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":"1 1","pages":""},"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/s2175-97902023e21414
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":"1 1","pages":""},"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/s2175-97902023e22540
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":"45 1","pages":""},"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}
Pub Date : 2023-05-08DOI: 10.1590/s2175-97902023e21117
S. Mendonça, Smail Aazza, Alexandre Alves de Carvalho, Diogo Mendes da Silva, N. S. Oliveira, J. P. Pinto, S. Bertolucci
The phenolic compound content, the antioxidant and α-amylase inhibition potentials of different extracts of the Plectranthus amboinicus , P. barbatus and P. ornatus were evaluated. We also evaluated the influence of plant growth and harvest time on the chemical composition of the essential oil (EO) of P. amboinicus , its antioxidant and anti-Candida activities and the α-amylase and lipoxygenase inhibitions. The turbo-extract of P. barbatus showed the greatest phenolic compound content and antioxidant activity. No α-amylase inhibition activity was observed in the analyzed extracts, but the turbo-extraction and refluxing extracts possessed high antioxidant activities. Protected cultivation and morning harvest conditions gave the best antioxidant activities, which was associated to the highest carvacrol content. P. amboinicu s EO antioxidant activity could contribute to the reduction of oxidative stress in diabetes. Causal Candida strains of diabetic foot ulcers showed sensitivity to P. amboinicus EO. C. albicans and C. dubliniensis were the most sensitive of the selected Candida strains. Turbo-extracts or refluxing of the three species extracts and the EO of P. amboinicus should be considered as a potential candidate for the management the complications of type 2 diabetes.
{"title":"Biological screening of herbal extracts and essential oil from Plectranthus species: α-amylase and 5-lipoxygenase inhibition and antioxidant and anti-Candida potentials","authors":"S. Mendonça, Smail Aazza, Alexandre Alves de Carvalho, Diogo Mendes da Silva, N. S. Oliveira, J. P. Pinto, S. Bertolucci","doi":"10.1590/s2175-97902023e21117","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21117","url":null,"abstract":"The phenolic compound content, the antioxidant and α-amylase inhibition potentials of different extracts of the Plectranthus amboinicus , P. barbatus and P. ornatus were evaluated. We also evaluated the influence of plant growth and harvest time on the chemical composition of the essential oil (EO) of P. amboinicus , its antioxidant and anti-Candida activities and the α-amylase and lipoxygenase inhibitions. The turbo-extract of P. barbatus showed the greatest phenolic compound content and antioxidant activity. No α-amylase inhibition activity was observed in the analyzed extracts, but the turbo-extraction and refluxing extracts possessed high antioxidant activities. Protected cultivation and morning harvest conditions gave the best antioxidant activities, which was associated to the highest carvacrol content. P. amboinicu s EO antioxidant activity could contribute to the reduction of oxidative stress in diabetes. Causal Candida strains of diabetic foot ulcers showed sensitivity to P. amboinicus EO. C. albicans and C. dubliniensis were the most sensitive of the selected Candida strains. Turbo-extracts or refluxing of the three species extracts and the EO of P. amboinicus should be considered as a potential candidate for the management the complications of type 2 diabetes.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67738868","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/s2175-97902023e21220
R. Coşkun, A. Celik, M. S. Coşgun, R. Mammadov
Exposure to methanol can cause serious consequences such as permanent visual disturbances and death. The heart tissue is highly vulnerable to ATP deficiency. Our study aimed to investigate whether exogenous ATP administration may alleviate methanol-induced ATP deficiency and subsequent oxidative damage in rat heart tissue. A total of 30 rats were divided into equal five groups; Healthy Group (HG), Methotrexate (MXG), Methanol (MeOH), Methotrexate+Methanol (MXM), and Methotrexate+Methanol+ATP (MMA) groups. We inhibited tetrahydrofolate synthesis by methotrexate to induce methanol toxicity. Methotrexate was administered to MXG, MXM, and MMA group animals for seven days with a catheter directly to the stomach at a 0,3 mg/kg dose per day. At the end of this period, % 20 methanol at a dose of 3 g/kg was administered to MeOH, MMA and MXM group animals. Immediately after methanol application, MMA group animals were injected with ATP at a 4 mg/kg dose intraperitoneally. Blood samples and heart tissues were used for biochemical analysis and histopathological examination. Co-exposure to methanol and methotrexate substantially exacerbated cardiac damage, indicating the potent cardiotoxic effects of methanol. However, the administration of exogenous ATP to MMA group animals brought biochemical oxidative damage parameters and histopathological findings closer to HG.
{"title":"The preventive effect of exogenous adenosine triphosphate on methanol-induced cardiotoxicity in rats","authors":"R. Coşkun, A. Celik, M. S. Coşgun, R. Mammadov","doi":"10.1590/s2175-97902023e21220","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21220","url":null,"abstract":"Exposure to methanol can cause serious consequences such as permanent visual disturbances and death. The heart tissue is highly vulnerable to ATP deficiency. Our study aimed to investigate whether exogenous ATP administration may alleviate methanol-induced ATP deficiency and subsequent oxidative damage in rat heart tissue. A total of 30 rats were divided into equal five groups; Healthy Group (HG), Methotrexate (MXG), Methanol (MeOH), Methotrexate+Methanol (MXM), and Methotrexate+Methanol+ATP (MMA) groups. We inhibited tetrahydrofolate synthesis by methotrexate to induce methanol toxicity. Methotrexate was administered to MXG, MXM, and MMA group animals for seven days with a catheter directly to the stomach at a 0,3 mg/kg dose per day. At the end of this period, % 20 methanol at a dose of 3 g/kg was administered to MeOH, MMA and MXM group animals. Immediately after methanol application, MMA group animals were injected with ATP at a 4 mg/kg dose intraperitoneally. Blood samples and heart tissues were used for biochemical analysis and histopathological examination. Co-exposure to methanol and methotrexate substantially exacerbated cardiac damage, indicating the potent cardiotoxic effects of methanol. However, the administration of exogenous ATP to MMA group animals brought biochemical oxidative damage parameters and histopathological findings closer to HG.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"74 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67738831","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/s2175-97902023e21738
Juliana Machado Kayser, Gabriela Zimmermann Prado Rodrigues, Carlos Henrique Thomazi, Alana Witt Hansen, Marina Griebeler Moreira, M. Pitta, I. Pitta, A. L. Ziulkoski, A. H. Betti
Schizophrenia is an illness that affects 26 million people worldwide. However, conventional antipsychotics present side effects and toxicity, highlighting the need for new antipsychotics. We aimed to evaluate the cytotoxicity of haloperidol (HAL), clozapine (CLO), and a new molecule with antipsychotic potential, PT-31, in NIH-3T3 cells. The neutral red uptake assay and the MTT assay were performed to evaluate cell viability and mitochondrial activity, morphological changes were assessed, and intracellular reactive oxygen species (ROS) detection was performed. HAL and CLO (0.1 μM) showed a decrease in cell viability in the neutral red uptake assay and in the MTT assay. In addition, cell detachment, content decrease, rounding and cell death were also observed at 0.1 μM for both antipsychotics. An increase in ROS was observed for HAL (0.001, 0.01 and 1 μM) and CLO (0.01 and 1 μM). PT-31 did not alter cell viability in any of the assays, although it increased ROS at 0.01 and 1 μM. HAL and CLO present cytotoxicity at 0.1 μM, possibly through apoptosis and necrosis. In contrast, PT-31 does not present cytotoxicity to NIH-3T3 cells. Further studies must be performed for a better understanding of these mechanisms and the potential risk of conventional antipsychotics.
{"title":"Cytotoxicity evaluation of haloperidol, clozapine and a new molecule with antipsychotic potential, PT-31, in NIH-3T3 cells","authors":"Juliana Machado Kayser, Gabriela Zimmermann Prado Rodrigues, Carlos Henrique Thomazi, Alana Witt Hansen, Marina Griebeler Moreira, M. Pitta, I. Pitta, A. L. Ziulkoski, A. H. Betti","doi":"10.1590/s2175-97902023e21738","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21738","url":null,"abstract":"Schizophrenia is an illness that affects 26 million people worldwide. However, conventional antipsychotics present side effects and toxicity, highlighting the need for new antipsychotics. We aimed to evaluate the cytotoxicity of haloperidol (HAL), clozapine (CLO), and a new molecule with antipsychotic potential, PT-31, in NIH-3T3 cells. The neutral red uptake assay and the MTT assay were performed to evaluate cell viability and mitochondrial activity, morphological changes were assessed, and intracellular reactive oxygen species (ROS) detection was performed. HAL and CLO (0.1 μM) showed a decrease in cell viability in the neutral red uptake assay and in the MTT assay. In addition, cell detachment, content decrease, rounding and cell death were also observed at 0.1 μM for both antipsychotics. An increase in ROS was observed for HAL (0.001, 0.01 and 1 μM) and CLO (0.01 and 1 μM). PT-31 did not alter cell viability in any of the assays, although it increased ROS at 0.01 and 1 μM. HAL and CLO present cytotoxicity at 0.1 μM, possibly through apoptosis and necrosis. In contrast, PT-31 does not present cytotoxicity to NIH-3T3 cells. Further studies must be performed for a better understanding of these mechanisms and the potential risk of conventional antipsychotics.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67741064","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/s2175-97902023e21308
Swarupanjali Padhi, R. Mazumder, Dr..Shradha Bisht
Development of ceftriaxone loaded nanostructured lipid carriers to increase permeability of ceftriaxone across uninflamed meninges after parenteral administration. Lipids were selected by theoretical and experimental techniques and optimization of NLCs done by response surface methodology using Box-Behnken design. The Δ δt for glyceryl monostearate and Capryol90 were 4.39 and 2.92 respectively. The drug had maximum solubility of 0.175% (w/w) in glycerol monostearate and 2.56g of Capryol90 dissolved 10mg of drug. The binary mixture consisted of glyceryl monostearate and Capryol90 in a ratio of 70:30. The optimized NLCs particle size was 130.54nm, polydispersity index 0.28, % entrapment efficiency 44.32%, zeta potential -29.05mV, and % drug loading 8.10%. In vitro permeability of ceftriaxone loaded NLCs was 5.06x10 -6 cm/s; evidently, the NLCs pervaded through uninflamed meninges, which, was further confirmed from in vivo biodistribution studies. The ratio of drug concentration between brain and plasma for ceftriaxone loaded NLCs was 0.29 and that for ceftriaxone solution was 0.02. With 44.32% entrapment of the drug in NLCs the biodistribution of ceftriaxone was enhanced 7.9 times compared with that of ceftriaxone solution. DSC and XRD studies revealed formation of imperfect crystalline NLCs. NLCs improved permeability of ceftriaxone through uninflamed meninges resulting in better management of CNS infections.
{"title":"Preformulation screening of lipids using solubility parameter concept in conjunction with experimental research to develop ceftriaxone loaded nanostructured lipid carriers","authors":"Swarupanjali Padhi, R. Mazumder, Dr..Shradha Bisht","doi":"10.1590/s2175-97902023e21308","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21308","url":null,"abstract":"Development of ceftriaxone loaded nanostructured lipid carriers to increase permeability of ceftriaxone across uninflamed meninges after parenteral administration. Lipids were selected by theoretical and experimental techniques and optimization of NLCs done by response surface methodology using Box-Behnken design. The Δ δt for glyceryl monostearate and Capryol90 were 4.39 and 2.92 respectively. The drug had maximum solubility of 0.175% (w/w) in glycerol monostearate and 2.56g of Capryol90 dissolved 10mg of drug. The binary mixture consisted of glyceryl monostearate and Capryol90 in a ratio of 70:30. The optimized NLCs particle size was 130.54nm, polydispersity index 0.28, % entrapment efficiency 44.32%, zeta potential -29.05mV, and % drug loading 8.10%. In vitro permeability of ceftriaxone loaded NLCs was 5.06x10 -6 cm/s; evidently, the NLCs pervaded through uninflamed meninges, which, was further confirmed from in vivo biodistribution studies. The ratio of drug concentration between brain and plasma for ceftriaxone loaded NLCs was 0.29 and that for ceftriaxone solution was 0.02. With 44.32% entrapment of the drug in NLCs the biodistribution of ceftriaxone was enhanced 7.9 times compared with that of ceftriaxone solution. DSC and XRD studies revealed formation of imperfect crystalline NLCs. NLCs improved permeability of ceftriaxone through uninflamed meninges resulting in better management of CNS infections.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67739710","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/s2175-97902023e19334
Jyotsna Sharma, Savita Sharma, A. Koul, R. Shankarayan, S. Mallubhotla
the therapeutic potential of traditionally acclaimed medicinal herb Nanorrhinum ramosissimum , using plant parts extracted with different solvents (10 mg/mL). Shoot extracts exhibited comparatively better antimicrobial properties, in comparison to root extracts. Total phenolic content was estimated, to ascertain its dependency on antioxidant properties of plant extracts. Antioxidant assay revealed promising results in comparison to IC 50 value of standard ascorbic acid (52.2±0.07 µg/mL), for methanolic extracts of shoot (61.07±0.53 µg/mL and 64.33±0.33 µg/mL) and root (76.705±0.12 µg/mL and 89.73±0.28 µg/ mL) for in vivo and in vitro regenerants respectively. Correlation coefficient R 2 values ranged between 0.90-0.95, indicating a positive correlation between phenolic contents and antioxidant activity. Plant extracts were also able to inhibit DNA oxidative damage again indicating their antioxidative potential. Antidiabetic potential was confirmed by alpha amylase inhibition assay where shoot methanolic extracts ( invivo , in vitro ) exhibited the best IC 50 values (54.42±0.16 µg/ mL, 66.09±0.12 µg/mL) in comparison to standard metformin (41.92±0.08 µg/mL). Ethanolic extracts of roots ( in vitro, invivo ) exhibited the relative IC 50 values (88.97±0.32µg/mL,96.63±0.44 µg/mL) indicating that shoot parts had a better alpha amylase inhibition property; thus proving the herb’s bioactive potential and its prospective therapeutic source for curing various ailments.
{"title":"Bioactivity evaluation of least explored traditionally acclaimed medicinally potent herb Nanorrhinum ramosissimum(Wall.) Betsche","authors":"Jyotsna Sharma, Savita Sharma, A. Koul, R. Shankarayan, S. Mallubhotla","doi":"10.1590/s2175-97902023e19334","DOIUrl":"https://doi.org/10.1590/s2175-97902023e19334","url":null,"abstract":"the therapeutic potential of traditionally acclaimed medicinal herb Nanorrhinum ramosissimum , using plant parts extracted with different solvents (10 mg/mL). Shoot extracts exhibited comparatively better antimicrobial properties, in comparison to root extracts. Total phenolic content was estimated, to ascertain its dependency on antioxidant properties of plant extracts. Antioxidant assay revealed promising results in comparison to IC 50 value of standard ascorbic acid (52.2±0.07 µg/mL), for methanolic extracts of shoot (61.07±0.53 µg/mL and 64.33±0.33 µg/mL) and root (76.705±0.12 µg/mL and 89.73±0.28 µg/ mL) for in vivo and in vitro regenerants respectively. Correlation coefficient R 2 values ranged between 0.90-0.95, indicating a positive correlation between phenolic contents and antioxidant activity. Plant extracts were also able to inhibit DNA oxidative damage again indicating their antioxidative potential. Antidiabetic potential was confirmed by alpha amylase inhibition assay where shoot methanolic extracts ( invivo , in vitro ) exhibited the best IC 50 values (54.42±0.16 µg/ mL, 66.09±0.12 µg/mL) in comparison to standard metformin (41.92±0.08 µg/mL). Ethanolic extracts of roots ( in vitro, invivo ) exhibited the relative IC 50 values (88.97±0.32µg/mL,96.63±0.44 µg/mL) indicating that shoot parts had a better alpha amylase inhibition property; thus proving the herb’s bioactive potential and its prospective therapeutic source for curing various ailments.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67736281","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/s2175-97902023e21460
M. B. Freitas-Marques, O. P. Almeida, Flávia Lidiane Oliveira da Silva, B. Araújo, J. Ardisson, R. Sebastião, W. Mussel, M. Yoshida, Guilherme Carneiro
Clay minerals are still widely used in pharmaceutical products for human health and cosmetic purposes. Pre-formulation studies were conducted to identify solid-state properties of pink clay, a sample from Diamantina, Brazil. Among the solid properties to be analyzed, we have selected type identification, iron phases, crystallinity, powder flow characteristics, thermal behavior, and non-isothermal phase transition kinetics. The pink clay is composed of (1:1) clay type and kaolinite as the main component. The Mössbauer spectrum of pink clay shows Fe 3+ (α-Fe 2 O 3 ) hematite, Fe 2+ , and Fe 3+ with large Δ/2ξq of about 2.80 and 2.69 mm.s -1 respectively, related to iron silicates, most likely pyroxene, and a superparamagnetic Fe 3+ . Pink clay exhibits poor flow properties. The thermal behavior indicates a phase-transition between 400 - 600 ºC associated with the dehydroxylation of the pink clay system requiring ~300 kJ mol -1 , being constant until the process reaches a conversion of ~50% when the energy is enhanced to ~530 kJ mol -1 , concluding the whole dehydroxylation process (α=80%). Solid-state properties and characteristics found for the pink clay must be considered for the proper design of formulations. This type of clay shows unique pharmaceutical properties that can be favorably exploited by the cosmetic industry.
{"title":"Solid-state properties of pink clay from Jequitinhonha Valley in Brazil for pre-formulation study","authors":"M. B. Freitas-Marques, O. P. Almeida, Flávia Lidiane Oliveira da Silva, B. Araújo, J. Ardisson, R. Sebastião, W. Mussel, M. Yoshida, Guilherme Carneiro","doi":"10.1590/s2175-97902023e21460","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21460","url":null,"abstract":"Clay minerals are still widely used in pharmaceutical products for human health and cosmetic purposes. Pre-formulation studies were conducted to identify solid-state properties of pink clay, a sample from Diamantina, Brazil. Among the solid properties to be analyzed, we have selected type identification, iron phases, crystallinity, powder flow characteristics, thermal behavior, and non-isothermal phase transition kinetics. The pink clay is composed of (1:1) clay type and kaolinite as the main component. The Mössbauer spectrum of pink clay shows Fe 3+ (α-Fe 2 O 3 ) hematite, Fe 2+ , and Fe 3+ with large Δ/2ξq of about 2.80 and 2.69 mm.s -1 respectively, related to iron silicates, most likely pyroxene, and a superparamagnetic Fe 3+ . Pink clay exhibits poor flow properties. The thermal behavior indicates a phase-transition between 400 - 600 ºC associated with the dehydroxylation of the pink clay system requiring ~300 kJ mol -1 , being constant until the process reaches a conversion of ~50% when the energy is enhanced to ~530 kJ mol -1 , concluding the whole dehydroxylation process (α=80%). Solid-state properties and characteristics found for the pink clay must be considered for the proper design of formulations. This type of clay shows unique pharmaceutical properties that can be favorably exploited by the cosmetic industry.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67739470","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/s2175-97902023e20229
B. Nwiloh, A. Uwakwe
Malaria, a disease of public health concern is a known cause of kidney failure, and dependence on herbal medicines for its treatment is increasing due to the high cost of drugs. So this study is designed to evaluate the ameliorating effect of ethanol extract from Salacia nitida root bark on electrolyte and renal perturbations in Plasmodium berghei-infected mice. Thirty malaria-infected mice divided into five groups of six mice each and another group of six uninfected mice were used for the study. 280, 430, and 580 mg/kg of extract were given to infected mice in groups B, C, and D, 4 mg/kg of artesunate given to group E mice, and 4 ml/kg of physiological saline given to group A and uninfected group F mice for five days. Serum Na + , K + , HCO 3-, Cl - , TB, urea, creatinine, BUN concentrations, and BUN/creatinine ratio were determined using standard methods. Results showed significant increases ( p < 0.05) in Na + , K + , and HCO 3-and decreases in Cl - , TB, urea, creatinine, BUN, and BUN/creatinine ratio in the infected treated mice in groups B - E. This study showed that ethanol extract of S. nitida root bark is efficient in the treatment of renal disorders and blood electrolyte perturbations.
{"title":"Ameliorating effects of ethanol extract of root bark of Salacia nitida on blood electrolyte and renal perturbations in Plasmodium berghei-infected mice","authors":"B. Nwiloh, A. Uwakwe","doi":"10.1590/s2175-97902023e20229","DOIUrl":"https://doi.org/10.1590/s2175-97902023e20229","url":null,"abstract":"Malaria, a disease of public health concern is a known cause of kidney failure, and dependence on herbal medicines for its treatment is increasing due to the high cost of drugs. So this study is designed to evaluate the ameliorating effect of ethanol extract from Salacia nitida root bark on electrolyte and renal perturbations in Plasmodium berghei-infected mice. Thirty malaria-infected mice divided into five groups of six mice each and another group of six uninfected mice were used for the study. 280, 430, and 580 mg/kg of extract were given to infected mice in groups B, C, and D, 4 mg/kg of artesunate given to group E mice, and 4 ml/kg of physiological saline given to group A and uninfected group F mice for five days. Serum Na + , K + , HCO 3-, Cl - , TB, urea, creatinine, BUN concentrations, and BUN/creatinine ratio were determined using standard methods. Results showed significant increases ( p < 0.05) in Na + , K + , and HCO 3-and decreases in Cl - , TB, urea, creatinine, BUN, and BUN/creatinine ratio in the infected treated mice in groups B - E. This study showed that ethanol extract of S. nitida root bark is efficient in the treatment of renal disorders and blood electrolyte perturbations.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67737163","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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