cometadata/datacite-titles-descriptions-related-identifiers huggingface dataset:
DOI: 10.6084/m9.figshare.7974989
title: Development and evaluation of multiparticulate biphasic system for the treatment of circadian diseases

description: Multiparticulate systems have biopharmaceutical advantages when compared to the monolithic systems, once they allow different patterns of drug release and can be used in different treatments. The aim of the present work was to develop a biphasic controlled release delivery system, using propranolol hydrochloride (PROP) that can be used for the treatment of circadian diseases. This system was obtained by the combination of cellulosic polymers hydroxypropyl methylcellulose (HPMC) and ethylcellulose (EC) in a 2² factorial experimental design, which allowed the optimization of the development stage. The pellets produced and used in biphasic formulations were evaluated for physical and chemical characteristics and presented acceptable results. The immediate fraction obtained showed the complete release in 30 min while the others kept the release of the drug for 24 h. This study showed that the combination of beads with different releasing characteristics allowed to obtain different release profiles, which can be modulated according to the pathological needs, especially with regard to circadian diseases that suffer alterations throughout the day.
DOI: 10.6084/m9.figshare.7974989.v1
title: Development and evaluation of multiparticulate biphasic system for the treatment of circadian diseases

description: Multiparticulate systems have biopharmaceutical advantages when compared to the monolithic systems, once they allow different patterns of drug release and can be used in different treatments. The aim of the present work was to develop a biphasic controlled release delivery system, using propranolol hydrochloride (PROP) that can be used for the treatment of circadian diseases. This system was obtained by the combination of cellulosic polymers hydroxypropyl methylcellulose (HPMC) and ethylcellulose (EC) in a 2² factorial experimental design, which allowed the optimization of the development stage. The pellets produced and used in biphasic formulations were evaluated for physical and chemical characteristics and presented acceptable results. The immediate fraction obtained showed the complete release in 30 min while the others kept the release of the drug for 24 h. This study showed that the combination of beads with different releasing characteristics allowed to obtain different release profiles, which can be modulated according to the pathological needs, especially with regard to circadian diseases that suffer alterations throughout the day.
DOI: 10.6084/m9.figshare.20039328.v1
title: Formulation development and evaluation of colon targeted delayed release methotrexate pellets for the treatment of colonic carcinoma

description: Colonic carcinoma is one of the most common internal malignancies and is the second leading cause of deaths in United States. Methotrexate (MTX) is a drug of choice in the treatment of colon cancer. The aim of the present research work was to develop and characterize colon targeted pellets of MTX for treatment of colonic carcinoma. The product and process parameters were optimized by screening methods. Pellets were prepared by extrusion spheronization using microcrystalline cellulose (MCC) as spheronizing aid and ethyl cellulose (EC) as release retardant in different ratio. Based on the physical appearance, sphericity and % in vitro drug release, batch P17 containing EC: MCC (3:7) was optimized for core pellets. The site specificity was obtained by screening the coating polymers and by coating the core pellets with EudragitS100. The 32 full factorial design was applied in which airflow rate (X1) and coating time (X2) were the independent parameters and physical appearance (Y1) and time taken for 100% drug release (Y2) were selected as the dependent variables. From the results obtained, 6min of coating time and 60cm3/min airflow rate was optimized. The batch B5 showed appropriate physical appearance and % in vitro drug release upto 17hr indicating sustained release property. The ex-vivo studies performed on rat colon indicated a significant relation with the in vitro drug release. The drug release followed Higuchi’s model indicating the diffusion pattern of drug release from the matrix of pellets. Thus, the coated pellets can be a good candidate for site specific delivery of MTX to colon by decreasing the gastric irritation and thus to improve bioavailability.
DOI: 10.6084/m9.figshare.20039328
title: Formulation development and evaluation of colon targeted delayed release methotrexate pellets for the treatment of colonic carcinoma

description: Colonic carcinoma is one of the most common internal malignancies and is the second leading cause of deaths in United States. Methotrexate (MTX) is a drug of choice in the treatment of colon cancer. The aim of the present research work was to develop and characterize colon targeted pellets of MTX for treatment of colonic carcinoma. The product and process parameters were optimized by screening methods. Pellets were prepared by extrusion spheronization using microcrystalline cellulose (MCC) as spheronizing aid and ethyl cellulose (EC) as release retardant in different ratio. Based on the physical appearance, sphericity and % in vitro drug release, batch P17 containing EC: MCC (3:7) was optimized for core pellets. The site specificity was obtained by screening the coating polymers and by coating the core pellets with EudragitS100. The 32 full factorial design was applied in which airflow rate (X1) and coating time (X2) were the independent parameters and physical appearance (Y1) and time taken for 100% drug release (Y2) were selected as the dependent variables. From the results obtained, 6min of coating time and 60cm3/min airflow rate was optimized. The batch B5 showed appropriate physical appearance and % in vitro drug release upto 17hr indicating sustained release property. The ex-vivo studies performed on rat colon indicated a significant relation with the in vitro drug release. The drug release followed Higuchi’s model indicating the diffusion pattern of drug release from the matrix of pellets. Thus, the coated pellets can be a good candidate for site specific delivery of MTX to colon by decreasing the gastric irritation and thus to improve bioavailability.
DOI: 10.6084/m9.figshare.20039332
title: Preparation and physicochemical characterization of prazosin conjugated PLGA nanoparticles for drug delivery of flutamide

description: In the current work, a sustained drug delivery system of flutamide (FLT) was developed using Poly(D,L-lactide-co-glycolide) (PLGA) decorated bypoly(ethylene glycol) (PEG) grafted prazosin (PLGA-PEG-Praz) as a targeting moiety. In a multi-step reaction, PLGA was linked to PEG and prazosin. The structure of the synthesized polymers was confirmed by FTIR and 1H-NMR. Flutamide-loaded nanoparticles were prepared by quasi-emulsion solvent diffusion technique. The nanoparticles were evaluated for size, zeta potential, polydispersity index, drug crystallinity, loading efficiency, and release properties. Also, the physicochemical properties of the nanoparticles were analyzed using Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry, and Powder X-Ray Diffractometry (XRD). The particle size of nanoparticles was ranged between 191 and 249 nm. Loading efficiency of nanoparticles was about 43%-69%. Results showed a steady release rate for nanoparticles compared to that of a pure drug powder. SEM characterization confirmed that particles were in nanosize range. DSC and XRPD results verified a decrease in drug crystallinity in the prepared formulations. In conclusion, the results of this study showed that PLGA-PEG-Praz nanoparticles could be a good choice to improve the physicochemical properties of the drug and these formulations can increase Flutamide efficacy.
DOI: 10.6084/m9.figshare.20039332.v1
title: Preparation and physicochemical characterization of prazosin conjugated PLGA nanoparticles for drug delivery of flutamide

description: In the current work, a sustained drug delivery system of flutamide (FLT) was developed using Poly(D,L-lactide-co-glycolide) (PLGA) decorated bypoly(ethylene glycol) (PEG) grafted prazosin (PLGA-PEG-Praz) as a targeting moiety. In a multi-step reaction, PLGA was linked to PEG and prazosin. The structure of the synthesized polymers was confirmed by FTIR and 1H-NMR. Flutamide-loaded nanoparticles were prepared by quasi-emulsion solvent diffusion technique. The nanoparticles were evaluated for size, zeta potential, polydispersity index, drug crystallinity, loading efficiency, and release properties. Also, the physicochemical properties of the nanoparticles were analyzed using Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry, and Powder X-Ray Diffractometry (XRD). The particle size of nanoparticles was ranged between 191 and 249 nm. Loading efficiency of nanoparticles was about 43%-69%. Results showed a steady release rate for nanoparticles compared to that of a pure drug powder. SEM characterization confirmed that particles were in nanosize range. DSC and XRPD results verified a decrease in drug crystallinity in the prepared formulations. In conclusion, the results of this study showed that PLGA-PEG-Praz nanoparticles could be a good choice to improve the physicochemical properties of the drug and these formulations can increase Flutamide efficacy.
DOI: 10.6084/m9.figshare.7974098
title: Determination of Gemifloxacin in human plasma by high performance liquid chromatography using Ultra Violet detector and its application to a bioequivalence study

description: A liquid chromatography method was developed and validated for the determination of gemifloxacin in human plasma using chloramphenicol as internal standard to achieve lower quantification limit. Acetonitrile was used to precipitated and extracted analyte and internal standard from plasma by Protein Precipitation. Analysis was performed isocratically on C18 column using 25% acetonitrile and 75% 0.02 M phosphate buffer as mobile phase. The method was demonstrated to be linear from 0.003 µg/mL to 5 µg/mL with the lower limit of quantitation of 0.003 µg/mL. The method was successfully applied for the bioequivalence study of gemifloxacin after a single oral administration of 320 mg gemifloxacin mesylate tablets to 12 healthy volunteers.
DOI: 10.6084/m9.figshare.7974098.v1
title: Determination of Gemifloxacin in human plasma by high performance liquid chromatography using Ultra Violet detector and its application to a bioequivalence study

description: A liquid chromatography method was developed and validated for the determination of gemifloxacin in human plasma using chloramphenicol as internal standard to achieve lower quantification limit. Acetonitrile was used to precipitated and extracted analyte and internal standard from plasma by Protein Precipitation. Analysis was performed isocratically on C18 column using 25% acetonitrile and 75% 0.02 M phosphate buffer as mobile phase. The method was demonstrated to be linear from 0.003 µg/mL to 5 µg/mL with the lower limit of quantitation of 0.003 µg/mL. The method was successfully applied for the bioequivalence study of gemifloxacin after a single oral administration of 320 mg gemifloxacin mesylate tablets to 12 healthy volunteers.
DOI: 10.6084/m9.figshare.20039334
title: Design, synthesis, biological evaluation, and nitric-oxide release studies of a novel series of celecoxib prodrugs possessing a nitric-oxide donor moiety

description: A new group of hybrid nitric oxide-releasing anti-inflammatory drugs (NONO-coxibs), in which an O 2-acetoxymethyl-1-(N-ethyl-N-methylamino)diazen-1-ium-1,2-diolate NO-donor moiety is attached directly to the carboxylic acid group of 1-(4-aminosulfonylphenyl)-5-aryl-1H-pyrazol-3-carboxylic acids (6a-c), were synthesized. A low amount of NO was released from the diazen-1-ium-1,2-diolate compounds 6a-c upon incubation with phosphate buffer saline (PBS) at pH 7.4 (range: pH 7.97-8.51), whereas, the percentage of NO released was significantly higher (84.5%-85.05% of the theoretical maximal release of two molecules of NO/molecule of the parent hybrid ester prodrug) when the diazen-1-ium-1,2-diolate ester prodrugs were incubated in the presence of rat serum. These incubation studies demonstrated that both NO and the anti-inflammatory 1-(4-aminosulfonylphenyl)-5-(4-H, 4-F or 4-Me-phenyl)-1H-pyrazol-3-carboxylic acid (4a-c) would be released from the parent NONO-coxib upon in vivo cleavage by non-specific serum esterases. The parent compounds 4a-c displayed good anti-inflammatory effects (ID50=81.4-112.4 mg/kg p.o.) between those exhibited by the reference drugs, aspirin (ID50=114.3 mg/kg p.o.) and celecoxib (ID50=12.6 mg/kg p.o.). Hybrid ester anti-inflammatory/NO-donor prodrugs (NONO-coxibs) offer a potential drug-design concept directed toward the development of anti-inflammatory drugs that are lacking adverse ulcerogenic and/or cardiovascular effects.
DOI: 10.6084/m9.figshare.7974119
title: Multifunctional photoprotection: corrective makeup for cutaneous dyschromias

description: The aim of this study was to develop and evaluate a corrective and photoprotective makeup for patients with dyschromias. An emulsion was prepared and pigment mixtures were incorporated in the formulation, producing five shades of corrective makeup: BEIGE (I, II, III), BRONZE and TAN. The sun protection factor (SPF) and UVA/UVB ratio of the corrective makeup were determined using spectrophotometry with a Labsphere® analyser. The spreadability, occlusivity, stability, and photostability of the photoprotective formulations were also evaluated. For all formulations there was no statistical difference among them (p &gt; 0.05) in terms of spreadability, occlusivity and SPF. They were considered to be photostable under solar radiation, with variations in SPF value and UVA/UVB ratio lower than 20%. The corrective makeup presented average-to-high UVB photoprotection and broad spectrum photoprotection. After 90 days, pH, density and SPF values showed no significant differences among formulations (p&gt;0.05). All corrective makeup presented separation of the pigments, however, they returned to a homogeneous aspect and to the original color shade after shaking. The corrective makeup presented a fine texture, little brightness, and a homogeneous, dry-to-the-touch aspect. This work may benefit patients with dyschromias, improving their quality of life, besides promoting photoprotection and covering the skin blemishes.
DOI: 10.6084/m9.figshare.7974119.v1
title: Multifunctional photoprotection: corrective makeup for cutaneous dyschromias

description: The aim of this study was to develop and evaluate a corrective and photoprotective makeup for patients with dyschromias. An emulsion was prepared and pigment mixtures were incorporated in the formulation, producing five shades of corrective makeup: BEIGE (I, II, III), BRONZE and TAN. The sun protection factor (SPF) and UVA/UVB ratio of the corrective makeup were determined using spectrophotometry with a Labsphere® analyser. The spreadability, occlusivity, stability, and photostability of the photoprotective formulations were also evaluated. For all formulations there was no statistical difference among them (p &gt; 0.05) in terms of spreadability, occlusivity and SPF. They were considered to be photostable under solar radiation, with variations in SPF value and UVA/UVB ratio lower than 20%. The corrective makeup presented average-to-high UVB photoprotection and broad spectrum photoprotection. After 90 days, pH, density and SPF values showed no significant differences among formulations (p&gt;0.05). All corrective makeup presented separation of the pigments, however, they returned to a homogeneous aspect and to the original color shade after shaking. The corrective makeup presented a fine texture, little brightness, and a homogeneous, dry-to-the-touch aspect. This work may benefit patients with dyschromias, improving their quality of life, besides promoting photoprotection and covering the skin blemishes.
DOI: 10.6084/m9.figshare.20039334.v1
title: Design, synthesis, biological evaluation, and nitric-oxide release studies of a novel series of celecoxib prodrugs possessing a nitric-oxide donor moiety

description: A new group of hybrid nitric oxide-releasing anti-inflammatory drugs (NONO-coxibs), in which an O 2-acetoxymethyl-1-(N-ethyl-N-methylamino)diazen-1-ium-1,2-diolate NO-donor moiety is attached directly to the carboxylic acid group of 1-(4-aminosulfonylphenyl)-5-aryl-1H-pyrazol-3-carboxylic acids (6a-c), were synthesized. A low amount of NO was released from the diazen-1-ium-1,2-diolate compounds 6a-c upon incubation with phosphate buffer saline (PBS) at pH 7.4 (range: pH 7.97-8.51), whereas, the percentage of NO released was significantly higher (84.5%-85.05% of the theoretical maximal release of two molecules of NO/molecule of the parent hybrid ester prodrug) when the diazen-1-ium-1,2-diolate ester prodrugs were incubated in the presence of rat serum. These incubation studies demonstrated that both NO and the anti-inflammatory 1-(4-aminosulfonylphenyl)-5-(4-H, 4-F or 4-Me-phenyl)-1H-pyrazol-3-carboxylic acid (4a-c) would be released from the parent NONO-coxib upon in vivo cleavage by non-specific serum esterases. The parent compounds 4a-c displayed good anti-inflammatory effects (ID50=81.4-112.4 mg/kg p.o.) between those exhibited by the reference drugs, aspirin (ID50=114.3 mg/kg p.o.) and celecoxib (ID50=12.6 mg/kg p.o.). Hybrid ester anti-inflammatory/NO-donor prodrugs (NONO-coxibs) offer a potential drug-design concept directed toward the development of anti-inflammatory drugs that are lacking adverse ulcerogenic and/or cardiovascular effects.
DOI: 10.6084/m9.figshare.7974272.v1
title: Barriers to the provision of asthma services and perceived practice towards asthma management among urban community pharmacists in Selangor, Malaysia

description: This study aims to assess the perceived practice and barriers towards the provision of asthma management services among urban community pharmacists in Selangor, Malaysia. The study also highlights both pharmacist and patient-related barriers in asthma counseling. One hundred fifty urban community pharmacists in Selangor, Malaysia, were randomly selected and recruited for the present cross sectional baseline study. Previous studies have explored pharmacists’ perception on their roles in asthma management in different parts of the world. The data was collected through self-explanatory questionnaires (containing 47 items). The extracted data from the completed questionnaires were analyzed descriptively and inferentially using Statistical Package for Social Science (SPSS) version 19. Results showed that pharmacists perceived their roles in asthma management along three major dimensions: ‘patient self-management’, ‘medication use’ and ‘asthma control’, mean (±SD) score of the perception towards asthma management was 99.29 ± 4.58 over a maximum possible score of 110 with 90.26%. There were significant differences between the pharmacy education level and perceived practice of asthma management while there were insignificant differences between age, gender, ethnicity, number of practicing year and perceived practice of asthma management among respondents. Most common barriers towards asthma counselling including lack of time, lack of asthma knowledge, lack of counselling space and cost of asthma drugs. Conclusively, urban community pharmacists in Selangor, Malaysia, demonstrate good perceived practice of better management of asthma with multidimensional dimensional role against in disease care.
DOI: 10.6084/m9.figshare.7974272
title: Barriers to the provision of asthma services and perceived practice towards asthma management among urban community pharmacists in Selangor, Malaysia

description: This study aims to assess the perceived practice and barriers towards the provision of asthma management services among urban community pharmacists in Selangor, Malaysia. The study also highlights both pharmacist and patient-related barriers in asthma counseling. One hundred fifty urban community pharmacists in Selangor, Malaysia, were randomly selected and recruited for the present cross sectional baseline study. Previous studies have explored pharmacists’ perception on their roles in asthma management in different parts of the world. The data was collected through self-explanatory questionnaires (containing 47 items). The extracted data from the completed questionnaires were analyzed descriptively and inferentially using Statistical Package for Social Science (SPSS) version 19. Results showed that pharmacists perceived their roles in asthma management along three major dimensions: ‘patient self-management’, ‘medication use’ and ‘asthma control’, mean (±SD) score of the perception towards asthma management was 99.29 ± 4.58 over a maximum possible score of 110 with 90.26%. There were significant differences between the pharmacy education level and perceived practice of asthma management while there were insignificant differences between age, gender, ethnicity, number of practicing year and perceived practice of asthma management among respondents. Most common barriers towards asthma counselling including lack of time, lack of asthma knowledge, lack of counselling space and cost of asthma drugs. Conclusively, urban community pharmacists in Selangor, Malaysia, demonstrate good perceived practice of better management of asthma with multidimensional dimensional role against in disease care.
DOI: 10.6084/m9.figshare.7974173
title: Treatment interruption of biological drugs and tofacitinib in rheumatoid arthritis: A systematic review of case reports

description: The aim of this study was to evaluate interruption of treatment with biological drugs and tofacitinib due to adverse events in patients with rheumatoid arthritis. A systematic review was performed in the electronic databases MEDLINE, Cochrane, Scopus, CRD, IPA, Lilacs and Scielo. Case reports addressing interruption of treatment due to any adverse event related to abatacept (ABA), adalimumab (ADA), anakinra (ANA), certolizumab pegol (CER), etanercept (ETA), golimumab (GOL), infliximab (IFX), rituximab (RTX), secukinumab (SEC), tocilizumab (TCZ), tofacitinib (TOF) or ustekinumab (UST) in rheumatoid arthritis patients were evaluated. Baseline data, patient profile, previous and current treatments, cause of discontinuation and information on reintroduction of treatment were extracted from the case reports. One hundred and fifty-four studies (154 patients) reported 162 discontinuations of rheumatoid arthritis treatment due to adverse events (ETA = 57; IFX = 46; ADA = 32; TCZ = 13; RTX = 5; ANA = 3; GOL = 2; ABA = 2; TOF = 1; CER = 1; SEC = 0 and UST = 0). The mean age of patients was 56 (± 12.1) years and 82% were female. Seventy-four adverse events were confirmed (related to used drug), and 138 were observed in patients using anti-TNF. The most common adverse events were infections (21%), skin disease (15%), autoimmune disease (13%) and hematological disorders (9%). Case reports are important in the detection of rare adverse events and should be considered in the choice of appropriate therapy for patients.