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Cajuína is a processed drink derived from cashew and is widely consumed in the northeast region of Brazil. This study evaluated the effect of a cajuína-based hydroelectrolytic drink on the aerobic performance and hydration status of recreational runners. Seventeen males (31.9 ± 1.6 years, 51.0 ± 1.4 ml/kg/min) performed three time-to-exhaustion running sessions on a treadmill at 70% VO2max, ingesting cajuína hydroelectrolytic drink (CJ), high carbohydrate commercial hydroelectrolytic drink (CH) and mineral water (W) every 15 min during the running test. The participants ran 80.3 ± 8.4 min in CJ, 70.3 ± 6.8 min in CH and 71.8 ± 6.9 min in W, with no statistical difference between procedures. Nevertheless, an effect size of η2 = 0.10 (moderate) was observed. No statistical difference was observed in the concentrations of sodium, potassium, and osmolality in both serum and urine between the three conditions. However, the effect size was moderate (urine sodium) and high (serum sodium, potassium, and osmolality). Urine specific gravity, sweating rate and heart rate were not significantly different between drinks. The cajuína-based hydroelectrolytic drink promotes similar effects compared to commercial hydroelectrolytic drink and water, considering specific urine gravity, heart rate, sweating, and time to exhaustion in recreational runners.
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We encapsulated MSZ in zein nanoparticles (NP-ZN) using a desolvation method followed by drying in a mini spray dryer. These nanoparticles exhibited a size of 266.6 ± 52 nm, IPD of 0.14 ± 1.1 and zeta potential of -36.4 ± 1.5 mV, suggesting colloidal stability. Quantification using HPLC showed a drug-loaded of 43.8 µg/mg. SEM demonstrated a spherical morphology with a size variation from 220 to 400 nm. A FTIR analysis did not show drug spectra in the NPs in relation to the physical mixture, which suggests drug encapsulation without changing its chemical structure. A TGA analysis showed thermal stability up to 300 °C. In vitro release studies demonstrated gastroresistance and a sustained drug release at pH 7.4 (97.67 ± 0.32%) in 120 h. The kinetic model used for the release of MSZ from the NP-ZN in a pH 1.2 medium was the Fickian diffusion, in a pH 6.8 medium it was the Peppas-Sahlin model with the polymeric relaxation mechanism and in a pH 7.4 medium it was the Korsmeyer-Peppas model with the Fickian release mechanism, or "Case I". An in vitro cytotoxicity study in the CT26.WT cell line showed no basal cytotoxicity up to 500 µg/mL. The NP-ZN showed to be a promising vector for the sustained release of MSZ in the colon by oral route.
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Ethyl ferulate, a phenylpropanoid derived from rice hulls has aroused interest because of its antioxidant, anti-inflammatory and neuroprotective properties. However, it has low solubility in water which compromises the absorption in the gastrointestinal tract, decreases the bioavailability and compromises the reproducibility of the effects in vivo. To increase the solubility of ethyl ferulate, inclusion complexes were obtained by physical mixing, malaxing, lyophilization and spray drying and characterized using thermal analysis, XRD and FTIR. The complexes obtained were evaluated for ethyl ferulate content, stability, dissolution profile and evaluation of anti-inflammatory activity in vivo through carrageenan-induced paw edema model in rats. The inclusion complexes obtained resulted in increased solubility and stability compared to the isolated ethyl ferulate. In addition, the complexes obtained by malaxage, lyophilization and spray drying showed greater inhibition of the edema formation induced by carrageenan compared to ethyl ferulate 100 mg/kg v.o. The inclusion of ethyl ferulate in B-cyclodextrin resulted in the formation of stable inclusion complexes with potent antidematogenic activity possibly attributed to the increased solubility, dissolution profile of the active.
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Ácidos Cafeicos/administração & dosagem , Edema/tratamento farmacológico , beta-Ciclodextrinas/química , Animais , Disponibilidade Biológica , Ácidos Cafeicos/química , Ácidos Cafeicos/farmacocinética , Carragenina/efeitos adversos , Modelos Animais de Doenças , Estabilidade de Medicamentos , Edema/induzido quimicamente , Ratos , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Resultado do TratamentoRESUMO
INTRODUCTION: Ethyl ferulate is a phenylpropanoid with anti-inflammatory, antioxidant and neuroprotective activities of natural and synthetic origin with potential uses in the nutraceutical and pharmaceutical industry. Therefore, the aim of this study was to investigate the current scenario regarding patents and scientific articles available involving the substance in question, regarding aspects such as quantity, areas of knowledge and depositor countries. AREAS COVERED: To do so, we conducted technological and scientific prospecting on the WIPO, EPO, USPTO and INPI and scientific databases in PubMed, Web of Science and Lilacs databases using the keywords 'ferulic acid ethyl ester' and 'ethyl ferulate' in English and Portuguese. A total of 16 articles and 17 patents of which 10 were Chinese and 11 claimed the use of ethyl ferulate or for the synthesis of other substances or synthetic methods of the same. Five of the patents selected claimed therapeutic applications related to the treatment of mycobacterial infections, use as a cosmetic and neuroprotective activity. The systematic review of the literature revealed antioxidant, neuroprotective, anti-inflammatory, antimutagenic, antiapoptotic, antimutagenic and antiproliferative activities. EXPERT OPINION: The technological and scientific prospection highlighted ethyl ferulate, despite its known pharmacological activities, is little explored by the pharmaceutical and nutraceutical industries.
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Antioxidantes/farmacologia , Ácidos Cafeicos/farmacologia , Fármacos Neuroprotetores/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Humanos , Patentes como AssuntoRESUMO
INTRODUCTION: Primary dysmenorrhea (PD) is another term for idiopathic menstrual cramps. Treatments include the use of oral non-steroidal anti-inflammatory drugs (NSAIDs). These drugs have several side effects. The objective of this study was to perform a systematic review on the transdermal administration of drugs and the use of alternative therapies for the treatment of PD. AREAS COVERED: The article bases were Web of Science, PubMed and Sciencedirect and the patent bases were INPI, EPO and WIPO with publications on Primary Dysmenorrhea and associations with Transdermal Administration; Complementary Therapies and Medicinal Plants. 21 articles and 12 patents were analyzed. The results demonstrate the need for alternative therapies for the treatment of PD, with greater effectiveness and lower side effects, mainly in an attempt to reduce the intensity and duration of pain as well as reducing the continuous use of medications. EXPERT OPINION: The study of technological prospection highlighted the relevant importance in seeking new methods for the relief of the symptoms provoked by this condition. The perspectives coexist in the discovery of new natural and biotechnological pharmacological applications, mainly in the development of new devices capable of facilitating and optimizing this form of administration in an attempt to reduce side effects.
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Terapias Complementares/métodos , Dismenorreia/tratamento farmacológico , Preparações de Plantas/administração & dosagem , Administração Cutânea , Biotecnologia/métodos , Terapias Complementares/efeitos adversos , Dismenorreia/fisiopatologia , Feminino , Humanos , Patentes como Assunto , Preparações de Plantas/efeitos adversos , Plantas Medicinais/químicaRESUMO
There are increasing concerns regarding the risks arising from the contamination of manipulators of antineoplastic drugs promoted by occupational exposure or even in the dosage of drugs. The present work proposes the use of an electrochemical sensor based on a biopolymer extracted from the babassu coconut (Orbignya phalerata) for the determination of an antineoplastic 5-fluorouracil (5-FU) drug as an alternative for the monitoring of these drugs. In order to reduce the cost of this sensor, a flexible gold electrode (FEAu) is proposed. The surface modification of FEAu was performed with the deposition of a casting film of the biopolymer extracted from the babassu mesocarp (BM) and modified with phthalic anhydride (BMPA). The electrochemical activity of the modified electrode was characterized by cyclic voltammetry (CV), and its morphology was observed by atomic force microscopy (AFM). The FEAu/BMPA showed a high sensitivity (8.8 µA/µmol/L) and low limit of detection (0.34 µmol/L) for the 5-FU drug in an acid medium. Electrochemical sensors developed from the babassu mesocarp may be a viable alternative for the monitoring of the 5-FU antineoplastic in pharmaceutical formulations, because in addition to being sensitive to this drug, they are constructed of a natural polymer, renewable, and abundant in nature. Graphical abstract á .
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Antimetabólitos Antineoplásicos/análise , Cocos/química , Técnicas Eletroquímicas/instrumentação , Eletrodos , Fluoruracila/análise , Ouro/química , Custos e Análise de Custo , Monitoramento de Medicamentos/instrumentação , Eletrodos/economia , Limite de Detecção , Microscopia de Força Atômica , Oxirredução , Anidridos Ftálicos/química , SolubilidadeRESUMO
OBJECTIVE: To develop an analytical method to simultaneous quantification of benznidazole (BNZ) and posaconazole (POS) by high-performance liquid chromatography with diode-array detection (HPLC-DAD) using design of experiments. METHODS: Percentages of organic phase, buffer pH and flow rates of mobile phase were selected as independent variables by full factorial design (33), totaling 27 experiments. Significant factors were evaluated using factorial analysis of variance with 95% confidence level. Method optimization was performed using desirability profiles, considering BNZ/POS chromatographic resolution and peak areas. Further, the method was evaluated regarding its suitability and properly validated according to the international compendiums using the parameters: specificity, linearity, accuracy, precision, limit of detection and limit of quantification. RESULTS: The optimized method was achieved using Discovery® C8 column (250 mm × 4.6 mm; 5 µm particle size), methanol/acetate buffer (pH 3.5)(71:29) and detection at 260 nm. Retention times were 3.6 and 7.6 min for BNZ and POS, respectively, with good suitability of system and it was specific and linear (r2 >0.99) for both drugs, proving the efficiency of the method even in the presence of degradation products of POS. CONCLUSION: This new method is a great alternative to perform reliable, faster and cheaper analysis since the simultaneous quantification of the association BZN/POS is not reported yet in the literature.
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BACKGROUND: Interleukin-6 (IL-6) is a multifunctional cytokine that plays a crucial role not only in the immune system but also in numerous biological processes. Elevated IL-6 levels have been observed in many types of cancer and inflammatory diseases. Among the techniques that have been used to quantify IL-6, a Lateral Flow Assay (LFA) is one of the most promising. OBJECTIVE: The objective of this study was to perform a technological and scientific exploration of the development of an LFA for IL-6. METHOD: The Instituto Nacional de Propriedade Industrial-INPI (Brazil), European Patent Office - Espacenet, and United States Patent and Trademark Office-USPTO were used for the technological prospection to consider all the patents regarding an LFA for IL-6 detection. For the scientific investigation, the following periodic databases were used: Web of Science, Science Direct, PubMed, and Scielo, and were monitored from 2007 to May 2017. RESULTS: We found no patents based on the searched keywords, and a limited number of scientific articles were found. Therefore, the development of an LFA sensor for the detection of IL-6 appears to be innovative with significant biotechnological importance, creating a technology transfer to promote economic and industrial growth. CONCLUSION: The development of lateral flow immunosensors for IL-6 is innovative, as we could not find patents describing such a biosensor. Scientific prospection reported two lateral flow immunosensors. However, the test for IL-6 cannot be completed without using some kind of equipment for detection, such as the one we propose in future developments.
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Técnicas Biossensoriais/métodos , Biotecnologia/estatística & dados numéricos , Imunoensaio/métodos , Interleucina-6/análise , Técnicas Biossensoriais/instrumentação , Bases de Dados Factuais , Humanos , Patentes como Assunto , Inquéritos e QuestionáriosRESUMO
INTRODUCTION: Diabetes Mellitus has been considered an epidemic by the World Health Organization, with a high risk of morbidity and mortality. The treatment of this pathology consists in glycemic control, which can be done by oral hypoglycemic agents, insulin therapy, dietary guidance, regular physical activity, and psychosocial support. In addition, other adjuvant treatments are employed, such as phytotherapic, and one of the most used plants is Bauhinia forficata. AREAS COVERED: In the current review, patents using Bauhinia forficata for the Diabetes Mellitus treatment have been analyzed. There were 03 patents in WIPO, 01 in Espacenet, 01 in USPTO, and 02 in INPI. EXPERT OPINION: Patents on the adjuvant treatment of Diabetes Mellitus by Bauhinia forficata are discussed. Although there are some phytotherapy products containing this medicinal plant which has hypoglycemic effect here is still a need for the development of more products based on natural resources, for the treatment of this pathology, without side effects and with other benefits, to assist in the glycemia control in diabetic patients, and to improve their quality of life.
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Bauhinia/química , Diabetes Mellitus/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Glicemia/efeitos dos fármacos , Diabetes Mellitus/fisiopatologia , Desenho de Fármacos , Humanos , Hipoglicemiantes/efeitos adversos , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Patentes como Assunto , Fitoterapia/métodos , Extratos Vegetais/efeitos adversosRESUMO
BACKGROUND: Research on natural bioactive compounds has increased exponentially over the last decades. The discovery of new phytochemicals that possess pharmaceutical properties is useful in the development of therapeutic alternatives. The nerolidol (3,7,11-trimetil-1,6,10-dodecatrien-3-ol or 3,7,11-trimetildodeca-1,6,10-trien-3-ol) has been extensively studied for its therapeutic potential because of its pharmacological activities in the treatment of neurodegenerative diseases. METHOD: All articles and patents regarding nerolidol and its pharmacological properties were revised, focusing mainly on the important properties in the treatment of neurodegenerative diseases. A thorough search in article databases (Science Direct, MEDLINE/PubMed, Scopus and Scielo) and patent database (WIPO, EPO, ESPTO, LATIPAT and INPI) was performed over the course of this study. RESULTS: Several studies stood out for their relevance regarding the treatment of neurodegenerative diseases. Nerolidol demonstrated anticholinesterasic, antioxidant, antinociceptive, anti-inflammatory and anxiolytic activities, thus classifying it as a promising phytochemical for the development of therapeutic drugs. CONCLUSION: Analysis suggested that nerolidol is a promising target for new drugs and treatment of neurodegenerative diseases.