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1.
Int J Pharm ; 653: 123857, 2024 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-38281693

RESUMO

Multidrug therapeutic hybrids constitute a promising proposal to overcome problems associated with traditional formulations containing physical mixtures of drugs, potentially improving pharmacological and pharmaceutical performance. Indomethacin (IND) is a non-selective non-steroidal anti-inflammatory drug (NSAIDs) that acts by inhibiting normal processes of homeostasis, causing a series of side effects, such as gastrointestinal symptoms. Proton pump inhibitors, such as omeprazole (OME), have been used to treat such gastrointestinal tract symptoms. In this work, two new multidrug therapeutic hybrids were prepared (an IND:OME salt and an IND:OME co-amorphous system) by ball mill grinding crystalline IND and OME under different conditions, i.e., liquid assisted grinding (LAG) with ethanol and dry grinding, respectively. The crystalline salt returned to a neutral state co-amorphous system when submitted to ball mill grinding in the absence of solvent (dry grinding), but the reverse process (LAG of the IND:OME co-amorphous system) showed partial decomposition of OME. The IND:OME co-amorphous system showed a higher physical stability than the neat IND and OME amorphous materials (with an amorphous stability longer than 100 days, compared to 4 and 16 h for the neat amorphous drugs, respectively, when stored at dry conditions at room temperature). Furthermore, OME presented a higher chemical stability in solution when dissolved from a salt form than from the pure crystalline form. The dissolution studies showed a dissolution enhancement for IND in both salt (1.8-fold after 8 h of dissolution) and co-amorphous (2.5-fold after 8 h of dissolution) forms. Anti-inflammatory activity using a mice paw oedema model showed an increase of the pharmacological response to IND at a lower dose (∼5mg/kg) for both IND:OME salt (2.8-fold) and IND:OME co-amorphous system (3.2-fold) after 6 h, when compared to the positive control group (IND, administered at 10 mg/kg). Additionally, the anti-inflammatory activity of both salt and co-amorphous form was faster than for the crystalline IND. Finally, an indomethacin-induced gastric ulceration assay in mice resulted in a higher mucosal protection at the same dose (40 mg/kg) for both IND:OME salt and IND:OME co-amorphous system when compared with crystalline OME.


Assuntos
Indometacina , Omeprazol , Camundongos , Animais , Indometacina/química , Estabilidade de Medicamentos , Cristalização , Difração de Raios X , Anti-Inflamatórios não Esteroides/farmacologia , Anti-Inflamatórios não Esteroides/química , Cloreto de Sódio , Solubilidade
2.
Neurochem Int ; 159: 105401, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-35842055

RESUMO

Over the years, the scientific community has sought improvements in the life quality of patients diagnosed with Alzheimer's disease (AD). Synaptic loss and neuronal death observed in the regions responsible for cognitive functions represent an irreversible progressive disease that is clinically characterized by impaired cognitive and functional abilities, along with behavioral symptoms. Currently, image and body fluid biomarkers can provide early dementia diagnostic, being it the best way to slow the disease's progression. The first signs of AD development are still complex, the existence of individual genetic and phenotypic characteristics about the disease makes it difficult to standardize studies on the subject. The answer seems to be related between Aß and tau proteins. Aß deposition in the medial parietal cortex appears to be the initial stage of AD, but it does not have a strong correlation with neurodegeneration. The strongest link between symptoms occurs with tau aggregation, which antecede Aß deposits in the medial temporal lobe, however, the protein can be found in cognitively healthy older people. The answer to the question may lie in some catalytic effect between both proteins. Amid so many doubts, Aducanumab was approved, which raised controversies and results intense debate in the scientific field. Abnormal singling of some blood biomarkers produced by adipocytes under high lipogenesis, such as TNFα, leptin, and interleukin-6, demonstrate to be linked to neuroinflammation worsens, diabetes, and also severe cases of COVID-19, howsoever, under higher lipolysis, seem to have therapeutic anti-inflammatory effects in the brain, which has increasingly contributed to the understanding of AD. In addition, the relationship of severe clinical complications caused by Sars-CoV-2 viral infection and AD, go beyond the term "risk group" and may be related to the development of dementia long-term. Thus, this review summarized the current emerging pharmacotherapies, alternative treatments, and nanotechnology applied in clinical trials, discussing relevant points that may contribute to a more accurate look.


Assuntos
Doença de Alzheimer , Tratamento Farmacológico da COVID-19 , Idoso , Doença de Alzheimer/genética , Peptídeos beta-Amiloides/metabolismo , Biomarcadores , Humanos , Tomografia por Emissão de Pósitrons , SARS-CoV-2 , Proteínas tau/metabolismo
3.
Int J Pharm ; 603: 120658, 2021 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-33964336

RESUMO

Vulvovaginal candidiasis (VVC) is an extremely common type of vaginal infection, which is mainly caused by Candida albicans. However, non-albicans Candida species are frequently more resistant to conventional antifungal agents and can represent up to 30% of cases. Due to side effects and increasing antifungal resistance presented by standard therapies, phenolic compounds, such as p-coumaric acid (p-CA), have been studied as molecules from natural sources with potential antifungal activity. p-CA is a poorly water-soluble compound, thus loading it into liquid crystals (LCs) may increase its solubility and effectiveness on the vaginal mucosa. Thereby, here we propose the development of mucoadhesive liquid crystalline systems with controlled release of p-CA, for the local treatment of VVC. Developed LCs consisted of fixed oily and aqueous phases (oleic acid and cholesterol (5:1) and poloxamer dispersion 16%, respectively), changing only the surfactant phase components (triethanolamine oleate (TEA-Oleate) or triethanolamine (TEA), the latter producing TEA-Oleate molecules when mixed with oleic acid). Systems were also diluted in artificial vaginal mucus (1:1 ratio) to mimic the vaginal environment and verify possible structural changes on formulations upon exposure to the mucosa. From the characterization assays, p-CA loaded TEA-Oleate systems presented mucoadhesive profile, liquid crystalline mesophases, well-organized structures and pseudoplastic behaviour, which are desirable parameters for topical formulations. Moreover, they were able to control the release of p-CA throughout the 12 h assay, as well as decrease its permeation into the vaginal mucosa. p-CA showed antifungal activity in vitro against reference strains of C. albicans (SC5314), C. glabrata (ATCC 2001) and C. krusei (ATCC 6258), and exhibited higher eradication of mature biofilms than amphotericin B and fluconazole. In vivo experiments demonstrated that the formulations reduced the presence of filamentous forms in the vaginal lavages and provided an improvement in swelling and redness present in the mice vaginal regions. Altogether, here we demonstrated the potential and feasibility of using p-CA loaded liquid crystalline systems as a mucoadhesive drug delivery system for topical treatment of VVC.


Assuntos
Candidíase Vulvovaginal , Cristais Líquidos , Animais , Antifúngicos/uso terapêutico , Candida albicans , Candidíase Vulvovaginal/tratamento farmacológico , Ácidos Cumáricos , Feminino , Humanos , Camundongos , Testes de Sensibilidade Microbiana , Propionatos
4.
Biomed Pharmacother ; 130: 110592, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32763822

RESUMO

OBJECTIVES: The most recent survey conducted by the World Health Organization described Tuberculosis (TB) as one of the top 10 causes of death and the leading cause of death from a single infectious agent. The increasing number of TB-resistant cases has contributed to this scenario. In light of this, new strategies to control and treat the disease are necessary. Our research group has previously described furoxan derivatives as promising scaffolds to be explored as new antitubercular drugs. RESULTS: Two of these furoxan derivatives, (14b) and (14c), demonstrated a high selectivity against Mycobacterium tuberculosis. The compounds (14b) and (14c) were also active against a latent M. tuberculosis strain, with MIC90 values of 6.67 µM and 9.84 µM, respectively; they were also active against monoresistant strains (MIC90 values ranging from 0.61 to 20.42 µM) and clinical MDR strains (MIC90 values ranging from 3.09 to 42.95 µM). Time-kill experiments with compound (14c) showed early bactericidal effects that were superior to those of the first- and second-line anti-tuberculosis drugs currently used in therapy. The safety of compounds (14b) and (14c) was demonstrated by the Ames test because these molecules were not mutagenic under the tested conditions. Finally, we confirmed the safety, and high efficacy of compounds (14b) and (14c), which reduced M. tuberculosis to undetectable levels in a mouse aerosol model of infection. CONCLUSION: Altogether, we have identified two advanced lead compounds, (14b) and (14c), as novel promising candidates for the treatment of TB infection.


Assuntos
Antituberculosos/uso terapêutico , Oxidiazóis/uso terapêutico , Tuberculose/tratamento farmacológico , Animais , Antituberculosos/farmacologia , Antituberculosos/toxicidade , Bactérias/efeitos dos fármacos , Farmacorresistência Bacteriana , Feminino , Camundongos , Camundongos Endogâmicos BALB C , Testes de Sensibilidade Microbiana , Testes de Mutagenicidade , Mycobacterium tuberculosis/efeitos dos fármacos , Oxidiazóis/farmacologia , Oxidiazóis/toxicidade , Tuberculose/microbiologia
5.
Pharmazie ; 75(5): 179-185, 2020 05 01.
Artigo em Inglês | MEDLINE | ID: mdl-32393424

RESUMO

Trans-resveratrol has antimicrobial effects; however, its hydrophobic properties hamper its incorporation into pharmaceutical formulations. The aim of this study was to develop liquid crystals and a liquid crystal precursor (microemulsion), a common nanotechnology-based drug delivery system using a surfactant, an oil phase, and a polymer dispersion, for topical administration against buccal candidiasis. A ternary diagram was constructed and a potential formulation was selected, in order to run characterization tests. We chose the formulation that presented microemulsion and crystal liquid characteristics through polarized light microscopy and smallangle X-ray scattering experiments. The stability and structural features of the formulations were observed by performing rheological assay, measuring mucoadhesion, and analyzing texture profiles. It was verified that the chosen system was capable of transiting from microemulsion to liquid crystals when added in aqueous phase; further, the presence of sodium alginate as the polymer increased its mucoadhesion strength. Microbiological assay of trans-resveratrol, using amphotericin B and fluconazole as controls against strains of Candida albicans, showed positive anti-microbiological effect; however, a high concentration of the compound was needed.


Assuntos
Alginatos/química , Candidíase Bucal/tratamento farmacológico , Cristais Líquidos , Resveratrol/farmacologia , Anfotericina B/farmacologia , Antifúngicos/administração & dosagem , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Sistemas de Liberação de Medicamentos , Emulsões , Fluconazol/farmacologia , Interações Hidrofóbicas e Hidrofílicas , Mucosa Bucal , Nanotecnologia , Resveratrol/administração & dosagem , Tensoativos/química
6.
Pharmazie ; 74(12): 715-720, 2019 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-31907109

RESUMO

A copper(II) complex-loaded castor oil-based nanostructured lipid carrier was evaluated to enhance the poor water solubility of antimicrobial compounds, improving their biological properties and antimicrobial activity against Mycobacterium tuberculosis. Nanostructured lipid carriers were composed of the castor oil, polyoxyethylene 40 stearate and caprylic/capric triglyceride, poloxamer 407, cetyltrimethylammonium bromide and three different copper(II) complexes. The systems were ultrasonicated at an amplitude of 8% for 20 min and an ice bath was used throughout the procedure. The blank nanostructured lipid carrier (F5) and nanostructured lipid carriers loaded with copper(II) complex 1, 2 and 3 (F5.1, F5.2 and F5.3, respectively) for 45 days presented values of mean diameter, poly dispersity index and zeta potential ranging from 186 to 199 nm, 0.14 to 0.2 and 24 to 30 mV, respectively. Atomic force microscopy indicated that the nanostructured lipid carriers were distributed at the nanoscale, corroborating the mean diameter data. Differential scanning calorimetry determined the melting points of the constituents of the nanostructured lipid carriers. The antimicrobial activity of copper(II) complexloaded F5 against M. tuberculosis H37Rv showed better anti-tuberculosis activity than the free complexes. In vivo biological assays of complex-loaded F5 demonstrated reduced toxicity. Our results suggest that nanostructured lipid carriers could be a potential nanotechnological strategy to optimise tuberculosis treatment.


Assuntos
Antibacterianos/farmacologia , Óleo de Rícino/farmacologia , Cobre/farmacologia , Portadores de Fármacos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Bioensaio , Lipídeos , Testes de Sensibilidade Microbiana , Nanoestruturas , Tamanho da Partícula
7.
Pharmazie ; 73(3): 128-132, 2018 03 05.
Artigo em Inglês | MEDLINE | ID: mdl-29544558

RESUMO

A reversed-phase liquid chromatography (RP-LC) method was successfully developed and validated for the determination of methotrexate in nanostructured liquid crystalline systems composed by polyether functional siloxane and silicone polyether copolymer. The LC method was performed on RP C18-ODS column, Agilent Zorbax® (4.6 x 250 mm, 5 µm), maintained at room temperature, with a mobile phase constituted by a mixture of 50 mM ammonium acetate buffer (pH 6.0) and methanol (77:23,v/v) with a flow rate of 1.0 mL/min, using ultraviolet detection at 313 nm. The parameters used in the validation process were linearity, specificity, intra and inter-day precision, accuracy, robustness. The quantitation and detection limits yielded good results. The calibration plot assumed linear behavior from 5.0-150.0 µg. mL-1 (r2 = 0.9999). The methotrexate was subjected to oxidation, acid, base and neutral degradation, photolysis and heat as stress conditions. There were no interfering peaks at or near the retention time of methotrexate. The nanostructured liquid crystalline systems did not interfere with the analysis and the recovery was quantitative. The intra and inter-day assay relative standard deviation were less than 0.20 %. The method developed proved to be simple, sensitive, accurate, precise, reproducible and therefore adequate for routine analysis of methotrexate in nanostructured liquid crystalline systems.


Assuntos
Metotrexato/análise , Cromatografia Líquida de Alta Pressão , Limite de Detecção , Cristais Líquidos , Metotrexato/administração & dosagem , Nanoestruturas , Padrões de Referência , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Espectrofotometria Ultravioleta
8.
Pharmazie ; 72(10): 563-567, 2017 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-29441878

RESUMO

Cutaneous penetration is a critical factor in the use of sunscreen, as the compounds should not reach systemic circulation in order to avoid the induction of toxicity. The evaluation of the skin penetration and permeation of the UVB filter octyl methoxycinnamate (OMC) is essential for the development of a successful sunscreen formulation. Liquid-crystalline systems are innovative and potential carriers of OMC, which possess several advantages, including controlled release and protection of the filter from degradation. In this study, a new and effective method was developed using ultra-high performance liquid chromatography (UPLC) with ultraviolet detection (UV) for the quantitative analysis of penetration of OMC-loaded liquid crystalline systems into the skin. The following parameters were assessed in the method: selectivity, linearity, precision, accuracy, robustness, limit of detection (LOD), and limit of quantification (LOQ). The analytical curve was linear in the range from 0.25 to 250 µg.m-1, precise, with a standard deviation of 0.05-1.24%, with an accuracy in the range from 96.72 to 105.52%, and robust, with adequate values for the LOD and LOQ of 0.1 and 0.25 µg.mL -1, respectively. The method was successfully used to determine the in vitro skin permeation of OMC-loaded liquid crystalline systems. The results of the in vitro tests on Franz cells showed low cutaneous permeation and high retention of the OMC, particularly in the stratum corneum, owing to its high lipophilicity, which is desirable for a sunscreen formulation.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Cinamatos/química , Cinamatos/farmacocinética , Cristais Líquidos/química , Absorção Cutânea , Protetores Solares/química , Protetores Solares/farmacocinética , Administração Cutânea , Animais , Calibragem , Composição de Medicamentos , Limite de Detecção , Reprodutibilidade dos Testes , Pele/citologia , Pele/metabolismo , Espectrofotometria Ultravioleta , Sus scrofa , Suínos
9.
Pharmazie ; 72(12): 721-727, 2017 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-29441956

RESUMO

Curcumin (CUM) possesses therapeutic activity against diverse skin disorders (SD); however, its clinical use faces many challenges related to physicochemical and bioavailability characteristics, that can be solve designing a new drug delivery system for CUM to treat SD. Cationic solid lipid nanoparticles (CSLN) were developed and physicochemically analyzed. The ingredients and methods adopted in this study promoted the successful preparation of CSLN with a monodispersed particle size of 218.4-238.6 nm and a polydispersity index of 0.156-0.350. A differential scanning calorimetric assay demonstrated that CUM was incorporated. The atomic force microscopy images showed uniform spherical particles, and light scattering technique confirmed the size of the particles. The zeta potential of the CSLN was +23.1 to +30.1 mV, which is important in targeting the drug to the diseased tissue that presents unregulated apoptosis. All formulations behaved as controlled drug delivery systems of CUM, as demonstrated by an in vitro drug release study, which delayed the start of drug release from formulations. At the end of the experiment, the formulations had released 14.74-21.23% of the incorporated CUM. In conclusion, the results suggest the potential of this CSLN as a controlled CUM delivery system for the treatment of SD.


Assuntos
Curcumina/administração & dosagem , Fármacos Dermatológicos/administração & dosagem , Sistemas de Liberação de Medicamentos , Nanopartículas , Varredura Diferencial de Calorimetria , Cátions , Química Farmacêutica/métodos , Curcumina/química , Preparações de Ação Retardada , Fármacos Dermatológicos/química , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Lipídeos/química , Microscopia de Força Atômica , Tamanho da Partícula , Dermatopatias/tratamento farmacológico
10.
Biomed Res Int ; 2013: 271276, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24369010

RESUMO

The aging process causes a number of changes in the skin, including oxidative stress and dyschromia. The kojic acid (KA) is iron chelator employed in treatment of skin aging, and inhibits tyrosinase, promotes depigmentation. Nanotechnology-based drug delivery systems, such as liquid crystalline systems (LCSs), can modulate drug permeation through the skin and improve the drug activity. This study is aimed at structurally developing and characterizing a kojic acid-loaded LCS, consists of water (W), cetostearyl isononanoate (oil-O) and PPG-5-CETETH-20 (surfactant-S) and evaluating its in vitro skin permeation and retention. Three regions of the diagram were selected for characterization: A (35% O, 50% S, 15% W), B (30% O, 50% S, 20% W) and C (20% O, 50% S, 30% W), to which 2% KA was added. The formulations were subjected to polarized light microscopy, which indicated the presence of a hexagonal mesophase. Texture and bioadhesion assay showed that formulation B is suitable for topical application. According to the results from the in vitro permeation and retention of KA, the formulations developed can modulate the permeation of KA in the skin. The in vitro cytotoxic assays showed that KA-unloaded LCS and KA-loaded LCS didn't present cytotoxicity. PPG-5-CETETH-20-based systems may be a promising platform for KA skin delivery.


Assuntos
Sistemas de Liberação de Medicamentos , Pironas/administração & dosagem , Envelhecimento da Pele/efeitos dos fármacos , Pele/efeitos dos fármacos , Humanos , Cristais Líquidos/química , Nanotecnologia , Pironas/química , Tensoativos/administração & dosagem , Tensoativos/química , Tetraciclinas/química , Água/química
11.
Colloids Surf B Biointerfaces ; 85(2): 182-8, 2011 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-21411295

RESUMO

Carrier systems for lipophilic drugs, such as the liquid crystalline systems (LCS) have been extensively studied to improve effect and selectivity. Retinyl palmitate (RP) is widely used in pharmaceutical and cosmetics products to improve the skin elasticity. The aim of this study was the development, characterization and the in vivo effectiveness of RP in non-ionic LCS structures. LCS containing polyether functional siloxane as oil phase, silicon glycol copolymer as surfactant and water in the ratio 30:10:60, with and without RP were studied. The results of the polarized light microscopy, small-angle X-ray scattering and rheology analysis indicated the presence of typical LCS structures with lamellar arrangement. Regardless of the presence of RP, the rheological studies showed the pseudo plastic behavior of the systems. However, highest hysteresis area was verified when comparing the system in the presence and in the absence of RP. Stability study SAXS monitored, carried out up to 30 days in various storage temperature conditions (25±2 °C, 37±2 °C and 5±2 °C) demonstrated the great structural stability of the LCS systems. The in vivo effectiveness analysis suggests that the RP-loaded LCS provided a significant reduction of the orbicular wrinkles in human volunteers (P=0.048).


Assuntos
Cosméticos/química , Cristais Líquidos/química , Tensoativos/química , Vitamina A/análogos & derivados , Adulto , Cosméticos/farmacologia , Diterpenos , Feminino , Humanos , Microscopia de Polarização , Pessoa de Meia-Idade , Ésteres de Retinil , Reologia , Espalhamento a Baixo Ângulo , Envelhecimento da Pele/efeitos dos fármacos , Solubilidade , Tensoativos/farmacologia , Vitamina A/química , Vitamina A/farmacologia , Água/química , Difração de Raios X
12.
Artigo em Português | LILACS | ID: lil-560257

RESUMO

Com o avanço da tecnologia e das pesquisas envolvendo liberação de fármacos, modernização de testes e maior ênfase da previsibilidade de efeitos terapêuticos por meio dos testes in vitro, os testes de dissolução e os estudos de perfis de dissolução têm ganhado cada vez mais importância. Apesar de terem sido introduzidos inicialmente como uma forma de caracterizar o perfil de liberação de fármacos pouco solúveis, atualmente os testes de dissolução fazem parte das monografias de quase todas as formas farmacêuticas sólidas orais. Este trabalho teve como objetivo estudar o perfil de dissolução (porcentagem de fármaco dissolvido versus tempo) dos medicamentos de referência, genérico e similar contendo cefalexina 500 mg na forma farmacêutica de cápsulas. Foram analisadas três especialidades farmacêuticas (referência, genérico e similar), os quais foram submetidos ao teste de dissolução e perfil de dissolução in vitro. Os resultados obtidos no teste de dissolução permitem concluir que as amostras encontraram-se de acordo com as especificações e o perfil de dissolução deste medicamento, nesta forma farmacêutica, é considerado de dissolução rápida (85% de fármaco dissolvido em 15 minutos). Portanto, existe uma grande semelhança entre as curvas obtidas, o que sugere que se trata de equivalentes farmacêuticos.


With recent advances in technology and research into drug delivery, the modernization of tests and greater emphasis on the predictability of therapeutic effect by means of in vitro tests, the dissolution test and the study of dissolution profiles are gaining more and more importance. Though introduced initially as a way of characterizing the release profile of poorly soluble drugs, dissolution tests are currently part of pharmacopoeial monographs on almost all the oral solid pharmaceutical forms. The objective of this study was to determine the dissolution profile (percent drug dissolved versus time) of the pioneer brand, generic and similar pharmaceutical capsules containing 500mg cephalexin. Three pharmaceutical brands (reference, generic and similar) were subjected to the dissolution test and in vitro dissolution profiles were recorded. From the results of the dissolution test, it was concluded that the samples met the acceptance criterion, as no difference was observed in the percentage of the drug dissolved in a standard time. The dissolution profile indicated that this medicine, in this pharmaceutical form, dissolves readily (85% of the drug dissolved in 15 minutes) and the curves showed great similarity, suggesting that the 3 brands are pharmaceutically equivalent.


Assuntos
Humanos , Cápsulas , Cefalexina/farmacocinética , Medicamentos Genéricos , Medicamentos de Referência , Medicamentos Similares
13.
Artigo em Português | LILACS | ID: lil-535423

RESUMO

Dimorphandra mollis Benth., Composita e, falso barbatimão, é utilizada topicamente como cicatrizante, adstringente e antimicrobiano. No presente estudo, verificou-se a atividade antibacteriana de sabonete líquido contendo extrato glicólico de D. mollis (EGD) em diferentes concentrações (8, 15 e 20%) e em diferentes pHs (6 e 8). Foram preparadas cinco formulações (F) de sabonete: F1 - triclosan (0,1%), F2 - EGD (8%), F3- EGD (15%), F4 - EGD (20%) e F5 - sem conservante. Cascas de D. mollis foram secas em estufa de ar circulante e pulverizadas. Os extratos brutos foram preparados por turbo-extração utilizando-se etanol. Após filtração, os extratos foram concentrados em evaporador rotatório, liofilizados e ressuspendidos em propilenoglicol para a obtenção do extrato glicólico. A atividade antibacteriana foi verificada pelo método de difusão em ágar, empregando cilindros em placa. Placas contendo Staphylococcus aureus, Pseudomonas aeruginosa e Escherichia coli foram incubadas a 37ºC durante 24 horas. Após incubação, as leituras foram realizadas com paquímetro, observando-se o diâmetro do halo de inibição de crescimento bacteriano. Verificou-se que o sabonete líquido contendo triclosan provocou inibição do crescimento bacteriano em ambos os pHs; já os sabonetes sem conservante e contendo EGD, independente da concentração e do pH empregados, não apresentaram atividade antibacteriana.


Dimorphandra mollis Benth., Compositae, false barbatimão, has been used topically as a healing, astringent and antibacterial. In this study, antibacterial activity was verified on liquid soap containing glycolic extract of D. mollis (DGE) at different concentrations (8, 15 and 20%) and at different pH levels (6 and8). Five soap formulations (F) were prepared: F1 -tryclosan (0.1%), F2 - DGE (8%), F3 - DGE (15%),F4 - DGE (20%) and F5 - without preservatives. Bark of D. mollis were dried in a circulating air oven and ground. The rude extracts were prepared by turboextraction with ethanol. After screening, the extract were concentrated in rotating evaporator, lyophilized and resuspended in propileneglycol to obtain the glycolic extract. The antimicrobial activity was verified by diffusion in agar method, using cylinder in plate. Plates containing Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli were incubated at 37ºC for 24 hours. After incubation, the results were analysed with a pachy meter, observing the bacterial grouth inhibition halo diameter. It was verified that the liquid soap containing tryclosan caused on inhibition of bacterial growth at both pH levels; the soaps without preservatives and containing DGE, independently of the concentration and pH levels used, did not present antibacterial activity.


Assuntos
Produtos com Ação Antimicrobiana , Imunodifusão/métodos
14.
Artigo em Português | LILACS | ID: lil-536697

RESUMO

Apesar de não ser desejável, alguns produtos cosméticos podem apresentar reações adversas aos usuários. Tais efeitos, muitas vezes, podem ser decorrentes de fatores individuais ou até mesmo pelo uso inadequado do produto. Logo, os ensaios biológicos para avaliação de segurança devem preceder a colocação do cosmético no mercado. Historicamente, estes ensaios sempre foram realizados in vivo, em animais, uma vez que podem ser utilizados para avaliar grande parte dos riscos potenciais envolvidos, seja irritação, alergia ou efeitos sistêmicos; todavia, atualmente alguns centros de pesquisa estão adotando alternativas in vitro aos ensaios com animais. Esta revisão enfatiza a necessidade de realização de ensaios biológicos para avaliação de segurança de produtos cosméticos, bem como apresenta os principais testes in vivo e in vitro empregados, abordando a necessidade de aplicar-se métodos alternativos aos ensaios in vivo na avaliação de segurança dos mesmos, de forma a oferecer aos consumidores o máximo de segurança com o menor risco, garantindo as melhores condições de uso do produto.


Despite efforts to the contrary, some cosmetic products can cause undesirable side effects in the users. These may often be due to individual factors or inappropriate use of the product. Thus, biological assays to assess the safety of a new cosmetic must precede its being placed on the market. Historically, these tests have always been carried out in vivo, in animals, since such tests can be used to evaluate many of the potential risks, such as irritation, allergy or systemic effects; but, recently, some research centers have been adopting in vitro alternatives, in order to replace the animal tests. This review emphasizes the need to employ biological assays to test the safety of cosmetic products, and reviews the main in vivo and in vitro tests used, focusing on the need to develop and use alternatives to the in vivo assays of product safety, so as to offer the consumers the maximum safety with the least possible risk, while ensuring the best conditions of use of the product.


Assuntos
Bioensaio , Cosméticos
15.
Rev. ciênc. farm. básica apl ; 28(1): 11-23, 2007. tab, ilus, graf
Artigo em Português | LILACS | ID: lil-485197

RESUMO

A experimentação animal nas pesquisas científicas tem contribuído sobremaneira para o desenvolvimento da ciência e tecnologia, promovendo ao longo dos anos a descoberta de medidas profiláticas e tratamentos de enfermidades que acometem os seres humanos. Animais de várias espécies têm sido utilizados nos últimos tempos,sendo os camundongos os mais intensamente utilizados e os mais profundamente conhecidos cientificamente. O objetivo deste trabalho foi realizar um levantamento bibliográfico, incluindo os trabalhos do nosso grupo, sobre o emprego de camundongos na experimentação animal, abordando sua biologia geral, fisiologia de reprodução, sistemas de criação, genética, habitação, alimentação, manejo, dor e eutanásia, técnicas de risco desenvolvidas na experimentação, coleta de sangue, experimentos farmacológicos e toxicológicos. Embora tendências atuais preconizem a utilização de métodos alternativos (estudos in vitro, culturas de células, etc.), os modelos animais, como os camundongos, apresentam como principal vantagem o fornecimento de informações sobre o organismo como um todo, fato que não é conseguido com outros métodos, o que ainda possibilita o seu emprego em pesquisas científicas


The animal experimentation in the scientific research has contributed excessively for the development of science and technology, promoting to long of the years the discovery of prophylactic measures and treatments for iseases that attack the humans. Animals of some species have been used in the last times, being the mouse the more intensely used and more deeply known scientifically. The objective of this work was to carry through a bibliographical survey including data of our research group, about the use of mice in the animal experimentation, approaching its general biology, reproduction physiology, creation systems, genetics, habitation, feeding, handling, pain and euthanasia, techniques of risk developed in the experimentation, blood collection, pharmacological and toxicological experiments. Although current trends praise the use of alternative methods (in vitro studies, cells cultures, etc.), the animal models, as the mouse, present as main advantage the supply of information on the organism as a whole, fact that is not obtained with other methods, what still it makes possible its utilization in scientific research.


Assuntos
Animais , Experimentação Animal , Animais de Laboratório/fisiologia , Animais de Laboratório/genética , Bioética , Camundongos
16.
Rev. ciênc. farm. básica apl ; 27(3): 237-246, 2006. tab
Artigo em Português | LILACS | ID: lil-466206

RESUMO

A tendência atual no desenvolvimento de formulações fotoprotetoras é a associação de filtros químicos de amplo espectro e filtros físicos microparticulados fotoestáveis. Para assegurar a estabilidade do filtro é indispensável sua incorporação em veículo adequado que contribua para a melhora da aparência, do sensorial e da aceitação do produto pelo consumidor. O objetivo deste trabalho foi desenvolver e realizar estudos preliminares de estabilidade de formulações cosméticas para incorporação de 20% de filtro solar constituído por metil bisbenzotriazolil tetrametilbutil fenol e dióxido de titânio (Granlux GAI-45 TS®). As formulações selecionadas foram então acrescidas do filtro solar e novamente sujeitas à estudos preliminares de estabilidade. De um total de 20 formulações desenvolvidas, foram selecionados um gel fluido, um gel viscoso, um gel-creme e uma emulsão, aos quais incorporou-se o filtro solar. Após serem submetidas a estudos preliminares de estabilidade, as formulações não apresentaram variação de pH e mantiveram-se estáveis frente ao teste de centrifugação. Diante das condições experimentais, conclui-se que as formulações selecionadas apresentaram espalhabilidade adequada,oleosidade mínima, não apresentaram variação de pH e mantiveram-se estáveis frente ao teste de centrifugação, sendo excipientes adequados para incorporação do Granlux GAI-45 TS®.


Assuntos
Estabilidade de Cosméticos , Protetores Solares/síntese química , Química Farmacêutica/métodos
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