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1.
Proc Natl Acad Sci U S A ; 121(29): e2406337121, 2024 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-38985759

RESUMO

Unlike inorganic nanoparticles, organic nanoparticles (oNPs) offer the advantage of "interior tailorability," thereby enabling the controlled variation of physicochemical characteristics and functionalities, for example, by incorporation of diverse functional small molecules. In this study, a unique inimer-based microemulsion approach is presented to realize oNPs with enhanced control of chemical and mechanical properties by deliberate variation of the degree of hyperbranching or cross-linking. The use of anionic cosurfactants led to oNPs with superior uniformity. Benefitting from the high initiator concentration from inimer and preserved chain-end functionality during atom transfer radical polymerization (ATRP), the capability of oNPs as a multifunctional macroinitiator for the subsequent surface-initiated ATRP was demonstrated. This facilitated the synthesis of densely tethered poly(methyl methacrylate) brush oNPs. Detailed analysis revealed that exceptionally high grafting densities (~1 nm-2) were attributable to multilayer surface grafting from oNPs due to the hyperbranched macromolecular architecture. The ability to control functional attributes along with elastic properties renders this "bottom-up" synthetic strategy of macroinitiator-type oNPs a unique platform for realizing functional materials with a broad spectrum of applications.

2.
Photochem Photobiol Sci ; 23(7): 1309-1321, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38839722

RESUMO

Current research of triplet-triplet annihilation upconversion (TTA-UC) faces difficulty such as overuse of organic solvents and quenching of excited triplet sensitizers by molecular oxygen. Herein, we propose an efficient and facile preparation strategy of TTA-UC microemulsion to overcome these issues. With simple device and short preparation process, air-stable TTA-UC with a high upconversion efficiency of 16.52% was achieved in microemulsion coassembled from TritonX114, tetrahydrofuran and upconverting chromophores (platinum octaethyl-porphyrin and 9,10-diphenylanthracene). This is comparable to the highest UC efficiency ever reported for TTA-UC microemulsion systems. The excellent UC performance of TX114-THF could be attributed to two perspectives. Firstly, small-size micelle accommodated chromophores up to high concentrations in organic phase, which promoted efficient molecular collision. Additionally, high absorbance at 532 nm ensured full use of excitation light, getting more long wavelength photons involved in the TTA-UC process. Moreover, air-stable TTA-UC also performed well in microemulsion with various surfactants, including nonionic surfactants (Tween 20, Tween 80, Triton X-110, Triton X-114), ionic surfactants (sodium dodecyl sulfate, cetyltrimethyl ammonium bromide) and block copolymers (pluronic F127, pluronic P123), through three conjectural assembly models according to the structural characteristics of surfactant molecules (concentrated, uncompacted and scattered). These discoveries could provide estimable reference for selection of surfactants in relevant fields of TTA-UC.

3.
Environ Res ; 260: 119626, 2024 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-39019143

RESUMO

The utilization of bio-oil derived from biomass presents a promising alternative to fossil fuels, though it faces challenges when directly applied in diesel engines. Microemulsification has emerged as a viable strategy to enhance bio-oil properties, facilitating its use in hybrid fuels. This study explores the microemulsification of Jatropha bio-oil with ethanol, aided by a surfactant, to formulate a hybrid liquid fuel. Additionally, a bio-nano CaO heterogeneous catalyst synthesized from eggshells is employed to catalyse the production of Jatropha biodiesel from the microemulsified fuel using microwave irradiation. The catalyst is characterized through UV-Vis, XRD, and SEM analysis. The investigation reveals a significant reduction in CO, CO2, and NOX emissions with the utilization of microemulsion-based biodiesel blends. Various blends of conventional diesel, Jatropha biodiesel, and ethanol are prepared with different ethanol concentrations (5, 10, and 20 wt%). Engine performance parameters, including fuel consumption, NOX emission, and brake specific fuel consumption, are analyzed. Results indicate that the conventional diesel/Jatropha biodiesel/ethanol (10 wt%) blend exhibits superior performance compared to conventional diesel, Jatropha biodiesel, and other blends. The fuel consumption of the conventional diesel/Jatropha biodiesel/ethanol (10 wt%) blend is measured at 554.6 g/h, surpassing that of conventional diesel and other biodiesel blends. The presence of water (0.14 %) in the blend reduces the heating value, consequently increasing the energy requirement. CO and CO2 emissions for the conventional diesel/Jatropha biodiesel/ethanol (10 wt%) blend are notably lower compared to conventional C-18 hydrocarbons and various biodiesel blends. These findings accentuate the efficacy of the microemulsion process in enhancing fuel characteristics and reducing emissions. Further investigations could explore optimizing the emulsifying agents and their impact on engine performance and emission characteristics, contributing to the advancement of sustainable fuel technologies.

4.
Drug Chem Toxicol ; 47(2): 235-242, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-37990576

RESUMO

Phytochemicals as therapeutic alternatives can have a fundamental impact on the various stages of inflammation and its resolution. Prunetin is a naturally occurring isoflavone and has been claimed to have numerous therapeutic potentials. The objective of this study is preparation, characterization, and toxicity evaluation of microemulsion formulation containing prunetin (PMF) for potential oral applications. With this research, it was targeted to emphasize the way of improving the therapeutic efficacy of natural biomolecules with a nontoxic and effective formulation. In the study, the pseudo-ternary phase diagram was developed and PMF was characterized by conductivity, droplet size, viscosity and pH. Effects against to cytokines (IL-1ß and IL-6) and TNF-α levels of the PMF were determined by ELISA technique. Genotoxicity and acute oral toxicity tests were carried out according to OECD guidelines. The results showed that PMF is a colloid system that reduced proinflammatory cytokine levels in LPS-induced macrophage cells compared to the control group. PMF demonstrated no mutagenic activity against TA98, TA100, TA1535, and TA1537 Salmonella strains. The in vivo oral acute toxicity test results indicated that PMF did not show mortality or significant side effects even at 2000 mg/kg bw. This study represents PMF showed a good safety profile in animal study. It is thought that this formulation may have anti-inflammatory potential with further in vivo testing.


Assuntos
Anti-Inflamatórios , Isoflavonas , Animais , Anti-Inflamatórios/farmacologia , Isoflavonas/farmacologia , Citocinas , Mutagênicos
5.
Nano Lett ; 23(17): 7815-7824, 2023 09 13.
Artigo em Inglês | MEDLINE | ID: mdl-37586706

RESUMO

Stem cells exhibit prominent clusters controlling the transcription of genes into RNA. These clusters form by a phase-separation mechanism, and their size and shape are controlled via an amphiphilic effect of transcribed genes. Here, we construct amphiphile-nanomotifs purely from DNA, and we achieve similar size and shape control for phase-separated droplets formed from fully synthetic, self-interacting DNA-nanomotifs. Increasing amphiphile concentrations induce rounding of droplets, prevent droplet fusion, and, at high concentrations, cause full dispersal of droplets. Super-resolution microscopy data obtained from zebrafish embryo stem cells reveal a comparable transition for transcriptional clusters with increasing transcription levels. Brownian dynamics and lattice simulations further confirm that the addition of amphiphilic particles is sufficient to explain the observed changes in shape and size. Our work reproduces key aspects of transcriptional cluster formation in biological cells using relatively simple DNA sequence-programmable nanostructures, opening novel ways to control the mesoscopic organization of synthetic nanomaterials.


Assuntos
Nanoestruturas , Peixe-Zebra , Animais , Núcleo Celular , Nanoestruturas/química , DNA/química
6.
J Microencapsul ; 41(2): 127-139, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38410926

RESUMO

Aim of the current study is to develop a microemulsion gel for transdermal delivery of tapentadol hydrochloride. Microemulsion was developed using phase diagram and subjected to assay, globule size, PDI, zeta potential, TEM and in vitro drug release studies. The optimized microemulsion was converted into gel using carbopol 934 NF and evaluated for viscosity, spreadability, in vitro, ex vivo, FTIR, DSC, stability and skin irritation studies. The mean globule size, PDI, zeta potential and in vitro drug release of microemulsion were found 247.3 nm, 0.298, -17.6 mV and 98.42% respectively. In vitro and ex vivo drug release of gel was found 92.2% and 88.6% in 24 h. Viscosity and spreadability results indicated ease of application and no incompatibility was observed from FTIR studies. The skin irritation studies showed absence of erythema. Key findings from the current research concluded that microemulsion gel was suitable for effective transdermal delivery.


Assuntos
Inflamação , Absorção Cutânea , Humanos , Tapentadol , Géis , Administração Cutânea , Liberação Controlada de Fármacos
7.
J Microencapsul ; 41(4): 296-311, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38709162

RESUMO

AIMS: To construct the microemulsion delivery system (ME) loading ATSO and NA and study their physicochemical characteristics to enhance their stability and water solubility. METHODS: By plotting ternary phase diagrams, the composition and proportions of the MEs were determined. The physicochemical characteristics and stability of MEs were evaluated by mean diameter, polydispersity index (PDI), pH, electrical conductivity, transmission electron microscopy (TEM), rheological behaviour measurement, and phase inversion temperature (PIT). RESULTS: The MEs was composed with EL-40 as a surfactant and specifically with the addition of ethanol as a cosurfactant in NA-loaded ME. The mean diameters of ATSO-loaded ME and NA-loaded ME were 39.65 ± 0.24 nm and 32.90 ± 2.65 nm, and PDI were 0.49 ± 0.01 and 0.28 ± 0.14, respectively. The TEM confirmed the spherical and smooth morphology of MEs. The rheological results indicated that MEs are dilatant fluids with the advantages of low viscosity, high fluidity, and tolerance to temperature fluctuations. The mean diameter and PDI of MEs showed no significant change after storage at 25 °C for 28 days and centrifugation. CONCLUSION: The prepared microemulsions could expand the application prospects of ATSO and NA products in cosmetics, medicine, foods and other fields.


Assuntos
Emulsões , Óleos de Plantas , Reologia , Emulsões/química , Óleos de Plantas/química , Acer/química , Ácidos Graxos/química , Sementes/química , Tensoativos/química , Estabilidade de Medicamentos , Viscosidade
8.
Molecules ; 29(13)2024 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-38999184

RESUMO

Surfactants play a crucial role in tertiary oil recovery by reducing the interfacial tension between immiscible phases, altering surface wettability, and improving foam film stability. Oil reservoirs have high temperatures and high pressures, making it difficult and hazardous to conduct lab experiments. In this context, molecular dynamics (MD) simulation is a valuable tool for complementing experiments. It can effectively study the microscopic behaviors (such as diffusion, adsorption, and aggregation) of the surfactant molecules in the pore fluids and predict the thermodynamics and kinetics of these systems with a high degree of accuracy. MD simulation also overcomes the limitations of traditional experiments, which often lack the necessary temporal-spatial resolution. Comparing simulated results with experimental data can provide a comprehensive explanation from a microscopic standpoint. This article reviews the state-of-the-art MD simulations of surfactant adsorption and resulting interfacial properties at gas/oil-water interfaces. Initially, the article discusses interfacial properties and methods for evaluating surfactant-formed monolayers, considering variations in interfacial concentration, molecular structure of the surfactants, and synergistic effect of surfactant mixtures. Then, it covers methods for characterizing microstructure at various interfaces and the evolution process of the monolayers' packing state as a function of interfacial concentration and the surfactants' molecular structure. Next, it examines the interactions between surfactants and the aqueous phase, focusing on headgroup solvation and counterion condensation. Finally, it analyzes the influence of hydrophobic phase molecular composition on interactions between surfactants and the hydrophobic phase. This review deepened our understanding of the micro-level mechanisms of oil displacement by surfactants and is beneficial for screening and designing surfactants for oil field applications.

9.
AAPS PharmSciTech ; 25(3): 53, 2024 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-38443698

RESUMO

Modern drug carrier technologies, such as microemulsions with small droplet sizes and high surface areas, improve the ability of low water solubility active ingredients to permeate and localize. The goal of this study was to create microemulsion formulations for wound healing that contained both fusidic acid (FA), an antibacterial agent, and benzocaine (BNZ), a local anesthetic. Studies on characterization were carried out, including viscosity, droplet size, and zeta potential. The drug-loaded microemulsion had a stable structure with -3.014 ± 1.265 mV of zeta potential and 19.388 ± 0.480 nm of droplet size. In both in vitro release and ex vivo permeability studies, the microemulsion was compared with Fucidin cream and oily BNZ solution. According to the drug release studies, BNZ release from the microemulsion and the BNZ solution showed a similar profile (p > 0.05), while FA release from the microemulsion had a higher drug release compared to Fucidin cream (p < 0.001). The microemulsion presented lower drug permeation (p > 0.05) for both active ingredients, on the other hand, provided higher drug accumulation compared to the control preparations. Moreover, according to the results of in vitro wound healing activity, the microemulsion indicated a dose-dependent wound healing potential with the highest wound healing activity at the highest concentrations. To the best of our knowledge, this developed BNZ- and FA-loaded microemulsion would be a promising candidate to create new opportunities for wound healing thanks to present the active ingredients, which have low water solubility, in a single formulation and achieved higher accumulation than control preparations.


Assuntos
Benzocaína , Ácido Fusídico , Ácido Fusídico/farmacologia , Anestésicos Locais , Cicatrização , Água
10.
Saudi Pharm J ; 32(1): 101919, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38178852

RESUMO

This study aimed to prepare an o/w mitiglinide microemulsion (MTGME) to improve the drug solubility and bioavailability. The formulation of o/w MTGME was optimized by the solubility study of drug, pseudo-ternary phase diagram and Box-Behnken design successively. MTGME was characterized by dynamic laser light scattering (DLS), zeta potential and transmission electron microscopy (TEM), moreover, the storage stability, pharmacodynamics and pharmacokinetics were investigated. The optimal prescription for MTGME consisted of Maisine 35-1 (oil), Cremophor EL (surfactant) and propylene glycol (PG, cosurfactant). MTGME with a spherical dimension of 58.1 ± 5.86 nm was stable when stored at 4 °C for 3 months. The blood glucose levers (BGL) of diabetic mice were uniformly and significantly decreased by intragastric (i.g.) administration of 1-4 mg/kg MTGME, in which BGL (i.g. 4 mg/kg MTGME) was reduced by 69% during 24 h. The pharmacokinetics study of MTGME (i.g., 20 mg/kg) in Wistar rats showed higher plasma drug concentration (Cmax, 2.9 folds), larger area under curve (AUC, 4.6 folds) and oral bioavailability than those of MTG suspensions. Generally, the MTGME (o/w) showed good effect on controlling hyperglycemia. Therefore, microemulsion can be used as an effective oral drug delivery system to improve the bioavailability of MTG.

11.
Saudi Pharm J ; 32(6): 102100, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38812945

RESUMO

We previously demonstrated that baicalin had efficacy against gouty arthritis (GA) by oral administration. In this paper, a novel baicalin-loaded microemulsion-based gel (B-MEG) was prepared and assessed for the transdermal delivery of baicalin against GA. The preparation method and transdermal capability of B-MEG was screened and optimized using the central composite design, Franz diffusion cell experiments, and the split-split plot design. Skin irritation tests were performed in guinea pigs. The anti-gout effects were evaluated using mice. The optimized B-MEG comprised of 50 % pH 7.4 phosphate buffered saline, 4.48 % ethyl oleate, 31.64 % tween 80, 13.88 % glycerin, 2 % borneol, 0.5 % clove oil and 0.5 % xanthan gum, with a baicalin content of (10.42 ± 0.08) mg/g and particle size of (15.71 ± 0.41) nm. After 12 h, the cumulative amount of baicalin permeated from B-MEG was (672.14 ± 44.11) µg·cm-2. No significant skin irritation was observed following B-MEG application. Compared to the model group, B-MEG groups significantly decreased the rate of auricular swelling (P < 0.01) and number of twists observed in mice (P < 0.01); and also reduced the rate of paw swelling (P < 0.01) and inflammatory cell infiltration in a mouse model of GA. In conclusion, B-MEG represents a promising transdermal carrier for baicalin delivery and can be used as a potential therapy for GA.

12.
Mol Pharm ; 20(1): 232-240, 2023 01 02.
Artigo em Inglês | MEDLINE | ID: mdl-36354760

RESUMO

Extensive use of microemulsions as delivery systems raises interest in the safe ingredients that can form such systems. Here, we assessed the use of two glycols, i.e., propylene glycol and pentylene glycol, and their mixtures to manipulate the properties and structure of microemulsions. Obtained systems with glycols were extensively characterized in terms of capacity to incorporate water phase, droplet size, polydispersity, structure type, and rheological and thermal properties. The results of these studies indicate that the composition, structure, and viscosity of the microemulsions can be changed by appropriate quantification of glycols. It has been shown that the type of glycol used and its amount may favor or worsen the formation of microemulsions with the selected oils. In addition, a properly selected composition of oils and glycols resulted in the formation of microemulsions with a reduced content of surfactants and consequently improved the safety of using microemulsions as delivery systems.


Assuntos
Óleos , Tensoativos , Tensoativos/química , Óleos/química , Propilenoglicol/química , Emulsões/química
13.
Pharm Res ; 40(3): 675-687, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36703027

RESUMO

PURPOSE: Aromatic turmerone, a major constituent of turmeric oil, has been recently reported for proliferation of neural stem cell showing great potential for effective treatment in neurodegenerative disorders. However, its effect as oral brain targeted formulation for neuroprotection has not yet reported. The objective of the study was to investigate the pharmacokinetic of curcumin loaded turmeric oil microemulsion for brain targeting and probing the protective effect against trimethyltin induced neurodegeneration in adult zebrafish. METHODS: Initially, in vivo plasma and brain pharmacokinetics was performed to determine improvement in relative bioavailability in rats followed by biodistribution and histopathological evaluation. Furthermore, the neuroprotective effect of the formulation was assessed in trimethyltin induced neurodegeneration model using adult zebrafish by behavioral analysis and biochemical analysis. RESULTS: The in vivo plasma and brain pharmacokinetics showed 2-fold and 1.87-fold improvement respectively. Biodistribution study revealed significantly lower concentration in organs other than brain. Furthermore, curcumin microemulsion exhibited improved spatial memory by remembering the training and made correct choices after curcumin microemulsion treatment than other treatment groups. Histopathological evaluation confirmed neuroprotective effect on zebrafish brains. The biochemical analysis revealed reduced oxidative stress in curcumin microemulsion treated group. CONCLUSIONS: Overall results showed a great potential of curcumin microemulsion for brain targeting in the effective treatment of neurological ailments.


Assuntos
Curcumina , Fármacos Neuroprotetores , Ratos , Animais , Peixe-Zebra , Distribuição Tecidual , Curcuma , Encéfalo
14.
J Fluoresc ; 33(3): 1111-1123, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36580202

RESUMO

Amino- and sulfhydryl- functionalized biomass carbon dots (BCDs) were prepared by one-pot reverse microemulsion for specific recognition of ferric ions (Fe3+) and L-cysteine (L-Cys). Green grapefruit peel was used as the carbon source while aminosilane and mercaptosilane were used as N- and S-supplier. Following the adsorption of Fe3+ on the surfaces of BCDs-NH2 and BCDs-SH, the fluorescence responses was quenched step by step, while adding L-Cys to the BCDs-NH2/Fe3+ system restored the fluorescence. The BCDs-NH2 and BCDs-SH system exhibited extremely low limits of detection for Fe3+ of 3.2 and 3.0 nM, respectively, within a wide linear ranges of 0.006-200 µM and 0.004-200 µM, respectively. The BCDs-NH2/Fe3+ systems were used as an optosensor for L-Cys in the concentration ranges of 0.08-30 and 30-1000 µM with a detection limit of 65 nM. Developed BCDs-NH2 and BCDs-SH were able to respond to Fe3+ in water samples with satisfactory recoveries of 100.1%-103.1% and 94.6%-108.5%, respectively, and the BCDs-NH2/Fe3+ system was also able to respond to BCDs-NH2/Fe3+ in actual lake water samples with recoveries from 87.3% to 98.8%. Meanwhile, The BCDs-NH2 exhibited good photoluminescence and stability, and the with a fluorescence quantum yield was as high as 25%. This work demonstrates the feasibility of using such materials to remove hazardous ions from water and employing the resulting complexes for optosensing in a sustainable manner.


Assuntos
Cisteína , Pontos Quânticos , Carbono , Biomassa , Água , Íons
15.
J Appl Microbiol ; 134(3)2023 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-36931893

RESUMO

AIMS: To solve the shortcomings of poor solubility, easy volatilization, and decomposition, propolis essential oil microemulsion (PEOME) was prepared. The antibacterial, antibiofilm activities, and action mechanism of PEOME against Streptococcus mutans was analyzed. METHODS: PEOME was prepared using anhydrous ethanol and Tween-80 as the cosurfactant and surfactant, respectively. The antibacterial activity of PEOME against S. mutans was evaluated using the agar disk diffusion method and broth microdilution method. The effects of PEOME on S. mutans biofilm was detected through the assays of crystal violet (CV), XTT reduction, lactic dehydrogenase (LDH) and calcium ions leaking, live/dead staining and scanning electron microscopy (SEM). And the antibiofilm mechanism of PEOME was elaborated by the assays of extracellular polysaccharide (EPS) production and glucosyltransferase (GTF) activity. RESULTS: The inhibition zone diameter (DIZ) of PEOME against S. mutans was 31 mm, while the minimal inhibitory concentration (MIC) was 2.5 µL mL-1. CV and XTT assays showed that PEOME could prevent fresh biofilm formation and disrupt preformed biofilm through decreasing the activities and biomass of biofilm. The leaking assays for LDH and calcium ions, as well as the live/dead staining assay, indicated that PEOME was able to damage the integrity of bacterial cell membranes within the biofilm. SEM revealed that PEOME had a noticeable inhibitory effect on bacterial adhesion and aggregation through observing the overall structure of biofilm. The assays of EPS production and GTF activity suggested that PEOME could reduce EPS production by inhibiting the activity of GTFs, thus showing an antibiofilm effect. CONCLUSIONS: The significant antibacterial and antibiofilm activities against S. mutans of PEOME meant that PEOME has great potential to be developed as a drug to prevent and cure dental caries caused by S. mutans.


Assuntos
Cárie Dentária , Óleos Voláteis , Própole , Humanos , Própole/farmacologia , Streptococcus mutans , Óleos Voláteis/farmacologia , Cálcio/farmacologia , Antibacterianos/farmacologia , Biofilmes , Polissacarídeos/farmacologia
16.
Nanomedicine ; 51: 102689, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37156330

RESUMO

Alzheimer's disease (AD) is an illness that affects people aged 65 or older and affects around 6.5 million in the United States. Resveratrol is a chemical obtained from natural products and it exhibits biological activity based on inhibiting the formation, depolymerization of the amyloid, and decreasing neuroinflammation. Due to the insolubility of this compound; its incorporation in surfactant-based systems was proposed to design an intranasal formulation. A range of systems has been produced by mixing oleic acid, CETETH-20 and water. Polarised light microscopy (PLM), small angle x-ray scattering (SAXS) and transmission electron microscopy (TEM) confirm the initial liquid formulation (F) presented as microemulsion (ME). After dilution, the gelled systems were characterized as hexagonal mesophase and they showed feasibility proprieties. Pharmacological assays performed after intranasal administration showed the ability to improve learning and memory in animals, as well as remission of neuroinflammation via inhibition of interleukin.


Assuntos
Doença de Alzheimer , Cristais Líquidos , Animais , Administração Intranasal , Doença de Alzheimer/tratamento farmacológico , Resveratrol/farmacologia , Resveratrol/uso terapêutico , Espalhamento a Baixo Ângulo , Cristais Líquidos/química , Doenças Neuroinflamatórias , Difração de Raios X
17.
Drug Dev Ind Pharm ; 49(1): 42-51, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36803628

RESUMO

OBJECTIVE: Formulation of curcumin in a microemulsion with a high loading capacity and that favors its penetration into the skin. SIGNIFICANCE: Take advantage of the properties of microemulsions to promote the penetration of curcumin into the skin, with the aim of enhancing its therapeutic effects. METHODS: Curcumin was formulated in microemulsions based on oleic acid (oil phase), Tween® 80 (surfactant), and Transcutol® HP (cosurfactant). The microemulsion formation area was mapped by constructing pseudo-ternary diagrams for surfactant:co-surfactant ratios 1:1, 1:2, and 2:1. Microemulsions were characterized through measurements of specific weight, refractive index, conductivity, viscosity, droplet size, and in vitro skin permeation studies. RESULTS: Nine microemulsions were prepared and characterized, showing clear, stable formulations with globule size dependent on the proportion of the components. The microemulsion with the highest loading capacity (60 mg/mL), based on Tween® 80, Transcutol® HP, oleic acid, and water (40:40:10:10) was able to penetrate the viable epidermis, finding a total amount of curcumin in the receptor medium at 24 h of 10.17 ± 9.7 µg/cm2. The distribution of curcumin in the skin, visualized by confocal laser scanning microscopy, showed that the maximum amount was located between 20 and 30 µm. CONCLUSION: The inclusion of curcumin in a microemulsion allows its passage into and through the skin. The localization of curcumin, especially in the viable epidermis, would be important for those cases where local conditions are sought to be treated.


Assuntos
Curcumina , Absorção Cutânea , Polissorbatos , Administração Cutânea , Ácido Oleico , Pele/metabolismo , Tensoativos/metabolismo , Emulsões/metabolismo
18.
Drug Dev Ind Pharm ; 49(2): 207-216, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36971611

RESUMO

OBJECTIVE: To investigate the safety and efficacy of resveratrol microemulsion gel in improving pigmentation. METHODS: Resveratrol microemulsion gel was prepared by the microemulsion solubilization method, and its quality was evaluated. The transdermal and drug retention rates of resveratrol in vivo were assessed using a transdermal test. The inhibitory effects of resveratrol suspension and microemulsion on tyrosinase activity and melanin production of A375 human melanocytes and zebrafish embryos were compared. A skin patch test was used to investigate the safety of the gel on 15 volunteers. RESULTS: The microemulsion gel was homogeneous and stable. Compared with suspension and microemulsion, the drug penetration rate and skin retention in the microemulsion gel group were significantly increased. Compared with the suspension group, the activity of melanocyte tyrosinase in A375 human melanocyte was significantly inhibited in the microemulsion group, and the melanin production rate of A375 human melanocyte and the melanin area of zebrafish yolk was decreased. All 15 volunteers tested negative for the human skin patch. CONCLUSIONS: The microemulsion gel could significantly enhance the ability of resveratrol to inhibit the formation of melanin without causing side effects. These data provide the experimental basis for developing and applying the preparation for improving pigmentation.


Assuntos
Absorção Cutânea , Peixe-Zebra , Animais , Humanos , Resveratrol , Pigmentação da Pele , Melaninas/metabolismo , Monofenol Mono-Oxigenase/metabolismo , Óleo de Rícino/metabolismo , Pele/metabolismo , Polietilenoglicóis/metabolismo , Emulsões/metabolismo
19.
Int J Mol Sci ; 24(10)2023 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-37240220

RESUMO

Curcumin is the principal curcuminoid found in the rhizomes of turmeric. Due to its therapeutic action against cancer, depression, diabetes, some bacteria, and oxidative stress, it has been used widely in medicine since ancient times. Due to its low solubility, the human organism cannot completely absorb it. Advanced extraction technologies, followed by encapsulation in microemulsion and nanoemulsion systems, are currently being used to improve bioavailability. This review discusses the different methods available for curcumin extraction from plant material, methods for the identification of curcumin in the resulting extracts, its beneficial effects on human health, and the encapsulation techniques into small colloidal systems that have been used over the past decade to deliver this compound.


Assuntos
Curcumina , Neoplasias , Humanos , Curcumina/uso terapêutico , Emulsões , Solubilidade , Neoplasias/tratamento farmacológico
20.
Int J Mol Sci ; 24(15)2023 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-37569488

RESUMO

Olea europaea L. leaves contain a wide variety of pentacyclic triterpenes (TTPs). TTPs exhibit many pharmacological activities, including antihyperlipidemic effects. Metabolic alterations, such as dyslipidemia, are an established risk factor for hepatocellular carcinoma (HCC). Therefore, the use of TTPs in the adjunctive treatment of HCC has been proposed as a possible method for the management of HCC. However, TTPs are characterized by poor water solubility, permeability, and bioavailability. In this work, a microemulsion (ME) loading a TTP-enriched extract (EXT) was developed, to overcome these limits and obtain a formulation for oral administration. The extract-loaded microemulsion (ME-EXT) was fully characterized, assessing its chemical and physical parameters and release characteristics, and the stability was evaluated for two months of storage at 4 °C and 25 °C. PAMPA (parallel artificial membrane permeability assay) was used to evaluate the influence of the formulation on the intestinal passive permeability of the TTPs across an artificial membrane. Furthermore, human hepatocarcinoma (HepG2) cells were used as a cellular model to evaluate the effect of EXT and ME-EXT on de novo lipogenesis induced by elevated glucose levels. The effect was evaluated by detecting fatty acid synthase expression levels and intracellular lipid accumulation. ME-EXT resulted as homogeneous dispersed-phase droplets, with significantly increased EXT aqueous solubility. Physical and chemical analyses showed the high stability of the formulation over 2 months. The formulation realized a prolonged release of TTPs, and permeation studies demonstrated that the formulation improved their passive permeability. Furthermore, the EXT reduced the lipid accumulation in HepG2 cells by inhibiting de novo lipogenesis, and the ME-EXT formulation enhanced the inhibitory activity of EXT on intracellular lipid accumulation.


Assuntos
Carcinoma Hepatocelular , Neoplasias Hepáticas , Olea , Triterpenos , Humanos , Triterpenos Pentacíclicos , Lipogênese , Células Hep G2 , Carcinoma Hepatocelular/tratamento farmacológico , Emulsões/química , Neoplasias Hepáticas/tratamento farmacológico , Triterpenos/farmacologia , Triterpenos/química , Membranas Artificiais , Folhas de Planta , Lipídeos
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