cancer cells. High antiproliferative activity of synthesized compounds kuz8b and kuz7 against MDA-MB-231 triple-negative cancer cells was revealed. The steroid kuz7 of natural 13β-configuration was more active against MDA-MB-231 cells than the 13α-steroid kuz8b . Cell cycle analysis revealed common patterns for the action of both tested compounds. The number of cells in the subG1 phase increased in a dose-dependent manner, indicating induction of apoptosis, which was also verified by PARP cleavage. In contrast, the number of cells in the G0/G1 phase decreases with increasing compound concentration. Steroid kuz7 at micromolar concentrations reduced the expression of GLUT1, a glucose transporter. High efficacy of the combination of kuz7 with biguanide metformin was shown, and synergistic effects on MDA-MB-231 cell growth and expression of the anti-apoptotic protein Bcl-2 were revealed. According to the obtained results, including the high activity of kuz7 against triple-negative cancer cells, the detected induction of apoptosis, and the decrease in GLUT1 expression, 13β-steroid kuz7 is of interest for further preclinical studies both alone and in combination with the metabolic drug metformin.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67742506","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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