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This study aimed to develop microemulsions (MEs) containing α-bisabolol for the topical treatment of cutaneous leishmaniasis (CL). Initially, pseudoternary phase diagrams were developed using α-bisabolol as the oil phase, Eumulgin® CO 40 as the surfactant, Polymol® HE as the co-surfactant, and distilled water as the aqueous phase. Two transparent liquid systems (TLS) containing 5% of α-bisabolol were selected and characterized (F5E25 and F5EP25). Next, skin permeation and retention assays were performed using Franz cells. The interaction of the formulation with the stratum corneum (SC) was evaluated using the FTIR technique. The cytotoxicity was evaluated in murine peritoneal macrophages. Finally, the antileishmanial activity of microemulsions was determined in promastigotes and amastigotes of L. amazonensis (strain MHOM/BR/77/LTB 0016). As a result, the selected formulations showed isotropy, nanometric size (below 25 nm), Newtonian behavior and pH ranging from 6.5 to 6.9. The MEs achieved a 2.5-fold increase in the flux and skin-permeated amount of α-bisabolol. ATR-FTIR results showed that microemulsions promoted fluidization and extraction of lipids and proteins of the stratum corneum, increasing the diffusion coefficient and partition coefficient of the drug in the skin. Additionally, F5E25 and F5EP25 showed higher activity against promastigotes (IC50 13.27 and 18.29, respectively) compared to unencapsulated α-bisabolol (IC50 53.8). Furthermore, F5E25 and F5EP25 also showed antileishmanial activity against intracellular amastigotes of L. amazonensis, with IC50 50 times lower than free α-bisabolol and high selectivity index (up to 15). Therefore, the systems obtained are favorable to topical administration, with significant antileishmanial activity against L. amazonensis promastigotes and amastigotes, being a promising system for future in vivo trials.
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Emulsões , Macrófagos Peritoneais , Sesquiterpenos Monocíclicos , Sesquiterpenos , Pele , Animais , Sesquiterpenos Monocíclicos/farmacologia , Sesquiterpenos Monocíclicos/química , Emulsões/química , Camundongos , Sesquiterpenos/farmacologia , Sesquiterpenos/química , Pele/parasitologia , Macrófagos Peritoneais/efeitos dos fármacos , Macrófagos Peritoneais/parasitologia , Leishmaniose Cutânea/tratamento farmacológico , Leishmaniose Cutânea/parasitologia , Espectroscopia de Infravermelho com Transformada de Fourier , Absorção Cutânea/efeitos dos fármacos , Camundongos Endogâmicos BALB C , Feminino , Leishmania/efeitos dos fármacos , Tensoativos/farmacologia , Tensoativos/química , Antiprotozoários/farmacologia , Antiprotozoários/químicaRESUMO
D-limonene, derived from citrus essential oils, holds significant therapeutic potential but faces challenges due to its high volatility, especially in pharmaceutical formulations. This study investigates microemulsions as a promising delivery system for volatile compounds, emphasizing their thermal protection for D-limonene. The formulation development was guided by a pseudo-ternary phase diagram and involved assays with different surfactants. Microemulsions were achieved solely with Labrasol® (Gattefossé Brasil, São Paulo, Brazil), encompassing concentrations of 7.1% to 30.8% D-limonene, 28.6% to 57.1% Labrasol®, and 20.0% to 64.3% water. All formulations were homogeneous, transparent, and presented low viscosity, with adequate D-limonene content, indicating that the production is feasible at room temperature. While the formulations demonstrated robust physical stability under mechanical stress, they exhibited destabilization at temperatures exceeding 50 °C. In terms of oxidative stability, pure D-limonene exhibited an induction period of 4.88 min, whereas microemulsions extended this period by four to eight times. Notably, the induction period of the microemulsions remained practically unchanged pre and post-heating (70 °C), suggesting the formulation's ability to enhance the D-limonene thermal stability. This highlights the value of oxidative stability analysis as a quicker tool than conventional oxidative tests, while affirming microemulsions as a viable encapsulation strategy for D-limonene protection against elevated temperatures.
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Microemulsions are important for soil and sediment remediation technology. The characteristics of the surfactants that make up these microemulsions include low sorption into soil or sediments, low surface and interfacial tension, the ability to penetrate tiny pores, and good solubilization of contaminants. This review revealed that microemulsions formulated with nonionic and anionic surfactants have higher recovery efficiencies for hydrophobic contaminants than cationic ones, as evidenced by the surveyed studies reporting effective remediation of soils and sediments using on microemulsions. These microemulsified systems have been found to remove petroleum and its derivatives from soil or sediments at percentages ranging from 40 to 100%. As such, this review can aid with the choice of surfactants used in microemulsions for remediation, such as those with plant-based components, which are promising solutions for the remediation of contaminated soils due to their contaminant extraction efficiency and biodegradability.
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Petróleo , Poluentes do Solo , Tensoativos/química , Solo , Poluentes do Solo/análise , Poluição AmbientalRESUMO
Nifedipine is a potent anti-hypertensive, which is poorly orally bioavailable on account of first-pass metabolism, short half-life, and low water solubility. This study aimed to develop a microemulsified system with low surfactant concentration and to evaluate the influence of microemulsion (ME) phase behavior on skin permeation of nifedipine, as drug model. Thereafter, MEs were obtained using PPG-5-CETETH-20, oleic acid, and phosphate buffer at pH 5.0. The selected MEs were isotropic, with droplet diameters less than 10 nm, polydispersity index < 0.25, and pH between 5.0 and 5.2. MEs presented low viscosity and Newtonian behavior. SAXS results confirmed bicontinuous and oil-in-water (o/w) MEs formation. The presence of the drug promoted only very slight modifications in the ME structure. The MEs presented ability to deliver nifedipine via the transdermal route when in comparison with the control. Nevertheless, the skin permeated and retained amounts from the o/w and bicontinuous formulations did not differ significantly. The ATR-FTIR demonstrated that both formulations promoted fluidization and disorganization of lipids and increased the drug diffusion and partition coefficients in the skin. In conclusion, PPG-5-CETETH-20 MEs obtained proved to be effective skin permeation enhancers, acting by rising the coefficients of partition and diffusion of the nifedipine in the skin.
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Nifedipino , Pele , Administração Cutânea , Emulsões/química , Nifedipino/metabolismo , Espalhamento a Baixo Ângulo , Pele/metabolismo , Tensoativos/química , Água/química , Difração de Raios XRESUMO
Lecithins are a phospholipid-rich mixture recovered from the degumming process of crude vegetable oils. Since the nineteenth century, this by-product of oil processing has been used as a food and pharmaceutical ingredient. Lecithins' popularity as an ingredient in the pharmaceutical and food industries arises from their particular properties, such as their hydrophilic-lipophilic balance, critical micellar concentration, and assembly properties. However, there is limited knowledge of the use of lecithins to formulate pharmaceutical- and food-grade microemulsions. Unlike conventional emulsions, microemulsions are thermodynamically stable systems that offer long-term stability. Besides, microemulsions show nano-sized droplets, transparency, ease of preparation and scale-up, and do not require expensive equipment. This review aims to provide a comprehensive overview of lecithins, their properties, and their use in formulating microemulsions, a promising method to incorporate, protect, and deliver bioactive compounds in pharmaceutical and food products. PRACTICAL APPLICATIONS: Lecithins are a phospholipid-rich mixture recovered from the degumming process of crude vegetable oils. Since the nineteenth century, this by-product of oil processing has been used as a food ingredient. Lecithin phospholipids are commonly used as emulsifier agents in the food and pharmaceutical industries because of their particular properties. However, there is limited knowledge of the use of lecithins to formulate pharmaceutical- or food-grade microemulsions. Unlike conventional emulsions, microemulsions are stable systems that offer long-term stability, nano-sized droplets, transparency, ease of preparation and scale-up, and do not require expensive equipment. This review aims to provide a comprehensive overview of lecithins, their properties, and their use in formulating microemulsions, a promising method to incorporate, protect, and deliver bioactive compounds such as vitamins, flavors, antioxidants, nutrients, colors, antimicrobials, and polyphenols.
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Lecitinas , Óleos de Plantas , Emulsões , Tamanho da Partícula , FosfolipídeosRESUMO
The impetus for the expanding interest in ionic liquids (ILs) is their favorable properties and important applications. Ionic liquid-based surfactants (ILBSs) carry long-chain hydrophobic tails. Two or more molecules of ILBSs can be joined by covalent bonds leading, e.g., to gemini compounds (GILBSs). This review article focuses on aspects of the chemistry and applications of ILBSs and GILBSs, especially in the last ten years. Data on their adsorption at the interface and micelle formation are relevant for the applications of these surfactants. Therefore, we collected data for 152 ILBSs and 11 biamphiphilic compounds. The head ions of ILBSs are usually heterocyclic (imidazolium, pyridinium, pyrrolidinium, etc.). Most of these head-ions are also present in the reported 53 GILBSs. Where possible, we correlate the adsorption/micellar properties of the surfactants with their molecular structures, in particular, the number of carbon atoms present in the hydrocarbon "tail". The use of ILBSs as templates for the fabrication of mesoporous nanoparticles enables better control of particle porosity and size, hence increasing their usefulness. ILs and ILBSs form thermodynamically stable water/oil and oil/water microemulsions. These were employed as templates for (radical) polymerization reactions, where the monomer is the "oil" component. The formed polymer nanoparticles can be further stabilized against aggregation by using a functionalized ILBS that is co-polymerized with the monomers. In addition to updating the literature on the subject, we hope that this review highlights the versatility and hence the potential applications of these classes of surfactants in several fields, including synthesis, catalysis, polymers, decontamination, and drug delivery.
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Poorly soluble active pharmaceutical ingredients (APIs) create major problems in drug dosage form formulation resulting in significant delays in drug pharmaceutical screening, impairing the drug dosage form production. Aiming to minimize the use of excipients for increasing drug apparent solubility and, as a result, its bioavailability, exploration of innovative approaches is an earnest need. Microemulsion is an alternative drug delivery system that emerged as a valuable tool to achieve safe formulations for insoluble compounds and to improve their biopharmaceutical properties and pharmacokinetics. This review aims to present the state of the art of microemulsion systems, bringing an overview about their origin and how they can be properly produced and thoroughly characterized by different approaches. Furthermore, comments on regulatory issues regarding stability assessment and toxicity evaluation are discussed. The review concludes with a current opinion on microemulsion systems. The overall objective of this work was to describe all the potentialities of microemulsion systems as a drug carrier for therapeutic purposes, highlighting the unique features of this nanotechnological platform. Display Image.
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Sistemas de Liberação de Medicamentos , Excipientes , Disponibilidade Biológica , Sistemas de Liberação de Medicamentos/métodos , Emulsões , Solubilidade , TensoativosRESUMO
Essential oils (EOs) have demonstrated antimicrobial activity against bacteria due to the effects of their major components. The direct application of EOs may present a rapid volatilization of its components and can decrease their effectiveness. Encapsulation by means of emulsification can provide protection to lipid compounds on a microscale. The aim of this study was to characterize microemulsions of cinnamon essential oil (CEO), oregano essential oil (OEO), and rosemary essential oil (REO) prepared by high-frequency ultrasound and evaluate their antimicrobial activities against Escherichia coli and Listeria monocytogenes. The microemulsions (oil-in-water, O/W) of EOs were prepared using high-frequency ultrasound, applying a wave amplitude of 84 µm for 15 min (REO and CEO) or 30 min (OEO). The antimicrobial activity was determined by inoculating 108 CFU/mL of bacteria. Nonsurvival of the bacteria was confirmed by plate count in tryptic soy agar, determining the minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC). The microemulsions exhibited droplet size diameters of 1.98 to 5.46 µm, showing high encapsulation efficiencies (79.91-81.97%) and low separation rates (2.50-6.67%). The MIC and MBC for the microemulsions for both bacteria were 20-75% less than values obtained for the non-encapsulated EOs. This study demonstrates that high-frequency ultrasound is a suitable technique for obtaining stable microemulsions to deliver natural antimicrobials that can be applied to control bacteria of high relevance in food safety.
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INTRODUCTION: There is a clinical need for pharmaceutical dosage forms devised to prolong the acting time of local anesthetic (LA) agents or to reduce their toxicity. Encapsulation of LA in drug delivery systems (DDSs) can provide long-term anesthesia for inpatients (e.g. in immediate postsurgical pain control, avoiding the side effects from systemic analgesia) and diminished systemic toxicity for outpatients (in ambulatory/dentistry procedures). The lipid-based formulations described here, such as liposomes, microemulsions, and lipid nanoparticles, have provided several nanotechnological advances and therapeutic alternatives despite some inherent limitations associated with the fabrication processes, costs, and preclinical evaluation models. AREAS COVERED: A description of the currently promising lipid-based carriers, including liposomes, microemulsions, and nanostructured lipid carriers, followed by a systematic review of the existing lipid-based formulations proposed for LA. Trends in the research of these LA-in-DDS are then exposed, from the point of view of administration route and alternatives for non-traditionally administered LA molecules. EXPERT OPINION: Considering the current state and potential future developments in the field, we discuss the reasons for why dozens of formulations published every year fail to reach clinical trials; only one lipid-based formulation for the delivery of local anesthetic (Exparel®) has been approved so far.
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Anestésicos Locais/administração & dosagem , Sistemas de Liberação de Medicamentos , Lipídeos/química , Anestesia Local/métodos , Animais , Portadores de Fármacos/química , Humanos , Lipossomos , Nanopartículas/administração & dosagem , NanoestruturasRESUMO
In this work, several normal, oil-in-water (o/w) microemulsions (MEs) were prepared using peppermint essential oil, jojoba oil, trans-anethole, and vitamin E as oil phases to test their capacity to load paclitaxel (PTX). Initially, pseudo-ternary partial phase diagrams were constructed in order to find the normal microemulsion region using d-α-tocopherol polyethylene glycol 1000 succinate (TPGS-1000) as surfactant and isobutanol (iso-BuOH) as co-surfactant. Selected ME formulations were loaded with PTX reaching concentrations of 0.6 mg mL-1 for the peppermint oil and trans-anethole MEs, while for the vitamin E and jojoba oil MEs, the maximum concentration was 0.3 mg mL-1. The PTX-loaded MEs were stable according to the results of heating-cooling cycles and mechanical force (centrifugation) test. Particularly, drug release profile for the PTX-loaded peppermint oil ME (MEPP) showed that â¼ 90% of drug was released in the first 48 h. Also, MEPP formulation showed 70% and 90% viability reduction on human cervical cancer (HeLa) cells after 24 and 48 h of exposure, respectively. In addition, HeLa cell apoptosis was confirmed by measuring caspase activity and DNA fragmentation. Results showed that the MEPP sample presented a major pro-apoptotic capability by comparing with the unloaded PTX ME sample.
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Antineoplásicos Fitogênicos/síntese química , Apoptose/efeitos dos fármacos , Citotoxinas/síntese química , Nanosferas/química , Paclitaxel/síntese química , Óleos de Plantas/síntese química , Antineoplásicos Fitogênicos/farmacocinética , Apoptose/fisiologia , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/fisiologia , Citotoxinas/farmacocinética , Relação Dose-Resposta a Droga , Liberação Controlada de Fármacos , Células HeLa , Humanos , Mentha piperita , Paclitaxel/farmacocinética , Óleos de Plantas/farmacocinética , Polietilenoglicóis/síntese química , Polietilenoglicóis/farmacocinética , Tensoativos/síntese química , Tensoativos/farmacocinética , Vitamina E/síntese química , Vitamina E/farmacocinéticaRESUMO
Enrichment of food and beverages with bioactive lipids is an important initiative to improve consumer's health. Eicosapentaenoic (EPA) and docosahexaenoic (DHA) acids present in fish oil have been reported as those with the greatest bioactivity. Emulsions are an interesting alternative to incorporate functional oil; however, there are few studies on food microemulsions as a way to include this kind of compounds. The present work is intended to deepen the analysis of the Kolliphor RH40 emulsifier with potential application in food microemulsions, characterizing its micellar size and thermo-rheological properties, as well as analyzing the effect of environmental stress on physical and oxidative stability of a microemulsion containing fish oil. No significant changes in droplets size (<15â¯nm) or in their distribution was observed in a wide range of pH (3-9), ionic strength (0.1-10% CaCl2), centrifuging and different thermal treatments. During freezing, a slight increase in size (<21â¯nm) was detected, maintaining its optically transparent appearance. The high surface area of the microemulsion droplets led to the decrease in oxidative stability compared to fish oil in bulk. However, when microemulsions were stored at 4⯰C, the EPA and DHA contents did not change during storage for 60â¯days.
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Fenômenos Químicos , Emulsões/química , Óleos de Peixe/química , Manipulação de Alimentos , Armazenamento de Alimentos , Congelamento , Temperatura Alta , Concentração de Íons de Hidrogênio , Concentração Osmolar , Oxirredução , Tamanho da Partícula , Reologia , TemperaturaRESUMO
Topical drug administration is frequently used for the treatment of vaginal candidiasis; however, most formulations using this route do not provide prolonged drug release. Our aim was to evaluate the antifungal efficacy of amphotericin B (AMB) and miltefosine (MFS) incorporated in nanocarriers for sustained drug release, in a murine model of vaginal candidiasis. AMB and MFS were incorporated in different topical formulations, namely: conventional vaginal cream (daily dose for 6 days; MFS-CR and AMB-CR groups), microemulsion that transforms into a liquid crystalline gel in situ (single dose, or in three doses, every 48 h; AMB-ME and MFS-ME groups) and alginate nanoparticles (single dose; MFS-AN group). Formulations were administered intravaginally in BALB/c female mice 24 h post-infection by Candida albicans yeasts. On the 7th day post-infection the animals were euthanized for mycological and histological analyses. Formulation persistence in the vaginal canal was assessed for 7 days by in vivo imaging, using nanocarriers labeled with Alexa-Fluor 647. AMB-ME(3×), MFS-ME(3×), and MFS-AN(1×) formulations were able to control fungal infection at comparable levels to those vaginal cream formulations. Notably, a single dose of MFS-AN was sufficient to reduce the fungal burden as effectively as MFS-ME(3×) and MFS-CR(6×). In vivo imaging showed that nanocarriers allowed prolonged antifungal activity by intravaginal administration reducing drug administration frequency. Therefore, AMB and MFS incorporated into a microemulsion and MFS encapsulated in alginate nanoparticles could be effective therapeutic alternatives for vaginal candidiasis, likely due to the sustained antifungal activity provided by these nanocarriers.
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The aim of this work was to predict the permeability of two model drugs, sulfamerazine (SMR) and indomethacin (INM), and to determine the effect on their apparent permeabilities by complexation with cyclodextrins and/or meglumine or incorporation in microemulsions. Permeation experiments were performed using two-chamber diffusion cells with a new composition of bio-mimetic membrane composed of 80% of Lipoid® S100 and 20% of cholesterol in n-octanol 10% w/w solution, at 37 ± 0.5°C and 14,000 rpm. The predictive capacity of the permeability of passive diffusion absorbed compounds was evaluated using 20 drug standards and showed an exponential correlation between the apparent permeability coefficients (Papp) and the fraction absorbed percentages in humans (Fa%), with an R2 value of 0.67942 and a constant value of - 4.1 ± 0.8. SMR and INM were classified as Class II and I, respectively, according to the Biopharmaceutical Classification System. These drugs were complexed and incorporated in microemulsions. The Fa% from all the drug products was higher than 90%. SMR in the complexes and both drugs in microemulsions were classified as highly soluble. Thus, SMR and INM incorporated in these pharmaceutical products could be classified as Class I.
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Materiais Biomiméticos/química , Materiais Biomiméticos/farmacocinética , Emulsões/química , Emulsões/farmacocinética , Membranas Artificiais , Biomimética/métodos , Ciclodextrinas/química , Ciclodextrinas/farmacocinética , Difusão , Indometacina/química , Indometacina/farmacocinética , Permeabilidade/efeitos dos fármacos , SolubilidadeRESUMO
Microemulsions are thermodynamically stable systems that have attracted considerable attention in the food industry as delivery systems for many hydrophobic nutrients. These spontaneous systems are highly dependent on ingredients and composition. In this work phase diagrams were constructed using two surfactants (Kolliphor RH40 and ELP), water, sunflower oil, and ethanol as cosurfactant, evaluating their physicochemical properties. Stability of the systems was studied at 25 and 60⯰C, monitoring turbidity at 550â¯nm for over a month to identify the microemulsion region. Conductivity was measured to classify between water-in-oil and oil-in-water microemulsions. The phase diagram constructed with Kolliphor RH40 exhibited a larger microemulsion area than that formulated with Kolliphor ELP. All formulations showed a monomodal droplet size distribution with low polydispersity index (<0.30) and a mean droplet size below 20â¯nm. Systems with higher water content presented a Newtonian behavior; increasing the dispersed phase content produced a weak gel-like structure with pseudoplastic behavior under flow conditions that was satisfactorily modeled to obtain structural parameters.
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Óleo de Rícino/química , Etanol/química , Manipulação de Alimentos/métodos , Óleo de Girassol/química , Tensoativos/química , Água/química , Elasticidade , Condutividade Elétrica , Emulsões , Géis , Modelos Químicos , Tamanho da Partícula , Transição de Fase , Reologia , Temperatura , Fatores de Tempo , ViscosidadeRESUMO
Designing soft, palatable and nutritious texture-modified foods for the elderly is a challenge for food technologists. The aim of this work was to produce and characterize emulsion-gelled microparticles (EGM) made from whey protein isolate (WPI) and sodium alginate (NaAlg) that may be used to modify the rheology of liquid foods and as carriers of lipids and lipophilic nutrients and bioactives. Olive oil microdroplets became embedded in the WPI/NaAlg gel matrix in the form of an emulsion produced by ultrasound (US) or high-speed blending (HSB). Oil microdroplets were obtained by US and HSB, with an average equivalent diameter varying between 2.0-3.2 µm and 4.5-6.7 µm, respectively. Oil incorporation increased compression stress of bulk emulsion gels at small deformations compared to the no-oil microgel, but this effect was reversed at high strains. EGM were prepared by shear-induced size reduction. Rheological tests at 20 â and 40 â showed that US-EGM and HSB-EGM exhibited a predominant elastic behavior, with G' > Gâ³ throughout the frequency range. However, when HSB-EGM were heated at 60 â their rheological behavior changed to a more fluid-like condition, but not that of US-EGM. Consequently, EGM have the properties needed to improve food texture for people with masticatory/swallowing dysfunctions or needing special nutrition.
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Alginatos/química , Emulsões/química , Tecnologia de Alimentos/métodos , Géis/química , Proteínas do Soro do Leite/química , Envelhecimento , Manipulação de Alimentos/métodos , Alimento Funcional , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Humanos , Valor Nutritivo , Tamanho da Partícula , ReologiaRESUMO
Microemulsions (MEs) loaded with methyl dihydrojasmonate (MJ) were developed to improve the aqueous solubility of this drug. The composition of the formulations ranged according to the oil/surfactant ratio (O/S). The MEs were characterized according to diameter of droplets, X-ray diffraction and polarized light microscopy. The MJ identification and quantification was performed by gas chromatography-mass spectrometry (GC-MS). The MJ showed a retention time of â¼16.7 min for all samples. The obtained correlation coefficient from the calibration graph was 0.991. The developed analytical method was effective enough to quantify low and high concentrations of MJ. The increase of the O/S ME ratio led to a reduction of the droplet diameter. All formulations showed an amorphous structure and the behavior varied between isotropic and anisotropic systems. A decrease in the release of MJ with the increase of the O/S ratio in the formulations was observed. The analytical method developed for the quantitative determination of MJ is suitable to detect and quantify the drug compound from different compositions of MEs in the in vitro release test, and by analogy in other prolonged effects related to the drug reservoir effect of these systems was observed, revealing that ME can be a promising nanocarrier for MJ delivery to tumor cells.
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Materiais Biocompatíveis/química , Emulsões/química , Óleos/química , Água/química , Química Farmacêutica/métodos , Preparações de Ação Retardada/química , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas/métodos , Nanopartículas/química , Tamanho da Partícula , Solubilidade/efeitos dos fármacos , Tensoativos/química , Difração de Raios X/métodosRESUMO
RESUMEN: El objetivo del presente trabajo fue evaluar el efecto de las microemulsiones de aceite esencial de romero (AER) y árbol de té (AET) sobre el eritrocito humano y microorganismos patógenos. Para ello, se elaboraron microemulsiones de AER y AET al 8.0% (v/v), 5.0% (v/v) y 2.5% (v/v). Las microemulsiones fueron probadas sobre el eritrocito humano para determinar el porcentaje de hemólisis, el porcentaje de inhibición de hemólisis y su actividad antibacterial contra E. coli O157:H7 y S. aureus. Las microemulsiones con AER no presentaron actividad hemolítica significativa, caso contrario con las microemulsiones de AET al 8.0% (≈70%) y 5.0% (33%) que presentaron mayor actividad hemolítica. Las microemulsiones de AER protegieron significativamente al eritrocito contra la presencia de radicales libres, en comparación con aquellas de AET (p< 0.05). Además, las emulsiones de AET al 8.0% mostraron efectos antibacterianos contra E. coli O157:H7 y S. aureus mientras que AER al 8.0% solo mostraron efecto contra E. coli O157:H7. La limitante del estudio fue que no utilizamos células nucleadas para establecer si los aceites esenciales dañan el material nuclear. Sin embargo, observamos que el tipo y la cantidad de aceite utilizado pueden tener implicaciones serias sobre la membrana eritrocitaria. Se concluye que las microemulsiones de AER presentaron mejor efecto protector eritrocitario, mientras que las microemulsiones de AET presentaron mejor actividad antibacterial contra las bacterias estudiadas, pero con mayor efecto tóxico sobre el eritrocito.
ABSTRACT: The aim of the study was to evaluate the effect of microemulsions of rosemary (AER) and tea tree (AET) essential oils on human erythrocyte and pathogen bacteria. Microemulsions of each oil were prepared at 8.0% (v/v), 5.0% (v/v) and 2.5% (v/v), and they were tested on human erythrocyte to determine the hemolysis percentage, hemolysis inhibition percentage and the antibacterial capacity against E. coli O157:H7 and S. aureus. All AER microemulsions showed no significant hemolytic activity. On the contrary, AET microemulsions showed hemolytic effect but those in concentrations of 8.0% (≈70 %) and 5.0% (33%) showed the highest effect. In addition, AER microemulsions showed protective effect against free radicals in comparison with the AET microemulsions (p< 0.05). On the other hand, the AET microemulsion at 8.0% showed antibacterial effect against E. coli O157:H7 and S. aureus, and the AER at 8.0% showed antibacterial effect against E. coli O157:H7. The limitation of this study was that nucleated cells were not used to observe the damage of the essential oils on nuclear material. However, the observed damage of erythrocyte's membrane is depending on type and amount of used oil. Therefore, it can be concluded that the AER microemulsions showed better protective effect of erythrocytes, while AET microemulsions showed better antibacterial effect against the tested bacteria, although with toxic effect on the erythrocytes.
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ABSTRACT This study was to develop, characterize, and evaluate the physical-chemical stability, in vitro antioxidant activity and in vitro safety profile of liquid crystalline systems (LCS) and microemulsions (MEs) with and without organic cocoa (OC) extract. LCS stabilized by surfactant polyoxyethylene 20 cetyl ether, containing water and oleic acid were studied. LCS and MEs were characterized using polarized light microscopy, small angle X-ray scattering, rheology and in vitro bioadhesion, and were evaluated for a period of 30 days by visual aspects, centrifuge test, pH value and relative density. PLM and SAXS assays showed the presence of domains of MEs, cubic and hexagonal mesophasephases, varying the proportions of the components of the formulations; where in the addition of the extract did not change rheological behavior of the formulations. All of the formulations were stable in the period analyzed and presented higher bioadhesive strength. In vitro antioxidant activity suggests that LCS and MEs presented a high capacity to maintain the antioxidant activity of OC extract. The results showed that the incorporation of OC in LCS improved the safety profile, according to cytotoxicity assays of systems may be a promising platform to OC extract for topical application for the potential treatment of skin disorders.
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Tensoativos , Cristais Líquidos/análise , Pele , Cacau/efeitos adversos , Sistemas de Liberação de Medicamentos , Microscopia de Polarização/métodosRESUMO
Microemulsions are thermodynamically stable systems of two immiscible liquids, one aqueous and the other of organic nature, with a surfactant and/or co-surfactant adsorbed in the interface between the two phases. Biodiesel-based microemulsions, consisting of alkyl esters of fatty acids, open a new means of analysis for the application of electroanalytical techniques, and is advantageous as it eliminates the required pre-treatment of a sample. In this work, the phase behaviours of biodiesel-based microemulsions were investigated through the electrochemical impedance spectroscopy (EIS) technique. We observed thatan increase in the amount of biodiesel in the microemulsion formulation increases the resistance to charge transfer at the interface. Also, the electrical conductivity measurements revealed that a decrease or increase in electrical properties depends on the amount of biodiesel. EIS studies of the biodiesel-based microemulsion samples showed the presence of two capacitive arcs: one high-frequency and the other low-frequency. Thus, the formulation of microemulsions plays an important role in estimating the electrical properties through the electrochemical impedance spectroscopy technique.
Assuntos
Arecaceae/química , Biocombustíveis/análise , Espectroscopia Dielétrica/métodos , Emulsões/análise , Espectroscopia Dielétrica/instrumentação , Condutividade Elétrica , Desenho de Equipamento , Transição de FaseRESUMO
Alzheimer's disease is a neurological disorder that results in cognitive and behavioral impairment. Conventional treatment strategies, such as acetylcholinesterase inhibitor drugs, often fail due to their poor solubility, lower bioavailability, and ineffective ability to cross the blood-brain barrier. Nanotechnological treatment methods, which involve the design, characterization, production, and application of nanoscale drug delivery systems, have been employed to optimize therapeutics. These nanotechnologies include polymeric nanoparticles, solid lipid nanoparticles, nanostructured lipid carriers, microemulsion, nanoemulsion, and liquid crystals. Each of these are promising tools for the delivery of therapeutic devices to the brain via various routes of administration, particularly the intranasal route. The objective of this study is to present a systematic review of nanotechnology-based drug delivery systems for the treatment of Alzheimer's disease.