Optimization the formulation parameters in preparation of α-tocopherol nanodispersions using low-energy solvent displacement technique

2020 ◽  
Vol 90 (1-2) ◽  
pp. 5-16 ◽  
Author(s):  
Naghmeh Jaberi ◽  
Navideh Anarjan ◽  
Hoda Jafarizadeh-Malmiri
Keyword(s):  
Particle Size ◽  
Average Particle Size ◽  
Weight Ratio ◽  
Polydispersity Index ◽  
Tween 20 ◽  
P Value ◽  
Average Particle ◽  
Regression Equations ◽  
Solvent Displacement ◽  
Formulation Parameters

Abstract. α-Tocopherol is the main compound of vitamin E with great antioxidant activity. However, like other functional lipid bioactive compounds, it suffers from low bioavailability due to its low water solubility and liable chemical structure. A bottom-up procedure based on a solvent-displacement method was constructed for fabrication of α-tocopherol nanodispersions using response surface methodology (RSM). The effects of main formulation parameters, namely, weight ratio of emulsifier to α-tocopherol and volumetric percent of acetone to water on the average particle size (nm), polydispersity index, concentration of α-tocopherol loss (% w/w) and turbidity of the nanodispersions were evaluated and optimized to gain the most desirable nanodispersions (least particle size, polydispersity index, turbidity and highest α-tocopherol concentrations). Second order regression equations, holding quite high coefficients of determination (R2 and adjusted R2 > 0.882), were significantly (p-value < 0.05) fitted for predicting the α-tocopherol nanodispersion characteristics variations as functions of studied formulation parameters. A multiple optimization analysis offered 6.5 and 10% for weight ratio of Tween 20 to α-tocopherol and volume percent of acetone, respectively, as overall optimum values for studied parameters. Statistically insignificant differences between experimental and predicted values of studied responses, verified the satisfactoriness of presented models for explaining the response characteristics as a function of formulation parameters. Thus, the employed solvent-displacement technique may provide the most desired water dispersible α-tocopherol nanoparticles for several water-based foods, cosmetic nutraceutical formulations.

scholarly journals PREPARATION AND CHARACTERIZATION OF GRAPEFRUIT OIL BASE MICROEMULSIONS OF CAFFEINE

2019 ◽  
pp. 231-238 ◽  
Author(s):  
EKAPOL LIMPONGSA ◽  
PATHOMTHAT SRISUK ◽  
NAPAPHAK JAIPAKDEE
Keyword(s):  
Particle Size ◽  
Ph Value ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Average Particle Size ◽  
Tween 20 ◽  
Average Particle ◽  
Surfactant System ◽  
Ternary Phase Diagrams ◽  
Formulation Parameters

Objective: The objective of the present work was to prepare and characterize grapefruit oil base microemulsions loaded with caffeine as a model hydrophilic compound. Methods: The formulation ingredients were selected based on surfactant efficiency and solubility studies. Ternary phase diagrams of grapefruit oil were constructed using the water titration method. Nine O/W microemulsions were constructed and prepared by mixing surfactant system, grapefruit oil, water and caffeine together. The resulting microemulsions were investigated for viscosity using Brookfield viscometer, for pH value using a digital pH meter, and for average particle size and polydispersity index (PDI) using a Zetasizer Nano. Ex vivo skin permeation through porcine ear skin was conducted using a side-by-side diffusion cell. The amount of caffeine was analyzed using HPLC-UV method. Results: Tween 20 yielded the highest emulsification ability for grapefruit oil and the highest caffeine solubility. It was selected as a major surfactant. Caffeine was slightly soluble in ethanol and isopropyl alcohol, but sparingly soluble in propylene glycol (PG). These ingredients were used as the cosurfactants. Nine grapefruit oil base microemulsions were prepared and characterized. The pH of microemulsions was within the range of 4.48-5.96. Particle size was in the range of 10.81±0.03 to 62.18±21.04 µm with the PDI of 0.13±0.02 to 0.64±0.11. Viscosity and particle size of microemulsions increased significantly with increasing grapefruit oil or tween 20 content. Addition of PG as cosurfactant resulted in the increases of viscosity, particle size and PDI. Depending on the formulation parameters, the permeation fluxes of caffeine from grapefruit oil base microemulsions were in the range of 28.4±3.4-361.4±15.2 µg/cm2/h. Conclusion: The grapefruit oil base microemulsions were successfully formulated. The physical properties and caffeine permeation of these microemulsions were found to be dependent on the grapefruit oil content, tween 20 content, cosurfactant type and content, as well as caffeine loading. The optimal formulation of grapefruit oil base microemulsion suggested composition of 5% grapefruit oil, 50% surfactant system (tween 20 and ethanol at the ratio of 9:1), and water.

Formulation and Evaluation of Polymeric Nanoparticles of an Antiviral Drug for Gastroretention

2012 ◽  
Vol 4 (4) ◽  
pp. 1557-1562 ◽  
Author(s):  
Ankit Anand Kharia ◽  
A K Singhai ◽  
R Verma
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Average Particle Size ◽  
Chlorinated Solvents ◽  
Entrapment Efficiency ◽  
The Body ◽  
Hydrophilic Polymers ◽  
Polydispersity Index ◽  
Average Particle ◽  
Loading Efficiency

The aim of present study was to formulate and evaluate nanoparticles of acyclovir by using different hydrophilic polymers. Acyclovir was selected as a suitable drug for gastro-retentive nanoparticles due to its short half life, low bioavailability, high frequency of administration, and narrow absorption window in stomach and upper part of GIT. The nano-precipitation method was used to prepare nanoparticles so as to avoid both chlorinated solvents and surfactants to prevent their toxic effect on the body. Nanoparticles of acyclovir were prepared by using hydrophilic polymers such as bovine serum albumin, chitosan, and gelatin. The prepared formulations were then characterized for particle size, polydispersity index, zeta potential, loading efficiency, encapsulation efficiency and drug-excipient compatibility. The prepared nanoparticulate formulations of acyclovir with different polymers in 1:1 ratio have shown particle size in the range of 250.12-743.07 nm, polydispersity index (PDI) in the range of 0.681-1.0, zeta potential in the range of -14.2 to +33.2 mV, loading efficiency in the range of 8.74-17.54%, and entrapment efficiency in the range of 55.7%-74.2%. Nanoparticulate formulation prepared with chitosan in 1:1 ratio showed satisfactory results i.e. average particle size 312.04 nm, polydispersity index 0.681, zeta potential 33.2 mV, loading efficiency 17.54%, and entrapment efficiency 73.4%. FTIR study concluded that no major interaction occurred between the drug and polymers used in the present study.  

Characterization of CeO2 Fine Particles Prepared by the Homogeneous Precipitation Method with a Mixed Solutionof Ethylene Glycol and Polyethylene Glycol

2004 ◽  
Vol 19 (4) ◽  
pp. 1087-1092 ◽  
Author(s):  
Naofumi Uekawa ◽  
Masayuki Ueta ◽  
Yong Jun Wu ◽  
Kazuyuki Kakegawa
Keyword(s):  
Particle Size ◽  
Polyethylene Glycol ◽  
Ethylene Glycol ◽  
Fine Particles ◽  
Average Particle Size ◽  
Weight Ratio ◽  
Cerium Nitrate ◽  
Precipitation Method ◽  
Average Particle ◽  
Nitrate Hydrate

Cerium oxide (CeO2) nanoparticles were obtained by heating a polyethylene glycol (PEG) solution of cerium nitrate hydrate [Ce(NO3)3 6H2O] at 383 K for 3 h. When the PEG, whose molecular weight was 20,000, was used for the preparation, the monodispersed CeO2, whose particle size was about 102 nm, was obtained. When the mixture of PEG20,000 and ethylene glycol (EG) was used to prepare the PEG solution of cerium nitrate hydrate, the average particle size increased from 102 nm to 660 nm with an increase in the EG content of the solution. The pore structure in the obtained CeO2 particles also depended on the weight ratio between EG and PEG20,000.

Evaluation of Formulation Parameters for Development of Aceclofenac Nanosuspension Using Doe Statistical Tool

2016 ◽  
Vol 6 (4) ◽  
Author(s):  
Sharma Shivkant ◽  
Issarani Roshan ◽  
Nagori Prakash
Keyword(s):  
Particle Size ◽  
Polyvinyl Alcohol ◽  
Optimization Technique ◽  
Average Particle Size ◽  
Experimental Methodology ◽  
Average Particle ◽  
Saturation Solubility ◽  
Formulation Parameters ◽  
Dissolution Efficiency ◽  
Formulation Variables

InThe objective of present study was to identify and evaluate formulation variables affecting characteristics of nanosuspension formulations. Full factorial design experimental methodology was used for development of aceclofenac nanosuspension. Formulation factors evaluated were drug to polymer (Polyvinyl alcohol) ratio, amount of surfactant (Sodium dodecyl sulphate) relative to drug and solvent employed for carrying the drug. Total 18 formulations were prepared and their saturation solubility in distilled water and z average particle size were regarded as responses in this study. The response surface methodology utilizing polynomial equation was used to quantify the effect of each formulation variables. All three variables exerted significant effect on particle size and saturation solubility. Optimized nanosuspensions were obtained using numerical optimization technique by the desirability approach. The optimum formulation parameters were found to be 400% w/w of drug to polymer ratio and 7.5% w/w of amount of SDS for both solvents. The best optimized formulation obtained from ethanol showed significantly improved saturation solubility 255.39 µg/ml, particle size 477.7 nm and better dissolution efficiency (DE05) 59.77%. The absence of interactions between drug and polymers was confirmed by Fourier transform infrared (FTIR) spectroscopy. The results demonstrated that polyvinyl alcohol was successfully employed for the development of nanosuspension of aceclofenac with higher dissolution efficiency leading to better oral bioavailability.

Preparation and Characterization of Silicone Oil/UF Resin Microcapsules as Erosion Inhibitor

2016 ◽  
Vol 723 ◽  
pp. 481-485 ◽  
Author(s):  
Hong Guang Li ◽  
Shao Sen Lin ◽  
Shi Guo Du ◽  
De Jiang Lin
Keyword(s):  
Particle Size ◽  
High Efficiency ◽  
In Situ Polymerization ◽  
Silicone Oil ◽  
Average Particle Size ◽  
Weight Ratio ◽  
Polymerization Process ◽  
Core Material ◽  
Molar Ratio ◽  
Average Particle

Microcapsules with silicone oil as core and poly (urea-formaldehyde) as shell were prepared by direct in-situ polymerization process. The influences of formaldehyde-urea molar ratios on microcapsules morphologies were investigated by scanning electron microscope (SEM). The microcapsules were characterized by fourier transform infrared spectrometer (FT-IR), particle size analyzer, simultaneous thermal analyzer. The results showed that well dispersive microcapsules were obtained with average particle size of 2.5 μm when formaldehyde-urea molar ratio was 1.8:1.0 and that the weight ratio of silicon dioxide to microcapsule was 15.4%, which produced from pyrolysis of core material silicone oil. The prepared microcapsules were expected to a kind of high-efficiency erosion inhibitor when used in propellant.

scholarly journals Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 3031
Author(s):  
Wan-Yi Liu ◽  
Chia-Chen Lin ◽  
Yun-Shan Hsieh ◽  
Yu-Tse Wu
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Oral Delivery ◽  
Encapsulation Efficiency ◽  
Average Particle Size ◽  
Amorphous State ◽  
Polydispersity Index ◽  
Morphological Observation ◽  
Average Particle ◽  
Biopharmaceutical Properties

This study aimed to design an effective nanoparticle-based carrier for the oral delivery of fisetin (FST) with improved biopharmaceutical properties. FST-loaded nanoparticles were prepared with polyvinyl alcohol (PVA) and poly(lactic-co-glycolic acid) (PLGA) by the interfacial deposition method. A central composite design of two independent variables, the concentration of PVA and the amount of PLGA, was applied for the optimization of the preparative parameter. The responses, including average particle size, polydispersity index, encapsulation efficiency, and zeta potential, were assessed. The optimized formulation possessed a mean particle size of 187.9 nm, the polydispersity index of 0.121, encapsulation efficiency of 79.3%, and zeta potential of −29.2 mV. The morphological observation demonstrated a globular shape for particles. Differential scanning calorimetry and powder X-ray diffraction studies confirmed that the encapsulated FST was presented as the amorphous state. The dissolution test indicated a 3.06-fold increase for the accumulating concentrations, and the everted gut sac test showed a 4.9-fold gain for permeability at the duodenum region. In conclusion, the optimized FST-loaded nanoparticle formulation in this work can be developed as an efficient oral delivery system of FST to improve its biopharmaceutic properties.

scholarly journals Nanosized and Enhancement of Solubility Fisetin

2019 ◽  
Vol 7 (2) ◽  
pp. 6-10
Author(s):  
Muhammad Dzakwan ◽  
Eko Pramukantoro Ganet ◽  
Mauludin Rachmat ◽  
Saleh Wikarsa
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Photon Correlation Spectroscopy ◽  
Average Particle Size ◽  
Correlation Spectroscopy ◽  
Polydispersity Index ◽  
Average Particle ◽  
Polysorbate 80 ◽  
Photon Correlation ◽  
The Poor

Fisetin (3,3,4,7-tetrahydroxyflavone) is a natural antioxidant that has shown to posses anticancer, antioxidant and anti-inflammatory properties. However, the poor solubility leads to poor bioavailability and limits its development.The aim of the research is to investigate the effect of fisetin nanosuspension using a nanoprecipitation technique and additional stabilizers polysorbat 80, SLS, PVA and Eudragit on particle size average, polydispersity index and zeta potential.The suspensions of microcrystalline FIS were prepared by a nanoprecipitation technique with different proportion of stabilizers fixed. The nanosuspension produced was then characterized using Photon Correlation Spectroscopy (PCS) in  term of particle size distribution, polydispersity index, zeta potential and morphology nanosuspensiom (TEM). Result showed fisetin nanosuspension were successfully prepared by anti-solvent precipitation with additional stabilizer SLS and polysorbat 80. The nanosuspension containing polysorbat 80 showed smaller average particle size of 225.7 nm ± 1.31, a polydispersity index of 0.272 ±0.02 and zeta potential -39.3 ± 0.26 was obtained. Conclusion, FIS nanosuspension successfully prepared by nanoprecipitation tecnique with the polysorbate 80 as stabilizer and ethanol as solvent were spherical in shape..

scholarly journals Karakterisasi Nanopartikel Ekstrak Bunga Kecombrang dengan Penambahan Poloksamer

2018 ◽  
Vol 1 (3) ◽  
pp. 121-124
Author(s):  
Tresna Lestari ◽  
Tita Nofianti ◽  
Lilis Tuslinah ◽  
Ruswanto Ruswanto ◽  
Firda Adityas
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Average Particle Size ◽  
Particle Morphology ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Average Particle ◽  
Flower Extract ◽  
Round Form ◽  
Nanoparticle Formulation

Bunga kecombrang diketahui memiliki aktivitas sebagai antioksidan. Teknologi formulasi nanopartikel diharapkan dapat meningkatkan aktivitas biologis dari ekstrak.Penelitian ini dilakukan untuk memperoleh nanopartikel dari ekstrak bunga kecombrang dengan karakteristik yang baik.Pembuatan nanopartikel dilakukan dengan penambahan poloksamer dengan variasi konsentrasi 1, 3 dan 5%. Formulasi selanjutnya dianalisis meliputi ukuran partikel rata-rata, indeks polidispersitas, potensial zeta, efisiensi penjeratan dan morfologi partikel menggunakan SEM.Hasil karakterisasi diperoleh ukuran partikel rata-rata ketiga formula berada dalam rentang 134,7-193,1 nm, indeks polidispersitas <0,5 untuk semua formula, nilai potensial zeta antara -41,0 - (-24,3) mV dan efisiensi penjeratan terhadap senyawa flavonoid 89,93-97,99 %. Berdasarkan hasil SEM nanopartikel diketahui berbentuk bulat dengan permukaan yang halus.Berdasarkan hasil penelitian disimpulkan bahwa nanopartikel ekstrak bunga kecombrang dengan penambahan poloksamer 1, 3 dan 5% memiliki karakteristik yang baik dan memenuhi syarat sebagai sediaan nanopartikel.   Kecombrang flowers are known to have antioxidant activity. Nanoparticle formulation technology is expected to increase the biological activity of the extract. This study was conducted to obtain the nanoparticles from kecombrang flower extract with good characteristics. The preparation of nanoparticles was carried out by adding poloxamer with various concentrations of 1, 3 and 5%.Furthermore, the formula were analyzed, including the average particle size, polydispersity index, zeta potential, entrapment efficiency and particle morphology using SEM. The results of the characterization obtained an average particle size of the three formulas in the range of 134.7-193.1 nm, polydispersity index <0 , 5 for all formulas, zeta potential values ​​in range of -41.0 - (-24.3) mV and entrapment efficiency of flavonoid compounds of 89.93-97.99%The results of SEM examination showed that nanoparticles  was in round form with a smooth surface. Based on the results of the study,  itcan be concluded that kecombrang flower extract nanoparticles with the addition of poloxamer 1, 3 and 5% had good characteristics and met the criteria of  nanoparticle

Determination of grinding parameters of fenugreek seed

1970 ◽  
Vol 26 (1) ◽  
pp. 16 ◽  
Author(s):  
S Balasubramanian ◽  
Rajkumar Rajkumar ◽  
K K Singh
Keyword(s):  
Particle Size ◽  
Energy Consumption ◽  
Moisture Content ◽  
Specific Energy ◽  
Feed Rate ◽  
Average Particle Size ◽  
Specific Energy Consumption ◽  
Average Particle ◽  
Fenugreek Seeds ◽  
Fenugreek Seed

Experiment to identify ambient grinding conditions and energy consumed was conducted for fenugreek. Fenugreek seeds at three moisture content (5.1%, 11.5% and 17.3%, d.b.) were ground using a micro pulverizer hammer mill with different grinding screen openings (0.5, 1.0 and 1.5 mm) and feed rate (8, 16 and 24 kg h-1) at 3000 rpm. Physical properties of fenugreek seeds were also determined. Specific energy consumptions were found to decrease from 204.67 to 23.09 kJ kg-1 for increasing levels of feed rate and grinder screen openings. On the other hand specific energy consumption increased with increasing moisture content. The highest specific energy consumption was recorded for 17.3% moisture content and 8 kg h-1 feed rate with 0.5 mm screen opening. Average particle size decreased from 1.06 to 0.39 mm with increase of moisture content and grinder screen opening. It has been observed that the average particle size was minimum at 0.5 mm screen opening and 8 kg h-1 feed rate at lower moisture content. Bond’s work index and Kick’s constant were found to increase from 8.97 to 950.92 kWh kg-1 and 0.932 to 78.851 kWh kg-1 with the increase of moisture content, feed rate and grinder screen opening, respectively. Size reduction ratio and grinding effectiveness of fenugreek seed were found to decrease from 4.11 to 1.61 and 0.0118 to 0.0018 with the increase of moisture content, feed rate and grinder screen opening, respectively. The loose and compact bulk densities varied from 219.2 to 719.4 kg m-3 and 137.3 to 736.2 kg m-3, respectively.  

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