scholarly journals Application of Plackett-Burman design for screening of factors affecting pitavastatin nanoparticle formulation development

Folia Medica ◽  
2021 ◽  
Vol 63 (5) ◽  
pp. 775-785
Author(s):  
Vinodkumar D. Ramani ◽  
Girish K. Jani ◽  
Girish U. Sailor

Introduction: Nanoparticle formulation of pitavastatin calcium is a potential alternative to solve the solubility related problem. However, the formulation of nanoparticle involves various parameters that affect product quality. Plackett-Burman design could facilitate an economical experimental plan that focuses on determining the relative significance of many. Aim: The objective of this study was to screen the variables which could significantly affect the pitavastatin nanoparticle formulation. Materials and methods: The pitavastatin nanoparticles were formulated by preparing nanosuspension using the emulsion solvent evaporation technique followed by freeze-drying. A Plackett-Burman screening design methodology was employed in which seven factors at two levels were tested at 12 runs to study the effect of formulation and process variables on particle size and polydispersity index of nanoparticles. The surface morphology and crystalline nature of nanoparticle were also evaluated. Results: The particle size and polydispersity index of nanosuspension was found in the range of 113.1 to 768.5 nm and 0.068 to 0.508, respectively. Statistical analysis of various variables revealed that stabilizer concentration, injection flow rate, and stirring rate were the most influential factors affecting the particle size and polydispersity index of the formulation. X-ray diffraction (XRD) and scanning electron microscopy (SEM) study suggested the amorphous nature of nanoparticles. Conclusions: This study concluded that the Plackett-Burman design was an efficient tool for screening the process and formulation variables affecting the properties of pitavastatin nanoparticles and also for the identification of the most prominent factor.

Author(s):  
Anubhav Anand ◽  
Gyanendra Singh ◽  
Shubhini A Saraf

Objective: Plackett–Burman experimental design is used to identify the most important factors early in the experimentation phase when complete knowledge about the system is usually unavailable. The objective of this study was to screen out the most important factors affecting the size and entrapment efficiency of rivastigmine hydrogen tartrate (RHT) nanostructured lipid carriers (NLCs).Methods: The RHT-loaded NLC was prepared by the modified solvent emulsification-diffusion method. The independent variables selected for Plackett–Burman design were drug: lipid ratio, solid lipid/liquid lipid (S/L) ratio, concentration Ryoto sugar ester (%w/v), the concentration of poloxamer 188 (%w/v), sonication time (min), sonication amplitude, and stirring time (h).Results: The R2 value for the particle size equation was 86.16%. p value was (<0.05) 0.048 in case of sonication time. In case of entrapment efficiency, the R2 value was 87.12%. The p value (p<0.05) for S/L ratio and the Ryoto sugar (% w/v) was 0.028 and 0.042, respectively.Conclusion: It can be concluded that sonication time has a significant effect on particle size, whereas S/L ratio and Ryoto sugar ester concentration have a significant effect on entrapment efficiency.


Author(s):  
Niwash Kumar

Abstract: The purpose of this study was to prepare Pyridostigmine nanoparticles for control release of Pyridostigmine to improve the oral bioavailability, enhance the solubility and dissolution rate by decreasing particle size of drug. Infrared spectroscopic studies confirmed that there was no interaction between drug and polymers. The controlled release Pyridostigmine nanoparticles were prepared by Solvent evaporation by using Ethyl cellulose, Chitosan & HPMC K100 at different ratios. The production yield of the formulated controlled release nanoparticles (F1 to F16) in the range of 76.11 % to 83.58 %. The drug content of the formulated controlled release nanoparticles (F1 to F16) in the range of 82.56 %to 98.20%. The Theoretical loading of the formulated controlled release nanoparticles (F1- F16) in the range of 24.43 % to 64.24%. The entrapment efficiency increased with increasing the concentration of polymers and the formulations containing chitosan nanoparticles F6 (1:2) showed better entrapment (90.94%) among all formulation. The solubility of selected formulation (F6) in 0.2 M Phosphate buffer pH 6.8 increased when compared to pure drug. Particle size distribution was determined by Malvern zeta size, the size range for produced nanoparticles in the range of 200 nm to 400 nm. The Polydispersity index of selected nanoparticle formulation (F6) was indicated a narrow range and a homogeneous size distribution of particles. The in vitro dissolution study was carried out in 0. 2N PBS for 2 hours and phosphate buffer pH 6.8 for 10 hours. The formulations shows controlled release of drug up to 12 hrs and all formulations showed more than 75% of drug release. The release kinetics showed that the formulations were complies with Zero order kinetics followed by diffusion controlled mechanism. The best formulation F6 was evaluated by infrared spectroscopy, particle size, Polydispersity index & zeta potential and Scanning Electron microscopy. Best formulation of nanoparticles shown the extent of drug release was found to be F6 (96.93%) in 12 hrs. SEM studies confirmed the morphology of the nanoparticle formulation. Keywords: Polydispersity index, Zeta potential, Scanning Electron microscopy, Pyridostigmine


Author(s):  
Asghar Azizi ◽  
Reza Ghaedrahmati

A response surface method using a central composite design was employed to evaluate, model and optimize the influence of five main factors in the gold cyanidation process. These factors were pH, solid percentage, NaCN concentration, particle size and leaching time. A second-order equation was proposed and developed for the relationship between the gold recoveries and influential factors. The modelling results indicated that the factors influencing the degree of cyanide leaching of gold were in the order of leaching time > NaCN concentration 2 > particle size > pH > NaCN concentration > leaching time 2 > solid percentage × particle size > solid percentage × NaCN concentration > solid percentage. Also, we obtained a coefficient of determination ( R 2 ) greater than 93%, which showed that the developed model was well fitted to the experimental data. In addition, the model equation was individually optimized by using quadratic programming to maximize gold recoveries within the experimental range. The optimum condition was found to be pH 10.11 for the solution, 36.07% for the solids content, 729.56 ppm for the NaCN concentration, 37.52  μ m for the particle size and 23.2 h for the leaching time. Under these conditions, the highest recovery of gold was achieved of approximately 91.5%.


2011 ◽  
Vol 10 (46) ◽  
pp. 9402-9409 ◽  
Author(s):  
Zauri Abdul Wahid Manisya ◽  
Salleh Madihah ◽  
Yusof Faridah ◽  
Ismail Abdul Karim Mohammed ◽  
Zahangir Alam Md

Author(s):  
Arti Bagada ◽  
K R Vadalia ◽  
M K Raval ◽  
Dolly Gadhia

This investigation aimed to prepare Cilnidipine Nanoparticles by nanoprecipitation ultrasonication method and to study the significance of processing variables by applying quality by design. Cilnidipine is fourth-generation dual L/N-type Ca2+ channel blocker used for the management of hypertension. It is BCS class-II drug exhibiting lower aqueous solubility, which tends to lower bioavailability. The combination of Poloxamer 188 and Tween 80 was used as a stabilizer. The design of the experiment is one of the tools of Quality by design. Plackett-Burman design was applied for the screening of processing variables, which are significant for the method. The processing variables screened were stirring speed, antisolvent ratio, drug concentration, polymer concentration, stabilizer concentration. The effect of each parameter evaluated by particle size, entrapment efficiency, and drug release at 10 minutes of prepared Nanoparticles of Cilnidipine. Analysis of variance and Pareto-plot of Plackett-Burman design were utilized to find the significance of the factor and extent of the effect. The surface morphology of Cilnidipine Nanoparticles was studied by SEM. The Pareto plot, as well as statistical analysis of design, had shown that the Concentration of drug, solvent: antisolvent ratio and concentration of poloxamer 188 were the significant parameters for the method. The stabilizer concentration, the stirring speed, and the antisolvent ratio had a negative effect of while the concentration of drug has a positive effect on the particle size of Nanoparticles and drug release at 10 minutes and positive effect of entrapment efficiency of Cilnidipine Nanoparticles. The Cilnidipine Nanoparticles were characterized by FTIR and DSC analysis.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 178
Author(s):  
Heba A. Ghanem ◽  
Ali M. Nasr ◽  
Tamer H. Hassan ◽  
Mahmoud M. Elkhoudary ◽  
Reem Alshaman ◽  
...  

The aim of the current study is to establish a comprehensive experimental design for the screening and optimization of Atorvastatin-loaded nanostructured lipid carriers (AT-NLCs). Initially, combined D-optimal screening design was applied to find the most significant factors affecting AT-NLCs properties. The studied variables included mixtures of solid and liquid lipids, the solid/liquid lipid ratio, surfactant type and concentration, homogenization speed as well as sonication time. Then, the variables homogenization speed (A), the ratio of solid lipid/liquid lipid (B), and concentration of the surfactant (C) were optimized using a central composite design. Particle size, polydispersity index, zeta potential, and entrapment efficiency were chosen as dependent responses. The optimized AT-NLCs demonstrated a nanometric size (83.80 ± 1.13 nm), Polydispersity Index (0.38 ± 0.02), surface charge (−29.65 ± 0.65 mV), and high drug incorporation (93.1 ± 0.04%). Fourier Transform Infrared Spectroscopy (FTIR) analysis showed no chemical interaction between Atorvastatin and the lipid mixture. Differential Scanning Calorimetry (DSC) analysis of the AT-NLCs suggested the transformation of Atorvastatin crystal into an amorphous state. Administration of the optimized AT-NLCs led to a significant reduction (p < 0.001) in serum levels of rats’ total cholesterol, triglycerides, and low-density lipoproteins. This change was histologically validated by reducing the relevant steatosis of the liver.


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