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1.
Molecules ; 28(14)2023 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-37513261

RESUMO

The development of novel scaffolds that can increase the effectiveness, safety, and convenience of medication therapy using drug conjugates is a promising strategy. As a result, drug conjugates are an active area of research and development in medicinal chemistry. This research demonstrates acetamide-sulfonamide scaffold preparation after conjugation of ibuprofen and flurbiprofen with sulfa drugs, and these scaffolds were then screened for urease inhibition. The newly designed conjugates were confirmed by spectroscopic techniques such as IR, 1HNMR, 13CNMR, and elemental analysis. Ibuprofen conjugated with sulfathiazole, flurbiprofen conjugated with sulfadiazine, and sulfamethoxazole were found to be potent and demonstrated a competitive mode of urease inhibition, with IC50 (µM) values of 9.95 ± 0.14, 16.74 ± 0.23, and 13.39 ± 0.11, respectively, and urease inhibition of 90.6, 84.1, and 86.1% respectively. Ibuprofen conjugated with sulfanilamide, sulfamerazine, and sulfacetamide, whereas flurbiprofen conjugated with sulfamerazine, and sulfacetamide exhibited a mixed mode of urease inhibition. Moreover, through molecular docking experiments, the urease receptor-binding mechanisms of competitive inhibitors were anticipated, and stability analysis through MD simulations showed that these compounds made stable complexes with the respective targets and that no conformational changes occurred during the simulation. The findings demonstrate that conjugates of approved therapeutic molecules may result in the development of novel classes of pharmacological agents for the treatment of various pathological conditions involving the urease enzyme.


Assuntos
Flurbiprofeno , Simulação de Acoplamento Molecular , Flurbiprofeno/farmacologia , Ibuprofeno/farmacologia , Inibidores Enzimáticos/farmacologia , Sulfacetamida , Cinética , Urease , Sulfamerazina , Canavalia , Relação Estrutura-Atividade , Sulfanilamida , Sulfonamidas/farmacologia , Estrutura Molecular
2.
Environ Res ; 215(Pt 2): 114314, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36116497

RESUMO

Nanoparticles are inevitable byproducts of modern industry. However, the environmental impacts arising from industrial applications of nanoparticles are largely under-reported. This study evaluated the ecotoxicological effects of aluminum oxide nanoparticles (Al2O3NP) and its influence on sulfacetamide (SA) biodegradation by a freshwater microalga, Scenedesmus obliquus. Although Al2O3NP showed limited toxicity effect on S. obliquus, we observed the toxicity attenuation aspect of Al2O3NP in a mixture of sulfacetamide on microalgae. The addition of 100 mg L-1 of Al2O3NP and 1 mg L-1 of SA reduced total chlorophyll by 23.3% and carotenoids by 21.6% in microalgal compared to control. The gene expression study demonstrated that ATPF0C, Lhcb1, HydA, and psbA genes responsible for ATP synthesis and the photosynthetic system were significantly downregulated, while the Tas gene, which plays a major role in biodegradation of organic xenobiotic chemicals, was significantly upregulated at 1 and 100 mg L-1 of Al2O3NP. The S. obliquus removed 16.8% of SA at 15 mg L-1 in 14 days. However, the removal was slightly enhanced (18.8%) at same concentration of SA in the presence of 50 mg L-1 Al2O3NP. This result proves the stability of sulfacetamide biodegradation capacity of S. obliquus in the presence of Al2O3NP co-contamination. The metabolic analysis showed that SA was degraded into simpler byproducts such as sulfacarbamide, sulfaguanidine, sulfanilamide, 4-(methyl sulfonyl)aniline, and N-hydroxy-benzenamine which have lower ecotoxicity than SA, demonstrating that the ecotoxicity of sulfacetamide has significantly decreased after the microalgal degradation, suggesting the environmental feasibility of microalgae-mediated wastewater technology. This study provides a deeper understanding of the impact of nanoparticles such as Al2O3NP on aquatic ecosystems.


Assuntos
Microalgas , Nanopartículas , Scenedesmus , Trifosfato de Adenosina/metabolismo , Trifosfato de Adenosina/farmacologia , Óxido de Alumínio/toxicidade , Carotenoides/metabolismo , Carotenoides/farmacologia , Clorofila/metabolismo , Clorofila/farmacologia , Ecossistema , Água Doce , Nanopartículas/toxicidade , Scenedesmus/metabolismo , Sulfacetamida/metabolismo , Sulfacetamida/farmacologia , Sulfaguanidina/metabolismo , Sulfaguanidina/farmacologia , Águas Residuárias , Xenobióticos/metabolismo
3.
Drug Dev Ind Pharm ; 45(7): 1120-1129, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30883240

RESUMO

Objective: The aim of this study was to explore the possibility of using natural deep eutectic solvents (NADES) as solvation media for enhancement of solubility of sulfonamides, as well as gaining some thermodynamic characteristics of the analyzed systems. Significance: Low solubility of many active pharmaceutical ingredients is a well-recognized difficulty in pharmaceutical industry, hence the need for different strategies addressing this problem. Among such strategies, those that are environmentally and economically beneficial are of particular interest. Methods: The solubility of sulfanilamide and sulfacetamide in 21 different NADES compositions comprising choline chloride with sugars or sugar alcohols was measured spectrophotometrically. Thermodynamic parameters describing the studied systems were determined using the COSMO-RS computational protocol. Results: All of the considered NADES compositions gave an increase in solubility of the studied sulfonamides, with the highest solubilities obtained for the system comprising choline chloride and glycerol in unimolar proportions, which gave a solubility advantage of 83.7 and 73.8 for sulfanilamide and sulfacetamide, respectively. Theoretical studies indicated that the dissolution of both considered sulfonamides has a low endothermic character, with the lowest enthalpy values obtained for the most optimal, i.e. unimolar, proportions. The non-monotonous trend of enthalpy of dissolution was also discussed in terms of intermolecular interactions. Conclusions: The obtained results show the feasibility of using NADES as solubility enhancers for sulfonamides and encourage for further exploration in this field.


Assuntos
Sulfacetamida/química , Sulfanilamida/química , Colina/química , Glicerol/química , Solubilidade , Solventes/química
4.
Rheumatol Int ; 37(12): 1949-1956, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28822009

RESUMO

Ankylosing spondylitis (AS) affects sacroiliac and axial joints as well as extraarticular organs, such as the eye, lung, bowel, and heart. Although examples of renal involvement in AS, such as IgA nephropathy, amyloidosis, and glomerulonephritis, have been reported, it has not been emphasized that urolithiasis is frequently formed in the clinical course of AS. Growing evidence indicates that urolithiasis may be observed in AS patients and is more frequent than other extraarticular features. In this review, we will discuss frequency and predictors of AS-related urolithiasis and summarize the possible underlying genetic and biochemical mechanisms. We believe an increased awareness of urolithiasis as a complication of AS will encourage future studies that will shed light on disease mechanisms and preventative therapies.


Assuntos
Espondilite Anquilosante/etiologia , Urolitíase/complicações , Anti-Infecciosos Urinários/efeitos adversos , Feminino , Humanos , Masculino , Fatores de Risco , Espondilite Anquilosante/genética , Espondilite Anquilosante/fisiopatologia , Sulfacetamida/efeitos adversos , Urolitíase/induzido quimicamente , Urolitíase/epidemiologia , Urolitíase/fisiopatologia
5.
Bioorg Med Chem Lett ; 26(12): 2870-2873, 2016 06 15.
Artigo em Inglês | MEDLINE | ID: mdl-27136718

RESUMO

Six new N [(4-aminophenyl)sulfonyl]acetamide based hydroxytriazenes have been synthesized and characterized using elemental analysis, IR, 1H NMR, 13C NMR and MASS spectral analysis. Further, their theoretical predictions for probable activities have been taken using PASS (Prediction of Activity Spectra for Substance). Although a number of activities have been predicted but specifically anti-inflammatory, antiradical, anti-diabetic activities have been experimentally validated which proves that theoretical predictions agree with the experimental results. The object of the Letter is to establish Computer Aided Drug Design (CADD) using our compounds.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Diabetes Mellitus Tipo 2/tratamento farmacológico , Edema/tratamento farmacológico , Hipoglicemiantes/farmacologia , Sulfacetamida/farmacologia , Triazenos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/química , Diabetes Mellitus Tipo 2/metabolismo , Relação Dose-Resposta a Droga , Radicais Livres/antagonistas & inibidores , Humanos , Hipoglicemiantes/síntese química , Hipoglicemiantes/química , Estrutura Molecular , Ratos , Relação Estrutura-Atividade , Sulfacetamida/síntese química , Sulfacetamida/química , Triazenos/química , alfa-Glucosidases/metabolismo
6.
Dermatol Online J ; 20(3)2014 Mar 17.
Artigo em Inglês | MEDLINE | ID: mdl-24656277

RESUMO

Acne vulgaris is a pervasive inflammatory disorder of the skin, with multiple etiologies and treatment options. Although first-line therapies exist, it is often the case that a patient will present with an underlying disorder that prohibits the use of most currently accepted treatment modalities. We present a patient with severe acne vulgaris and a history of retinitis pigmentosa who was treated with 595 nanometer pulsed dye laser therapy, in conjunction with therapeutic alternatives to first-line acne medications. Our patient exhibited a significant and sustained improvement with the combined use of 595 nanometer pulsed dye laser, Yaz (drospirenone-ethinyl estradiol), dapsone, topical metronidazole, sodium-sulfacetamide wash, and topical azelaic acid. The positive results in this case, suggest that this combined treatment modality may serve as an example of a safe and effective treatment alternative in the management of acne vulgaris complicated by medical co-morbidities that contraindicate the use of most first-line treatment options.


Assuntos
Acne Vulgar/radioterapia , Lasers de Corante/uso terapêutico , Retinose Pigmentar/complicações , Acne Vulgar/complicações , Administração Cutânea , Adulto , Androstenos/uso terapêutico , Anti-Infecciosos Locais/administração & dosagem , Anti-Infecciosos Locais/uso terapêutico , Terapia Combinada , Contraindicações , Dapsona/uso terapêutico , Ácidos Dicarboxílicos/administração & dosagem , Ácidos Dicarboxílicos/uso terapêutico , Etinilestradiol/uso terapêutico , Feminino , Humanos , Metronidazol/administração & dosagem , Metronidazol/uso terapêutico , Antagonistas de Receptores de Mineralocorticoides/administração & dosagem , Antagonistas de Receptores de Mineralocorticoides/uso terapêutico , Fármacos Fotossensibilizantes , Descolamento Retiniano/prevenção & controle , Rosácea/complicações , Rosácea/radioterapia , Sulfacetamida/uso terapêutico , Telangiectasia/etiologia , Telangiectasia/radioterapia
7.
Cell Biol Int ; 37(4): 348-58, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-23450781

RESUMO

The broad spectrum of the pharmacological effects of sulphonamide family of drugs motivated us to investigate the cellular mechanisms for anti-cancer effects of sulphathiazole and sulphacetamide on T-47D breast cancer cells. Fluorescent microscopy, flow cytometric analysis, caspase-3 activity and DNA fragmentation assays were used to detect apoptosis. The distribution of the cells among different phases of the cell cycle was measured by flow cytometry. The expression of several genes with important roles in some critical cellular pathways including apoptosis, mTOR/AKT pathway and autophagy were determined by real-time RT-PCR analysis. Sulphathiazole and sulphacetamide induced anti-proliferative effects on T-47D cells were independent of apoptosis and cell cycle arrest. The overexpression of critical genes involved in autophagy including ATG5, p53 and DRAM indicated that the main effect of the drug-induced anti-proliferative effects was through induction of autophagy. This process was induced in two different forms, including death inducing and cytoprotective autophagy. Sulphathiazole treatment was followed by higher expression of p53/DRAM and downregulation of Akt/mTOR pathway resulting in death autophagy. In contrast, sulphacetamide treatment lowered expression of p53/DRAM pathway in parallel with upregulation of Akt/mTOR pathway promoting cytoprotective autophagy. The results indicated that autophagy is the main mechanism mediating the anti-cancer effects of sulphathiazole and sulphacetamide on T-47D cells. Alignment of the p53 and DRAM expression along with activation level of Akt survival pathway therefore determines the type of autophagy that occurs.


Assuntos
Antibacterianos/farmacologia , Autofagia/efeitos dos fármacos , Sulfacetamida/farmacologia , Sulfatiazóis/farmacologia , Apoptose , Caspase 3/metabolismo , Ciclo Celular , Linhagem Celular Tumoral , Citoproteção , Fragmentação do DNA , Ativação Enzimática , Humanos , Dose Letal Mediana , Sulfatiazol
8.
Australas J Dermatol ; 54(2): 144-6, 2013 May.
Artigo em Inglês | MEDLINE | ID: mdl-22897159

RESUMO

We present a case of a 15-year-old boy who developed toxic epidermal necrolysis (TEN) from sulfacetamide eyedrops. He presented with conjunctival injection and an erythematous rash that rapidly progressed to epidermal necrosis of over 30% of his body. A skin biopsy revealed an acute lichenoid reaction pattern consistent with TEN. After 22 days in hospital, he was left with significant scarring to his eyes, mouth and anogenital areas. An extensive search for an infective aetiology was negative. Previously exposed to bactrim tablets, he used Bleph-10 eyedrops 3 days before admission to hospital. The patient had a strong family history of sulphur allergy. The onset of TEN after topical administration of medication has been reported rarely in the literature. This case highlights the need for a thorough medication history that includes topical preparations.


Assuntos
Anti-Infecciosos Locais/efeitos adversos , Soluções Oftálmicas/efeitos adversos , Síndrome de Stevens-Johnson/etiologia , Sulfacetamida/efeitos adversos , Adolescente , Humanos , Masculino , Medicamentos sem Prescrição/efeitos adversos , Síndrome de Stevens-Johnson/patologia , Síndrome de Stevens-Johnson/terapia
11.
Tuberculosis (Edinb) ; 142: 102393, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-37684080

RESUMO

In recent years, our knowledge of leprosy in the past has substantially been enriched. Nonetheless, much still remains to be discovered, especially in regions and periods from where no written sources are available. To fill in some research gaps, we provide the comparative analysis of eight Avar-period leprosy cases from the Danube-Tisza Interfluve (Hungary). In every case, to reconstruct the biological consequences of leprosy, the detected bony changes were linked with palaeopathological and modern medical information. To reconstruct the social consequences of being affected by leprosy, conceptualisation of the examined individuals' treatment in death was conducted. In every case, the disease resulted in deformation and disfigurement of the involved anatomical areas (rhinomaxillary region, feet, and/or hands) with difficulties in conducting certain physical activities. These would have been disadvantageous for the examined individuals and limited or changed their possibilities to participate in social situations. The most severe cases would have required continuous support from others to survive. Our findings indicate that, despite their very visible disease and associated debility, the examined communities did not segregate leprosy sufferers but provided and cared for them, and maintained a strong enough social network that made their survival possible even after becoming incapable of self-sufficiency.


Assuntos
Hanseníase , Mycobacterium tuberculosis , Humanos , Hungria , Lacunas de Evidências , Hanseníase/diagnóstico , Hanseníase/tratamento farmacológico , Sulfacetamida
13.
Skin Therapy Lett ; 17(10): 1-4, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23223767

RESUMO

Rosacea is a common chronic skin disorder that has significant impact on the self-esteem and quality of life of affected individuals. Currently understood as an inflammatory condition that occurs in the context of an altered innate immune response, the available topical and systemic therapies function as immunomodulators to restore cutaneous homeostasis. The goals of therapy include reduction of papules, pustules, erythema and physical discomfort with improvement in quality of life. Standard topical treatments include metronidazole and azelaic acid, although many other agents and regimens have been presented. Subantimicrobial/antiinflammatory dose oral doxycycline was US FDA approved in 2006 for the management of rosacea, but Health Canada clearance was only recently granted for this indication. Furthermore, renewed research interest has led to the development of other emerging therapies including topical ivermectin, brimonidine and oxymetazoline that hold promise for patients suffering from this condition.


Assuntos
Adrenérgicos/administração & dosagem , Anti-Infecciosos/administração & dosagem , Antiparasitários/administração & dosagem , Fármacos Dermatológicos/administração & dosagem , Rosácea/tratamento farmacológico , Administração Cutânea , Tartarato de Brimonidina , Ácidos Dicarboxílicos/administração & dosagem , Doxiciclina/administração & dosagem , Feminino , Humanos , Ivermectina/administração & dosagem , Masculino , Metronidazol/administração & dosagem , Oximetazolina/administração & dosagem , Qualidade de Vida , Quinoxalinas/administração & dosagem , Ensaios Clínicos Controlados Aleatórios como Assunto , Rosácea/fisiopatologia , Sulfacetamida/administração & dosagem , Resultado do Tratamento
14.
Sci Total Environ ; 826: 154436, 2022 Jun 20.
Artigo em Inglês | MEDLINE | ID: mdl-35276146

RESUMO

Antibiotic contamination in the environment has significant adverse effects on benthic microorganisms, which causes dysfunction of normal ecological processes. However, in-depth molecular mechanisms underlying the potential ecological impacts of these emerging pollutants are poorly understood. In this study, metabolic perturbations in a freshwater microalga, Desmodesmus quadricauda by sulfacetamide (SFM) were investigated using transcriptomics. The results found 28 genes in the tricarboxylic acid cycle and oxidative phosphorolysis pathways were significantly downregulated by 3.97 to 6.07, and 2.47 to 5.99 folds by 0.1 and 1 mg L-1 SFM, respectively. These results indicated that SFM disrupted the microalgal cellular activities through inhibition of energy metabolism. Whilst, the upregulated genes have been most enriched in porphyrin and chlorophyll metabolism (hemE, hemL, hemY, chlD, chlP, PAO, and CAO), and arachidonic acid metabolism (GGT1_5 and gpx). Expression of these genes was significantly upregulated by up to 3.36 times for tolerance against SFM. Moreover, the genes encoding decarboxylase, oxidoreductases, α-amylase, hydrolases, O-acetyltransferase, and lyase were upregulated by >2 folds, which can induce di/hydroxylation, decarboxylation, bond cleavage and deamination. These findings provide insights into the molecular mechanisms of the ecotoxicological effects of antibiotics on microalgae, and supply useful information for their environmental risk assessment and management.


Assuntos
Microalgas , Sulfacetamida , Biodegradação Ambiental , Água Doce , Transcriptoma
15.
Int J Biol Macromol ; 222(Pt A): 1465-1475, 2022 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-36113599

RESUMO

In this study, a novel magnetic organic-inorganic composite was fabricated. Chitosan, sulfacetamide and ethylacetoacetae were used to prepare a new Sulfacetamide-Ethylacetoacetate hydrazone-chitosan Schiff-base (SEH-CSB) with a variety of active sites that capable of forming coordinate covalent bonds with Cr(VI). This was followed by modification of the formed SHE-CSB with NiFe2O4 to obtain the magnetic Chitosan-Schiff-base composite (NiFe2O4@SEH-CSB). NiFe2O4@SEH-CSB was characterized using FTIR, zeta potential, SEM, VSM and XPS. Results clarified that SHE played a crucial role in the removal of Cr(VI). The removal of Cr(VI) on NiFe2O4@SEH-CSB was found to be more fitted to pseudo-second order kinetics model and Freundlich isotherm. Besides, the maximum adsorption capacity of NiFe2O4@SEH-CSB towards Cr(VI) was found to be 373.61 mg/g. The plausible mechanism for the removal of Cr(VI) by NiFe2O4@SEH-CSB composite suggested the domination of coulombic interaction, outer-sphere complexation, ion-exchange, surface complexation and coordinate-covalent bond pathways. The magnetic property enabled easy recycling of NiFe2O4@SEH-CSB composite for seven sequential cycles.


Assuntos
Quitosana , Poluentes Químicos da Água , Purificação da Água , Quitosana/química , Sulfacetamida , Poluentes Químicos da Água/química , Hidrazonas , Concentração de Íons de Hidrogênio , Cromo/química , Adsorção , Bases de Schiff/química , Cinética , Fenômenos Magnéticos , Purificação da Água/métodos
16.
Ann Dermatol Venereol ; 138 Suppl 2: S158-62, 2011 Sep.
Artigo em Francês | MEDLINE | ID: mdl-21907876

RESUMO

A range of treatment options are available in rosacea, which include several topical (mainly metronidazole, azelaic acid, other antibiotics, sulfur, retinoids) and oral drugs (mainly tetracyclines, metronidazole, macrolides). In some cases, the first choice is a systemic therapy because patients may have sensitive skin and topical medications can be irritant. Isotretinoin can be used in resistant cases of rosacea. Unfortunately, the majority of studies on rosacea treatments are at high or unclear risk of bias. A recent Cochrane review found that only topical metronidazole, azelaic acid, and oral doxycycline (40 mg) had some evidence to support their effectiveness in moderate to severe rosacea and concluded that further well-designed, adequately-powered randomised controlled trials are required. In our practice, we evaluate our patients for the presence of two possible triggers, Helicobacter pylori infection and small intestinal bacterial overgrowth. When they are present we use adapted antibiotic protocols. If not, we use oral metronidazole or oral tetracycline to treat papulopustolar rosacea. We also look for Demodex folliculorum infestation. When Demodex concentration is higher than 5/cm(2) we use topical crotamiton 10% or metronidazole.


Assuntos
Rosácea/tratamento farmacológico , Adapaleno , Anti-Infecciosos/uso terapêutico , Ciclosporina/uso terapêutico , Fármacos Dermatológicos/uso terapêutico , Ácidos Dicarboxílicos/uso terapêutico , Humanos , Imunossupressores/uso terapêutico , Isotretinoína/uso terapêutico , Ceratolíticos/uso terapêutico , Metronidazol/uso terapêutico , Infestações por Ácaros/tratamento farmacológico , Naftalenos/uso terapêutico , Sulfacetamida/uso terapêutico , Tacrolimo/uso terapêutico , Tetraciclina/uso terapêutico , Toluidinas/uso terapêutico , Tretinoína/uso terapêutico
17.
Ann Dermatol Venereol ; 138 Suppl 3: S211-4, 2011 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-22183101

RESUMO

A range of treatment options are available in rosacea, which include several topical (mainly metronidazole, azelaic acid, other antibiotics, sulfur, retinoids) and oral drugs (mainly tetracyclines, metronidazole, macrolides). In some cases, the first choice is a systemic therapy because patients may have sensitive skin and topical medications can be irritant. Isotretinoin can be used in resistant cases of rosacea. Unfortunately, the majority of studies on rosacea treatments are at high or unclear risk of bias. A recent Cochrane review found that only topical metronidazole, azelaic acid, and oral doxycycline (40 mg) had some evidence to support their effectiveness in moderate to severe rosacea and concluded that further well-designed, adequately-powered randomised controlled trials are required. In our practice, we evaluate our patients for the presence of two possible triggers, Helicobacter pylori infection and small intestinal bacterial overgrowth. When they are present we use adapted antibiotic protocols. If not, we use oral metronidazole or oral tetracycline to treat papulopustolar rosacea. We also look for Demodex folliculorum infestation. When Demodex concentration is higher than 5/cm(2) we use topical crotamiton 10% or metronidazole.


Assuntos
Rosácea/terapia , Anti-Infecciosos/uso terapêutico , Ciclosporina/uso terapêutico , Fármacos Dermatológicos/uso terapêutico , Ácidos Dicarboxílicos/uso terapêutico , Humanos , Imunossupressores/uso terapêutico , Isotretinoína/uso terapêutico , Ceratolíticos/uso terapêutico , Lasers de Corante , Metronidazol/uso terapêutico , Infestações por Ácaros/tratamento farmacológico , Naftalenos/uso terapêutico , Fototerapia , Sulfacetamida/uso terapêutico , Tacrolimo/uso terapêutico , Tetraciclina/uso terapêutico , Toluidinas/uso terapêutico , Tretinoína/uso terapêutico
18.
Bull Exp Biol Med ; 151(5): 619-21, 2011 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-22462060

RESUMO

Sulfamide-resistant (SulR) natural strains of enterobacteria (11.9% of a total of 797 cultures, isolated with enteric microflora of honeybee gut, bee-fermented pollen, and plant issues) were tested for class 1 antibiotic resistance integrons (MRI). Only 5.3% of SulR strains were MRI-positive. Mutability of weak (wild type) MRI promotor has been shown. A more active hybrid promotor type has been amplified in isolated Klebsiella oxytoca strains. Regulatory genetic modifications in MRI are fraught with the development of multiple drug resistance of opportunistic strains.


Assuntos
Farmacorresistência Bacteriana/genética , Enterobacteriaceae/genética , Variação Genética , Integrons/genética , Animais , Antibacterianos/farmacologia , Sequência de Bases , Abelhas/microbiologia , Enterobacteriaceae/isolamento & purificação , Genes Bacterianos , Dados de Sequência Molecular , Regiões Promotoras Genéticas , Análise de Sequência de DNA , Sulfacetamida/farmacologia
19.
J Pharm Pharm Sci ; 13(4): 510-23, 2010.
Artigo em Inglês | MEDLINE | ID: mdl-21486528

RESUMO

PURPOSE: Polymeric nanosuspension was prepared from an inert polymer resin (Eudragit® RL100) with the aim of improving the availability of sulfacetamide at the intraocular level to combat bacterial infections. METHODS: Nanosuspensions were prepared by the solvent displacement method using acetone and Pluronic® F108 solution. Drug to polymer ratio was selected as formulation variable. Characterization of the nanosupension was performed by measuring particle size, zeta potential, Fourier Transform infrared spectra (FTIR), Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD), drug entrapment efficiency and in vitro release. In addition, freeze drying, redispersibility and short term stability study at room temperature and at 4(0)C were performed. RESULTS: Spherical, uniform particles (size below 500 nm) with positive zeta potential were obtained. No significant chemical interactions between drug and polymer were observed in the solid state characterization of the freeze dried nanosuspension (FDN). Drug entrapment efficiency of the selected batch was increased by changing the pH of the external phase and addition of polymethyl methacrylate in the formulation. The prepared nanosuspension exhibited good stability after storage at room temperature and at 4(0)C. Sucrose and Mannitol were used as cryoprotectants and exhibited good water redispersibility of the FDN. CONCLUSION: The results indicate that the formulation of sulfacetamide in Eudragit® RL100 nanosuspension could be utilized as potential delivery system for treating ocular bacterial infections.


Assuntos
Resinas Acrílicas/química , Antibacterianos/administração & dosagem , Excipientes/química , Sulfacetamida/administração & dosagem , Antibacterianos/farmacocinética , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Estabilidade de Medicamentos , Armazenamento de Medicamentos , Infecções Oculares Bacterianas/tratamento farmacológico , Liofilização , Concentração de Íons de Hidrogênio , Manitol/química , Nanopartículas , Tamanho da Partícula , Polimetil Metacrilato/química , Solventes/química , Sacarose/química , Sulfacetamida/farmacocinética , Suspensões , Temperatura
20.
J Drugs Dermatol ; 9(3): 234-6, 2010 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-20232584

RESUMO

Prior to 1962, some of the most versatile drugs in dermatology were approved by the U.S. Food and Drug Administration (FDA) solely on the basis of safety. One of these is the combination 10% sodium sulfacetamide and 5% sulfur. Sodium sulfacetamide possesses anti-inflammatory and antibacterial properties while sulfur is a nonspecific antibacterial and antifungal. A new emollient foam formulation of 10% sodium sulfacetamide and 5% sulfur allows a thinner application film and leaves behind no residue on hair bearing or non-hair bearing skin. The sulfur smell is also more quickly dissipated with reduced irritation. This uncontrolled, observational, prospective, open-label, single site, eight-week study enrolled 24 subjects (eight with rosacea, eight with seborrheic dermatitis, eight with acne vulgaris) to evaluate the safety and efficacy of this novel foam formulation. At eight weeks, statistically significant improvement was seen in inflammatory rosacea lesion counts and the signs of seborrheic dermatitis. A 50% reduction was noted in the total acne lesion counts. These findings confirm the versatility of an emollient 10% sodium sulfacetamide and 5% sulfur foam.


Assuntos
Emolientes/administração & dosagem , Dermatoses Faciais/tratamento farmacológico , Sulfacetamida/administração & dosagem , Enxofre/administração & dosagem , Acne Vulgar/tratamento farmacológico , Dermatite Seborreica/tratamento farmacológico , Humanos , Estudos Longitudinais , Estudos Prospectivos , Rosácea/tratamento farmacológico
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