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1.
AAPS PharmSciTech ; 22(3): 111, 2021 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-33748928

RESUMO

Dihydromyricetin (DMY) is highly effective in counteracting acute alcohol intoxication. However, its poor aqueous solubility and permeability lead to the low oral bioavailability and limit its clinic application. The aim of this work is to use Solutol®HS15 (HS 15) as surfactant to develop novel micelle to enhance the oral bioavailability of DMY by improving its solubility and permeability. The DMY-loaded Solutol®HS15 micelles (DMY-Ms) were prepared by the thin-film hydration method. The particle size of DMY-Ms was 13.97 ± 0.82 nm with an acceptable polydispersity index of 0.197 ± 0.015. Upon entrapped in micelles, the solubility of DMY in water was increased more than 25-fold. The DMY-Ms had better sustained release property than that of pure DMY. In single-pass intestinal perfusion models, the absorption rate constant (Ka) and permeability coefficient (Papp) of DMY-Ms were 5.5-fold and 3.0-fold than that of pure DMY, respectively. The relative bioavailability of the DMY-Ms (AUC0-∞) was 205% compared with that of pure DMY (AUC0-∞), indicating potential for clinical application. After administering DMY-Ms, there was much lower blood alcohol level and shorter duration of the loss of righting relax (LORR) in drunk animals compared with that treated by pure DMY. In addition, the oral administration of DMY-Ms greatly reduced oxidative stress, and significantly defended liver and gastric mucosa from alcoholic damages in mice with alcohol-induced tissue injury. Taken together, HS 15-based micelle system greatly improves the bioavailability of DMY and represents a promising strategy for the management of acute alcoholism. Graphical abstract.


Assuntos
Intoxicação Alcoólica/tratamento farmacológico , Flavonóis/administração & dosagem , Flavonóis/uso terapêutico , Intoxicação Alcoólica/patologia , Animais , Área Sob a Curva , Disponibilidade Biológica , Depressores do Sistema Nervoso Central/sangue , Etanol/sangue , Excipientes , Flavonóis/farmacocinética , Mucosa Gástrica/patologia , Hepatite Alcoólica/prevenção & controle , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Micelas , Nanopartículas , Equilíbrio Postural/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley , Tensoativos
2.
Bioresour Technol ; 330: 124963, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33744735

RESUMO

Microbial surfactants are a large number of amphipathic biomolecules with a myriad of biomolecule constituents from various microbial sources that have been studied for their surface tension reduction activities. With unique properties, their applications have been increased in different areas including environment, medicine, healthcare, agriculture and industries. The present review aims to study the biochemistry and biosynthesis of biosurfactants exhibiting varying biomolecular structures which are produced by different microbial sources. It also provides details on roles played by biosurfactants in nature as well as their potential applications in various sectors. Basic biomolecule content of all the biosurfactants studied showed presence of carbohydrates, aminoacids, lipids and fattyacids. The data presented here would help in designing, synthesis and application of tailor-made novel biosurfactants. This would pave a way for perspectives of research on biosurfactants to overcome the existing bottlenecks in this field.


Assuntos
Agricultura , Tensoativos , Tensão Superficial
3.
Viruses ; 13(2)2021 02 20.
Artigo em Inglês | MEDLINE | ID: mdl-33672561

RESUMO

In the face of new emerging respiratory viruses, such as SARS-CoV2, vaccines and drug therapies are not immediately available to curb the spread of infection. Non-pharmaceutical interventions, such as mask-wearing and social distance, can slow the transmission. However, both mask and social distance have not prevented the spread of respiratory viruses SARS-CoV2 within the US. There is an urgent need to develop an intervention that could reduce the spread of respiratory viruses. The key to preventing transmission is to eliminate the emission of SARS-CoV2 from an infected person and stop the virus from propagating in the human population. Rhamnolipids are environmentally friendly surfactants that are less toxic than the synthetic surfactants. In this study, rhamnolipid products, 222B, were investigated as disinfectants against enveloped viruses, such as bovine coronavirus and herpes simplex virus 1 (HSV-1). The 222B at 0.009% and 0.0045% completely inactivated 6 and 4 log PFU/mL of HSV-1 in 5-10 min, respectively. 222B at or below 0.005% is also biologically safe. Moreover, 50 µL of 222B at 0.005% on ~1 cm2 mask fabrics or plastic surface can inactivate ~103 PFU HSV-1 in 3-5 min. These results suggest that 222B coated on masks or plastic surface can reduce the emission of SARS-CoV2 from an infected person and stop the spread of SARS-CoV2.


Assuntos
Coronavirus Bovino/efeitos dos fármacos , Desinfetantes/farmacologia , Glicolipídeos/farmacologia , Herpesvirus Humano 1/efeitos dos fármacos , Tensoativos/farmacologia , /prevenção & controle , Humanos
4.
Waste Manag ; 124: 339-347, 2021 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-33662765

RESUMO

The surfactant-assisted thermal hydrolysis pretreatment (THP) of waste activated sludge (WAS) was investigated, focusing on the effect of the surfactant addition on the results of sludge disintegration, dewaterability, organic release, and production of volatile fatty acids (VFAs) via fermentation. Typical anionic surfactant sodium dodecyl sulfate (SDS) and cationic surfactant cetyl trimethyl ammonium bromide (CTAB) were used for the THP experiments. The supernatant of the THP-treated sludge was anaerobically fermented to determine its potential VFAs yield. The results showed that the surfactant addition, particularly CTAB, enhanced the hydrolysis and organic solubilization of the sludge during THP. CTAB addition led to a 36% increase of dissolved organic and a 27% increase of VFAs production. For the THP-treated sludge with the surfactant addition, its dewaterability was also greatly improved. When the CTAB dosage increased from 0 to 0.10 g/g VSS, the minimum capillary suction time (CST) of the sludge decreased from 205 to 50 s/g TSS, and the sludge particles became smaller and less negative with the zeta potential changing from -12.4 to -8.2 mV. Analysis of extracellular polymeric substances (EPS) of the sludge revealed that the surfactant addition increased the sludge disintegration and organic dissolution during the THP process. The surfactant-assisted THP is shown to be a promising technology to enhance the WAS treatment for improved sludge dewaterability, waste reduction, and resource recovery.


Assuntos
Esgotos , Tensoativos , Ácidos Graxos Voláteis , Fermentação , Hidrólise , Eliminação de Resíduos Líquidos
5.
Chemosphere ; 271: 129818, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33736217

RESUMO

The use of carbohydrates, as a part of surface-active compounds, has been studied due to their biodegradability and nontoxic profile. A series of alkyl glycosides containing d-lyxose and l-rhamnose with alkyl chains of 8-12 carbon atoms were investigated. The effects of structural variations on their physico-chemical and biological properties have been evaluated for a detailed understanding of their properties. Alkyl glycosides were tested on their toxicity against bacterial cells of the genus Pseudomonas (MTT assay), microbiological adhesion to hydrocarbons (MATH assay), cell surface hydrophobicity (Congo red assay), cell membrane permeability (crystal violet assay), and bacterial biofilm formation. Furthermore, their antifungal activity against two pathogenic microorganisms Candida albicans and Aspergillus niger was investigated using the disc diffusion method. Toxicological studies revealed that compounds could reduce the metabolic activity of bacterial cells only moderately but they increased the hydrophobicity of cell surface in Pseudomonas strains. In addition, alkyl glycosides changed the permeability of the cell membranes to the level of 30-40% for this strain. The compounds with an even number of carbon atoms in their alkyl chain promoted stronger bacterial biofilm formation on the glass surface. All studied derivatives demonstrated very strong antifungal activity against fungus A. niger but very small effect against C. albicans. Overall, the results showed that long-chain alkyl glycosides could be considered as inexpensive, biocompatible, nontoxic agents, and serve for the surface design to avoid bacterial adhesion as an alternative solution to antibiotic treatment.


Assuntos
Anti-Infecciosos , Tensoativos , Antibacterianos/toxicidade , Anti-Infecciosos/toxicidade , Antifúngicos/toxicidade , Candida albicans , Testes de Sensibilidade Microbiana , Tensoativos/toxicidade
6.
Int J Nanomedicine ; 16: 1457-1472, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33654396

RESUMO

Purpose: Rheumatoid arthritis is an autoimmune disorder that directly affects joints. However, other body organs including heart, eyes, skin, blood vessels and lungs may also be affected. The purpose of this study was to design and evaluate a nanoemulgel formulation of diflunisal (DIF) and solubility enhanced diflunisal (DIF-IC) for enhanced topical anti-inflammatory activity. Methodology: Nanoemulsion formulations of both DIF and DIF-IC were prepared and incorporated in three different gelling agents, namely carboxymethylcellulose sodium (CMC-Na), sodium alginate (Na-ALG) and xanthan gum (XG). All the formulations were evaluated in term of particle size, pH, conductivity, viscosity, zeta potential and in vitro drug release. The formulation 2 (NE2) of both DIF and DIF-IC which expressed optimum release and satisfactory physicochemical properties was incorporated with gelling agents to produce final nanoemulgel formulations. The optimized nanoemulgel formulation was subjected to three different in vivo anti-inflammatory models including carrageenan-induced paw edema model, histamine-induced paw edema model and formalin-induced paw edema model. Results: DIF-IC-loaded nanoemulgel formulations yielded significantly enhanced in vitro skin permeation than DIF-loaded nanoemulgel. The nanoemulgel formulation of DIF-IC formulated with XG produced improved in vivo anti-inflammatory activity. Conclusion: It was recommended that DIF-IC-based nanoemulgel formulation prepared with XG could be a better option for effective topical treatment of inflammatory conditions.


Assuntos
Diflunisal/administração & dosagem , Sistemas de Liberação de Medicamentos , Emulsões/química , Nanogéis/química , Polietilenoglicóis/química , Polietilenoimina/química , Administração Tópica , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Carragenina , Diflunisal/química , Diflunisal/farmacologia , Diflunisal/uso terapêutico , Modelos Animais de Doenças , Composição de Medicamentos , Liberação Controlada de Fármacos , Edema/tratamento farmacológico , Edema/patologia , Condutividade Elétrica , Concentração de Íons de Hidrogênio , Masculino , Tamanho da Partícula , Permeabilidade , Transição de Fase , Ratos , Pele/efeitos dos fármacos , Absorção Cutânea/efeitos dos fármacos , Solubilidade , Tensoativos/química , Viscosidade
7.
Sheng Wu Gong Cheng Xue Bao ; 37(2): 615-624, 2021 Feb 25.
Artigo em Chinês | MEDLINE | ID: mdl-33645159

RESUMO

To effectively solve the serious impact of high oil in the kitchen wastewater on the downstream treatment process, an excellent oil-degrading strain Aeromonas allosaccarophila CY-01 was immobilized to prepare Chitosan-Aeromonas pellets (CH-CY01) by using chitosan as a carrier. Oil degradation condition and efficiency of CH-CY01 pellets were assessed. The growth of immobilized CH-CY01 was almost unaffected, and the maximum degradation rate of soybean oil was 89.7%. Especially at 0.5% NaCl concentration, oil degradation efficiency of CH-CY01 was increased by 20% compared with free cells. In the presence of a surfactant (sodium dodecylbenzene sulfonate) at 1 mg/L, the degradation efficiency of oil by CH-CY01 was increased by 40%. Moreover, using the high-oil catering wastewater as the substrate, more than 80% of the solid oil was degraded with 1% (V/V) CH-CY01 pellets treatment for 7 days, significantly higher than that of free cells. In summary, immobilized CH-CY01 significantly improved the efficiency of oil degradation.


Assuntos
Aeromonas , Quitosana , Tensoativos , Águas Residuárias
8.
Molecules ; 26(4)2021 Feb 11.
Artigo em Inglês | MEDLINE | ID: mdl-33670378

RESUMO

Biodegradable and antimicrobial waterborne polyurethane dispersions (PUDs) and their casted solid films have recently emerged as important alternatives to their solvent-based and non-biodegradable counterparts for various applications due to their versatility, health, and environmental friendliness. The nanoscale morphology of the PUDs, dispersion stability, and the thermomechanical properties of the solid films obtained from the solvent cast process are strongly dependent on several important parameters, such as the preparation method, polyols, diisocyanates, solid content, chain extension, and temperature. The biodegradability, biocompatibility, antimicrobial properties and biomedical applications can be tailored based on the nature of the polyols, polarity, as well as structure and concentration of the internal surfactants (anionic or cationic). This review article provides an important quantitative experimental basis and structure evolution for the development and synthesis of biodegradable waterborne PUDs and their solid films, with prescribed macromolecular properties and new functions, with the aim of understanding the relationships between polymer structure, properties, and performance. The review article will also summarize the important variables that control the thermomechanical properties and biodegradation kinetics, as well as antimicrobial and biocompatibility behaviors of aqueous PUDs and their films, for certain industrial and biomedical applications.


Assuntos
Anti-Infecciosos/química , Plásticos Biodegradáveis/química , Polímeros/química , Poliuretanos/química , Ânions/química , Ânions/uso terapêutico , Anti-Infecciosos/uso terapêutico , Plásticos Biodegradáveis/uso terapêutico , Humanos , Polímeros/uso terapêutico , Poliuretanos/uso terapêutico , Solventes/química , Tensoativos/química , Tensoativos/uso terapêutico , Água/química
9.
Molecules ; 26(4)2021 Feb 17.
Artigo em Inglês | MEDLINE | ID: mdl-33671247

RESUMO

In the present study, naphthyl acetohydrazide (HL) ligand was prepared and used for the synthesis of new six amorphous transition metal (Co(II), Ni(II), Cu(II), Zn(II), Pb(II), Cd(II)) complexes. All the compounds were characterized by elemental analysis, UV-vis, FT-IR, 1H- and 13C-NMR, and Matrix-Assisted Laser Desorption Ionization (MALDI). The solubilization study was carried out by estimating the interaction between the metal complexes with surfactants viz. sodium stearate (SS) and Cetyltrimethylammonium bromide (CTAB). UV-Visible spectroscopy was employed to determine partitioning and binding parameters, whereas electrical conductivity measurements were employed to estimate critical micellar concentration (CMC), the extent of dissociation, and free energy of micellization. The CT-DNA interaction of synthesized compounds with DNA represents the major groove binding. The synthesized ligand and metal complexes were also tested against bacterial and fungal strains and it has been observed that Cu(II) complex is active against all the strains except Candida albicans, while Cd(II) complex is active against all bacterial and fungal strains except Pseudomonas. Among all compounds, only the Pd(II) complex shows reasonable activity against cervical cancer HeLa cell lines, representing 97% inhibition.


Assuntos
Anti-Infecciosos/farmacologia , Complexos de Coordenação/síntese química , DNA/metabolismo , Hidrazonas/síntese química , Hidrazonas/farmacologia , Metais/química , Micelas , Neoplasias/patologia , Bactérias/efeitos dos fármacos , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Sobrevivência Celular/efeitos dos fármacos , Condutividade Elétrica , Células HeLa , Humanos , Hidrazonas/química , Ligantes , Testes de Sensibilidade Microbiana , Espectroscopia de Prótons por Ressonância Magnética , Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Tensoativos/química
10.
Food Chem ; 350: 129275, 2021 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-33601090

RESUMO

Oleofoams have emerged as attractive low-calorie aeration systems, but saturated lipids or large amount of surfactants are commonly required. Herein, an innovative strategy was proposed to create oleofoams using medium-long chain diacylglycerol (MLCD) and ß-sitosterol (St). The oleofoams prepared using MLCD and St in ratios of 15:5 and 12:8 exhibited smaller bubble size and much higher stability. MLCD crystals formed rigid Pickering shell, whereby air bubbles acted as "active fillers" leading to enhanced rigidity. Both Pickering and network stabilization for the MLCD-St oleofoam provided a steric hindrance against coalescence. The gelators interacted via hydrogen bonding, causing a condensing effect in improving the gel elasticity. The oleofoams and foam-based emulsions exhibited a favorable capacity in controlling volatile release where the maximum headspace concentrations and partition coefficients showed a significantly decrease. Overall, the oleofoams have shown great potential for development of low-calorie foods and delivery systems with enhanced textural and nutritional features.


Assuntos
Diglicerídeos/química , Sitosteroides/química , Ligação de Hidrogênio , Tensoativos/química
11.
Environ Pollut ; 276: 116742, 2021 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-33621735

RESUMO

Biodiesel side stream waste glycerol was identified as a cheap carbon source for rhamnolipids (RLs) production which at the same time could improve the management of waste. The present study aimed to produce RLs by using Pseudomonas aeruginosa RS6 utilizing waste glycerol as a substrate and to evaluate their physico-chemicals properties. Fermentation conditions such as temperature, initial medium pH, waste glycerol concentration, nitrogen sources and concentrations resulted in different compositions of the mono- and di-RLs produced. The maximum RLs production of 2.73 g/L was obtained when P. aeruginosa RS6 was grown in a basal salt medium supplemented with 1% waste glycerol and 0.2 M sodium nitrate at 35 °C and pH 6.5. At optimal fermentation conditions, the emulsification index (E24) values of cooking oil, diesel oil, benzene, olive oil, petroleum, and kerosene were all above E24=50%. The surface tension reduction obtained from 72.13 mN/m to 29.4-30.4 mN/m was better than the surface activity of some chemical-based surfactants. The RLs produced possessed antimicrobial activities against Gram-negative and Gram-positive bacteria with values ranging from 37% to 77% of growth inhibition when 1 mg/mL of RLs was used. Concentrations of RLs below 1500 µg/mL did not induce phytotoxicity effects on the tested seeds (Vigna radiata) compared to the chemical-based- surfactant, SDS. Furthermore, RLs tested on zebrafish (Danio rerio) embryos only exhibited low acute toxicity with an LC50 value of 72.97 µg/mL at 48 h of exposure suggesting a green and eco-biochemical worthy of future applications to replace chemical-based surfactants.


Assuntos
Glicerol , Pseudomonas aeruginosa , Animais , Biocombustíveis , Glicolipídeos , Rios , Tensoativos , Peixe-Zebra
12.
Med Hypotheses ; 148: 110508, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33571758

RESUMO

Several studies have reported that certain psychoactive drugs could have a protective effect against SARS-CoV-2. Herein, we propose that antihistamines (anti-H1) and cationic amphiphilic drugs (CAD), specifically, have the capacity to disrupt virus entry and replication. In addition, several of these molecules have limited side effects and as such could be promising prophylactic candidates against SARS-CoV-2 infection.


Assuntos
/tratamento farmacológico , Antagonistas dos Receptores Histamínicos H1/farmacologia , Tensoativos/farmacologia , /virologia , Reposicionamento de Medicamentos , Humanos , Modelos Biológicos , Pandemias , /fisiologia , Internalização do Vírus/efeitos dos fármacos , Replicação Viral/efeitos dos fármacos
13.
ACS Appl Mater Interfaces ; 13(7): 7825-7838, 2021 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-33583172

RESUMO

Fabry disease is a rare lysosomal storage disorder characterized by a deficiency of α-galactosidase A (GLA), a lysosomal hydrolase. The enzyme replacement therapy administering naked GLA shows several drawbacks including poor biodistribution, limited efficacy, and relatively high immunogenicity in Fabry patients. An attractive strategy to overcome these problems is the use of nanocarriers for encapsulating the enzyme. Nanoliposomes functionalized with RGD peptide have already emerged as a good platform to protect and deliver GLA to endothelial cells. However, low colloidal stability and limited enzyme entrapment efficiency could hinder the further pharmaceutical development and the clinical translation of these nanoformulations. Herein, the incorporation of the cationic miristalkonium chloride (MKC) surfactant to RGD nanovesicles is explored, comparing two different nanosystems-quatsomes and hybrid liposomes. In both systems, the positive surface charge introduced by MKC promotes electrostatic interactions between the enzyme and the nanovesicles, improving the loading capacity and colloidal stability. The presence of high MKC content in quatsomes practically abolishes GLA enzymatic activity, while low concentrations of the surfactant in hybrid liposomes stabilize the enzyme without compromising its activity. Moreover, hybrid liposomes show improved efficacy in cell cultures and a good in vitro/in vivo safety profile, ensuring their future preclinical and clinical development.


Assuntos
Terapia de Reposição de Enzimas , Doença de Fabry/terapia , Nanoestruturas/química , alfa-Galactosidase/metabolismo , Doença de Fabry/enzimologia , Humanos , Oligopeptídeos/química , Tamanho da Partícula , Propriedades de Superfície , Tensoativos/química
14.
Int J Nanomedicine ; 16: 905-924, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33603359

RESUMO

Purpose: The purpose of this proposed research was to investigate a nano-formulation developed using self-nanoemulsifying drug delivery system (SNEDDS) to improve the pharmacodynamic potential of rosuvastatin by assisting its transportation through lymphatic circulation. Methods: The utilized lipids, surfactants, and co-surfactants for SNEDDS were selected on the basis of solubility studies. The SNEDDS formulation was optimized by implementing a D-optimal mixture design, wherein the effect of concentration of Capmul MCM EP (X1), Tween 20 (X2) and Transcutol P (X3) as independent variables was studied on droplet size (Y1), % cumulative drug release (Y2) and self-emulsification time (Y3) as dependent variables. The optimized formulation was evaluated via in vitro parameters and in vivo pharmacodynamic potential in Wistar rats. Results: The D-optimal mixture design and subsequent ANOVA application resulted in the assortment of the optimized SNEDDS formulation that exhibited a droplet size of nano range (14.91nm), in vitro drug release of >90% within 30 minutes, and self-emulsification time of 16 seconds. The in vivo pharmacodynamic study carried out using Wistar rats confirmed the better antihyperlipidemic potential of developed formulation in normalizing the lipidic level of serum in contrast to pure drug and marketed tablets. Conclusion: This research reports the application of D-optimal mixture design for successful and systematic development of rosuvastatin-loaded SNEDDS with distinctly enhanced in vitro and in vivo performance in comparison to marketed formulation. Eventually, improved anti-hyperlipidemic efficacy was envisaged which might be attributed to increased drug solubility and absorption. Overall, this study shows the utility of SNEDDS for improving the dissolution rate and bioavailability of poor aqueous-soluble drugs. The present SNEDDS formulation could be a promising approach and alternative to conventional dosage form.


Assuntos
Sistemas de Liberação de Medicamentos , Emulsões/química , Nanopartículas/química , Rosuvastatina Cálcica/farmacologia , Análise de Variância , Animais , Disponibilidade Biológica , Varredura Diferencial de Calorimetria , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Lipídeos/química , Masculino , Nanopartículas/ultraestrutura , Tamanho da Partícula , Transição de Fase , Ratos Wistar , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Eletricidade Estática , Tensoativos/química , Comprimidos , Viscosidade
15.
Int J Nanomedicine ; 16: 1245-1259, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33633449

RESUMO

Purpose: To enhance the oral bioavailability of revaprazan (RVP), a novel solid, supersaturable micelle (SSuM) was developed. Methods: Surfactants and solid carriers were screened based on a solubility and a flowability test, respectively. Supersaturating agents, including Poloxamer 407 (P407), were screened. The SSuM was optimized using a Box-Behnken design with three independent variables, including Gelucire 44/14:Brij L4 (G44/BL4; X1) and the amounts of Florite PS-10 (FLO; X2) and Vivapur 105 (VP105; X3), and three response variables, ie, dissolution efficiency at 30 min (Y1), dissolution enhancing capacity (Y2), and Carr's index (Y3). The solid state property was evaluated, and a dissolution test was conducted. RVP, Revanex®, solid micelle (P407-free from the composition of SSuM), and SSuM were orally administrated to rats (RVP 20 mg equivalent/kg) for in vivo pharmacokinetic study. Results: G44 and BL4 showed great solubility, with a critical micelle concentration range of 119.2-333.0 µg/mL. P407 had an excellent supersaturating effect. FLO and VP105 were selected as solid carriers, with a critical solidifying ratio (g/mL) of 0.30 and 0.91, respectively. With optimized values of X1 (-0.41), X2 (0.31), and X3 (-0.78), RVP (200 mg)-containing SSuM consisting of G44 (253.8 mg), BL4 (106.2 mg), FLO (99.3 mg), VP105 (199.8 mg), and P407 (40 mg) was developed, resulting in Y1 (40.3%), Y2 (0.008), and Y3 (12.3%). RVP existed in an amorphous state in the optimized SSuM, and the SSuM formed a nanosized dispersion in the aqueous phase, with approximately 71.7% dissolution at 2 h. The optimized SSuM improved the relative bioavailability of RVP in rats by approximately 478%, 276%, and 161% compared to raw RVP, Revanex®, and solid micelle, respectively. Conclusion: The optimized SSuM has great potential for the development of solidified formulations of poorly water-soluble drugs with improved oral absorption.


Assuntos
Micelas , Pirimidinonas/farmacologia , Tetra-Hidroisoquinolinas/farmacologia , Administração Oral , Animais , Disponibilidade Biológica , Composição de Medicamentos , Masculino , Modelos Teóricos , Tamanho da Partícula , Polietilenoglicóis , Pirimidinonas/farmacocinética , Ratos Sprague-Dawley , Solubilidade , Soluções , Tensoativos/química , Tetra-Hidroisoquinolinas/farmacocinética
16.
Sci Adv ; 7(6)2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-33547083

RESUMO

The profound consequences of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) mandate urgent development of effective vaccines. Here, we evaluated an Amphiphile (AMP) vaccine adjuvant, AMP-CpG, composed of diacyl lipid-modified CpG, admixed with the SARS-CoV-2 Spike-2 receptor binding domain protein as a candidate vaccine (ELI-005) in mice. AMP modification efficiently delivers CpG to lymph nodes, where innate and adaptive immune responses are generated. Compared to alum, immunization with AMP-CpG induced >25-fold higher antigen-specific T cells that produced multiple T helper 1 (TH1) cytokines and trafficked into lung parenchyma. Antibody responses favored TH1 isotypes (IgG2c and IgG3) and potently neutralized Spike-2-ACE2 receptor binding, with titers 265-fold higher than natural convalescent patient COVID-19 responses; T cell and antibody responses were maintained despite 10-fold dose reduction in Spike antigen. Both cellular and humoral immune responses were preserved in aged mice. These advantages merit clinical translation to SARS-CoV-2 and other protein subunit vaccines.


Assuntos
/administração & dosagem , Imunidade Celular , Imunidade Humoral , Linfonodos/imunologia , Tensoativos/administração & dosagem , Adjuvantes Imunológicos/administração & dosagem , Animais , Anticorpos Neutralizantes/imunologia , Anticorpos Antivirais/imunologia , /imunologia , Feminino , Células HEK293 , Humanos , Imunogenicidade da Vacina , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos C57BL , Testes de Neutralização , Oligodesoxirribonucleotídeos/administração & dosagem , Oligodesoxirribonucleotídeos/imunologia , Domínios e Motivos de Interação entre Proteínas/imunologia , Glicoproteína da Espícula de Coronavírus/química , Glicoproteína da Espícula de Coronavírus/imunologia , Resultado do Tratamento , Vacinação/métodos , Vacinas de Subunidades/imunologia
19.
Ecotoxicol Environ Saf ; 212: 111964, 2021 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-33524909

RESUMO

A systematic study had been carried out to get insight into the micellar behavior of anionic lipopeptide (LT) and nonionic sophorolipid (SL) in their different mass ratio mixed state using the technique of tensiometry. The models proposed by Clint, Rubingh and Gibbs et al. had been employed to interpret the formation of mixed micelles and found out synergism. The obtained experimental critical micelle concentrations (CMC) were lower than the ideal CMCs, indicating negative deviation from ideal behavior for all multi-component mixed micelles formation. A suited binary bio-surfactant mixing system was selected as the washing agents to treat the oily sludge produced from Huabei oilfield by the thermal bio-surfactant washing method. The results showed that in case of the mass ratios of 8:2 the CMC was dramatically decreased and synergism was the strongest in LT and SL bi mixed surfactant systems. The studied binary mixed bio-surfactant system showed higher washing efficiency for oily sludge than single surfactant system. In addition, the washing power of binary mixed bio-surfactants towards oily sludge was the best at below washing conditions: (a) the concentration of the mixed system (100 mg/L), (b) temperature (55 â„ƒ), (c) ratio of sludge/liquid (1:3), (d) washing time (3 h), and (e) stirring speed (300 rpm). Certainly, the washing abilities of the selected surfactants not only depend on their mixing ratio and washing conditions but also associate with microstructure and mineral components of oily sludge.


Assuntos
Recuperação e Remediação Ambiental/métodos , Campos de Petróleo e Gás , Surfactantes Pulmonares , Lipopeptídeos , Micelas , Ácidos Oleicos , Esgotos , Tensoativos/química
20.
J Environ Sci (China) ; 102: 363-372, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33637261

RESUMO

The pollution characteristics of surfactant substances in fine particles (PM2.5) in spring were studied in the Beibu Gulf Region of China, 68 samples of PM2.5 were collected at Weizhou Island in Beihai City from March 12 to April 17, 2015. The Anionic Surfactant Substances (ASS) and Cationic Surfactant Substances (CSS) in the samples were analyzed using Byethyl Violet Spectrophotometry and Disulfide Blue Spectrophotometry, respectively. Combined with the data from backward trajectory simulation, the effects of air pollutants from remote transport on the pollution characteristics of surfactant substances in PM2.5 in the Beibu Gulf Region were analyzed and discussed. The results showed that the daily mean concentrations of ASS and CSS in spring in the Beibu Gulf Region were 165.20 pmol/m3 and 8.05pmol/m3, and the variation ranges were 23.21-452.55 pmol/m3 and 0.65-31.31 pmol/m3, accounting for 1.82‰ ± 1.65‰ and 0.12‰ ± 0.11‰ of the mass concentration of PM2.5, respectively. These concentrations were lower than those in comparable regions around the world. There was no clear correlation between the concentrations of ASS and CSS in PM2.5 and the mass concentrations of PM2.5. Tourism and air transport had a positive contribution on the concentrations of ASS. The concentration of surfactant substances in PM2.5 was significantly impacted by wind speed and wind direction. Atmospheric temperature, air pressure and precipitation had little effect on the concentrations of surfactant substances. Surfactant substances in PM2.5 significantly impacted visibility. Results also showed that the main sources of surfactant substances were from the southern China and Southeast Asia.


Assuntos
Poluentes Atmosféricos , Poluição do Ar , Poluentes Atmosféricos/análise , Poluição do Ar/análise , China , Cidades , Monitoramento Ambiental , Material Particulado/análise , Estações do Ano , Tensoativos
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