cometadata/datacite-titles-descriptions-related-identifiers huggingface dataset:
DOI: 10.6084/m9.figshare.11452239.v1
title: Retrospective cost-utility and budget impact assessments of Hypericum perforatum in contrast with Fluoxetine treatment for depression in Karachi, Pakistan

description: In this study we have compared two different types of therapies i.e. herbal and allopathic system of therapies for Depression and studied them from the social perspectives. The Hypericum perforatum is compared with Fluoxetine [HCL] in terms of cost-utility and financial savings thereby evaluating its influence on annual expenditure of depressive patients that were randomly selected from 178 union councils of the city of Karachi, Pakistan. For both system of therapies a total of 356 patients were selected by stratified random sampling. Taking frequency of depression as ‘1’ annually with discount rate at 3% for calculating the burden-of-illness in terms of disability-adjusted-life-years. The cost-utility and the budget-impact assessments were carried out to assess incremental-cost-effectiveness-ratio, and the budget-impact-per-onset as well as budget-impact-per-year values. In comparison with the Fluoxetine therapy, the Hypericum perforatum was found to relieve symptoms in 21.47% less cost; owing 29.23% less disability-adjusted-life-years and 21.45% less budget-impact-per-onset as well as budget-impact-per-year. The annual mean incremental-cost-effectiveness-ratio was found to be at 36.95±270.74 (less than GDP per capita threshold of Rs. 38,173.02). Hypericum perforatum provide the optimal utility with less impact on budget of a patient in comparison with the treatment of symptoms of depression with Fluoxetine.
DOI: 10.6084/m9.figshare.11452242.v1
title: Simultaneous determination of anti-diabetic drugs

description: A novel reverse phase, isocratic HPLC method is described to separate five anti-diabetic drugs i.e., glimepiride, metformin, sitagliptin, rosiglitazone and pioglitazone. Nucleosil C18 analytical column was used as stationary phase, while mobile phase consisted of acetonitrile:phosphate buffer: methanol (40/40/20, v/v) pH 2.0. Effluent was monitored at a flow rate 1 mL/min and detected at wavelength of 240 nm. This research produced excellent chromatography over a wide concentration range of 25-10000 ng/mL. Sepprated and well resolved quantifiable peaks were obtained and test results were linear in this range. Correlation coefficient of more than 0.9990 was witnessed as well as Low %RSD values i.e., maximum 2.0% documented excellent precision of the method. Good recoveries from pharmaecutical (99-101%), urine and plasma samples (&gt;96%) in a range of concentrtion granted very good linearity, accuracy and precision. The projected method has satisfactory applications in quality control of these molecules as well as quantification of these molecules in urine and plasma samples.
DOI: 10.6084/m9.figshare.11452242
title: Simultaneous determination of anti-diabetic drugs

description: A novel reverse phase, isocratic HPLC method is described to separate five anti-diabetic drugs i.e., glimepiride, metformin, sitagliptin, rosiglitazone and pioglitazone. Nucleosil C18 analytical column was used as stationary phase, while mobile phase consisted of acetonitrile:phosphate buffer: methanol (40/40/20, v/v) pH 2.0. Effluent was monitored at a flow rate 1 mL/min and detected at wavelength of 240 nm. This research produced excellent chromatography over a wide concentration range of 25-10000 ng/mL. Sepprated and well resolved quantifiable peaks were obtained and test results were linear in this range. Correlation coefficient of more than 0.9990 was witnessed as well as Low %RSD values i.e., maximum 2.0% documented excellent precision of the method. Good recoveries from pharmaecutical (99-101%), urine and plasma samples (&gt;96%) in a range of concentrtion granted very good linearity, accuracy and precision. The projected method has satisfactory applications in quality control of these molecules as well as quantification of these molecules in urine and plasma samples.
DOI: 10.6084/m9.figshare.11452245
title: Development and optimization of erythromycin-loaded lipid-based gel by Taguchi design: In vitro characterization and antimicrobial evaluation

description: The foremost aim of the current research was to prolong and sustain the release of erythromycin (ERY) by preparing a solid lipid nanoparticles (SLNs)-based gel formulation for the safe and effective treatment of acne. ERY-loaded SLNs were developed, and various process variables were optimized with respect to particle size, zeta potential, and entrapment efficiency using the Taguchi model. The average particle size, PDI, zeta potential, drug entrapment efficiency, and drug loading of optimized SLN (F4) were found to be 176.2±1.82 nm, 0.275±0.011, -34.0±0.84, 73.56%, and 69.74% respectively. The optimized SLN (F4) was successfully incorporated into the carbopol-based hydrogel. The in vitro release of ERY from the SLN gel and plain gel were compared and found to be 90.94% and 87.94% respectively. In vitro study of ERY-loaded SLN gel showed sustained delivery of drug from formulation thus enhancing the antimicrobial activity after 30 hours when compared to ERY plain gel.
DOI: 10.6084/m9.figshare.11452245.v1
title: Development and optimization of erythromycin-loaded lipid-based gel by Taguchi design: In vitro characterization and antimicrobial evaluation

description: The foremost aim of the current research was to prolong and sustain the release of erythromycin (ERY) by preparing a solid lipid nanoparticles (SLNs)-based gel formulation for the safe and effective treatment of acne. ERY-loaded SLNs were developed, and various process variables were optimized with respect to particle size, zeta potential, and entrapment efficiency using the Taguchi model. The average particle size, PDI, zeta potential, drug entrapment efficiency, and drug loading of optimized SLN (F4) were found to be 176.2±1.82 nm, 0.275±0.011, -34.0±0.84, 73.56%, and 69.74% respectively. The optimized SLN (F4) was successfully incorporated into the carbopol-based hydrogel. The in vitro release of ERY from the SLN gel and plain gel were compared and found to be 90.94% and 87.94% respectively. In vitro study of ERY-loaded SLN gel showed sustained delivery of drug from formulation thus enhancing the antimicrobial activity after 30 hours when compared to ERY plain gel.
DOI: 10.6084/m9.figshare.11452236
title: Assessment of an anti-ageing structured cosmetic formulation containing goji berry

description: Based on previous studies, it has been found that goji berry (GB), popularly known as a ‘miracle fruit’, has excellent antioxidant potential and can be used in the treatment of skin disorders associated with ageing. This study aimed to incorporate GB into a structured cosmetic in order to optimise its penetration. Stability studies of the formulation, determination of the antioxidant activity of the extract and of the formulation, rheological measurements, SAXS, polarised light microscopy and bioadhesion analyses were performed. The results indicated the antioxidant activity of the extract, which can be incorporated into an emulsified cosmetic formulation. The emulsified formulation containing the extract remained stable, even after being submitted to thermal and luminous stresses for 30 days. In addition, rheological tests revealed that the addition of the GB soft extract reduced the viscosity of the formulation, increasing thixotropy and deformation. These systems were characterised by SAXS as a lamellar phase, which was confirmed by polarised light microscopy. These highly organised structures indicate their excellent stability. In vitro bioadhesion experiments revealed that these formulations exhibited skin adhesion strength statistically similar to commercial anti-ageing formulation. These results suggest that this formulation has excellent potential to be used as a topical treatment for ageing.
DOI: 10.6084/m9.figshare.11452236.v1
title: Assessment of an anti-ageing structured cosmetic formulation containing goji berry

description: Based on previous studies, it has been found that goji berry (GB), popularly known as a ‘miracle fruit’, has excellent antioxidant potential and can be used in the treatment of skin disorders associated with ageing. This study aimed to incorporate GB into a structured cosmetic in order to optimise its penetration. Stability studies of the formulation, determination of the antioxidant activity of the extract and of the formulation, rheological measurements, SAXS, polarised light microscopy and bioadhesion analyses were performed. The results indicated the antioxidant activity of the extract, which can be incorporated into an emulsified cosmetic formulation. The emulsified formulation containing the extract remained stable, even after being submitted to thermal and luminous stresses for 30 days. In addition, rheological tests revealed that the addition of the GB soft extract reduced the viscosity of the formulation, increasing thixotropy and deformation. These systems were characterised by SAXS as a lamellar phase, which was confirmed by polarised light microscopy. These highly organised structures indicate their excellent stability. In vitro bioadhesion experiments revealed that these formulations exhibited skin adhesion strength statistically similar to commercial anti-ageing formulation. These results suggest that this formulation has excellent potential to be used as a topical treatment for ageing.
DOI: 10.6084/m9.figshare.11452233
title: Influence of sonication and in vitro evaluation of nifedipine self-nanoemulsifying drug delivery system

description: In order to develop a self-nanoemulsifying system, three components, olive oil, Tween 80, and Capmul, were used to construct a ternary phase diagram that helped to find the optimum formulation, which was loaded with nifedipine. The effect of sonication on drug loading was also evaluated. After that, measurement of the droplet size, size distribution, zeta potential, and scanning electron microscopy were conducted for evaluation and characterisation of the formulations. The phase diagram of four formulations showed nanosizes below 200 nm; however, only one was selected to be loaded with nifedipine. The selected formulation had the lowest droplet size of 98 nm and size distribution 0.192, and was composed of 48% Tween 80, 32% Capmul, and 20% olive oil. The nifedipine self-nanoemulsifying drug delivery system (SNEDDS) showed a significant change in the particle size (97 nm) and size distribution (0.257) after sonication. Its zeta potential was -32.3 mV indicating good stability. The SEM photographs of nifedipine showed particles with spherical shape and smooth surface. Finally, a self-nanoemulsifying formulation containing nifedipine, loaded in olive oil, was successfully prepared by mixing the oil with various types of surfactants and co-surfactants. A significant nifedipine self-nanoemulsifying system was developed and significantly improved accordingly.
DOI: 10.6084/m9.figshare.11452233.v1
title: Influence of sonication and in vitro evaluation of nifedipine self-nanoemulsifying drug delivery system

description: In order to develop a self-nanoemulsifying system, three components, olive oil, Tween 80, and Capmul, were used to construct a ternary phase diagram that helped to find the optimum formulation, which was loaded with nifedipine. The effect of sonication on drug loading was also evaluated. After that, measurement of the droplet size, size distribution, zeta potential, and scanning electron microscopy were conducted for evaluation and characterisation of the formulations. The phase diagram of four formulations showed nanosizes below 200 nm; however, only one was selected to be loaded with nifedipine. The selected formulation had the lowest droplet size of 98 nm and size distribution 0.192, and was composed of 48% Tween 80, 32% Capmul, and 20% olive oil. The nifedipine self-nanoemulsifying drug delivery system (SNEDDS) showed a significant change in the particle size (97 nm) and size distribution (0.257) after sonication. Its zeta potential was -32.3 mV indicating good stability. The SEM photographs of nifedipine showed particles with spherical shape and smooth surface. Finally, a self-nanoemulsifying formulation containing nifedipine, loaded in olive oil, was successfully prepared by mixing the oil with various types of surfactants and co-surfactants. A significant nifedipine self-nanoemulsifying system was developed and significantly improved accordingly.
DOI: 10.6084/m9.figshare.11452254.v1
title: Toxicological effects of ciprofloxacin and chlorhexidine on growth and chlorophyll a synthesis of freshwater cyanobacteria

description: Cyanobacteria are phytoplanktonic microorganisms that are susceptible to the deleterious effects of pharmaceutical residues in the aquatic environment, which poses a challenge to the environment exposed to diverse pharmaceutical products and their potential effects. The objective of this study was to evaluate the effects of the antibiotic substances ciprofloxacin and chlorhexidine in pharmaceutical preparations on the growth and production of chlorophyll of two cyanobacterial strains, Microcystis aeruginosa and Microcystis panniformis, isolated from a lake in a Brazilian environmental protection area. The EC50 and EC10 of chlorhexidine for M. aeruginosa were 206.4 µg/L and 108.5 µg/L, respectively, and for M. panniformis were 171.4 µg/L and 116.6 µg/L, respectively. The EC50 and EC10 of ciprofloxacin for M. aeruginosa were 17.24 µg/L and 3.21 µg/L, respectively, and for M. panniformis were 13.56 µg/L and 1.50 µg/L, respectively. The toxicity of the antibiotic ciprofloxacin (drug) and chlorhexidine (standard solution) to the Microcystis species was demonstrated, and these species were both very sensitive to ciprofloxacin. Our results suggest that the strains of M. aeruginosa and M. panniformis may be affected by exposure to residues of ciprofloxacin (&gt;1.5 µg/L), which may represent a risk to the survival of aquatic species.
DOI: 10.6084/m9.figshare.11452254
title: Toxicological effects of ciprofloxacin and chlorhexidine on growth and chlorophyll a synthesis of freshwater cyanobacteria

description: Cyanobacteria are phytoplanktonic microorganisms that are susceptible to the deleterious effects of pharmaceutical residues in the aquatic environment, which poses a challenge to the environment exposed to diverse pharmaceutical products and their potential effects. The objective of this study was to evaluate the effects of the antibiotic substances ciprofloxacin and chlorhexidine in pharmaceutical preparations on the growth and production of chlorophyll of two cyanobacterial strains, Microcystis aeruginosa and Microcystis panniformis, isolated from a lake in a Brazilian environmental protection area. The EC50 and EC10 of chlorhexidine for M. aeruginosa were 206.4 µg/L and 108.5 µg/L, respectively, and for M. panniformis were 171.4 µg/L and 116.6 µg/L, respectively. The EC50 and EC10 of ciprofloxacin for M. aeruginosa were 17.24 µg/L and 3.21 µg/L, respectively, and for M. panniformis were 13.56 µg/L and 1.50 µg/L, respectively. The toxicity of the antibiotic ciprofloxacin (drug) and chlorhexidine (standard solution) to the Microcystis species was demonstrated, and these species were both very sensitive to ciprofloxacin. Our results suggest that the strains of M. aeruginosa and M. panniformis may be affected by exposure to residues of ciprofloxacin (&gt;1.5 µg/L), which may represent a risk to the survival of aquatic species.
DOI: 10.6084/m9.figshare.20039430
title: Tadalafil-loaded PLGA microspheres for pulmonary administration: preparation and evaluation

description: Tadalafil, a long-acting PED-5 inhibitor, is commonly used for the treatment of pulmonary arterial hypertension (PAH). However, its efficacy and clinical application are severely limited by the poor water solubility, low bioavailability and a series adverse effects (e.g. headaches, indigestion). In this study, tadalafil was prepared and loaded into biodegradable PLGA (poly(lactic-co-glycolic acid)) microspheres (TDF-PLGA-MS) via emulsification-solvent evaporation. The resulting microspheres were processed into pulmonary inhalant by freeze drying. The TDF-PLGA-MS was spherical and uniform, with an average particle diameter ~10.29 µm. The encapsulation efficiency and drug loading yield of TDF-PLGA-MS were 81.68% and 8.52%, respectively. The investigation of micromeritics showed that the TDF-PLGA-MS had low moisture content. The fluidity of powders was relatively good. The aerodynamic diameter and emptying rate of microspheres powders were 3.92 µm and 95.41%, respectively. Therefore, the microspheres powders were easy to be atomized, and can meet the requirements of pulmonary administration. In vitro release results showed that the microspheres group released slowly. The cumulative release in 24 h and 10 d was 46.87% and 84.06%, respectively. The in vitro release profile of TDF-PLGA-MS was in accordance with the Weibull model. The results of Pharmacokinetics showed that tadalafil from microspheres slowly released into the blood after intratracheal instillation. The pulmonary drug residue in 0.5 h was 3.5 times compared with solution group. The residual concentration in lung after 10d was still higher than that of solution group in 48 h. The t1/2β and MRT0-∞ were 3.10 times and 3.96 times that of solution group, respectively. Moreover, the Cmax and AUC of drug residues in lung were 3.48 times and 16.36 times that of solution group, respectively. The results of tissue distribution showed that the Re in lung was 16.358, which indicated the lung targeting. In conclusion, the TDF-PLGA-MS for pulmonary administration in this study can significantly improve the pulmonary targeting, increase efficacy of tadalafil and reduce other non-target organs toxicity. This study will have an important clinical significance for PAH patients who need long-term drug therapy.
DOI: 10.6084/m9.figshare.11453151
title: Delay of neuropathic pain sensitization after application of dexamethasone-loaded implant in sciatic nerve-injured rats

description: Neuroimmune interactions underlying the development of pain sensitization in models of neuropathic pain have been widely studied. In this study, we evaluated the development of allodynia and its reduction associated with peripheral antineuroinflammatory effects induced by a dexamethasone-loaded biodegradable implant. Chronic constriction injury (CCI) of the sciatic nerve was performed in Wistar rats. The electronic von Frey test was applied to assess mechanical allodynia. The dexamethasone-loaded implant was placed perineurally at the moment of CCI or 12 days after surgery. Dorsal root ganglia (DRG; L4-L5) were harvested and nuclear extracts were assayed by Western blot for detection of nuclear factor (NF)-κB p65/RelA translocation. Dexamethasone delivered from the implant delayed the development of allodynia for approximately three weeks in CCI rats when the implantation was performed at day 0, but allodynia was not reversed when the implantation was performed at day 12. NF-κB was activated in CCI rat DRG compared with naïve or sham animals (day 15), and dexamethasone implant inhibited p65/RelA translocation in CCI rats compared with control. This study demonstrated that the dexamethasone-loaded implant suppresses allodynia development and peripheral neuroinflammation. This device can reduce the potential side effects associated with oral anti-inflammatory drugs.
DOI: 10.6084/m9.figshare.11453151.v1
title: Delay of neuropathic pain sensitization after application of dexamethasone-loaded implant in sciatic nerve-injured rats

description: Neuroimmune interactions underlying the development of pain sensitization in models of neuropathic pain have been widely studied. In this study, we evaluated the development of allodynia and its reduction associated with peripheral antineuroinflammatory effects induced by a dexamethasone-loaded biodegradable implant. Chronic constriction injury (CCI) of the sciatic nerve was performed in Wistar rats. The electronic von Frey test was applied to assess mechanical allodynia. The dexamethasone-loaded implant was placed perineurally at the moment of CCI or 12 days after surgery. Dorsal root ganglia (DRG; L4-L5) were harvested and nuclear extracts were assayed by Western blot for detection of nuclear factor (NF)-κB p65/RelA translocation. Dexamethasone delivered from the implant delayed the development of allodynia for approximately three weeks in CCI rats when the implantation was performed at day 0, but allodynia was not reversed when the implantation was performed at day 12. NF-κB was activated in CCI rat DRG compared with naïve or sham animals (day 15), and dexamethasone implant inhibited p65/RelA translocation in CCI rats compared with control. This study demonstrated that the dexamethasone-loaded implant suppresses allodynia development and peripheral neuroinflammation. This device can reduce the potential side effects associated with oral anti-inflammatory drugs.
DOI: 10.6084/m9.figshare.11453145
title: Antimicrobial activity of actinomycetes and characterization of actinomycin-producing strain KRG-1 isolated from Karoo, South Africa

description: In the present study we reported the antimicrobial activity of actinomycetes isolated from aridic soil sample collected in Karoo, South Africa. Eighty-six actinomycete strains were isolated and purified, out of them thirty-four morphologically different strains were tested for antimicrobial activity. Among 35 isolates, 10 (28.57%) showed both antibacterial and antifungal activity. The ethyl acetate extract of strain KRG-1 showed the strongest antimicrobial activity and therefore was selected for further investigation. The almost complete nucleotide sequence of the 16S rRNA gene as well as distinctive matrix-assisted laser desorption/ionization-time-of-flight/mass spectrometry (MALDI-TOF/MS) profile of whole-cell proteins acquired for strain KRG-1 led to the identification of Streptomyces antibioticus KRG-1 (GenBank accession number: KX827270). The ethyl acetate extract of KRG-1 was fractionated by HPLC method against the most suppressed bacterium Staphylococcus aureus (Newman). LC//MS analysis led to the identification of the active peak that exhibited UV-VIS maxima at 442 nm and the ESI-HRMS spectrum showing the prominent ion clusters for [M-H2O+H]+ at m/z 635.3109 and for [M+Na]+ at m/z 1269.6148. This information could be assigned to chromopeptide lactone antibiotic - actinomycin. Our results suggest that unexplored soils could be an interesting source for exploring antibacterial secondary metabolites.