cometadata/datacite-titles-descriptions-related-identifiers huggingface dataset:
DOI: 10.6084/m9.figshare.6125348
title: Investigation of the parameters affecting the release of flurbiprofen from chitosan microspheres

description: ABSTRACT Flurbiprofen (FLB), a NSAID, widely used for preventing pain generally for arthritis or dental problems. In this study, FLB loaded chitosan microspheres were prepared by ionotropic gelation method. In this method, microspheres were formed by dropping chitosan solutions containing FLB into sodium alginate solutions including sodium tripolyphosphate (TPP). A variety of formulation parameters like drug:polymer ratio, drug concentration, polymer’s molecular weight, polymer concentration, pH and the concentration of TPP solutions, drying method and stirring time were analyzed. The dissolution studies were performed in a shaking water bath in pH 7.4 phosphate buffer saline (PBS) at 37 °C. Laser diffractometer was used for particle size analysis, and scanning electron microscope (SEM) was used for morphological properties. Drug loading and loading efficiency were calculated by using UV spectrophotometer. The particles obtained were spherical with 0.7-1.3 mm size range, and the loading efficiency was approximately 21-79%. The dissolution studies conducted revealed that drug:polimer ratio and the polymer type and concentration affected the drug release from microspheres. It was observed that increasing the polymer concentration, polymer’s molecular weight and TPP concentration decreased the FLB release from microspheres, which was according to Higuchi kinetics.
DOI: 10.6084/m9.figshare.6125348.v1
title: Investigation of the parameters affecting the release of flurbiprofen from chitosan microspheres

description: ABSTRACT Flurbiprofen (FLB), a NSAID, widely used for preventing pain generally for arthritis or dental problems. In this study, FLB loaded chitosan microspheres were prepared by ionotropic gelation method. In this method, microspheres were formed by dropping chitosan solutions containing FLB into sodium alginate solutions including sodium tripolyphosphate (TPP). A variety of formulation parameters like drug:polymer ratio, drug concentration, polymer’s molecular weight, polymer concentration, pH and the concentration of TPP solutions, drying method and stirring time were analyzed. The dissolution studies were performed in a shaking water bath in pH 7.4 phosphate buffer saline (PBS) at 37 °C. Laser diffractometer was used for particle size analysis, and scanning electron microscope (SEM) was used for morphological properties. Drug loading and loading efficiency were calculated by using UV spectrophotometer. The particles obtained were spherical with 0.7-1.3 mm size range, and the loading efficiency was approximately 21-79%. The dissolution studies conducted revealed that drug:polimer ratio and the polymer type and concentration affected the drug release from microspheres. It was observed that increasing the polymer concentration, polymer’s molecular weight and TPP concentration decreased the FLB release from microspheres, which was according to Higuchi kinetics.
DOI: 10.6084/m9.figshare.20039250
title: Antioxidant activity, antibacterial potential and characterization of active fraction of Dioscorea pentaphylla L. tuber extract collected from Similipal Biosphere Reserve, Odisha, India

description: ABSTRACT Dioscorea pentaphylla L., a wild tuber is used both as food and medicines among different ethnic groups of Similipal Biosphere Reserve, India. Tubers are used against skin infections. In order to establish and confirm tribal claims, methanol extract was subjected to fractionation. The active fraction (DP1) was subsequently used for further purification and NMR (Nuclear magnetic resonance) characterization. The phytochemical analysis revealed the presence of saponin groups. The antibacterial activity of DP1 was done against selected bacterial strains (Salmonella typhi, Shigella flexneri, Streptococcus pyogenes, Streptococcus mutans and Vibrio cholerae) using DD (disc diffusion), AWD (agar well diffusion) and broth dilution assay. The activity was compared with antibiotics Penicillin and Kanamycin. It was observed that DP1 showed significant inhibitory activity against the tested bacteria. The characterization of DP1 through NMR analysis and presence of proton in carbon position at C-3, C-19, C-18, C-21 and C-27 was same as the known compound “Diosgenin”. Therefore, isolated compound was confirmed to be Diosgenin. The study for the first time showed that, diosgenin present in D. pentaphylla tuber was responsible for antibacterial and antioxidant potential. Present study highlights the importance of Dioscorea species as sources of diverse secondary metabolites for the isolation of active compound(s).
DOI: 10.6084/m9.figshare.20039250.v1
title: Antioxidant activity, antibacterial potential and characterization of active fraction of Dioscorea pentaphylla L. tuber extract collected from Similipal Biosphere Reserve, Odisha, India

description: ABSTRACT Dioscorea pentaphylla L., a wild tuber is used both as food and medicines among different ethnic groups of Similipal Biosphere Reserve, India. Tubers are used against skin infections. In order to establish and confirm tribal claims, methanol extract was subjected to fractionation. The active fraction (DP1) was subsequently used for further purification and NMR (Nuclear magnetic resonance) characterization. The phytochemical analysis revealed the presence of saponin groups. The antibacterial activity of DP1 was done against selected bacterial strains (Salmonella typhi, Shigella flexneri, Streptococcus pyogenes, Streptococcus mutans and Vibrio cholerae) using DD (disc diffusion), AWD (agar well diffusion) and broth dilution assay. The activity was compared with antibiotics Penicillin and Kanamycin. It was observed that DP1 showed significant inhibitory activity against the tested bacteria. The characterization of DP1 through NMR analysis and presence of proton in carbon position at C-3, C-19, C-18, C-21 and C-27 was same as the known compound “Diosgenin”. Therefore, isolated compound was confirmed to be Diosgenin. The study for the first time showed that, diosgenin present in D. pentaphylla tuber was responsible for antibacterial and antioxidant potential. Present study highlights the importance of Dioscorea species as sources of diverse secondary metabolites for the isolation of active compound(s).
DOI: 10.6084/m9.figshare.6125351.v1
title: Development of radioimmunoconjugate for diagnosis and management of head-and-neck subclinical cancer and colorectal carcinoma

description: ABSTRACT Scientific innovations in diagnostic methods are important drivers of cancer control and prevention. Noninvasive imaging of the epidermal growth factor receptor (EGFR) in head-and-neck squamous, cell carcinoma and colorectal cancer could be valuable to select patients for EGFR-targeted therapy, as well as to monitor the efficacy and occurrence of resistance to immunotherapy. In order to develop the first Brazilian radioimmunoconjugate for diagnosis, Cetuximab has been conjugated to p-SCN-Bn-DTPA chelator and radiolabeled with Indium-111. The conjugation methodology was optimized using different mAb:DTPA molar ratios, time was then reduced for immunoconjugate preparation, besides the protein recovery’ percentage increased after purification (m = 83.8 ± 0.91 %). The stability of Cetuximab-DTPA at - 20 oC was evaluated for six months, and its integrity was greater than 90% (m =93.9 ± 1.5%, N = 24). The radioimmunoconjugate with specific activity of 185 MBq/mg showed radiochemical purity above 95% (m=96.8 ± 1.31 %, N = 15). We conclude that the radioimmunoconjugate 111In-DTPA-cetuximab is stable and may be applied to the diagnosis of EGFR-positive tumors.
DOI: 10.6084/m9.figshare.6125351
title: Development of radioimmunoconjugate for diagnosis and management of head-and-neck subclinical cancer and colorectal carcinoma

description: ABSTRACT Scientific innovations in diagnostic methods are important drivers of cancer control and prevention. Noninvasive imaging of the epidermal growth factor receptor (EGFR) in head-and-neck squamous, cell carcinoma and colorectal cancer could be valuable to select patients for EGFR-targeted therapy, as well as to monitor the efficacy and occurrence of resistance to immunotherapy. In order to develop the first Brazilian radioimmunoconjugate for diagnosis, Cetuximab has been conjugated to p-SCN-Bn-DTPA chelator and radiolabeled with Indium-111. The conjugation methodology was optimized using different mAb:DTPA molar ratios, time was then reduced for immunoconjugate preparation, besides the protein recovery’ percentage increased after purification (m = 83.8 ± 0.91 %). The stability of Cetuximab-DTPA at - 20 oC was evaluated for six months, and its integrity was greater than 90% (m =93.9 ± 1.5%, N = 24). The radioimmunoconjugate with specific activity of 185 MBq/mg showed radiochemical purity above 95% (m=96.8 ± 1.31 %, N = 15). We conclude that the radioimmunoconjugate 111In-DTPA-cetuximab is stable and may be applied to the diagnosis of EGFR-positive tumors.
DOI: 10.6084/m9.figshare.6235592
title: Solubility and dissolution enhancement of flurbiprofen by solid dispersion using hydrophilic carriers

description: ABSTRACT The intent of the current work is to study the effect of polyethylene glycol 8000 and polyethylene glycol 10000 as hydrophilic carriers on dissolution behaviour of flurbiprofen. In the present study, solvent evaporation method was used to prepare flurbiprofen solid dispersions and evaluated for physico-chemical properties, drug-carrier compatibility studies and dissolution behaviour of drug. Solubility studies showed more solubility in higher pH values and formulations SD4 and SD8 were selected to prepare the fast dissolving tablets. FTIR and DSC study showed no interaction and drug was dispersed molecularly in hydrophilic carrier. XRD studies revealed that there was change in the crystallinity of the drug. The results of In vitro studies showed SD8 formulation confer significant improvement (p&lt;0.05) in drug release, Q20 was 99.08±1.35% compared to conventional and marketed tablets (47.31±0.74% and 56.86±1.91%). The mean dissolution time (MDT) was reduced to 8.79 min compared to conventional and marketed tablets (25.76 and 22.22 min.) indicating faster drug release. The DE (% dissolution efficiency) was increased by 2.5 folds (61.63%) compared to conventional tablets (23.71%). From the results, it is evident that polyethylene glycol solid dispersions in less carrier ratio may enhance the solubility and there by improve the dissolution rate of flurbiprofen.
DOI: 10.6084/m9.figshare.6235592.v1
title: Solubility and dissolution enhancement of flurbiprofen by solid dispersion using hydrophilic carriers

description: ABSTRACT The intent of the current work is to study the effect of polyethylene glycol 8000 and polyethylene glycol 10000 as hydrophilic carriers on dissolution behaviour of flurbiprofen. In the present study, solvent evaporation method was used to prepare flurbiprofen solid dispersions and evaluated for physico-chemical properties, drug-carrier compatibility studies and dissolution behaviour of drug. Solubility studies showed more solubility in higher pH values and formulations SD4 and SD8 were selected to prepare the fast dissolving tablets. FTIR and DSC study showed no interaction and drug was dispersed molecularly in hydrophilic carrier. XRD studies revealed that there was change in the crystallinity of the drug. The results of In vitro studies showed SD8 formulation confer significant improvement (p&lt;0.05) in drug release, Q20 was 99.08±1.35% compared to conventional and marketed tablets (47.31±0.74% and 56.86±1.91%). The mean dissolution time (MDT) was reduced to 8.79 min compared to conventional and marketed tablets (25.76 and 22.22 min.) indicating faster drug release. The DE (% dissolution efficiency) was increased by 2.5 folds (61.63%) compared to conventional tablets (23.71%). From the results, it is evident that polyethylene glycol solid dispersions in less carrier ratio may enhance the solubility and there by improve the dissolution rate of flurbiprofen.
DOI: 10.6084/m9.figshare.6504290.v1
title: Importance of the agar-media in the evaluation of bacteriocin activity against the same test-microorganisms

description: Abstract Bacteriocins are peptides produced by various species of bacteria, especially lactic acid bacteria, which exhibit a large spectrum of action against spoilage bacteria and foodborne pathogens. Successful application of techniques for quantitative or qualitative bacteriocin determination relies not only on the sensitivity of the test-microorganisms, but also on the agar-medium employed. Cell free supernatants are routinely used to preliminary screen for antimicrobial activity of bacteria by means of the agar well diffusion method, but the supernatant may also include other molecules (such as medium components and/or intracellular compounds) accidentally released during cell free supernatant preparation, which may interfere with the assay. Reproducibility of bacteriocin activity against the same test-microorganisms is an important factor to be considered. Unfortunately, no specific information about bioassays standardization to determine bacteriocin activity is available in the literature. In this work, growth inhibition by means of the agar well diffusion assays were carried out on different agar-media showing a strong dependence on the agar-medium used, indicating that the inhibitory effects could also depend on the diffusion of exudates that are included in the cell-free supernatant. The results presented in this communication show that selection of the agar-medium is crucial for the bioassay response.
DOI: 10.6084/m9.figshare.6504290
title: Importance of the agar-media in the evaluation of bacteriocin activity against the same test-microorganisms

description: Abstract Bacteriocins are peptides produced by various species of bacteria, especially lactic acid bacteria, which exhibit a large spectrum of action against spoilage bacteria and foodborne pathogens. Successful application of techniques for quantitative or qualitative bacteriocin determination relies not only on the sensitivity of the test-microorganisms, but also on the agar-medium employed. Cell free supernatants are routinely used to preliminary screen for antimicrobial activity of bacteria by means of the agar well diffusion method, but the supernatant may also include other molecules (such as medium components and/or intracellular compounds) accidentally released during cell free supernatant preparation, which may interfere with the assay. Reproducibility of bacteriocin activity against the same test-microorganisms is an important factor to be considered. Unfortunately, no specific information about bioassays standardization to determine bacteriocin activity is available in the literature. In this work, growth inhibition by means of the agar well diffusion assays were carried out on different agar-media showing a strong dependence on the agar-medium used, indicating that the inhibitory effects could also depend on the diffusion of exudates that are included in the cell-free supernatant. The results presented in this communication show that selection of the agar-medium is crucial for the bioassay response.
DOI: 10.6084/m9.figshare.6272816
title: The role of selenium in insulin resistance

description: ABSTRACT In recent years, there has been growing interest in clarifying the pathogenesis of some chronic diseases, such as obesity and type 2 diabetes mellitus. Metabolic alterations in these diseases are characterized by chronic hyperglycemia and insulin resistance. Studies have demonstrated the participation of minerals in the pathogenesis of insulin resistance, more specifically their involvement in the synthesis and regulation of insulin. Selenium is an anti-inflammatory and antioxidant micronutrient that is essential for the activity of selenoproteins. Two selenoproteins (glutathione peroxidase and selenoprotein P) are known to be involved in the insulin signaling pathway. The aim of this review is to provide an update on the role of selenium in insulin resistance mechanisms. Evidence shows that adequate concentrations of selenium play a key role in the secretion and action of insulin, but an excess of selenium in the body is associated with the pathogenesis of insulin resistance and the development of diabetes mellitus.
DOI: 10.6084/m9.figshare.6272816.v1
title: The role of selenium in insulin resistance

description: ABSTRACT In recent years, there has been growing interest in clarifying the pathogenesis of some chronic diseases, such as obesity and type 2 diabetes mellitus. Metabolic alterations in these diseases are characterized by chronic hyperglycemia and insulin resistance. Studies have demonstrated the participation of minerals in the pathogenesis of insulin resistance, more specifically their involvement in the synthesis and regulation of insulin. Selenium is an anti-inflammatory and antioxidant micronutrient that is essential for the activity of selenoproteins. Two selenoproteins (glutathione peroxidase and selenoprotein P) are known to be involved in the insulin signaling pathway. The aim of this review is to provide an update on the role of selenium in insulin resistance mechanisms. Evidence shows that adequate concentrations of selenium play a key role in the secretion and action of insulin, but an excess of selenium in the body is associated with the pathogenesis of insulin resistance and the development of diabetes mellitus.
DOI: 10.6084/m9.figshare.6272834
title: Phage therapy: progress in pharmacokinetics

description: ABSTRACT The concept of phage therapy exists in the history and it has been ignored for a long time, but the consequence of drug resistance in pathogen bacteria has forced the forgotten kingdom of phage therapy to be re-explored. However, for the successful implementation and acceptance of phage therapy worldwide, the number of factors need to be addressed. In pharmacology of phage therapy, pharmacodynamics is a straightforward concept, on the other hand, owing to the unique feature of phages to replicate and their high sensitivity, pharmacokinetics is rather complex. In this review, we have discussed pharmacokinetics and some recent advances in delivery systems as to achieve the therapeutically effective concentrations of phage in their activated form.
DOI: 10.6084/m9.figshare.6272834.v1
title: Phage therapy: progress in pharmacokinetics

description: ABSTRACT The concept of phage therapy exists in the history and it has been ignored for a long time, but the consequence of drug resistance in pathogen bacteria has forced the forgotten kingdom of phage therapy to be re-explored. However, for the successful implementation and acceptance of phage therapy worldwide, the number of factors need to be addressed. In pharmacology of phage therapy, pharmacodynamics is a straightforward concept, on the other hand, owing to the unique feature of phages to replicate and their high sensitivity, pharmacokinetics is rather complex. In this review, we have discussed pharmacokinetics and some recent advances in delivery systems as to achieve the therapeutically effective concentrations of phage in their activated form.
DOI: 10.6084/m9.figshare.6504509
title: Glycemic effects of simvastatin: Where do we stand?

description: ABSTRACT In clinical practice, simvastatin is usually used in the treatment of dyslipidemia patients and those at risk of or with established cardiovascular disease. However, previous studies have shown that simvastatin has the potential to affect glycemic parameters as it reportedly reduced insulin secretion and sensitivity. The exact mechanism by which simvastatin affects glycemia is still unknown, but previous studies have postulated the involvement of the glucose-insulin secretion mechanism. This review focuses on the effects of simvastatin, either alone or in combination with other lipid lowering agents, antidiabetics and antihypertensives, on glucose homeostasis. Some studies have reported that simvastatin might impair the levels of glucose metabolism markers in the blood while others have reported no effect or improvement in glycemia.
DOI: 10.6084/m9.figshare.6504509.v1
title: Glycemic effects of simvastatin: Where do we stand?

description: ABSTRACT In clinical practice, simvastatin is usually used in the treatment of dyslipidemia patients and those at risk of or with established cardiovascular disease. However, previous studies have shown that simvastatin has the potential to affect glycemic parameters as it reportedly reduced insulin secretion and sensitivity. The exact mechanism by which simvastatin affects glycemia is still unknown, but previous studies have postulated the involvement of the glucose-insulin secretion mechanism. This review focuses on the effects of simvastatin, either alone or in combination with other lipid lowering agents, antidiabetics and antihypertensives, on glucose homeostasis. Some studies have reported that simvastatin might impair the levels of glucose metabolism markers in the blood while others have reported no effect or improvement in glycemia.
DOI: 10.6084/m9.figshare.6504521
title: Medication-related inpatient falls: a critical review

description: Abstract Falls are the second leading cause of accidental and unintentional injury deaths worldwide. Inpatient falls in hospital settings are likely to prolong the length of stay of patients in nearly 6.3 days, leading to increased hospitalization costs. The causes of fall incidents in healthcare facilities are multifactorial in nature and certain medications use could be associated with these incidents. This review seeks to critically evaluate the available literature regarding the relationship between inpatient falls and medication use. A comprehensive search was performed on MEDLINE, EMBASE and Lilacs with no time restriction. The search was filtered using English, Spanish or Portuguese languages. Our study evaluated medication use and inpatients falls that effectively happen, considering all ages and populations. An assessment of bias and quality of the studies was carried out using an adapted tool from the literature. The drugs were classified according to the Anatomic Therapeutics Chemical Code. The search strategy retrieved 563 records, among which 23 met the eligibility criteria; ninety three different pharmacological subgroups were associated with fall incidents. Our critical review suggests that the use of central nervous system drugs (including anxiolytics; hypnotics and sedatives; antipsychotics; opioids; antiepileptics and antidepressants) has a greater likelihood of causing inpatient falls. A weak relationship was found between other pharmacological subgroups, such as diuretics, cardiovascular system-related medications, and inpatient fall. Remarkably, several problems of quality were encountered with regard to the eligible studies. Among such quality problems included retrospective design, the grouping of more than one medication in the same statistical analysis, limited external validity, problems related to medication classifications and description of potential confounders.