Application of Plakett-Burman Screening Design in Optimization of Process Parameters for Formulation of Canaglifozin Nanosuspension

2020 ◽  
Vol 13 (6) ◽  
pp. 5208-5216
Author(s):  
Nisha Patel ◽  
Hitesh A Patel
Keyword(s):  
Particle Size ◽  
Particle Diameter ◽  
Spherical Shape ◽  
Water Soluble ◽  
Pareto Chart ◽  
Independent Variables ◽  
Mean Particle Size ◽  
Screening Design ◽  
Stirring Time ◽  
Response Variables

In this study, we sought to improve the dissolution characteristics of a poorly water-soluble BCS class IV drug canaglifozin, by preparing nanosuspension using media milling method. A Plackett–Burman screening design was employed to screen the significant formulation and process variables. A total of 12 experiment were generated by design expert trial version 12 for screening 5 independent variables namely the amount of stabilizer in mg (X1), stirring time in hr (X2), amt of Zirconium oxide beads in gm (X3), amount of drug in mg (X4) and stirring speed in rpm (X5) while mean particle size in nm (Y1) and drug release in 10 min. were selected as the response variables. All the regression models yielded a good fit with high determination coefficient and F value. The Pareto chart depicted that all the independent variables except the amount of canaglifozin had a significant effect (p<0.001) on the response variables. The mathematical model for mean particle size generated from the regression analysis was given by mean particle size = +636.48889 -1.28267 amt of stabilizer(X1) -4.20417 stirring time (X2) -7.58333 amt of ZrO2 beads(X3) -0.105556 amt of drug(X4) -0.245167 stirring speed(X5) (R2=0.9484, F ratio=22.07, p<0.001). Prepared canaglifozin nanosuspension exemplified a significant improvement (p<0.05) in the release as compared to pure canaglifozin and marketed tablet with the optimum formulation releasing almost 80% drug within first 10min. Optimized nanosuspension showed spherical shape with surface oriented stabilizer molecules and a mean particle diameter of 120.5 nm. There was no change in crystalline nature after formulation and it was found to be chemically stable with high drug content.

Development and Optimization of Inhalable Levofloxacin Nanoparticles for The Treatment of Tuberculosis.

2020 ◽  
Vol 17 ◽  
Author(s):  
Sunny Shah ◽  
Rohit Ghetiya ◽  
Moinuddin Soniwala ◽  
Jayant Chavda
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Factorial Design ◽  
Full Factorial Design ◽  
Pareto Chart ◽  
Mean Particle Size ◽  
Screening Design ◽  
The Mean ◽  
Full Factorial ◽  
32 Full Factorial Design

Background:: Levofloxacin has been recommended by WHO for the treatment of pulmonary tuberculosis and inhalable delivery of levofloxacin can be advantageous over conventional delivery. Objective:: This study aimed to develop and optimize inhalable levofloxacin loaded chitosan nanoparticles (LCN). The objective was to achieve the mean particle size of LCN less than 300nm, sustain the drug release up to 24 h and achieve MMAD of LCN of less than 5μm. Methods:: LCN were prepared by ionic gelation of chitosan with sodium tripolyphosphate (STPP) and subsequent lyophilization. A Plackett Burman screening design, 32 full factorial design, and overlay plot were sequentially employed to optimize the formulation. The mean particle size, % entrapment efficiency, in vitro drug release, and Minimum inhibitory concentration were evaluated. Results:: The Pareto chart from Placket Burman screening design revealed that the concentration of chitosan and concentration of STPP were found to be significant (p < 0.05). Further analysis by 32 full factorial design revealed that F-ratio for each model generated was found to be greater than the theoretical value (p < 0.05), confirming the significance of each model. Conclusion:: The optimized formulation showed a mean particle size of 171.5 nm, sustained the drug release up to 24 h in simulated lung fluid, and revealed MMAD of 3.18 μm, which can confirm delivery of the drug to deep lung region. However, further in vivo studies are required to design suitable dosage regimen and establish the fate of nanoparticles for safe and efficacious delivery of the drug.

scholarly journals DEVELOPMENT OF SODIUM ALGINATE COATED NANOPARTICLES OF METRONIDAZOLE FOR THE TREATMENT OF PERIODONTITIS

2019 ◽  
pp. 105-110 ◽  
Author(s):  
MUKUL SINGH ◽  
GAURAV JAIN
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Biological Membrane ◽  
Spherical Shape ◽  
Prolonged Treatment ◽  
Prolonged Action ◽  
Sem Images ◽  
Mean Particle Size ◽  
Coated Nanoparticles ◽  
Acceptable Range

Objective: The present study was aimed to develop metronidazole (MNZ) loaded poly lactic-co-glycolic acid (PLGA) based mucoadhesive nanoparticles (NPs) in prolonged treatment in periodontitis. Methods: Nanoparticles were prepared by using single (SE) and double (DE) emulsion method to determine the suitability of methods. Prepared NPs were evaluated for surface morpholgy, mean particle size, polydispersity index, zeta potential, mucoadhesion ability and invitro-drug release, Results: SEM images confirmed that NPs were of spherical shape and smooth surface. Mean particle size, of MNZ loaded NPs were found 583.28±18.22 and 872.72±63.18 prepared by SE and DE method. Similarly, polidispersity index (0.68±0.1 and 0.83±0.06) and zeta potention (-33.29±0.7 and-31.28.0.6) was found in acceptable range. Prepared NPs were surface treated with Sodium alginate (SA) to increase mucoadhesive property. It was observe that particles remain adhere till 24 hr with biological membrane. Prepared NPs allow release of MNZ upto 24 h in sustained manner. Conclusion: This study confirms that the prepared MNZ loaded NPs may be used as an better alternate with addition application such as prolonged action thus improved patient compliance.

Novel Solid Lipid Nanocarrier of Glibenclamide: A Factorial Design Approach with Response Surface Methodology

2018 ◽  
Vol 24 (16) ◽  
pp. 1811-1820 ◽  
Author(s):  
Sonia Pandey ◽  
Payal Patel ◽  
Arti Gupta
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Response Surface ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
Design Approach ◽  
Therapeutic Effectiveness ◽  
Regression Equations ◽  
Independent Variables ◽  
Solid Lipid

Background: In the present investigation, a factorial design approach attempt was applied to develop the Solid Lipid Nanoparticles (SLN) of Glibenclamide (GLB) a poorly water-soluble drug (BCS -II) used in the treatment of type 2 diabetes. Objectives: Prime objectives of this experiment are to optimize the SLN formulation of Glibenclamide and improve the therapeutic effectiveness of the developed formulation. Methods: Glibenclamide loaded SLNs (GLB-SLN) were fabricated by High speed homogenization technique. A 32-factorial design approach has been employed to assess the influence of two independent variables, namely amount of Poloxamer 188 and Glyceryl Monostearate on entrapment efficiency (% EE) (Y1), Particle Size (nm) (Y2), % drug release at 8hr Q8 (Y3) and 24 hr Q24 (Y4) of prepared SLNs. Differential scanning calorimetry analysis revealed the compatibility of the drug into lipid matrix with a surfactant, while Transmission electron and Scanning electron microscopy studies indicated the size and shape of SLN. Results: The entrapment efficiency, particle size, Q8 and Q24 of the optimized SLNs were 88.93%, 125 nm, 31.12±0.951% and 86.07±1.291% respectively. Optimized GLB-SLN formula was derived from an overlay plot. Three-dimensional response surface plots and regression equations confirmed the corresponding influence of selected independent variables on measured responses. In vivo testing of the GLB-SLN in diabetic albino rats demonstrated the significant antidiabetic effect of GLB-SLN. Conclusion: The hypoglycemic effect obtained by GLB-SLN remained significantly higher than that given by drug alone and marketed formulation, further confirming the higher therapeutic effectiveness of the GLB-SLN formulation. Our findings suggested the feasibility of the investigated system for oral administration of Glibenclamide.

scholarly journals Formulation and Optimization of Nanosuspension Prepared By Media Milling Technique to Enhance the Solubility of Isradipine

2017 ◽  
Vol 9 (04) ◽  
Author(s):  
Umang Motka ◽  
Mahesh Dabhi ◽  
Navin Sheth ◽  
Ashvin Dudhrejiya
Keyword(s):  
Particle Size ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Particle Size Reduction ◽  
Saturation Solubility ◽  
Lattice Design ◽  
Media Milling ◽  
Stirring Time ◽  
Selection Of

Isradipine is a poorly water soluble antihypertensive drug has low bioavailability. The aim of this study was to formulate and characterize isradipine nanosuspension to enhance the solubility of isradipine and thus its bioavailability. Media milling technique was used for the formulation of nanosuspension. The effects of different important process parameters, i.e. the selection of stirring time, selection of concentration of zirconium beads, stirring speed were investigated by preliminary studies while concentration of stabilizers were optimized by simplex lattice design. Concentration of HPMC E3 LV(X1), Carbopol 934P(X2) and PVP K25(X3) were selected as the independent variables whereas mean particle size (Y1), saturation solubility (Y2) and cumulative percentage drug release (cpr) (Y3) were selected as dependent variables. The optimized batch had 100% w/v of zirconium beads, 0.5%w/v of PVP K25 as stabilizer, 0.1%w/v of isradipine, 15 ml of distilled water and 20 hours of stirring time. The particle size and zeta potential of optimized nanosuspension were 248.6 ± 20 nm and 13.96 ± 5 mV respectively. The size of particles of nanosuspension was measured by particle size analyser and transmission electron microscopy (TEM). Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR) analysis indicated that there was no interaction between drug and stabilizers. The saturation solubility and in vitro dissolution rate of isradipine was significantly increased by particle size reduction and which may leads to increase the bio-availability of the Isaradipine. The stability study of the formulation was carried out for a period of 12 months.

scholarly journals Diagnosis of Prostate Cancer and Prostatitis Using near Infra-Red Fluorescent AgInSe/ZnS Quantum Dots

2021 ◽  
Vol 22 (22) ◽  
pp. 12514
Author(s):  
Vuyelwa Ncapayi ◽  
Neethu Ninan ◽  
Thabang C. Lebepe ◽  
Sundararajan Parani ◽  
Aswathy Ravindran Girija ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Quantum Dots ◽  
Cancer Cells ◽  
Near Infrared ◽  
Particle Diameter ◽  
Spherical Shape ◽  
Water Soluble ◽  
Prostate Cancer Cells ◽  
Intracellular Targeting ◽  
Low Toxicity

The link between the microbiome and cancer has led researchers to search for a potential probe for intracellular targeting of bacteria and cancer. Herein, we developed near infrared-emitting ternary AgInSe/ZnS quantum dots (QDs) for dual bacterial and cancer imaging. Briefly, water-soluble AgInSe/ZnS QDs were synthesized in a commercial kitchen pressure cooker. The as-synthesized QDs exhibited a spherical shape with a particle diameter of 4.5 ± 0.5 nm, and they were brightly fluorescent with a photoluminescence maximum at 705 nm. The QDs showed low toxicity against mouse mammary carcinoma (FM3A-Luc), mouse colon carcinoma (C26), malignant fibrous histiocytoma-like (KM-Luc/GFP) and prostate cancer cells, a greater number of accumulations in Staphylococcus aureus, and good cellular uptake in prostate cancer cells. This work is an excellent step towards using ternary QDs for diagnostic and guided therapy for prostate cancer.

Advances in the Characterization of Particle Size Distributions of Abrasive Particles used in CMP

2007 ◽  
Vol 991 ◽  
Author(s):  
Mungai Kamiti ◽  
Stacey Popadowski ◽  
Edward E. Remsen
Keyword(s):  
Particle Size ◽  
Colloidal Silica ◽  
Particle Diameter ◽  
Water Soluble ◽  
Size Distributions ◽  
Organic Additives ◽  
Particle Size Distributions ◽  
Abrasive Particles ◽  
Theoretical Simulations

ABSTRACTThe use of density gradient stabilized centrifugal sedimentation (disc centrifugation) for the characterization of abrasive particles in CMP slurries is reported. For slurries prepared with ceria and colloidal silica abrasives, the technique is demonstrated as capable of providing highly repeatable analyses of the abrasive's apparent particle size distribution (PSD). The addition of water soluble organic additives to the slurries is shown to produce large shifts in the apparent PSD relative to the PSD of the pure abrasive particles. Particle-additive interactions driving the shift in apparent PSD could not be interpreted with confidence due to the lack of accurate densities for particle-abrasive complexes formed in the slurry. To address this problem, sucrose density gradients prepared using H2O and D2O were tested as spin fluids of different densities to analyze a colloidal silica standard with a narrow PSD. Preliminary results comparing experimental disc centrifuge data with theoretical simulations of the disc sedimentation pattern suggest that this technique can potentially characterize both the particle diameter and density of abrasive particles in a CMP slurry.

Preparation and In Vivo Characterization of Niosomal Carriers of the Antidiabetic Drug Repaglinide

2015 ◽  
Vol 8 (1) ◽  
pp. 2756-2767 ◽  
Author(s):  
Shrishti Namdev ◽  
Kishore Gujar ◽  
Satish Mandlik ◽  
Preeti Jamkar
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Therapeutic Effects ◽  
Drug Release Profile ◽  
Independent Variables ◽  
Span 60

The objective of this study is to prepare and characterise repaglinide niosomes using the Factorial Design strategy.Repaglinide is a potent second-generation oral hypoglycemic agent and has short half-life of 1 hour and oral bioavailability of 50%. Preparing Niosomal drugdelivery of repaglinide may increase its bioavailability which would lead to better therapeutic effects, reduce the frequency of dosing from twice a day to once a day and decrease side effects. The preliminary study was carried out for selection of surfactant and method of preparation based on least particle size and highest entrapment efficiency. For niosome preparation, organic solvent injection method was selected and span 60, cholesterol were selected as variable. A32 factorial design was used to optimize the effect of amounts of span 60(X1) and cholesterol (X2) which were the independent variables. Particle size (Y1) and entrapment efficiency (Y2) were the dependent variables. Relation between the dependent and independent variables were drawn out from the mathematical equations and response surface plots.Statistical analysis was performed using ANOVA which was found to be significant and quadratic equation was obtained by MLRA. The particle size was found to be in range of 144-497 nm and entrapment efficiency between 54-88%. Scanning electron microscopy indicated the spherical shape of the niosomes and formation of vesicle. Zeta potential analysis showed negatively charged surface with value of-36.7 mV. In vitro drug release profile showed that drug released fast initially followed by a slow release. In vivo pharmacokinetic study revealed that the niosomal preparation showed significant decrease in blood glucose level when compared to free repaglinide. The developed niosomal system also has potential of maintaining therapeutic level of RPG for longer period of time.Thus,the niosomes could be promising carriers for delivery ofrepaglinide with increased 

scholarly journals EXPLORING THE POTENTIAL OF EUDRAGIT FOR DEVELOPMENT OF MICROPARTICLES OF WATER SOLUBLE DRUG USING QUALITY BY DESIGN APPROACH

2019 ◽  
pp. 110-116
Author(s):  
SHAILESH SHARMA ◽  
NIMRATA SETH
Keyword(s):  
Drug Release ◽  
Optimization Design ◽  
Optimization Technique ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
Statistical Interpretation ◽  
Independent Variables ◽  
Water Soluble Drug ◽  
Response Variables

Objective: In the present protocol, employability of polymethacrylate polymer Eudragit RS100 for development of microparticles of water soluble drug with desired values of response variables was investigated by central composite optimization design through application of Design Expert® software (Series DX10). Methods: The microparticles were developed by emulsion solvent evaporation process employing Eudragit RS100. Two effective independent variables drug: polymer ratio and stirring speed were selected to assess performance prospective of Eudragit on mean particle size, entrapment efficiency, percent yield and drug release in 12 h of microparticles. Thirteen batches generated by software were prepared and subjected to different characterization test parameters obligatory for the evaluation of formulation. Validation of optimization model and Statistical interpretation of results was done using Analysis of Variance (ANOVA) Results: ANOVA indicated that the independent variables had significant effect on response variables. Optimized formulation demonstrated close agreement amongst experimental and predicted responses with high desirability factor. In vitro drug liberation study for optimized formulation proposed a sustained release of drug from microparticles. Conclusion: In conclusion, optimization technique was imperative in indicating the efficient applicability of Eudragit RS100 polymer in controlling the drug release of hydrophilic drugs.

Characterization of Cooling Rate and Microstructure of Rapidly Solidified Spherical Mono-Sized Sn-1.0Ag-0.5Cu Particles

2019 ◽  
Vol 960 ◽  
pp. 274-283
Author(s):  
Ying Yan Hu ◽  
Jun Feng Wang ◽  
Can Li ◽  
Jian Qiang Li
Keyword(s):  
Particle Size ◽  
Cooling Rate ◽  
Rapid Solidification ◽  
Great Influence ◽  
Particle Diameter ◽  
Spherical Shape ◽  
Phase Size ◽  
Rapidly Solidified ◽  
The Relationship

Spherical mono-sized Sn-1.0Ag-0.5Cu (wt.%) particles with diameter ranging from 124.0 to 337.4μm were prepared by the pulsated orifice ejection method (termed “POEM”).These spherical Sn-1.0Ag-0.5Cu particles exhibit a good spherical shape and a narrow size distribution, suggesting that liquid Sn-1.0Ag-0.5Cu can completely break the balance between the surface tension and the liquid static pressure in the crucible micropores and accurately control the volume of the droplets. Furthermore, the relationship between cooling rate and microstructures of spherical Sn-1.0Ag-0.5Cu particles was studied with a specific focus on different particle diameter during the rapid solidification. The cooling rate of spherical Sn-1.0Ag-0.5Cu particles with different diameter was evaluated by the Newton’s cooling model. It is revealed that the cooling rate decreases gradually with the increase of particle size during the rapidly solidified process. When the particle diameter is equal to 75 μm, the cooling rate of the Sn-1.0Ag-0.5Cu particle achieves 4.30×103 K/s which indicates that smaller particles can rapidly solidified due to their higher cooling rate. Meanwhile, the cooling rate decreases rapidly when the particle diameter increases between 75 and 100 μm. Furthermore, the different particle diameter with different cooling rate has a great influence on the solidification microstructure of Sn-1.0Ag-0.5Cu particles. The cooling rate and grain boundary size decreases with the increase of particle diameter during the rapid solidification. In addition, the phase size of βSn increases with the decrease of particle size. Smaller particles have relatively high cooling rate and it gives less solidification time as compared to larger particles. It is an effective route for fabrication of high-quality spherical Sn-1.0Ag-0.5Cu particles. Keywords: Spherical Sn-1.0Ag-0.5Cu particles; Rapid solidification; Structural; Cooling rate

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