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1.
Int J Pharm Pharm Sci ; 2024 May; 16(5): 54-66
Artigo | IMSEAR | ID: sea-231180

RESUMO

Objective: The present investigation aimed to prepare a smilax china loaded nanoemulsion using tween 80 as a surfactant and propylene glycol as a co-surfactant. Formulation of such drugs in nanoparticulate drug delivery will be advantageous for reducing dosing frequency, longer residence time, improved permeation, and patient compliance.Methods: High-speed homogenization method. The smilax china oil was prepared by collecting the extract of smilax china leaves into the coconut oil and then used as a solvent. The authentication studies of smilax china and coconut oil were evaluated for their organoleptic and physicochemical characteristics. The quantitative estimation and pre-formulation study of quercetin was carried out which has major anti-psoriatic properties. Surfactant and co-surfactant were selected and the solubility studies of oil and Surfactants were done. The nanoemulsion was characterized by particle size, polydispersity index, zeta potential, and entrapment efficiency (%).Results: This nanoemulsion provides the particle size and entrapment efficiency range between 80.52 to 89.78 nm and 68.66 to 70.16 % respectively. Batch SC1 showed the lowest particle size, PDI, and optimized drug entrapment effectiveness (%), indicating good particle size consistency within the remaining formulation batches. The optimized formulation SC 1 was found to be stable for 90 d.Conclusion: The formulated nanoemulsion showed significant antipsoriasis activity due to the presence of quercetin which has a rhetorical yield of 1.066 mg per 5 gm powder of smilax china leaves. Formulated smilax china-loaded nanoemulsion, has the potential as an effective antipsoriasis agent with a good spreading property with faster absorption which is beneficial for reducing drug concentration with maximum therapeutic effect.

2.
Artigo | IMSEAR | ID: sea-231684

RESUMO

According to earlier research, using niosomes as drug carriers, particularly for antifungal drugs, produces greater results than using alternative carriers. Niosomes has the capacity to encapsulate both hydrophilic and hydrophobic pharmaceuticals, as well as their prolonged stability in circulation. This work aimed to prepare and evaluate luliconazole niosomal gel for antifungal activity. In this study, niosomes containing luliconazole were prepared by thin film hydration technique using non-ionic surfactant (Span 60 and Tween 80) and cholesterol at different concentrations. The prepared formulations were evaluated for optical microscopy, drug entrapment efficiency, drug content, in-vitro drug release study, and stability studies. The ratio 2:1 of span 60 and cholesterol showed better results. Hence it was optimized as the final vesicle formulation. The FTIR study concluded there was no interaction between Luliconazole and any of the excipients. The niosomes gel was evaluated for various parameters of all the formulations. The 1% Carbopol 934 gel shows the best and most promising results. The niosomal gel formulation could be a useful dosage form to increase efficacy by the transdermal route. The potential of a secure and efficient therapy for difficult clinical applications is made possible by the development of niosomes with target specificity. Therefore, niosomes gel may be considered the best vesicular carrier for the effective delivery of luliconazole through the skin.

3.
Artigo | IMSEAR | ID: sea-231663

RESUMO

Dolutegravir sodium (DG) is a recently approved antiretroviral drug belonging to BCS class II having poor aqueous solubility and only 16% oral bioavailability. Hence aim of the present work was to develop solid self micro-emulsifying drug delivery system (S-SMEDDS) of Dolutegravir for enhanced solubility and dissolution behaviour. Initially, solubility of DG was checked to select oil, surfactant, and co-surfactant. Pseudo ternary phase diagram was constructed to identify microemulsion region. Liquid SMEDDS of DG were prepared using Campul MCM, Tween 80 and Transcutol P as oil, surfactant, and co-surfactant, respectively. The effect of different oil, surfactant and co-surfactant concentrations on particle size, zeta potential and %transmittance was studied using Box–Behnken factorial design. The obtained liquid SMEDDS was evaluated for its thermodynamic stability, globule size, robustness to dilution, viscosity, dye solubilization test, cloud point, etc. Satisfactory formulations of liquid SMEDDS were converted to solid form by adsorption technique using Neusilin US2 as a solid carrier. Evaluation of S-SMEDDS showed that solubility of DG in S-SMEDDS increases from 0.270 to 33.52 mg/mL. In-vitro drug release of S-DG4 showed 99.86 ± 1.47% drug release within 120 minutes while plain DG showed 32.55 ± 1.52%. Hence study revealed that S-SMEDDS is a promising approach to enhance solubility, dissolution and hence bioavailability of poorly aqueous soluble drug like DG.

4.
Artigo em Chinês | WPRIM | ID: wpr-973144

RESUMO

ObjectiveTo explore the pretreatment methods to promote the enzymatic digestion and extraction of active ingredients from Magnoliae Officinalis Cortex dregs(MOCD), and to provide a reference basis for the utilization of resource components in MOCD. MethodLiquid chromatography-mass spectrometry(LC-MS) was used for qualitative analysis of resource components in MOCD with an Agilent C18 reversed-phase column(3.0 mm×100 mm, 2.7 µm) at the flow rate of 0.4 mL·min-1, the mobile phase was water(A)-acetonitrile(B) for gradient elution(0-3 min, 25%-48%B; 3-6 min, 48%-59%B; 6-10 min, 59%-80%B; 10-20 min, 80%-90%B; 20-25 min, 90%B), electrospray ionization(ESI) was employed with negative ion mode scanning and scanning range of m/z 50-1 200. A high performance liquid chromatography(HPLC), which refered to the determination in the 2020 edition of Chinese Pharmacopoeia, was used for quantitative analysis of resource components in MOCD. Four kinds of pretreatment agents were used to separate the resource components from MOCD, and the mechanism of different pretreatment agents was investigated by field emission scanning electron microscopy(FESEM), X-ray powder diffraction(XRD) and Fourier transform infrared spectroscopy(FT-IR). ResultMagnolol, honokiol and lignocellulose were identified as the main resource components of MOCD by qualitative and quantitative analysis. Under the conditions of 1% NaOH, reaction temperature at 80 ℃ and reaction time of 60 min, the concentration of reducing sugar produced by the enzymatic hydrolysis was 32.18 g·L-1, which was 79.8% higher than that of the untreated MOCD. After adding tween-80, the enzymatic hydrolysis time was reduced to 1/3 of the original time, the concentration of reducing sugar was increased by 102.0%. And the total recovery of magnolol and honokiol in the pretreatment solution was 69.23%. ConclusionMagnolol, honokiol and lignocellulosic components in MOCD are valuable for development and utilization, the combination of alkaline pretreatment and tween-80 can realize the recovery and utilization of these three resource components, which can provide a new idea for comprehensive utilization of resource components in MOCD.

5.
Chinese Pharmacological Bulletin ; (12): 1227-1230, 2022.
Artigo em Chinês | WPRIM | ID: wpr-1014038

RESUMO

Abstract; Aim To solve the problems in the appliea- tion of egg yolk leeithin endotoxin test method, and and to establish the baeterial endotoxin examination method for egg yolk lecithin (for injeetion). Methods The ethanol solution of Tween 80 ( the volume ratio of tween 80 to anhydrous ethanol was 2. 5 • 2. 7, mixed for 4 min) was used to prepare lecithin solution of egg yolk at 0. 1 kg • L 1 , and 10 test water was added to 1 mL lecithin solution of egg yolk (500 EU • mL 1 standard solution of endotoxin IOjxL was added for pos¬itive control). After diluted 20 times with endotoxin test water, the standard curve range was 10 ~0. 01 EU • mL 1 by kinetic-turbidimetrie assay. Methodology of endotoxin test was studied using limulus lysate from two manufacturers and eight hatches of samples. Results The recoveries of eight hatches of samples all met the requirement of interference test between 50% and 200% stipulated in the pharmacopoeia, which solved the problems of the current endotoxin test method in practical application. Conclusions The bacterial en¬dotoxin test method of egg yolk lecithin with good dura-bility is established to provide the basis for the revision of pharmacopoeia.

6.
Artigo em Chinês | WPRIM | ID: wpr-910315

RESUMO

Objective:To study the effect of emulsifier Tween-80 on radiation-induced bile acid enterohepatic circulation disturbance and the treatment strategy.Methods:Male C57BL/6 J mice were randomly divided into healthy control group, radiation-only group, radiation + Tween-80 group and radiation + Tween-80 + butyric acid group. The mice were exposed to total abdominal irradiation (TAI) using a specific steel lead chamber and γ-ray irradiator was used throughout the experiments. Mice in radiation+ Tween-80 group and radiation+ Tween-80+ butyric acid group were intragastrically administrated with Tween-80 for 7 d before irradiation, while healthy control group and radiation-only group were treated with sterile water. After irradiation, butyric acid was administrated to mice in radiation+ Tween-80+ butyric acid group until euthanasia, while healthy control group, radiation-only group and radiation+ Tween-80 group were treated with sterile water until euthanasia. Small intestine and fecal particles were collected 21 d after irradiation. The concentrations of bile acid in small intestinal and fecal samples were measured using enzyme linked immunosorbent assay (ELISA), the expression of TGR5 and JAM-A, as well as the ratio of IL-10/IL-12 in intestine were detected by quantitative real-time PCR (qRT-PCR). The expression levels of GPR43 in the colon were compared using immunohistochemistry (IHC).Results:Tween-80 pretreated mice exhibited lower concentration of bile acid in small intestine and higher level of bile acid in fecal sample after irradiation (7.92%, 7.99%, t=3.93, 2.94, P<0.05), the expression of TGR5, which mediating the biological function of bile acid, and it′s downstream JAM-A gene were down-regulated (20.93%, 9.91%, t=4.85, 5.14, P<0.05), the ratio of IL-10/IL-12 (indicator related to inhibition of inflammation) (4.59%, t=3.39, P<0.05) as well as the expression of GPR43 protein, a G-protein-coupled receptor for butyric acid, decreased in the colon of Tween-80-pretreated mice compared with the radiation-only group. ELISA assay revealed that butyric acid administration elevated bile acid level in small intestines (8.06%, t=9.25, P<0.05), but reduced that in feces (14.41%, t=4.71, P<0.05). In addition, TGR5 and JAM-A showed higher expression in the intestine of butyric acid-treated mice (19.35%, 32.71%, t=7.69, 19.23, P<0.05), as well as the ratio of IL-10/IL-12 (2.39%, 4.05%, t=3.38, 5.92, P<0.05) and the content of GPR43 protein in colon. Conclusions:Tween-80 deteriorates the disturbance of bile acid enterohepatic circulation induced by ionizing radiation in mice. Butyric acid administration erases the adverse effects of Tween-80.

7.
Artigo | IMSEAR | ID: sea-210711

RESUMO

Oxyresveratrol is a polyphenolic compound found in Mulberry (Morus alba L.) twigs and has known as a skinlightening agent. Many methods can be applied to extract oxyresveratrol from Mulberry twigs. This researchaimed to optimize the extraction method by using surfactant Tween 80 and Tween 20-based microwave-assistedextraction (MAE). Extraction parameters, including solvent concentration, liquid–solid ratio, and extraction time foroxyresveratrol, were optimized using response surface methodology based on Box–Behnken Design. This researchalso extracted the oxyresveratrol by maceration, and then the oxyresveratrol content from each extraction methodwas compared. Oxyresveratrol content was determined using high-performance liquid chromatography (HPLC). ForTween 80, the optimum condition was obtained at 10.5 mM, 30:1 ml/g liquid–solid ratio, and 10 minutes extractiontime. For Tween 20, the optimum condition was obtained at 100 mM, 40:1 ml/g liquid–solid ratio, and 5 minutesextraction time. Oxyresveratrol content was 0.0146 mg/g dried sample and 0.0172 mg/g dried sample at the optimumcondition of Tween 80 and Tween 20 surfactant, respectively. Meanwhile, the oxyresveratrol content of the macerationmethod with 96% ethanol was 1.5704 mg/g dried sample. In conclusion, these results show that the application ofTween 80 and Tween 20 as solvents for MAE of Oxyresveratrol from mulberry twigs was not fully successful sinceother extraction conditions should be considered, such as temperature, pH, and microwave energy.

8.
Int J Pharm Pharm Sci ; 2019 Aug; 11(8): 4-10
Artigo | IMSEAR | ID: sea-205927

RESUMO

Objective: The objective of the present investigation was to develop olive and soybean oil-based oleogels with Span 40 and/or Tween 80 (as gelator and/or surfactant) and determine the critical gelator concentration (CGC), characterise and compare the rheological, thermal properties and drug release profile of the gels formed for topical delivery. Methods: Olive and soybean oil-based Span 40 and Span 40/Tween 80 oleogel formulations were prepared by solid fiber mechanism and subjected to organoleptic evaluation, FT-IR spectroscopy, thermal analysis, rheological study, kinetic modeling of gelation and drug release. Results: The critical gelator (Span 40) concentration was found to be lower for olive oil (12% w/v) and depend on the type of oil. Tween 80 reduced CGC of soybean oleogels only. Soybean oil-based oleogel containing 18% w/v Span 40 was found to form more flexible, less viscous and thermally less stable formulation with better release of paracetamol as evident from lower melt flow index, Tg value, lower β and higher α value compared to olive oil-based oleogel with 12% w/v Span 40 (CGC). Surfactant addition can be assumed to modify the microarchitecture of the oleogels to a great extent to produce more flexible and thermally stable gels with even better drug release profile. Span-Tween based soybean oleogel formed a gel-matrix whereas matrix in olive oil-based oleogels containing Span only became slightly flexible to release the drug in zero-order fashion on the addition of surfactant cogelator. Conclusion: Nature of oil exerts profound influence on the rheological, thermal and release profile of oleogels containing Span 40 as gelator and/or Tween 80 as surfactant cogelator.

9.
Zhongguo Zhong Yao Za Zhi ; (24): 743-747, 2018.
Artigo em Chinês | WPRIM | ID: wpr-771674

RESUMO

Based on the fact that chromogenic reaction of blue complex, a reaction product which can be dissolved in organic solvents, can be realized by polyethoxy and ammonium thiocyanate in tween 80, a rapid and accurate way for the determination for tween 80 in pharmaceutical adjuvant was established in this study, providing reliable technical means for quality control of traditional Chinese medicine injections. Based on the study of reaction kinetics, chromogenic reaction temperature and time, as well as extraction of organic solvents and other key conditions were optimized, and Kumu injection was used as the test material for method validation and applicability investigation. It was finally determined that 3 mL ammonium thiocyanate solution was added in the sample solution, and the reaction was carried out in a boiling water bath for 2 h. After cooling to room temperature, 5 mL of dichloromethane was added to extract the chromogenic product. The absorbance value was measured at the wavelength of 623 nm to calculate the tween 80 content in the sample. Under optimized conditions, tween 80 solution showed a good linear relationship with the absorbance in the range from 0.8 mg to 3.0 mg. The linear regression equation was =0.258-0.047. The correlation coefficient was 0.999 6. Under the experimental conditions, the average recovery was 99.66%, and the precision RSD was less than 2.0%. The results showed that this method can quickly and accurately determine the content of tween 80 in Kumu injection, and it could be applicable to the quality control of traditional Chinese medicine injections.


Assuntos
Adjuvantes Farmacêuticos , Química , Medicina Tradicional Chinesa , Polissorbatos , Química , Controle de Qualidade , Solventes , Temperatura
10.
Rev. colomb. biotecnol ; 19(1): 116-123, ene.-jun. 2017. tab, graf
Artigo em Espanhol | LILACS | ID: biblio-900429

RESUMO

Resumen Se llevaron a cabo procesos de biosíntesis de carbonato de calcio, empleando una cepa de Bacillus cereus, aislada de los jardines de la Universidad Pontificia Bolivariana (Medellín, Colombia). Se evaluó el efecto disgregante del Tween® 80 a tres concentraciones: 0.00% p/v, 0.25% p/v y 0.50% p/v. Los experimentos se monitorizaron por 6 días con mediciones de pH y análisis mineralógicos a los precipitados finales por microscopía electrónica de barrido, difracción de rayos X y espectroscopia de infrarrojo con transformada de Fourier. El Tween® 80 tuvo un papel importante como desaglomerante de las estructuras de carbonato formadas por los microorganismos. Aunque los ensayos con el surfactante presentaron menor formación de precipitado, las concentraciones evaluadas no inhibieron el crecimiento bacteriano. Adicionalmente, este compuesto favoreció la formación de vaterita incrementando su proporción en comparación con la calcita (alrededor del 98%, utilizando Tween® 80 al 0.50% p/v).


Abstract This research presents the sprinkling effect of Tween® 80 for three concentrations (0.00% w, 0.25% w y 0.50% w) in a processes of calcium carbonate biosynthesis. The assays used a culture of Bacillus cereus, isolated from the gardens of the Universidad Pontificia Bolivariana (Medellin, Colombia). The experiments were monitored for 6 days measuring pH as well as through mineralogical analyses for precipitates using scanning electron microscopy, X-ray diffraction and Fourier transform infrared spectroscopy. Tween® 80 had an important role as deagglomerate, decreasing the precipitation of biomineralized-carbonate structures (generated by bacteria). It was also found that the evaluated concentrations did not inhibit the bacterial growth. Additionally, Tween® 80 favored the production of vaterite, increasing its ratio in comparison to calcite (around 98% by using 0.50% w of Tween® 80).

12.
Braz. arch. biol. technol ; Braz. arch. biol. technol;59: e16150362, 2016. tab, graf
Artigo em Inglês | LILACS | ID: lil-774489

RESUMO

The objective of this work was to optimize the spray drying of pequi pulp using maltodextrin as carrier agent and Tween 80 as surfactant agent. A central composite rotatable design was used to evaluate the influence of inlet air temperature (140 to 200°C), maltodextrin (15 to 30%) and surfactant (0 to 5%) concentration on the process performance and physicochemical and nutritional properties of the dried powdered pulp. The dependent variables were process yield (27.4 - 51.7%), outlet air temperature (106.5 - 135°C), energetic efficiency (29.9 - 44.8%), moisture content (0.25 - 1.43%), water activity (0.09 to 0.21), hygroscopicity (9.1 - 12.1 g adsorbed moisture/100g dry matter), vitamin C content (129.8 - 303.0 mg/g solids pequi) and total carotenoids content (8.2 - 94.9 mg carotenoids/g solids pequi). The spray drying of pequi pulp was optimized for maximum vitamin C and total carotenoids content using response surface methodology, which were attained at 152°C, surfactant concentration of 1% and maltodextrin concentration of 18%. The characterization of the pequi pulp powder obtained at the optimized condition evaluating the particles sizes, bulk density and porosity. The morphology showed spherical and smooth particles with several sizes.

13.
Artigo em Chinês | WPRIM | ID: wpr-499906

RESUMO

Objective To explore the shielding effect that Tween has made on the erythrocyte’ s surface antigen( ABO and D antigen mainly) and the stability of the RBC. Methods Various types red blood cells’ surface antigens were incubated with different concentrations of Tween,then the titers of RBC’ s surface antigen before and after incubation were compared. The erythrocyte’ s function alterations and sta-bility through the morphological obersavation,the osmotic fragility,RBC’ s own hemolysis rate,oxygen saturation( SO2 ) ,routine test of blood as well as the supernatant of free hemoglobin determination were confirmed. Results The masking effect of the Tween-20 on D antigen with the weaken titer keeping above“ +” was better and more stable than that on A,B antigen. The impact on B antigen was a little worse,and A was the worst. The advantaged concentration is about 0. 004%. Besides,the influence of Tween-80’s on B and D antigen was not apparent e-nough. Among all of the concentration,0. 74% and 0. 80% did a relatively better job,which also could keep the weaken titer above “ +”. Conclulsion The shielding effect that Tween has made on the erythrocyte’ s surface antigen( ABO and D antigen mainly) is stable,which keeps above “ +”. The morphology and function of the RBC does not change.

14.
Artigo em Inglês | IMSEAR | ID: sea-163216

RESUMO

Aims: The aim of this study was to explore the practicability of preparation of solid lipid nanoparticles of Glyceryl monostearate containing Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs. The physicochemical properties of the prepared formulae like particle size, drug entrapment efficiency, drug loading capacity, yield content and in-vitro drug release behavior were also measured. Methodology: Solid lipid nanoparticles loaded with three model lipophilic drugs were prepared by high shear hot homogenization method. The model drugs used are Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide. Glyceryl monostearate was used as lipid core; Tween 20 and Tween 80 were employed as surfactants and lecithin as co-surfactant. Many formulation parameters were controlled to obtain high quality nanoparticles. The prepared solid lipid nanoparticles were evaluated by different standard physical and imaging methods. The efficiency of drug release form prepared formulae was studied using in vitro technique with utilize of dialysis bag technique. The stability of prepared formulae was studied by thermal procedures and infrared spectroscopy. Results: The mean particle diameter measured by laser diffraction technique was (194.6±5.03 to 406.6±15.2 nm) for Dibenzoyl peroxide loaded solid lipid nanoparticles, (220±6.2 to 328.34±2.5) nm for Erythromycin loaded solid lipid nanoparticles and (227.3±2.5 to 480.6±24) nm for Triamcinolone acetonide loaded solid lipid nanoparticles. The entrapment efficiency and drug loading capacity, determined with ultraviolet spectroscopy, were 80.5±9.45% and 0.805±0.093%, for Dibenzoyl peroxide, 96±11.5 and 0.96±0.012 for Triamcinolone acetonide and 94.6±14.9 and 0.946±0.012 for Erythromycin base respectively. It was found that model drugs showed significant faster release patterns when compared with commercially available formulations and pure drugs (p˂0.05). Thermal analysis of prepared solid lipid nanoparticles gave indication of solubilization of drugs within lipid matrix. Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drugs and lipid matrix and being only dissolved in it. Electron microscope of scanning and transmission techniques indicated sphere form of prepared solid lipid nanoparticles with smooth surface with size below 100 nm. Conclusions: Solid lipid nanoparticles with small particle size have high encapsulation efficiency, and relatively high loading capacity for Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs can be obtained by this method.

15.
International Journal of Biomedical Engineering ; (6): 193-196,229,后插1, 2012.
Artigo em Chinês | WPRIM | ID: wpr-597951

RESUMO

Objective To investigate the feasibility of using a novel docetaxel-loaded polycaprolactoneTween 80 (PCL-Tween 80) nanoparticles for glioma therapy.Methods Two types of docetaxel-loaded nanoparticles were made from commercial polycaprolactone (PCL) and a self-synthesized PCL-Tween 80 copolymer using a modified solvent extraction/evaporation method.A C6 glioma cell line was used to investigate the uptake of polymeric nanoparticles by brain cancer cells.In vitro cancer cell viability was assessed using MTT toxic assay.Results The nanoparticles were found by FESEM to have a spherical shape and be around 200 nm in diameter.The copolymers could encapsulate 10% of the drug in the nanoparticles and release 34.9% of the encapsulated drug over 28 days.The drug-loaded PCL-Tween 80 nanoparticles showed better in vitro cytotoxicity towards C6 cancer cells than Taxotere at the same drug concentration.Conclusion Nanoparticles using PCL-Tween 80 copolymer as drug delivery vehicles may have a promising outcome for glioma patients.

16.
Braz. arch. biol. technol ; Braz. arch. biol. technol;54(6): 1117-1124, Nov.-Dec. 2011. graf, tab
Artigo em Inglês | LILACS | ID: lil-608432

RESUMO

A glucan producing Weissella confusa isolated from fermented cabbage, as identified earlier, was used for optimization of its fermentation medium. The effects of various macronutrients such as sucrose, glucose as cosubstrate, yeast extract, beef extract, peptone, sodium acetate, K2HPO4 and Tween 80 were studied on glucansucrase and glucan production from Weissella confusa. The medium used as control gave 6.0 U/ml enzyme activity and 34 mg/ml glucan concentration. Sucrose (5 percent), glucose as cosubstrate (5 percent for glucansucrase and 3 percent for glucan production), Tween 80 (0.1 percent), yeast extract (1.5 percent), Peptone (2.0 percent) and K2HPO4 (1.5 percent) were effective nutrients displaying higher glucansucrase and glucan production giving 18.2, 18.0, 7.0, 6.4, 6.2 and 6.4 U/ml enzyme activity and 103, 100, 46, 41, 39 and 37 mg/ml glucan concentration, respectively. Sodium acetate and beef extract were not effective for enzyme and glucan production. The new strain Weissella confusa can be used for commercial production of glucansucrase and glucan using optimized medium.

17.
Artigo em Chinês | WPRIM | ID: wpr-349783

RESUMO

This study examined the effect of self-microemulsiflying drug delivery system (SMEDDS) containing Cremophor RH40 or Tween 80 at various dilutions on cytochrome P450 3A (CYP3A) enzymes in rat hepatocytes, with midazolam serving as a CYP3A substrate. The particle size and zeta potential of microemulsions were evaluated upon dilution with aqueous medium. In vitro release was detected by a dialysis method in reverse. The effects of SMEDDS at different dilutions and surfactants at different concentrations on the metabolism of MDZ were investigated in murine hepatocytes. The cytotoxicity of SMEDDS at different dilutions was measured by LDH release and MTT technique. The effects of SMEDDS on the CYP3A enzymes activity were determined by Western blotting. Our results showed that dilution had less effect on the particle size and zeta potential in the range from 1:25 to 1:500. The MDZ was completely released in 10 h. A significant decrease in the formation of 1'-OH-MDZ in rat hepatocytes was observed after treatment with both SMEDDS at dilutions ranging from 1:50 to 1:250 and Cremophor RH 40 or Tween 80 at concentrations ranging from 0.1% to 1% (w/v), with no cytotoxicity observed. A significant decrease in CYP3A protein expression was observed in cells by Western blotting in the presence of either Cremophor RH40 or Tween 80-based SMEDDS at the dilutions ranging from 1:50 to 1:250. This study suggested that the excipient inhibitor-based formulation is a potential protective platform for decreasing metabolism of sensitive drugs that are CYP3A substrates.

18.
Braz. arch. biol. technol ; Braz. arch. biol. technol;50(6): 913-920, Nov. 2007. graf, tab
Artigo em Inglês | LILACS | ID: lil-476217

RESUMO

Production of manganese-dependent peroxidase (MnP) by the white-rot fungus Phanerochaete chrysosporium BKM-F-1767 (ATCC 24725) was monitored during growth in different media and growth conditions. The effect of some activators of MnP production, Mn2+, Tween 80, phenylmethylsulphonylfloride (PMSF), oxygen, temperature, pH, glycerol and nitrogen was studied. Supplementing the cultures with Tween 80 (0.05 percent, v/v) and Mn2+ (174 µM) resulted a maximum MnP activity of 356 U/L which was approximately two times higher than that obtained in the control culture (without Tween 80). Decolourisation of Direct Blue 15 and Direct Green 6 (50 mg/L) was also achieved with MnP.

19.
Artigo em Chinês | WPRIM | ID: wpr-580400

RESUMO

Objective To study the applicability of ultrafiltration of tween-80 and it solubilizing schizonepeta volatile oil and paeonol of ultrafiltration. Method Taking components content as index, temperature, pressure, concentration and membrane pore size were selected as factors for orthogonal design method. The concentration was determinated in medical solution before and after ultrafiltration, and the transmittance rate (TS) was calculated to observe the content variation of tween-80 and it solubilizing solution. Results The four factors had markedly effect on TS of tween-80, concentration was statistically significant (P

20.
Artigo em Chinês | WPRIM | ID: wpr-685115

RESUMO

The effects of surfactants on the production of cellulase by Trichoderma viride in liquid substrate fermentation process were investigated. Straw was used as the sole carbon source and the surfactants were biosurfactant rhamnolipid from Pseudomonas aeruginosa and Tween 80. The changes of FPA,CMCase,Avicelase and surface tension with time were analyzed under different concentrations of the two surfactants. The results showed that the surfactants can enhance the enzyme activity of Trichoderma viride. The FPA,CMCase,Avicelase were promoted 1.08,1.6 and 1.03 times higher than the controls by rhamnolipid. The enhancement of the enzyme activity by rhamnolipid was much higher than that of Tween 80. At the same time,rhamnolipid was not degraded prior to other substrate.

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