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1.
Nanotechnology ; 34(26)2023 Apr 12.
Artículo en Inglés | MEDLINE | ID: mdl-36972569

RESUMEN

Plasma-based sputtering onto liquids (SoL) is a straightforward approach for synthesizing small metal nanoparticles (NPs) without additional stabilizing reagents. In this work, nonionic surfactant Triton X-100 was used for the first time as a host liquid for the SoL process and the production of colloidal solutions of gold, silver and copper NPs was demonstrated. The average diameter of spherical Au NPs lies in the range from 2.6 to 5.5 nm depending on the conditions. The approach presented here opens the pathway to the production of concentrated dispersions of metal NPs of high purity that can be dispersed in water for future usage, therefore extending further the reach of this synthesis pathway.

2.
Nano Lett ; 22(21): 8574-8583, 2022 Nov 09.
Artículo en Inglés | MEDLINE | ID: mdl-36279311

RESUMEN

A highly stable interface for aqueous rechargeable Zn batteries is of importance to inhibit the growth of Zn dendrites and suppress the side reactions. In this work, we have developed a stable honeycomb-like ZnO passivation protective layer on the Zn surface, which is in situ generated with the assistance of a nonionic surfactant additive (polyethylene glycol tert-octylphenyl ether, denoted as PEGTE). The ZnO passivation layer can facilitate the uniform distribution of the electric field, guiding the uniform deposition of Zn2+ and inhibit the generation of dendrites. As a result, the symmetric cell using the electrolyte with PEGTE shows an excellent performance at high areal capacity, reflected by stable cycling for over 2400 h at 5 mAh/cm2 and 1300 h at 10 mAh/cm2. The full cell paired with V2O5 demonstrates a long lifespan for more than 600 cycles at a low negative/positive capacity ratio.

3.
Molecules ; 28(9)2023 May 08.
Artículo en Inglés | MEDLINE | ID: mdl-37175362

RESUMEN

Owing to their surface active properties, surfactants have numerous applications in different fields of life. In the present research work, the solubilization of reactive red 2 (RR2) has been studied in single and mixed micellar systems (MMS) using UV-visible spectroscopy and electrical conductivity measurements. The interaction of RR2 with ionic micelles of cetylpyridinium chloride (CPC) was investigated. In order to probe the interaction of RR2 in MMS, mixtures of CPC and TX-114 (Triton X-114, a nonionic surfactant) were used. UV-visible spectroscopy has been used to obtain the degree of solubilization of RR2 in terms of the partition coefficient (Kc) and Gibbs free energy of partitioning (ΔG°p). Electrical conductivity data have been employed to detect the critical micelle concentration (CMC) of the surfactant systems in the presence of RR2 and, accordingly, to calculate the thermodynamic parameters of the micellization. From the obtained data, it is concluded that the micellization is spontaneous at all studied temperatures. Moreover, the micellization was observed to be driven by both enthalpy and entropy. The results also indicated that MMS have better solubilizing power than single micellar solutions.

4.
Molecules ; 28(12)2023 Jun 13.
Artículo en Inglés | MEDLINE | ID: mdl-37375302

RESUMEN

Inhalable coal dust poses a serious threat to coal mining safety, air quality, and the health of miners. Therefore, the development of efficient dust suppressants is crucial for addressing this issue. This study evaluated the ability of three high-surface-active OPEO-type nonionic surfactants (OP4, OP9, and OP13) to improve the wetting properties of anthracite via extensive experiments and a molecular simulation and determined the micro-mechanism of different wetting properties. The surface tension results show that OP4 has the lowest surface tension (27.182 mN/m). Contact angle tests and wetting kinetics models suggest that OP4 exhibits the strongest wetting improvement ability on raw coal with the smallest contact angle (20.1°) and the fastest wetting rate. In addition, FTIR and XPS experimental results also reveal that OP4-treated coal surfaces introduce the most hydrophilic elements and groups. UV spectroscopy testing shows that OP4 has the highest adsorption capacity on the coal surface, reaching 133.45 mg/g. The surfactant is adsorbed on the surface and pores of anthracite, while the strong adsorption ability of OP4 results in the least amount of N2 adsorption (8.408 cm3/g) but the largest specific surface area (1.673 m2/g). In addition, the filling behavior and aggregation behavior of surfactants on the anthracite coal surface were observed using SEM. The MD simulation results indicate that OPEO reagents with overly long hydrophilic chains would produce spatial effects on the coal surface. Under the influence of the π-π interaction between the hydrophobic benzene ring and the coal surface, OPEO reagents with fewer ethylene oxide quantities are more prone to adsorb onto the coal surface. Therefore, after the adsorption of OP4, both the polarity and the water molecule adhesion ability of the coal surface are greatly enhanced, which helps to suppress dust production. These results provide important references and a foundation for future designs of efficient compound dust suppressant systems.

5.
Molecules ; 27(15)2022 Jul 23.
Artículo en Inglés | MEDLINE | ID: mdl-35897880

RESUMEN

The wetting properties of the rhamnolipid and surfactin mixtures with Triton X-165 were considered based on the contact angle measurements of their aqueous solution on the polytetrafluoroethylene (PTFE), polymethyl methacrylate (PMMA) and quartz (Q) surfaces. The obtained contact angle isotherms were described by the exponential function of the second order as well as by Szyszkowski equation in some cases. Using the contact angle isotherms of individual biosurfactants and TX165 as well as the earlier obtained isotherms of their surface tension the contact angle isotherms of the biosurfactants mixtures with TX165 were deduced. As follows the presence of the maxima on the contact angle isotherms of the biosurfactants mixtures with TX165 is justified. They do not prove negative adsorption of the biosurfactant and TX165 at the interfaces. However, the mutual exchange of the biosurfactant and TX165 molecules is observed in the layers at the interfaces. The concentration of the studied mixtures at the PTFE-solution interface was established to be close to that at the solution-air one but that at the PTFE-air is equal to zero. However, the concentration of the studied mixtures at the PMMA-solution and quartz-solution is greater than zero. The concentration at the PMMA(quartz)-air and PMMA(quartz)-solution interfaces is smaller than that at the solution-air one.


Asunto(s)
Polimetil Metacrilato , Cuarzo , Derivados del Benceno , Glucolípidos , Polietilenglicoles , Politetrafluoroetileno , Tensoactivos
6.
Molecules ; 27(21)2022 Nov 02.
Artículo en Inglés | MEDLINE | ID: mdl-36364294

RESUMEN

Detergent formulations for cleaning a carbonized soil­degreasers­typically comprise surfactants, organic solvents, phosphate-based cleaning agents, and alkaline agents, which results in high pH values (>11) that raise human and environmental risks. It is important to develop eco-friendly and safer degreasers, while maintaining their cleaning efficiency. In this work, simple degreaser formulations, with a pH below 11 and without phosphates, were developed by using a mixture of solvent, surfactant, and water to remove carbonized soil. The efficiency of the new degreaser formulations (with 5 wt% solvent, 5 wt% nonionic or ionic surfactant, and 90 wt% water) was evaluated by an abrasion test in the removal of carbonized soil from ceramic and stainless steel surfaces and compared with a commercial product. The results obtained show that the formulations comprising isopropylene glycol (IPG) with C11−C13 9EOs and diethylene glycol butyl ether (BDG) with octyltrimethylammonium octanoate ([N1118][C8O2]) present the best cleaning efficiency for both surfaces. The composition of these formulations was optimized for each surface using a mixture design. The resulting formulations, despite having a simpler composition, a pH lower than 11, and being phosphate-free, presented a cleaning efficiency equal or slightly higher than the commercial control. These results show that it is possible to design degreasers that are much less aggressive to the environment and user, while simultaneously fulfilling the market requirements.


Asunto(s)
Detergentes , Suelo , Humanos , Tensoactivos/química , Agua , Solventes
7.
Mol Pharm ; 18(12): 4354-4370, 2021 12 06.
Artículo en Inglés | MEDLINE | ID: mdl-34807627

RESUMEN

Type III lipid-based formulations (LBFs) combine poorly water-soluble drugs with oils, surfactants, and cosolvents to deliver the drugs into the systemic circulation. However, the solubility of the drug can be influenced by the colloidal phases formed in the gastrointestinal tract as the formulation is dispersed and makes contact with bile and other materials present within the GI tract. Thus, an understanding of the phase behavior of LBFs in the gut is critical for designing efficient LBFs. Molecular dynamics (MD) simulation is a powerful tool for the study of colloidal systems. In this study, we modeled the internal structures of five type III LBFs of loratadine containing poly(ethylene oxide) nonionic surfactants polysorbate 80 and polyoxyl hydrogenated castor oil (Kolliphor RH40) using long-timescale MD simulations (0.4-1.7 µs). We also conducted experimental investigations (dilution of formulations with water) including commercial Claritin liquid softgel capsules. The simulations show that LBFs form continuous phase, water-swollen reverse micelles, and bicontinuous and phase-separated systems at different dilutions, which correlate with the experimental observations. This study supports the use of MD simulation as a predictive tool to determine the fate of LBFs composed of medium-chain lipids, polyethylene oxide surfactants, and polymers.


Asunto(s)
Lípidos/química , Loratadina/química , Tensoactivos/química , Composición de Medicamentos , Excipientes/química , Simulación de Dinámica Molecular , Polisorbatos/química , Agua/química
8.
Int J Med Sci ; 18(6): 1363-1374, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33628092

RESUMEN

Introduction: Acute lung injury (ALI) has a great impact and a high mortality rate in intensive care units (ICUs). Excessive air may enter the lungs, causing pulmonary air embolism (AE)-induced ALI. Some invasive iatrogenic procedures cause pulmonary AE-induced ALI, with the presentation of severe inflammatory reactions, hypoxia, and pulmonary hypertension. Pulmonary surfactants are vital in the lungs to reduce the surface tension and inflammation. Nonionic surfactants (NIS) are a kind of surfactants without electric charge on their hydrophilic parts. Studies on NIS in AE-induced ALI are limited. We aimed to study the protective effects and mechanisms of NIS in AE-induced ALI. Materials and methods: Five different groups (n = 6 in each group) were created: sham, AE, AE + NIS pretreatment (0.5 mg/kg), AE + NIS pretreatment (1 mg/kg), and AE + post-AE NIS (1 mg/kg). AE-induced ALI was introduced by the infusion of air via the pulmonary artery. Aerosolized NIS were administered via tracheostomy. Results: Pulmonary AE-induced ALI showed destruction of the alveolar cell integrity with increased pulmonary microvascular permeability, pulmonary vascular resistance, pulmonary edema, and lung inflammation. The activation of nuclear factor-κB (NF-κB) increased the expression of pro-inflammatory cytokines, and sodium-potassium-chloride co-transporter isoform 1 (NKCC1). The pretreatment with NIS (1 mg/kg) prominently maintained the integrity of the epithelial lining and suppressed the expression of NF-κB, pro-inflammatory cytokines, and NKCC1, subsequently reducing AE-induced ALI. Conclusions: NIS maintained the integrity of the epithelial lining and suppressed the expression of NF-κB, pro-inflammatory cytokines, and NKCC1, thereby reducing hyperpermeability, pulmonary edema, and inflammation in ALI.


Asunto(s)
Lesión Pulmonar Aguda/prevención & control , Alveolos Pulmonares/efectos de los fármacos , Embolia Pulmonar/tratamiento farmacológico , Mucosa Respiratoria/efectos de los fármacos , Tensoactivos/administración & dosificación , Lesión Pulmonar Aguda/etiología , Lesión Pulmonar Aguda/patología , Administración por Inhalación , Aerosoles , Animales , Citocinas/metabolismo , Modelos Animales de Enfermedad , Humanos , Inflamación/tratamiento farmacológico , Inflamación/inmunología , Inflamación/patología , Masculino , FN-kappa B/metabolismo , Alveolos Pulmonares/metabolismo , Embolia Pulmonar/complicaciones , Embolia Pulmonar/patología , Ratas , Mucosa Respiratoria/metabolismo , Mucosa Respiratoria/ultraestructura , Transducción de Señal/efectos de los fármacos , Transducción de Señal/inmunología
9.
Luminescence ; 36(7): 1638-1647, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-34142436

RESUMEN

The aim of the present work was the preparation of Li/Al nanoparticles (NPs) functionalized with graphene oxide quantum dots (GOQDs) for the controlled release of chlorpheniramine maleate (CPAM). The role of lemon and egg white extracts as oxidation agents were investigated for the morphology and particle size of the products. GOQDs were synthesized using green, environmentally friendly, and cost-effective precursors. This work demonstrates that Li/Al NPs functionalized with graphene oxide as a nanolayer structure can be used as efficient nanocarriers for loading and delivery of CPAM as water-insoluble aromatic drugs The final products were identified with X-ray diffraction, scanning electron microscopy, atomic force microscopy, ultraviolet-visible spectroscopy, dynamic light scattering, thermogravimetric analysis, and transmission electron microscopy nitrogen adsorption [i.e. Brunauer-Emmett-Teller (BET) surface area analysis] techniques. The calibration curve for Li/Al nanoparticles functionalized with GOQDs for controlled released of CPAM was calculated as y = 0.0137x + 0.0103 with R2  = 0.9995. The data found through BET and Barrett-Joyner-Halenda analysis using the adsorption/desorption isotherm method demonstrated by total pore volumes and dead volume were calculated respectively as 0.162 nm2 , 0.0439 cm3 g-1 . The mean pore diameter was calculated as 20.33 nm using BET isotherm data.


Asunto(s)
Nanoestructuras , Puntos Cuánticos , Clorfeniramina , Grafito , Liposomas , Tensoactivos
10.
J Food Sci Technol ; 57(9): 3259-3266, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-32728274

RESUMEN

Lipid nanocarrier displays the advantages over conventional drug carriers as they are formulated with biodegradable and non-irritant lipids. However, the main drawbacks are the agglomeration of lipid particles, instability over storage, low drug loading, and the burst release of active ingredients. In this study, we investigated the effects of various polysorbate nonionic surfactants namely Tween 20, 40, 60, or 80 on the nanostructured lipid carrier (NLC). NLC incorporated with polysorbate nonionic surfactant was prepared by using high-pressure homogenization technique. The average size was reduced to 139.9 ± 15.8 nm in the presence of Tween 80 and remained stable in nano-size even incubated for 28 days. Encapsulation of l-ascorbic acid or Gold Tri.E 30 showed a high encapsulation efficiency of more than 75%, where the highest was Gold Tri.E in the presence of Tween 60 at 99.7%. In vitro release study showed that the release of both l-ascorbic acid and Gold Tri.E was significantly reduced in NLC with Tween as compared to bare active ingredients and NLC without Tween. In conclusion, the incorporation of Tween successfully produced a lipid nanocarrier that has the potential to be developed as a carrier of various active ingredients such as nutrients, extracts, and drugs.

11.
Mol Pharm ; 16(2): 618-631, 2019 02 04.
Artículo en Inglés | MEDLINE | ID: mdl-30608696

RESUMEN

Amphipathic, nonionic, surfactants are widely used in pharmaceutical, food, and agricultural industry to enhance product features; as pharmaceutical excipients, they are also aimed at increasing cell membrane permeability and consequently improving oral drugs absorption. Here, we report on the concentration- and time-dependent succession of events occurring throughout and subsequent exposure of Caco-2 epithelium to a "typical" nonionic surfactant (Kolliphor HS15) to provide a molecular explanation for nonionic surfactant cytotoxicity. The study shows that the conditions of surfactant exposure, which increase plasma membrane fluidity and permeability, produced rapid (within 5 min) redox and mitochondrial effects. Apoptosis was triggered early during exposure (within 10 min) and relied upon an initial mitochondrial membrane hyperpolarization (5-10 min) as a crucial step, leading to its subsequent depolarization and caspase-3/7 activation (60 min). The apoptotic pathway appears to be triggered prior to substantial surfactant-induced membrane damage (observed ≥60 min). We hence propose that the cellular response to the model nonionic surfactant is triggered via surfactant-induced increase in plasma membrane fluidity, a phenomenon akin to the stress response to membrane fluidization induced by heat shock, and consequent apoptosis. Therefore, the fluidization effect that confers surfactants the ability to enhance drug permeability may also be intrinsically linked to the propagation of their cytotoxicity. The reported observations have important implications for the safety of a multitude of nonionic surfactants used in drug delivery formulations and to other permeability enhancing compounds with similar plasma membrane fluidizing mechanisms.


Asunto(s)
Excipientes/efectos adversos , Polietilenglicoles/farmacología , Estearatos/farmacología , Apoptosis/efectos de los fármacos , Células CACO-2 , Caspasa 3/metabolismo , Caspasa 7/metabolismo , Permeabilidad de la Membrana Celular/efectos de los fármacos , Humanos , Oxidación-Reducción/efectos de los fármacos , Polietilenglicoles/efectos adversos , Estearatos/efectos adversos
12.
AAPS PharmSciTech ; 20(5): 203, 2019 May 28.
Artículo en Inglés | MEDLINE | ID: mdl-31139965

RESUMEN

D-α-Tocopheryl polyethylene glycol succinate (TPGS), a polyethylene glycol condensate, is a biologically important nonionic amphiphile. In this study, we report on aqueous solution behavior of TPGS with a focus on its clouding, surface activity, micellar characteristics, and solubilization capacity for a model hydrophobic drug, carbamazepine (CBZ). Micelles were characterized by dynamic light and small-angle neutron scattering studies as a function of temperature, salt addition, and CBZ solubilization. TPGS showed a cloud point of 78°C and possessed good surface activity (as observed from surface tension reduction and adsorption parameters). The critical micelle concentration (CMC), obtained from surface tension and fluorescence studies, was 0.02 mM. Scattering studies showed formation of stable micelles (average diameter-12 nm), exhibiting no significant changes in size upon salt addition (up to 1 M NaCl), CBZ incorporation (up to 5 mM), and temperature increase (40°C). Micelles in 5 wt% TPGS showed about twentyfold enhancement in CBZ solubility. Considering the remarkable CBZ solubilization and its positioning in the core, we suggest that the formulation can be exploited as a sustained delivery vehicle.


Asunto(s)
Carbamazepina/química , Portadores de Fármacos/química , Micelas , Temperatura , Vitamina E/química , Anticonvulsivantes/química , Anticonvulsivantes/farmacocinética , Carbamazepina/farmacocinética , Relación Dosis-Respuesta a Droga , Portadores de Fármacos/farmacocinética , Electrólitos/química , Electrólitos/farmacocinética , Excipientes/química , Excipientes/farmacocinética , Interacciones Hidrofóbicas e Hidrofílicas , Dispersión del Ángulo Pequeño , Solubilidad , Vitamina E/farmacocinética
13.
World J Microbiol Biotechnol ; 35(1): 13, 2019 Jan 02.
Artículo en Inglés | MEDLINE | ID: mdl-30603886

RESUMEN

Filamentous fungi Monascus sp. has been utilized for fermentative production of food colorant (Red Yeast Rice) for more than 1000 years in China. The main colorant components of Red Yeast Rice are mixture of red Monascus pigments (RMPs) with various primary amine residues. In the present work, the non-natural primary amine p-aminobenzamide, exhibiting as non-involved in nitrogen microbial metabolism, nontoxicity to microbial cells, and chemical reactivity with orange Monascus pigments (OMPs), was screened. Based on the screened result, RMPs with the single p-aminobenzamide residue were produced by cell suspension culture in a nonionic surfactant micelle aqueous solution via in situ chemical modification of OMPs. Furthermore, in situ chemical modification of OMPs also provided a strategy for maintaining a relatively low OMP concentration and then efficient accumulation of high concentration of RMPs (3.3 g/l).


Asunto(s)
Aminas/química , Monascus/metabolismo , Pigmentos Biológicos/química , Pigmentos Biológicos/metabolismo , Tensoactivos/química , Benzamidinas/química , Técnicas de Cultivo de Célula
14.
Appl Microbiol Biotechnol ; 102(1): 117-126, 2018 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-29098409

RESUMEN

Monascus pigments are promising sources of natural food colorants, and their productivity can be improved by a novel extractive fermentation technology. In this study, we investigated the variations in pigment characteristics and biosynthetic gene expression levels in resting cell culture systems combined with extractive fermentation in Monascus anka GIM 3.592. Although the biomass was low at about 6 g/L DCW, high pigment titer of approximately 130 AU470 was obtained in the resting culture with cells from extractive fermentation, illustrating that it had a good biocatalytic activity for pigment synthesis. The oxidation-reduction potential value correlated with the rate of relative content of the intracellular orange pigments to the yellow pigments (O/Y, r > 0.90, p < 0.05), indicating that the change in pigment characteristics may be responsible for the cellular redox activity. The up- or down-regulation of the pigment biosynthetic genes (MpFasA2, MpFasB2, MpPKS5, mppD, mppB, mppR1, and mppR2) in the resting culture with extractive culture cells was demonstrated by real-time quantitative polymerase chain reaction analysis. Moreover, the mppE gene associated with the yellow pigment biosynthesis was significantly (p < 0.05) down-regulated by about 18.6%, whereas the mppC gene corresponding to orange pigment biosynthesis was significantly (p < 0.05) up-regulated by approximately 21.0%. These findings indicated that extractive fermentation was beneficial for the biosynthesis of the intracellular orange pigment. The mechanism described in this study proposes a potential method for the highly efficient production of Monascus pigments.


Asunto(s)
Regulación Fúngica de la Expresión Génica , Monascus/genética , Monascus/metabolismo , Pigmentos Biológicos/biosíntesis , Pigmentos Biológicos/genética , Biomasa , Técnicas de Cultivo de Célula/métodos , Fermentación , Colorantes de Alimentos , Monascus/crecimiento & desarrollo , Micelio/crecimiento & desarrollo , Micelio/metabolismo , Oxidación-Reducción , Pigmentos Biológicos/análisis , Pigmentos Biológicos/metabolismo , Tensoactivos/metabolismo
15.
BMC Vet Res ; 14(1): 138, 2018 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-29699558

RESUMEN

BACKGROUND: Low concentrations of nonionic surfactants can change the physical properties of cell membranes, and thus and in turn increase drug permeability. Porcine circovirus 2 (PCV2) is an extremely slow-growing virus, and PCV2 infection of PK-15 cells yields very low viral titers. The present study investigates the effect of various nonionic surfactants, namely, Tween-20, Tween-28, Tween-40, Tween-80, Brij-30, Brij-35, NP-40, and Triton X-100 on PCV2 infection and yield in PK-15 cells. RESULT: Significantly increased PCV2 infection was observed in cells treated with Tween-20 compared to those treated with Tween-28, Tween-40, Brij-30, Brij-35, NP-40, and Triton X-100 (p < 0.01). Furthermore, 24 h incubation with 0.03% Tween-20 has shown to induce significant cellular morphologic changes (cell membrane underwent slight intumescence and bulged into a balloon, and the number of microvilli decreased), as well as to increase caspase-3 activity and to decrease cell viability in PCV2-infected PK-15 cells cmpared to control group; all these changes were restored to normal after Tween-20 has been washed out from the plate. CONCLUSION: Our data demonstrate that Tween-20 transiently changes the surface morphology of PK-15 cells and improves PCV2 infection. The findings of the present study may be utilized in the development of a PCV2 vaccine.


Asunto(s)
Infecciones por Circoviridae/veterinaria , Circovirus/metabolismo , Polisorbatos/farmacología , Tensoactivos/farmacología , Animales , Caspasa 3/metabolismo , Línea Celular , Supervivencia Celular/efectos de los fármacos , Infecciones por Circoviridae/virología , Circovirus/fisiología , Riñón/citología , Riñón/virología , Microscopía Electroquímica de Rastreo/veterinaria , Porcinos , Replicación Viral/efectos de los fármacos
16.
Mol Pharm ; 14(7): 2450-2458, 2017 07 03.
Artículo en Inglés | MEDLINE | ID: mdl-28570823

RESUMEN

Small interfering RNAs (siRNA) have a broad potential as therapeutic agents to reversibly silence any target gene of interest. The clinical application of siRNA requires the use of safe and effective delivery systems. In this study, we investigated the use of nonionic surfactant vesicles (NISV) for the delivery of siRNA. Different types of NISV formulations were synthesized by microfluidic mixing and then evaluated for their physiochemical properties and cytotoxicity. The ability of the NISV to carry and transfect siRNA targeting green fluorescent protein (GFP) into A549 that stably express GFP (copGFP-A549) was evaluated. Flow cytometry and Western blotting were used to study the GFP expression knockdown, and significant knockdown was observed as a result of siRNA delivery to the cells by NISV. This occurred in particular when using Tween 85, which was able to achieve more than 70% GFP knockdown. NISV were thus demonstrated to provide a promising and effective platform for therapeutic delivery of siRNA.


Asunto(s)
Microfluídica/métodos , ARN Interferente Pequeño/administración & dosificación , Tensoactivos/química , Células A549 , Citometría de Flujo , Proteínas Fluorescentes Verdes/genética , Proteínas Fluorescentes Verdes/metabolismo , Humanos , Interferencia de ARN
17.
J Liposome Res ; 27(2): 161-170, 2017 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-27184460

RESUMEN

This work describes the preparation of a PEGylated niosomes-mediated drug delivery systems for Paeonol, thereby improving the bioavailability and chemical stability of Paeonol, prolonging its cellular uptake and enhancing its synergistic anti-cancer effects with 5-Fu. PEGylated niosomes, which are prepared from biocompatible nonionic surfactant of Spans 60 and cholesterol, and modified with PEG-SA. Pae-PEG-NISVs were evaluated in vitro and in vivo. The cytotoxicity of Pae-PEG-NISVs was investigated against HepG2 cells. Fluorescence microscope was used to detect the apoptotic morphological changes. Growth inhibition assays were carried out to investigate whether Pae-PEG-NISVs could enhance the antiproliferative effects of Pae co-treated with 5-FU on HepG2 cells. The optimized Pae-PEG-NISVs had mean diameters of approximately 166 nm and entrapment efficiency (EE) of 61.8%. Furthermore, the in vitro release study of Paeonol from PEGylated niosomes exhibited a relatively prolonged release profile for 12 h. Pharmacokinetic studies in rats after i.v. injection showed that Pae-PEG-NISVs had increased elimination half-lives (t1/2, 87.5 versus 17.0 min) and increased area under the concentration-time curve (AUC0-t, 38.0 versus 19.48 µg/ml*min) compared to Paeonol solution. Formulated Paeonol had superior cytotoxicity versus the free drug with IC50 values of 22.47 and 85.16 µg/mL at 24 h on HepG2 cells, respectively, and we found that low concentration of Pae-PEG-NISVs and 5-Fu in conjunction had obviously synergistic effect. Our results indicate that the PEG-NISVs system has the potential to serve as an efficient carrier for Paeonol by effectively solubilizing, stabilizing and delivering the drug to the cancer cells.


Asunto(s)
Acetofenonas/farmacocinética , Antineoplásicos/farmacología , Sistemas de Liberación de Medicamentos , Fluorouracilo/farmacología , Polietilenglicoles/química , Acetofenonas/administración & dosificación , Acetofenonas/química , Animales , Antineoplásicos/administración & dosificación , Antineoplásicos/química , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Fluorouracilo/administración & dosificación , Fluorouracilo/química , Células Hep G2 , Humanos , Liposomas/química , Masculino , Estructura Molecular , Ratas , Ratas Sprague-Dawley , Relación Estructura-Actividad , Células Tumorales Cultivadas
18.
Bioprocess Biosyst Eng ; 40(6): 857-866, 2017 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-28239774

RESUMEN

Monascus pigments that were generally produced intracellularly from Monascus spp. are important natural colorants in food industry. In this study, change of pigment metabolism and secretion was investigated through fed-batch extractive fermentation and continuous extractive fermentation. The biomass, secreting rate of pigment and total pigment yield closely correlated with the activated time of extractive fermentation as well as the composition of feeding nutrients. Metal ions played a key role in both the cell growth and pigment metabolism. Nitrogen source was necessary for a high productivity of biomass but not for high pigment yield. Furthermore, fermentation period for the fed-batch extractive fermentation could be reduced by 18.75% with a nitrogen source free feeding medium. Through a 30-day continuous extractive fermentation, the average daily productivity for total pigments reached 74.9 AU day-1 with an increase by 32.6 and 296.3% compared to that in a 6-day conventional batch fermentation and a 16-day fed-batch extractive fermentation, respectively. At the meantime, proportions of extracellular pigments increased gradually from 2.7 to 71.3%, and yellow pigments gradually became dominated in both intracellular and extracellular pigments in the end of continuous extractive fermentation. This findings showed that either fed-batch or continuous extractive fermentation acted as a promising method in the efficient production of Monascus pigments.


Asunto(s)
Monascus , Fermentación , Micelas , Pigmentos Biológicos , Tensoactivos
19.
Drug Dev Ind Pharm ; 43(6): 1011-1022, 2017 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-28157445

RESUMEN

CONTEXT: Novel, safe, efficient and cost effective nano-carriers from renewable resources have got greater interest for enhancing solubility and bioavailability of hydrophobic dugs. OBJECTIVES: This study reports the synthesis of a novel biocompatible non-phospholipid human metabolite "Creatinine" based niosomal delivery system for Azithromycin improved oral bioavailability. METHODS: Synthesized surfactant was characterized through spectroscopic and spectrometric techniques and then the potential for niosomal vesicle formation was evaluated using Azithromycin as model drug. Drug loaded vesicles were characterized for size, polydispersity index (PDI), shape, drug encapsulation efficiency (EE), in vitro release and drug-excipient interaction using zetasizer, atomic force microscope (AFM), LC-MS/MS and FTIR. The biocompatibility of surfactant was investigated through cells cytotoxicity, blood hemolysis and acute toxicity. Azithromycin encapsulated in niosomes was investigated for in vivo bioavailability in rabbits. RESULTS: The vesicles were spherical with 247 ± 4.67 nm diameter hosting 73.29 ± 3.51% of the drug. Surfactant was nontoxic against cell cultures and caused 5.80 ± 0.51% hemolysis at 1000 µg/mL. It was also found safe in mice up to 2.5 g/kg body weight. Synthesized surfactant based niosomal vesicles revealed enhanced oral bioavailability of Azithromycin in rabbits. CONCLUSIONS: The results of the present study confirm that the novel surfactant is highly biocompatible and the niosomal vesicles can be efficiently used for improving the oral bioavailability of poor water soluble drugs.


Asunto(s)
Antibióticos Antineoplásicos/administración & dosificación , Antibióticos Antineoplásicos/farmacocinética , Azitromicina/administración & dosificación , Azitromicina/farmacocinética , Creatinina/química , Animales , Disponibilidad Biológica , Células Cultivadas , Sistemas de Liberación de Medicamentos , Estabilidad de Medicamentos , Hemólisis/efectos de los fármacos , Humanos , Liposomas , Ratones , Tamaño de la Partícula , Tensoactivos/química
20.
Pharm Dev Technol ; 22(3): 418-425, 2017 May.
Artículo en Inglés | MEDLINE | ID: mdl-27499352

RESUMEN

Evaluate the effects of nonionic surfactants Brij 58 and Tween 40 with different structures but similar hydrophilic lipophilic balances (HLBs) on theophylline (TH)-loaded ethylcellulose (EC) microspheres. Microspheres were formulated using ratios of the surfactants with matching HLB values but different chemical-structures at temperatures (22/35 °C) by hydrophobic solvent-emulsion evaporation. Particle size, GMD, drug loading, encapsulation efficiency and dissolution were evaluated. Drug release was determined using the zero- and first-order, Higuchi and Hixson-Crowell models. EC microspheres prepared with surfactant Brij 58 showed discrete, free-flowing spherical particles, solid interiors and increased particle smoothness as temperature increased; those prepared with Tween 40 appeared porous with coarser surface morphology as temperature increased; both were CHLB (Combined HLB) dependent. Dissolution obeyed the Higuchi model drug release for both microspheres prepared with Tween 40 and Brij 58 except for those prepared with Brij 58 at 35 °C, which presented as zero order. The results were ascribed to the different chemical structure of Brij 58 versus Tween 40 and preparation temperature. Surfactant chemical structure is an unreported processing parameter shown here to be important in microsphere formulation. Brij 58 possesses properties unique to its chemical structure that influence pharmaceutical and molecular biopharmaceutical research.


Asunto(s)
Celulosa/análogos & derivados , Portadores de Fármacos/química , Composición de Medicamentos/métodos , Tensoactivos/química , Teofilina/administración & dosificación , Celulosa/química , Cetomacrogol/química , Liberación de Fármacos , Microscopía Electrónica de Rastreo , Microesferas , Tamaño de la Partícula , Polisorbatos/química , Solubilidad , Propiedades de Superficie
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