cometadata/datacite-titles-descriptions-related-identifiers huggingface dataset:
DOI: 10.6084/m9.figshare.20039004
title: Liquid crystalline systems containing Vitamin E TPGS for the controlled transdermal nicotine delivery

description: ABSTRACT Transdermal nicotine patches have been used in smoking cessation therapy, suggested for the treatment of skin disorders with eosinophilic infiltration and have been found to improve attention performance in patients with Alzheimer's disease and age-associated memory impairment. However, skin irritation with extended patch use is still a problem. The aim of this work was to develop a simple to prepare liquid crystalline system containing vitamin E TPGS that would be able to control nicotine delivery and reduce irritation and sensitization problems. The liquid crystalline phases were macroscopically characterized by visual analysis and examined microscopically under a polarized light microscope. Topical and transdermal delivery of nicotine were investigated in vitro using porcine ear skin mounted on a Franz diffusion cell. Nicotine skin permeation from the developed cubic phase followed zero-order kinetics (r = 0.993) and was significantly enhanced after 12 h when compared to the control formulation (nicotine solution) (p &lt; 0.05) (138.86 ± 20.44 and 64.91 ± 4.06 μg/cm2, respectively). Cubic phase was also able to target viable skin layers in comparison to control solution (8.18 ± 1.89 and 2.63 ± 2.51 μg/cm2, respectively). Further studies to evaluate skin sensitization and irritation are now necessary.
DOI: 10.6084/m9.figshare.20039006
title: Isolation and preliminary evaluation of Mulva Neglecta mucilage: a novel tablet binder

description: ABSTRACT The aim of this study was to evaluate binding potential of Mulva neglecta mucilage (MNM) with subsequent comparison to PVP K30. Eight batches of Diclofenac sodium tablets were prepared by wet granulation technique keeping different concentrations (4, 6, 8 & 10% w/w) of Mulva neglecta mucilage (extracted from leaves of Mulva neglecta) and PVP K30 as standard binder. The granules of formulated batches showed bulk density (g/mL) 0.49 ± 0.00 to 0.57 ± 0.00, tapped density (g/mL) 0.59 ± 0.01 to 0.70 ± 0.01, Carr's index 09.27 ± 0.95 to 19.65 ± 0.59, Hausner's ratio 1.12 ± 0.00 to 1.24 ± 0.01 and angle of repose 30.37 ± 2.90 °C to 36.86 ± 0.94 °C. Tablets were compressed to hardness 7.50 to 7.95 kg/cm2. The tablets showed 0.39 ± 0.02 to 0.39 ± 0.01% friability and 7:20 to 14:00 min disintegration time. Granules and post-compression evaluation revealed that parameters assessed were all found to be within the pharmacopoeial limits. The results (hardness, disintegration and dissolution) proved that Mulva neglecta mucilage has better binding capacity for preparation of uncoated tablet dosage form as compared to PVP K30. Among all the formulations, MN-1 to MN-4 showed slow release as compared to PV-1 to PV-4 and thereby Mulva neglecta mucilage exhibited satisfactory drug release phenomenon tablets of diclofenac sodium.
DOI: 10.6084/m9.figshare.20039006.v1
title: Isolation and preliminary evaluation of Mulva Neglecta mucilage: a novel tablet binder

description: ABSTRACT The aim of this study was to evaluate binding potential of Mulva neglecta mucilage (MNM) with subsequent comparison to PVP K30. Eight batches of Diclofenac sodium tablets were prepared by wet granulation technique keeping different concentrations (4, 6, 8 & 10% w/w) of Mulva neglecta mucilage (extracted from leaves of Mulva neglecta) and PVP K30 as standard binder. The granules of formulated batches showed bulk density (g/mL) 0.49 ± 0.00 to 0.57 ± 0.00, tapped density (g/mL) 0.59 ± 0.01 to 0.70 ± 0.01, Carr's index 09.27 ± 0.95 to 19.65 ± 0.59, Hausner's ratio 1.12 ± 0.00 to 1.24 ± 0.01 and angle of repose 30.37 ± 2.90 °C to 36.86 ± 0.94 °C. Tablets were compressed to hardness 7.50 to 7.95 kg/cm2. The tablets showed 0.39 ± 0.02 to 0.39 ± 0.01% friability and 7:20 to 14:00 min disintegration time. Granules and post-compression evaluation revealed that parameters assessed were all found to be within the pharmacopoeial limits. The results (hardness, disintegration and dissolution) proved that Mulva neglecta mucilage has better binding capacity for preparation of uncoated tablet dosage form as compared to PVP K30. Among all the formulations, MN-1 to MN-4 showed slow release as compared to PV-1 to PV-4 and thereby Mulva neglecta mucilage exhibited satisfactory drug release phenomenon tablets of diclofenac sodium.
DOI: 10.6084/m9.figshare.20039007
title: Development of nanotechnology-based drug delivery systems with olive vegetable oil for cutaneous application

description: ABSTRACT Liquid-Crystalline Systems represent active compounds delivery systems that may be able to overcome the physical barrier of the skin, especially represented by the stratum corneum. To obtain these systems, aqueous and oily components are used with surfactants. Of the different association structures in such systems, the liquid-crystalline offer numerous advantages to a topical product. This manuscript presents the development of liquid-crystalline systems consisting, in which the oil component is olive oil, its rheological characterizations, and the location of liquid crystals in its phase map. Cytotoxic effects were evaluated using J-774 mouse macrophages as the cellular model. A phase diagram to mix three components with different proportions was constructed. Two liquid crystalline areas were found with olive oil in different regions in the ternary diagram with two nonionic surfactants, called SLC1 (S1) and SLC2 (S2). These systems showed lamellar liquid crystals that remained stable during the entire analysis time. The systems were also characterized rheologically with pseudoplastic behavior without thixotropy. The texture and bioadhesion assays showed that formulations were similar statistically (p &lt; 0.05), indicating that the increased amount of water in S2 did not interfere with the bioadhesive properties of the systems. In vitro cytotoxic assays showed that formulations did not present cytotoxicity. Olive oil-based systems may be a promising platform for skin delivery of drugs.
DOI: 10.6084/m9.figshare.20039007.v1
title: Development of nanotechnology-based drug delivery systems with olive vegetable oil for cutaneous application

description: ABSTRACT Liquid-Crystalline Systems represent active compounds delivery systems that may be able to overcome the physical barrier of the skin, especially represented by the stratum corneum. To obtain these systems, aqueous and oily components are used with surfactants. Of the different association structures in such systems, the liquid-crystalline offer numerous advantages to a topical product. This manuscript presents the development of liquid-crystalline systems consisting, in which the oil component is olive oil, its rheological characterizations, and the location of liquid crystals in its phase map. Cytotoxic effects were evaluated using J-774 mouse macrophages as the cellular model. A phase diagram to mix three components with different proportions was constructed. Two liquid crystalline areas were found with olive oil in different regions in the ternary diagram with two nonionic surfactants, called SLC1 (S1) and SLC2 (S2). These systems showed lamellar liquid crystals that remained stable during the entire analysis time. The systems were also characterized rheologically with pseudoplastic behavior without thixotropy. The texture and bioadhesion assays showed that formulations were similar statistically (p &lt; 0.05), indicating that the increased amount of water in S2 did not interfere with the bioadhesive properties of the systems. In vitro cytotoxic assays showed that formulations did not present cytotoxicity. Olive oil-based systems may be a promising platform for skin delivery of drugs.
DOI: 10.6084/m9.figshare.20039009
title: Anti- Sporothrix spp. activity of medicinal plants

description: ABSTRACT Cases of sporotrichosis in humans and animals without satisfactory clinical response have increased, a warning sign of strains resistant to conventional antifungal agents. The urgent search for alternative therapies was an incentive for research on medicinal plants with anti-Sporothrix spp. properties. A bibliographic survey was performed based on scientific papers about in vitro and in vivo antifungal activity of essential oils and extracts of plants in differents solvents against the fungal of the Sporothrix schenckii complex. The study methodology consisted of a literature review in Google Scholar, Science Direct, Pubmed, Bireme and Springer link with papers from 1986 to 2015. We found 141 species of plants that were investigated, of which 100 species were concentrated in 39 botanical families that had confirmed anti-Sporothrix activity. Combretaceae, Asteraceae and Lamiaceae represented the botanical families with the greatest number of plants species with antifungal potential, using different methodologies. However, there are few studies with medicinal plants in experimental infection in animals that prove their activity in the treatment of sporotrichosis. It reinforces the need for further research related to standardization of in vitro methodologies and in vivo studies related to safety and to toxicity potential of these plants with anti-Sporothrix spp. activity.
DOI: 10.6084/m9.figshare.20039009.v1
title: Anti- Sporothrix spp. activity of medicinal plants

description: ABSTRACT Cases of sporotrichosis in humans and animals without satisfactory clinical response have increased, a warning sign of strains resistant to conventional antifungal agents. The urgent search for alternative therapies was an incentive for research on medicinal plants with anti-Sporothrix spp. properties. A bibliographic survey was performed based on scientific papers about in vitro and in vivo antifungal activity of essential oils and extracts of plants in differents solvents against the fungal of the Sporothrix schenckii complex. The study methodology consisted of a literature review in Google Scholar, Science Direct, Pubmed, Bireme and Springer link with papers from 1986 to 2015. We found 141 species of plants that were investigated, of which 100 species were concentrated in 39 botanical families that had confirmed anti-Sporothrix activity. Combretaceae, Asteraceae and Lamiaceae represented the botanical families with the greatest number of plants species with antifungal potential, using different methodologies. However, there are few studies with medicinal plants in experimental infection in animals that prove their activity in the treatment of sporotrichosis. It reinforces the need for further research related to standardization of in vitro methodologies and in vivo studies related to safety and to toxicity potential of these plants with anti-Sporothrix spp. activity.
DOI: 10.6084/m9.figshare.20039012
title: Influence of glucose and stirring in the fermentation process in order to produce anti- Candida metabolites produced by Streptomyces sp.

description: ABSTRACT This study evaluated the influence of glucose and stirring in the fermentation process in order to produce anti-Candida metabolites produced by Streptomyces sp. MPO4 isolated from Amazon soil. The anti-Candida metabolites production was registered after 24 h of fermentation in stirred ISP2 medium, having antifungal inhibition halos between 12.3 mm and 25.3 mm, yielding higher production of anti-Candida agents after 96 h. Stirring was a determining factor for the production of anti-Candida secondary metabolites, since the absence of glucose reflected in the late production of the antifungal starting from Streptomyces sp.
DOI: 10.6084/m9.figshare.20039012.v1
title: Influence of glucose and stirring in the fermentation process in order to produce anti- Candida metabolites produced by Streptomyces sp.

description: ABSTRACT This study evaluated the influence of glucose and stirring in the fermentation process in order to produce anti-Candida metabolites produced by Streptomyces sp. MPO4 isolated from Amazon soil. The anti-Candida metabolites production was registered after 24 h of fermentation in stirred ISP2 medium, having antifungal inhibition halos between 12.3 mm and 25.3 mm, yielding higher production of anti-Candida agents after 96 h. Stirring was a determining factor for the production of anti-Candida secondary metabolites, since the absence of glucose reflected in the late production of the antifungal starting from Streptomyces sp.
DOI: 10.6084/m9.figshare.20039013
title: Phenobarbital loaded microemulsion: development, kinetic release and quality control

description: ABSTRACT This study aimed to obtain and characterize a microemulsion (ME) containing phenobarbital (PB). The PB was incorporated in the proportion of 5% and 10% in a microemulsion system containing Labrasol(r), ethanol, isopropyl myristate and purified water. The physicochemical characterization was performed and the primary stability of the ME was evaluated. An analytical method was developed using spectrophotometry in UV = 242 nm. The kinetics of the in vitro release (Franz model) of the ME and the emulsion (EM) containing PB was evaluated. The incorporation of PB into ME at concentrations of 5 and 10% did not change pH and resistance to centrifugation. There was an increase in particle size, a decrease of conductivity and a change in the refractive index in relation to placebo ME. The ME remained stable in preliminary stability tests. The analytical method proved to be specific, linear, precise, accurate and robust. Regarding the kinetics of the in vitro release, ME obtained an in vitro release profile greater than the EM containing PB. Thus, the obtained ME has a potential for future transdermal application, being able to compose a drug delivery system for the treatment of epilepsy.
DOI: 10.6084/m9.figshare.20039013.v1
title: Phenobarbital loaded microemulsion: development, kinetic release and quality control

description: ABSTRACT This study aimed to obtain and characterize a microemulsion (ME) containing phenobarbital (PB). The PB was incorporated in the proportion of 5% and 10% in a microemulsion system containing Labrasol(r), ethanol, isopropyl myristate and purified water. The physicochemical characterization was performed and the primary stability of the ME was evaluated. An analytical method was developed using spectrophotometry in UV = 242 nm. The kinetics of the in vitro release (Franz model) of the ME and the emulsion (EM) containing PB was evaluated. The incorporation of PB into ME at concentrations of 5 and 10% did not change pH and resistance to centrifugation. There was an increase in particle size, a decrease of conductivity and a change in the refractive index in relation to placebo ME. The ME remained stable in preliminary stability tests. The analytical method proved to be specific, linear, precise, accurate and robust. Regarding the kinetics of the in vitro release, ME obtained an in vitro release profile greater than the EM containing PB. Thus, the obtained ME has a potential for future transdermal application, being able to compose a drug delivery system for the treatment of epilepsy.
DOI: 10.6084/m9.figshare.20039015.v1
title: Simultaneous determination of amoxicillin and clavulanic acid in pharmaceutical preparations by capillary zone electrophoresis

description: ABSTRACT Clavulanic acid enhances the antibacterial spectrum of amoxicillin by rendering most β-lactamase producing isolates susceptible to the drug. A fast, simple and efficient capillary electrophoresis method was developed for the simultaneous determination of amoxicillin and clavulanic acid from complex mixtures. Using a 25 mM sodium tetraborate as background electrolyte at a pH of 9.30, + 25 kV applied voltage, 25 °C system temperature, UV determination at 230 nm; we succeeded in simultaneous separation of amoxicillin and clavulanic acid in approximately 2 minutes. The analytical performance of the method was evaluated in terms of reproducibility, precision, accuracy, and linearity. The optimized analytical method was applied for the determination of the two analytes from combined commercial pharmaceutical preparations. This CE method is fast, inexpensive, efficient, and environmentally friendly when compared with the more frequently used high performance liquid chromatography methods described in the literature.
DOI: 10.6084/m9.figshare.20039015
title: Simultaneous determination of amoxicillin and clavulanic acid in pharmaceutical preparations by capillary zone electrophoresis

description: ABSTRACT Clavulanic acid enhances the antibacterial spectrum of amoxicillin by rendering most β-lactamase producing isolates susceptible to the drug. A fast, simple and efficient capillary electrophoresis method was developed for the simultaneous determination of amoxicillin and clavulanic acid from complex mixtures. Using a 25 mM sodium tetraborate as background electrolyte at a pH of 9.30, + 25 kV applied voltage, 25 °C system temperature, UV determination at 230 nm; we succeeded in simultaneous separation of amoxicillin and clavulanic acid in approximately 2 minutes. The analytical performance of the method was evaluated in terms of reproducibility, precision, accuracy, and linearity. The optimized analytical method was applied for the determination of the two analytes from combined commercial pharmaceutical preparations. This CE method is fast, inexpensive, efficient, and environmentally friendly when compared with the more frequently used high performance liquid chromatography methods described in the literature.
DOI: 10.5281/zenodo.6628490
title: T1D in vitro (conditionner) datatests

description: in vitro T1D data tests on conditionner at 9.4T
DOI: 10.5281/zenodo.6628489
title: T1D in vitro (conditionner) datatests

description: in vitro T1D data tests on conditionner at 9.4T
DOI: 10.6084/m9.figshare.20039016
title: Synthesis and cytotoxicity evaluation of thiosemicarbazones and their thiazole derivatives

description: ABSTRACT The aims of this study were to synthesize a series of thiosemicarbazones and their thiazole derivatives, to investigate their cytotoxic activity against three human cancers and normal (Vero cells) cell lines, and to evaluate the pro-apoptotic potential of the most active compounds. Materials and Methods: The thiosemicarbazones were obtained by reacting an aromatic aldehyde with thiosemicarbazide (yield 71-96%), which were subjected to a cyclization with α-bromoacetophenone to yield the required thiazole heterocycles (yield 63-100%). All the synthesized compounds were screened at 50 µM concentration against three cell lines representing HL60 (promyelocytic leukemia), Jurkat (acute lymphoblastic leukemia), and MCF-7 (breast cancer). The pro-apoptotic effect was measured by flow cytometry as the percentage of cells with hypodiploid DNA. Results: Three thiazole compounds showed activity against at least one tumor cell line (IC50 = 43-76 µM) and low cytotoxicity against Vero cells (IC50 &gt; 100 M). The most active compound of this series induced 91% and 51% DNA fragmentation in HL60 and MCF-7 cell lines, respectively, suggesting that this compound triggered apoptosis in these cells. Conclusion: Among the synthesized compounds, one in particular was found to exert antiproliferative and pro-apoptotic activity on tumor cells and can be considered promising as a lead molecule for the design of new analogues with improved activity.
DOI: 10.6084/m9.figshare.20039016.v1
title: Synthesis and cytotoxicity evaluation of thiosemicarbazones and their thiazole derivatives

description: ABSTRACT The aims of this study were to synthesize a series of thiosemicarbazones and their thiazole derivatives, to investigate their cytotoxic activity against three human cancers and normal (Vero cells) cell lines, and to evaluate the pro-apoptotic potential of the most active compounds. Materials and Methods: The thiosemicarbazones were obtained by reacting an aromatic aldehyde with thiosemicarbazide (yield 71-96%), which were subjected to a cyclization with α-bromoacetophenone to yield the required thiazole heterocycles (yield 63-100%). All the synthesized compounds were screened at 50 µM concentration against three cell lines representing HL60 (promyelocytic leukemia), Jurkat (acute lymphoblastic leukemia), and MCF-7 (breast cancer). The pro-apoptotic effect was measured by flow cytometry as the percentage of cells with hypodiploid DNA. Results: Three thiazole compounds showed activity against at least one tumor cell line (IC50 = 43-76 µM) and low cytotoxicity against Vero cells (IC50 &gt; 100 M). The most active compound of this series induced 91% and 51% DNA fragmentation in HL60 and MCF-7 cell lines, respectively, suggesting that this compound triggered apoptosis in these cells. Conclusion: Among the synthesized compounds, one in particular was found to exert antiproliferative and pro-apoptotic activity on tumor cells and can be considered promising as a lead molecule for the design of new analogues with improved activity.
DOI: 10.6084/m9.figshare.20039019
title: Evaluation of the Brazilian Cosmetic Legislation and its impact on the industries during the 20th century

description: ABSTRACT Cosmetics have been used since the very first days of human life. This early and continuing consumption has resulted in the growth of the Cosmetic Industry (C.I.). The C.I. must continue to invest in the development of innovative products which are safe for the consumers. On the other hand, the Health Agency should issue laws regulating the development of products. Thus, the aim of this study was to evaluate the Brazilian Cosmetic Legislation before ANVISA and the challenges for the C.I. during the 20th century regarding the development of safe and effective cosmetics, and to show the importance of this legislation in the R&D. A Bibliographic and Documentary Exploratory Research was conducted based on safety and efficacy data contained in scientific studies and legal documents. The study showed that the creation of ANVISA was necessary because no resolution had been published about the safety and efficacy of cosmetics for the C.I. before ANVISA. However, the challenges faced by the C.I. may have had a negative impact on the health of consumers. Finally, it was concluded that the actions before ANVISA were insufficient to the C.I.. Thus, the creation of ANVISA was essential to have a regulatory basis fot the C.I.
DOI: 10.6084/m9.figshare.20039019.v1
title: Evaluation of the Brazilian Cosmetic Legislation and its impact on the industries during the 20th century

description: ABSTRACT Cosmetics have been used since the very first days of human life. This early and continuing consumption has resulted in the growth of the Cosmetic Industry (C.I.). The C.I. must continue to invest in the development of innovative products which are safe for the consumers. On the other hand, the Health Agency should issue laws regulating the development of products. Thus, the aim of this study was to evaluate the Brazilian Cosmetic Legislation before ANVISA and the challenges for the C.I. during the 20th century regarding the development of safe and effective cosmetics, and to show the importance of this legislation in the R&D. A Bibliographic and Documentary Exploratory Research was conducted based on safety and efficacy data contained in scientific studies and legal documents. The study showed that the creation of ANVISA was necessary because no resolution had been published about the safety and efficacy of cosmetics for the C.I. before ANVISA. However, the challenges faced by the C.I. may have had a negative impact on the health of consumers. Finally, it was concluded that the actions before ANVISA were insufficient to the C.I.. Thus, the creation of ANVISA was essential to have a regulatory basis fot the C.I.