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The difficulty in swallowing is a frequent problem when oral solid dosage forms (conventional tablets or capsules) are administered to paediatric population or patients with dysphagia. An interesting alternative to overcome these problems are non-conventional formulations like chewable gels, commonly known as 'gummies'. Therefore, this work addresses the design, development and characterization of gummies using gelatine and pectin, for the vehiculization of the antiarrhythmic amiodarone (AMIO). Applying a Design of Experiments (DoE) approach, four gelatine (GG1-GG4) and eight pectin formulations (PG1-PG8) were developed. Considering the obtained results for responses during DoE evaluation (i.e., volume, syneresis, hardness, and gumminess), GG3 and PG8 were selected for complete characterization. Water activity, pH, drug content, texture parameters (adhesiveness, springiness, cohesiveness, and fracturability), disintegration time, in vitro dissolution, and microbiological features were evaluated. The obtained results were within the expected values for this type of formulation. The dissolution profiles showed a 94 % - 99 % of the AMIO content released for GG3 and PG8, respectively, so they could be considered suitable as immediate release dosage forms. In conclusion, the chewable gels were successfully developed and characterised, suggesting a potential means to accomplish a final prototype for the improvement of congenital cardiopathies treatment.
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Amiodarona , Antiarrítmicos , Géis , Cardiopatias Congênitas , Pectinas , Amiodarona/administração & dosagem , Amiodarona/química , Humanos , Pectinas/química , Antiarrítmicos/administração & dosagem , Antiarrítmicos/química , Cardiopatias Congênitas/tratamento farmacológico , Gelatina/química , Animais , Criança , Administração Oral , Liberação Controlada de Fármacos , Composição de Medicamentos/métodos , Solubilidade , Química Farmacêutica/métodosRESUMO
Chagas disease (CD) is a worldwide public health problem. Benznidazole (BZ) is the drug used to treat it. However, in its commercial formulation, it has significant side effects and is less effective in the chronic phase of the infection. The development of particulate systems containing BZ is therefore being promoted. The objective of this investigation was to develop polymeric nanoparticles loaded with BZ and examine their trypanocidal impact in vitro. Two formulas (BNP1 and BNP2) were produced through double emulsification and freeze drying. Subsequent to physicochemical and morphological assessment, both formulations exhibited adequate yield, average particle diameter, and zeta potential for oral administration. Cell viability was assessed in H9C2 and RAW 264.7 cells in vitro, revealing no cytotoxicity in cardiomyocytes or detrimental effects in macrophages at specific concentrations. BNP1 and BNP2 enhanced the effect of BZ within 48 h using a treatment of 3.90 µg/mL. The formulations notably improved NO reduction, particularly BNP2. The findings imply that the compositions are suitable for preclinical research, underscoring their potential as substitutes for treating CD. This study aids the quest for new BZ formulations, which are essential in light of the disregard for the treatment of CD and the unfavorable effects associated with its commercial product.
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The significance of accurate determination of ethanol content in hydrogel formulations was accentuated during COVID-19 pandemic coinciding with the heightened demand for sanitizing agents. The present article proposes three robust methodologies for this purpose: Fourier Transform Infrared Spectroscopy (FTIR), Raman spectroscopy, and Densitometry with matrix effect correction by Near-Infrared Spectroscopy (NIR). All three methods demonstrated outstanding linearity (R2 ≥ 0.99) and minimal errors (< 1.7%), offering simplicity and operational efficiency. FTIR and Raman, being non-destructive and requiring minimal preparation, enable practical on-site analysis capabilities, underscoring the potential of the spectroscopic methods to expedite health investigations and inspections, empowering on-site ethanol determination, and relieving the burden on official laboratories. Additionally, the densitometry with NIR-based approach showcased superior accuracy and precision compared to spectroscopic methods, meeting validation criteria while offering operational advantages over the costly official distillation-based method. Therefore, it stands as a reliable and reproducible technique for comprehensive health and criminal compliance assessments, making it a compelling alternative for both industry and official laboratories.
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Etanol , Hidrogéis , Análise Espectral Raman , Hidrogéis/química , Etanol/química , Etanol/análise , Análise Espectral Raman/métodos , Humanos , Espectroscopia de Infravermelho com Transformada de Fourier , COVID-19 , Espectroscopia de Luz Próxima ao Infravermelho/métodosRESUMO
INTRODUCTION: Benznidazole, the drug of choice for treating Chagas Disease (CD), has significant limitations, such as poor cure efficacy, mainly in the chronic phase of CD, association with side effects, and parasite resistance. Understanding parasite resistance to benznidazole is crucial for developing new drugs to treat CD. AREAS COVERED: Here, the authors review the current understanding of the molecular basis of benznidazole resistance. Furthermore, they discuss the state-of-the-art methods and critical outcomes employed to evaluate the efficacy of potential drugs against T. cruzi, aiming to select better compounds likely to succeed in the clinic. Finally, the authors describe the different strategies employed to overcome resistance to benznidazole and find effective new treatments for CD. EXPERT OPINION: Resistance to benznidazole is a complex phenomenon that occurs naturally among T. cruzi strains. The combination of compounds that inhibit different metabolic pathways of the parasite is an important strategy for developing a new chemotherapeutic protocol.
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Doença de Chagas , Descoberta de Drogas , Resistência a Medicamentos , Nitroimidazóis , Tripanossomicidas , Trypanosoma cruzi , Trypanosoma cruzi/efeitos dos fármacos , Nitroimidazóis/farmacologia , Doença de Chagas/tratamento farmacológico , Doença de Chagas/parasitologia , Tripanossomicidas/farmacologia , Humanos , Animais , Descoberta de Drogas/métodos , Desenvolvimento de MedicamentosRESUMO
Both intrinsic and extrinsic aging lead to a series of morphological changes in the skin including the flattening of the dermal-epidermal junction, increased stratum corneum dryness, reduction in sebaceous gland activity and enzyme activity as well as atrophy of blood vessels. In this study, the impact of these changes on the transport of molecules through the skin was revised. The increase in the number of transdermal formulations on the market in recent decades and life expectancy represent the main reasons for an in-depth discussion of this topic. Furthermore, elderly subjects have often been excluded from clinical trials due to polypharmacy, raising concerns in terms of efficacy and safety. In this way, ex vivo and in vivo studies comparing the transport of molecules through the mature and young skin were analyzed in detail. The reduced water content in mature skin had a significant impact on the transport rate of hydrophilic molecules. The lower enzymatic activity in aged skin, in turn, would explain changes in the activation of prodrugs. Interestingly, greater deposition of nanoparticles was also found in mature skin. In vivo models should be prioritized in future experimental studies as they allow to evaluate both absorption and metabolism simultaneously, providing more realistic information.
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Administração Cutânea , Envelhecimento , Absorção Cutânea , Pele , Humanos , Pele/metabolismo , Envelhecimento/metabolismo , Animais , Transporte Biológico , Nanopartículas/metabolismo , Nanopartículas/química , Envelhecimento da Pele , Preparações Farmacêuticas/metabolismo , Preparações Farmacêuticas/administração & dosagem , Pró-Fármacos/farmacocinética , Pró-Fármacos/metabolismoRESUMO
The TRPV1 receptor, which is known to contribute significantly to pain perception, has recently been identified as a useful tool for predicting eye stinging potential in cosmetics. In this study, HEK-293 cells with high TRPV1 expression were utilized to evaluate calcium influx related to receptor activation triggered by chemicals and cosmetic formulations. The cells were exposed to increasing concentrations of substances to cause or not some aggression to the eye, and TRPV1 activity was assessed by measuring intracellular FURA-2 AM fluorescence signal. To confirm TRPV1 channel activation, capsazepine, a capsaicin antagonist, was employed in addition to using capsaicin as a positive control. The study's results indicate that this novel model can identify compounds known to cause some aggression to the eye, such as stinging, considering a cut-off value of 60% of Ca2+ influx exposed to the lowest evaluated concentration (0.00032%). When applied to the cosmetic baby formulation, although the presented model exhibited higher sensitivity by classifying as stinging formulations that had previously undergone clinical testing and were deemed non-stinging, the assay could serve as a valuable in vitro tool for predicting human eye stinging sensation and can be used as a tier 1 in an integrated testing strategy.
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Cálcio , Cosméticos , Canais de Cátion TRPV , Humanos , Cosméticos/toxicidade , Células HEK293 , Canais de Cátion TRPV/metabolismo , Cálcio/metabolismo , Olho/efeitos dos fármacos , Capsaicina/análogos & derivados , Capsaicina/farmacologia , Alternativas aos Testes com AnimaisRESUMO
This work aimed to study and characterize a product based on vegetable extract of quinoa (WVEQ) fermented with water kefir grains. The effect of sucrose concentration (SC), inulin concentration (IC), and xanthan gum (XG) concentration were evaluated using a central composite design (CCD) 23. They were subsequently characterized regarding cellular growth of the grains, beverage yield, pH, soluble solids, carbon dioxide (CO2) production, lactic acid, and ethanol production. Therefore, for the final stage, two formulations (F1 and F8) of the CCD were chosen to be characterized in terms of proximate composition, microbiological composition of the kefir culture, analysis of organic compounds, sensory analysis, and enzymatic and microbiological characterization before and after simulation of in vitro gastrointestinal digestion. In the two chosen products, one can see that fermentation optimized the bioavailability of proteins due to the high proteolytic activity of the microorganisms in kefir and the increase in lipid content. In identifying microorganisms, there was a prevalence of Saccharomyces sp. yeasts. In the sensory analysis, the F8 formulation showed better results than the F1 formulation. In vitro, gastrointestinal digestion showed reduced lactic acid bacteria and yeast and increased acetic acid bacteria in the liquid phase for both formulations. In the enzymatic profile, there was a reduction in all enzymes analyzed for both formulations, except for amylase in F1, which went from 14.05 U/mL to 39.41 U/mL. Therefore, it is concluded that using WVEQ as a substrate for the product appears to be a viable alternative with nutritional and technological advantages for serving a specific market niche.
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Chenopodium quinoa , Kefir , Lactobacillales , Kefir/análise , Kefir/microbiologia , Verduras , Leveduras , Extratos Vegetais , FermentaçãoRESUMO
Among all the neglected diseases, schistosomiasis is considered the second most important parasitic infection after malaria. Praziquantel is the most widely used drug for this disease, but its exclusive use may result in the development of drug-resistant schistosomiasis. To increase the control of the disease, new drugs have been developed as alternative treatments, among them 2-(-5-bromo-1-h-indole-3-yl-methylene)-N-(naphthalene-1-ylhydrazine-carbothiamide (LQIT/LT-50), which showed promising schistosomicidal activity in nonclinical studies. However, LQIT/LT-50 presents low solubility in water, resulting in reduced bioavailability. To overcome this solubility problem, the present study aimed to develop LQIT/LT-50 solid dispersions for the treatment of schistosomiasis. Solid dispersions were prepared through the solvent method using Soluplus©, polyethylene glycol (PEG) or polyvinylpyrrolidone (PVP K-30) as hydrophilic carriers. The formulations with the best results in the compatibility tests, aqueous solubility and preliminary stability studies have undergone solubility tests and physicochemical characterizations by Fourier-transform infrared spectroscopy (FTIR), x-ray diffractometry (XRD), exploratory differential calorimetry (DSC), thermogravimetry (TG) and Raman spectroscopy. Finally, the schistosomicidal activity was evaluated in vitro. The phycochemical analyzes showed that when using PVP K-30, there was an interaction between the PVP K-30 and LQIT/LT-50, proving the successful development of the solid dispersion. Furthermore, an increase in the solubility of the new system was observed (LQIT/LT-50:PVP K-30) in addition to the improvement in the in vitro shistosomidal activity at 1:4 (w/w) molar ratio (i.e., 20% drug loading) when compared to LQIT/LT-50 alone. The development of the LQIT/LT-50:PVP K-30 1:4 solid dispersion is encouraging for the future development of new pharmaceutical solid formulations, aiming the schistosomicidal treatment.
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Esquistossomose , Esquistossomicidas , Humanos , Esquistossomicidas/farmacologia , Química Farmacêutica/métodos , Povidona/química , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Naftalenos , Água , Indóis/farmacologia , Difração de Raios X , Portadores de Fármacos/químicaRESUMO
This study aimed to incorporate nanocapsules containing 3,3'-diindolylmethane (DIM) with antitumor activity into a bilayer film of karaya and gellan gums for use in topical melanoma therapy. Nanocarriers and films were prepared by interfacial deposition of the preformed polymer and solvent casting methods, respectively. Incorporating DIM into nanocapsules increased its antitumor potential against human melanoma cells (A-375) (IC50 > 24.00 µg/mL free DIM × 2.89 µg/mL nanocapsules). The films were transparent, hydrophilic (θ < 90°), had homogeneous thickness and weight, and had a DIM content of 106 µg/cm2. Radical ABTS+ scavenger assay showed that the DIM films presented promising antioxidant action. Remarkably, the films showed selective bioadhesive potential on the karaya gum side. Considering the mechanical analyses, the nanotechnology-based films presented appropriate behavior for cutaneous application and controlled DIM release profile, which could increase the residence time on the application site. Furthermore, the nanofilms were found to increase the permeation of DIM into the epidermis, where melanoma develops. Lastly, the films were non-hemolytic (hemolysis test) and non-irritant (HET-CAM assay). In summary, the combination of karaya and gellan gum in bilayer films that contain nanoencapsulated DIM has demonstrated potential in the topical treatment of melanoma and could serve as a viable option for administering DIM for cutaneous melanoma therapy.
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Since the inception of the transcranial magnetic stimulation (TMS) technique, it has become imperative to numerically compute the distribution of the electric field induced in the brain. Various models of the coil-brain system have been proposed for this purpose. These models yield a set of formulations and boundary conditions that can be employed to calculate the induced electric field. However, the literature on TMS simulation presents several of these formulations, leading to potential confusion regarding the interpretation and contribution of each source of electric field. The present study undertakes an extensive compilation of widely utilized formulations, boundary value problems and numerical solutions employed in TMS fields simulations, analyzing the advantages and disadvantages associated with each used formulation and numerical method. Additionally, it explores the implementation strategies employed for their numerical computation. Furthermore, this work provides numerical expressions that can be utilized for the numerical computation of TMS fields using the finite difference and finite element methods. Notably, some of these expressions are deduced within the present study. Finally, an overview of some of the most significant results obtained from numerical computation of TMS fields is presented. The aim of this work is to serve as a guide for future research endeavors concerning the numerical simulation of TMS.
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Albendazole is a broad-spectrum anthelmintic drug used for parasitic infections. In addition, due to its mechanism of action, it has been studied as an anticancer agent. However, poor and highly variable bioavailability are limiting factors for its use in systemic illnesses. The present study aimed to develop two parenteral formulations of albendazole and to compare its pharmacokinetic profile with the conventional oral administration. Parenteral formulations were developed using two different approaches: a phosphonooxymethylated prodrug and cosolvents. For the albendazole prodrug, once synthetized, its solubility and hydrolysis with alkaline phosphatase were evaluated. A factorial design of experiments was used for the cosolvent formulation. Stability and hemolytic activity were assessed. A pharmacokinetic study was performed on New Zealand rabbits. Both formulations were administered intravenously, and the prodrug was also administered intramuscularly. Results were compared with those obtained after the oral administration of albendazole. A 20,000-fold and 6000-fold increase in albendazole solubility was found with the prodrug and cosolvent formulations, respectively. Both parenteral formulations displayed higher albendazole plasma concentrations for the first 2 h compared with oral administration, even when the oral dose was doubled. The absolute bioavailability of oral albendazole was 15.5% while for the intramuscular administration of the prodrug was 102.6%. Both parenteral formulations showed a significant decrease in the formation of albendazole sulfoxide (ANOVA p<0.05) and allowed greater exposure to albendazole. Albendazole cosolvent parenteral formulation could be a promising option in systemic illnesses considering its ease of preparation and superb pharmacokinetic performance.
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Anti-Helmínticos , Antineoplásicos , Pró-Fármacos , Animais , Coelhos , Albendazol , Pró-Fármacos/farmacocinética , Disponibilidade Biológica , Administração OralRESUMO
Herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) infect, respectively, 67% and 13% of the world population, most commonly causing mild symptoms, such as blisters/ulcers. However, severe conditions such as keratitis, encephalitis, and systemic infections may occur, generally associated with the patient's immunological condition. Although Acyclovir® (ACV) and its analogs are the reference drugs for herpetic infections, the number of ACV-resistant HSV infections is growing exponentially. Therefore, new natural products' bioactive compounds have been studied to develop novel effective anti-herpetics. Trichilia catigua is a plant widely used in traditional medicine, including the treatment of skin diseases and sexual infections. In our study, 16 extracts from the bark of T. catigua, obtained with different solvents and their combinations, were evaluated against HSV-1 AR and HSV-2, respectively, ACV resistance and genital strains in vitro. The extracts with the highest selectivity index were used to prepare new topical anti-herpetic formulations and confirmed in vivo. Two new topical formulations were suggested to treat cutaneous and genital herpetic recurrent lesions. The cytotoxicity and antiviral activity were tested using the MTT method. The cytotoxic (CC50) and inhibitory (IC50) concentrations of 50% and the selectivity index (SI: CC50/IC50) were determined. Tc12, Tc13, and Tc16 were added to the formulations. Infected BALB/c mice were treated for 8 days, and the severity of the herpetic lesions was analyzed daily. All CEs showed a CC50 value ranging from 143 to 400 µg/mL, except for Tc3 and Tc10. Tc12, Tc13, and Tc16 showed the best SI in the 0 h, virucidal, and adsorption inhibition assays. In the in vivo test against HSV-1 AR, the infected animals treated with creams were statistically different from the infected non-treated animals and similar to ACV-treated mice. In HSV-2-infected genitalia, similar effects were found for Tc13 and Tc16 gels. The present study demonstrated that extracts from the bark of T. catigua, traditionally used in folk medicine, are a valuable source of active compounds with anti-herpetic activity. The extracts showed a virucidal mechanism of action and prevented the initial stages of viral replication. The cutaneous and genital infections were strongly inhibited by the Tc12, Tc13, and Tc16 extracts. New topical therapeutic alternatives using Trichilia catigua extracts are suggested for patients infected with ACV-resistant strains of HSV.
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Herpes Simples , Herpesvirus Humano 1 , Meliaceae , Camundongos , Animais , Aciclovir/farmacologia , Aciclovir/uso terapêutico , Reinfecção , Antivirais/farmacologia , Antivirais/uso terapêutico , Herpes Simples/tratamento farmacológico , Herpesvirus Humano 2/fisiologia , GenitáliaRESUMO
Development of new medicinal products for particular therapeutic treatment or for better manipulations with better quality and less side effects are possible as a result of advanced inorganic and organic materials application, among which zeolites, due to their properties and versatility, have been gaining attention. This paper is an overview of the development in the use of zeolite materials and their composites and modifications as medicinal products for several purposes such as active agents, carriers, for topical treatments, oral formulations, anticancer, the composition of theragnostic systems, vaccines, parenteral dosage forms, tissue engineering, etc. The objective of this review is to explore the main properties of zeolites and associate them with their drug interaction, mainly addressing the advances and studies related to the use of zeolites for different types of treatments due to their zeolite characteristics such as molecule storage capacity, physical and chemical stability, cation exchange capacity, and possibility of functionalization. The use of computational tools to predict the drug-zeolite interaction is also explored. As conclusion was possible to realize the possibilities and versatility of zeolite applications as being able to act in several aspects of medicinal products.
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Nitrogen(N) is the most required nutrient in the cultivation of corn (Zea maysL.), also representing a significantshare in the production costs. The objective was to evaluate the efficiency for one experimental year of different sourcesof nitrogen fertilizers applied in topdressing on the corn grain yield and their respective fertilization costs. The experiment was carried out under field conditions and without irrigation under no-tillage system, in a Red Oxissol. For sowing, 280 kg ha-1of NPK fertilizer 12-30-20 was used for all treatments. In addition to the control treatment (NPK), four nitrogen formulations wereapplied in topdressing: Urea, Super N, Nitromag, and Sulfammo, both formulations applied 50% in the V3/V4 and 50% V7/V8 stages, in four replicates.Grain yield was determined at the physiological maturation. The type of nitrogen fertilizer did not influence corn grain yield, an average of 9016 kg ha-1. The largest profits were achieved with the application of Super N, Urea and Nitromag. Nitrogen fertilizers with slow and controlled N release does not promote an increase in corn grain yield in relation to Urea. The use of Super N in topdressing has the highest profitability in corn cultivation.(AU)
O nitrogênio (N) é o nutriente mais requerido no cultivo do milho (Zea maysL.), ainda representa significativa participação no custo de produção. O objetivo foi avaliar a eficiência em um ano experimental de diferentes fontes de fertilizantes nitrogenados aplicados em cobertura na produtividade de grãos demilho e os seus respectivos custos da adubação. O experimento foi realizado em condições de campo e sem irrigação sob sistema plantio direto, em Latossolovermelho. Na semeadura foi utilizado 280 kgha-1de adubo NPK 12-30-20 para todos os tratamentos. Além do tratamento testemunha (NPK), quatro formulações nitrogenadas foram aplicadas em cobertura: Ureia, Super N, Nitromag, e Sulfammo, ambas as formulaçõesaplicadas 50% no estádioV3/V4 e 50% V7/V8,em quatro repetições. Na maturação fisiológica foi determinada a produtividade de grãos.O tipo de fertilizante nitrogenado não influenciou na produtividade de grãos de milho, média de 9016 kg ha-1. Os maiores lucros foram com a aplicação de Super N, Ureia e Nitromag. O uso em cobertura de fertilizantes nitrogenados de lenta e controlada liberação de N não promovem aumento na produtividade de grãos de milho em relação a Ureia. O uso de Super N em cobertura apresenta a maior lucratividadeno cultivo do milho.(AU)
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Zea mays/fisiologia , Fertilizantes/análise , Análise Custo-Benefício/métodos , Nitrogênio/químicaRESUMO
BACKGROUND: A drug with poor water-solubility, like Dexamethasone acetate, can present lower bioavailability conventional for pharmaceutical formulations, and the presence of polymorphs in the raw material can lead to drug quality problems. OBJECTIVE: In this study, nanocrystals of dexamethasone acetate were synthesized by high pressure homogenizer (HPH) method in surfactant poloxamer 188 (P188) solid dispersion and the bioavailable in raw material with polymorphism presence was evaluated. METHODS: The powder pre-suspension was prepared by the HPH process, and the nanoparticles formed were incorporated in P188 solutions. The nanocrystals formed were characterized by techniques of XRD, SEM, FTIR, thermal analysis by differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA), dynamic light scattering (DLS) to analyze the particle size and zeta potential, and in vitro evaluation by dissolution studies. RESULTS: The characterization techniques were adequate to show the presence of raw material with physical moisture between two dexamethasone acetate polymorphs. The nanocrystals formed in the presence of the P188 in the formulation showed a considerable increase in the rate of dissolution of the drug in the medium and in the size of the stable nanocrystals, even in the presence of dexamethasone acetate polymorphs. CONCLUSION: The results showed that it was possible to produce dexamethasone nanocrystals by HPH process with regular size by the presence of the small amount of P188 surfactant. This article presents a novelty in the development of dexamethasone nanoparticles that have different polymorphic forms in their physical composition.
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Nanopartículas , Poloxâmero , Solubilidade , Poloxâmero/química , Dexametasona , Tensoativos , Nanopartículas/químicaRESUMO
Resumo O objetivo deste artigo é investigar as evidências nacionais e internacionais disponíveis sobre o descarte de medicamentos e os impactos em matrizes ambientais. Trata-se de uma revisão integrativa da literatura realizada nas bases de dados PubMed, SciELO e Biblioteca Virtual em Saúde (BVS) e que incluiu artigos em inglês, espanhol e português publicados entre 2010 e 2020. Foram selecionados 26 artigos, que evidenciaram o descarte incorreto de medicamentos por profissionais e consumidores devido, principalmente, à falta de conhecimentos sobre os impactos ambientais que esses podem ocasionar. Estudos apontaram a contaminação de água, esgoto e sedimentos por fármacos descartados de forma incorreta. Além disso, observou-se que seres vivos aquáticos podem ser impactados pela presença de medicamentos em matrizes ambientais. O descarte de medicamentos incorreto ainda é uma realidade nas evidências avaliadas, que promove a contaminação de matrizes ambientais e muitas vezes não é removido por estações de tratamento de águas residuárias e interfere no equilíbrio da vida ambiental.
Abstract The scope of this article is to investigate the national and international evidence available on the forms of drug disposal and the presence of drugs in environmental matrices. It involved an integrative review of the literature conducted in the PubMed, SciELO and Virtual Health Library (VHL) databases, which included articles in English, Spanish and Portuguese published between 2010 and 2020. Twenty-six articles were selected, which revealed the incorrect disposal of medicines by professionals and consumers due mainly to the lack of knowledge about the environmental impacts that they may cause. Studies have highlighted the contamination of water, sewage and sediments by incorrectly discarded drugs. Furthermore, it was observed that aquatic living creatures can be impacted by the presence of drugs in environmental matrices. The incorrect disposal of drugs continues to be a reality in the evidence assessed, which leads to the contamination of environmental matrices and is often not removed by wastewater treatment plants and interferes with the equilibrium of environmental life.
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The prophylactic and therapeutic overuse of antimicrobials on the farm has contributed to the emergence of hard-to-fight bacterial strains causing bovine mastitis. Aiming at alternative therapies, this study evaluated the antimicrobial activity of 20 essential oils against clinical Staphylococcus aureus strains. Of them, five with strong activities were selected and evaluated for their minimum inhibitory concentrations (MIC) in culture medium and milk, cytotoxicity against bovine mammary cells (MAC-T), antiadhesive properties, and interactions among themselves and with cefoperazone. The oils remained active on milk, were not cytotoxic, and some concentrations stimulated MAC-T cells growth, suggesting healing potential. Subinhibitory concentrations of Coriandrum sativum, Origanum vulgare, Syzygium aromaticum, and Thymus vulgaris reduced biofilm formation by at least 80%. Several oil and cefoperazone combinations displayed additive interaction, with O. vulgare and C. sativum showing the most promising results. We developed formulations for being used as prophylactic postdipping solutions in the field, containing different concentrations (1% or 3%) of the active oils, alone or in combination, with 3% glycerin, 1% Tween 80, and water. The formulations showed strong antimicrobial activity in milk and enhanced antiadhesive properties, specially when two oils were combined in the formula, indicating promising biotechnological and therapeutical applications.
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Anti-Infecciosos , Mastite Bovina , Óleos Voláteis , Infecções Estafilocócicas , Feminino , Bovinos , Animais , Humanos , Óleos Voláteis/farmacologia , Staphylococcus aureus , Cefoperazona/uso terapêutico , Infecções Estafilocócicas/tratamento farmacológico , Infecções Estafilocócicas/veterinária , Infecções Estafilocócicas/microbiologia , Anti-Infecciosos/farmacologia , Plantas , Condimentos , Medicina Tradicional , Mastite Bovina/tratamento farmacológico , Mastite Bovina/microbiologia , Testes de Sensibilidade Microbiana , Antibacterianos/farmacologia , Antibacterianos/uso terapêuticoRESUMO
Public health, production and preservation of food, development of environmentally friendly (cosmeto-)textiles and plastics, synthesis processes using green technology, and improvement of water quality, among other domains, can be controlled with the help of chitosan. It has been demonstrated that this biopolymer exhibits advantageous properties, such as biocompatibility, biodegradability, antimicrobial effect, mucoadhesive properties, film-forming capacity, elicitor of plant defenses, coagulant-flocculant ability, synergistic effect and adjuvant along with other substances and materials. In part, its versatility is attributed to the presence of ionizable and reactive primary amino groups that provide strong chemical interactions with small inorganic and organic substances, macromolecules, ions, and cell membranes/walls. Hence, chitosan has been used either to create new materials or to modify the properties of conventional materials applied on an industrial scale. Considering the relevance of strategic topics around the world, this review integrates recent studies and key background information constructed by different researchers designing chitosan-based materials with potential applications in the aforementioned concerns.
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OBJECTIVE: Coffee is one of the most consumed beverages worldwide, and its production and consumption generate large amounts of by-products annually. Coffee by-products and coffee beans are rich in bioactive compounds of great commercial value, including potential applications as active ingredients in skin care products and cosmetic formulations. In addition, there has been growing interest in the use of natural ingredients for cosmetic purposes. Considering the importance of coffee in the world economy, its chemical constituents with potential for cosmetic and dermatological application, and the importance of patents for innovation and technological development, the present study aimed to review recent patents involving coffee and coffee by-product use in cosmetics. METHODS: This review was carried out using Espacenet. The following inclusion criteria were established: patents that included the terms "coffee" and "skin" in the title, abstract and claims and belonged to the classification A61Q, which is related to the "specific use of cosmetics or similar toilet preparations" considering the International Patent Classification (IPC) or Cooperative Patent Classification (CPC). RESULTS: Considering the 52 patents analysed, the bean was the main way to obtain extracts (39), followed by green beans (7), silverskin (3), peel and pulp (1), pulp (1) and beans and leaves (1). The formulations are mainly intended for use in nonspecific areas of skin (29), eye areas (12), scalp hair (9) and lip skin (2) with claims of anti-ageing, moisturizers, sun protection, hair growth, anti-dandruff, etc. CONCLUSION: Coffee and its residues have high amounts of phenolic compounds, caffeine, fatty acids and other substances known to have important biological properties for the skin. Coffee and its by-products are promising ingredients to be incorporated into topical formulations, ensuring skin health benefits and reducing the environmental impact.
OBJECTIF: Le café est l'une des boissons les plus consommées dans le monde, et sa production et sa consommation génèrent chaque année de grandes quantités de sous-produits. Les sous-produits du café et les grains de café sont riches en composés bioactifs d'une grande valeur commerciale, y compris des applications potentielles en tant qu'ingrédients actifs dans les produits de soins de la peau et les formulations cosmétiques. De plus, il y a eu un intérêt croissant pour l'utilisation d'ingrédients naturels à des fins cosmétiques. Compte tenu de l'importance du café dans l'économie mondiale, de ses constituants chimiques ayant un potentiel d'application cosmétique et dermatologique, et de l'importance des brevets pour l'innovation et le développement technologique, la présente étude visait à examiner les brevets récents concernant l'utilisation du café et des sous-produits du café dans les cosmétiques. MÉTHODES: Cette revue a été réalisée à l'aide d'Espacenet. Les critères d'inclusion suivants ont été établis: les brevets qui incluaient les termes "café" et "peau" dans le titre, l'abrégé et les revendications et appartenaient à la classification A61Q, qui est liée à "l'utilisation spécifique de cosmétiques ou de préparations de toilette similaires" compte tenu de la Classification internationale des brevets ou Classification coopérative des brevets. RÉSULTATS: Considérant les 52 brevets analysés, le grain était le principal moyen d'obtenir des extraits (39), suivi du grain vert (7), du silverskin (3), de la peau et de la pulpe (1), de la pulpe (1) et des grains et des feuilles (1). Les formulations sont principalement destinées à être utilisées dans des zones non spécifiques de la peau (29), des yeux (12), des cheveux du cuir chevelu (9) et de la peau des lèvres (2) avec des revendications anti-âge, hydratantes, protection solaire, croissance des cheveux, antipelliculaire, etc. CONCLUSION: Le café et ses résidus contiennent de grandes quantités de composés phénoliques, de caféine, d'acides gras et d'autres substances connues pour avoir des propriétés biologiques importantes pour la peau. Le café et ses sous-produits sont des ingrédients prometteurs à incorporer dans des formulations topiques, garantissant des bienfaits pour la santé de la peau et réduisant l'impact environnemental.
Assuntos
Café , Cosméticos , Cosméticos/química , Café/química , Patentes como AssuntoRESUMO
Vulvovaginal candidiasis (VVC) is an opportunistic and endogenous infection caused by a fungus of the Candida genus, which can cause pruritus, dysuria, vulvar edema, fissures and maceration of the vulva. The treatment of vaginal candidiasis is carried out mainly by antifungal agents of azole and polyene classes; however, fungal resistance cases have been often observed. For this reason, new therapeutic agents such as essential oils, probiotics and antimicrobial peptides are being investigated, which can be combined with conventional drugs. Local administration of antimicrobials has also been considered to allow greater control of drug delivery and reduce or avoid undesirable systemic adverse effects. Conventional dosage forms such as creams and ointments result in reduced residence time in the mucosa and non-sustained and variable drug delivery. Therefore, advanced solid formulations such as intravaginal rings, vaginal films, sponges and nanofibers have been purposed. In these systems, polymers in different ratios are combined aiming to achieve a specific drug release profile and high mucoadhesion. Overall, a more porous matrix structure leads to a higher rate of drug release and mucoadhesion. The advantages, limitations and technological aspects of each dosage form are discussed in detail in this review.