Full Factorial Design and Optimization of Olmesartan Medoxomil–Loaded Oily-Core Polymeric Nanocapsules with Improved In-Vitro Stability

Author(s):  
Waleed M. Khattab ◽  
Esmat E. Zein El-Dein ◽  
Sanaa A. El-Gizawy
2019 ◽  
Vol 15 (4) ◽  
pp. 651-663
Author(s):  
Radwa M. A. Abd-Elal ◽  
Ghada H. Elosaily ◽  
Shadeed Gad ◽  
El-Sayed Khafagy ◽  
Yasser Mostafa

Author(s):  
SATISH K. MANDLIK ◽  
PAYAL P. AGARWAL ◽  
HARSHAL P. DANDGAVHAL

Objective: Ritonavir is an antiretroviral drug used for HIV-AIDS treatment. The purpose of this research work was to implement the quality by design (QbD) approach in formulation of ritonavir sustained-release pellets by industrially applied extrusion spheronization technique. Methods: Pellets were prepared by extrusion spheronization method and evaluated for their physicochemical properties. Initially, on the basis of prior knowledge Quality Target Product Profile (QTTP) element was identified and further Critical Quality Attributes (CQA) elements were defined. Risk assessment (RA) was done by two tools as failure mode and effect analysis (FMEA) and fishbone diagram (Ishikawa plot). Placket Burman design was implemented as a screening design using seven high-risk factors (spheronization speed, spheronization time, extrusion speed, drying method, PVP K 30, cross povidone, and solvent). Optimization study was done by 23 full factorial design with three critical factors as (spheronization speed, extrusion speed and PVP K 30). The in vitro drug release was studied in both gastric and intestinal fluids for 12 h using USP Ι apparatus. Control space was established for the sustained release pellets. Results: Among all batches obtained in 23 full factorial design, batch R7 was found to be effective with carr’s index value of 5.281, percentage yield of 69.6%, time required to release 50% drug was 8 h and percent drug release after 12 h was found 83.132 %, R7 batch was selected as optimized batch. Statistical analysis showed model terms were significant. Conclusion: We can conclude that; sustained-release pellets of ritonavir were successfully designed using QbD approach.


2015 ◽  
Vol 2015 ◽  
pp. 1-12
Author(s):  
Yen-Sheng Chen ◽  
Ting-Yu Ku

This paper presents an extremely efficient method for antenna design and optimization. Traditionally, antenna optimization relies on nature-inspired heuristic algorithms, which are time-consuming due to their blind-search nature. In contrast, design of experiments (DOE) uses a completely different framework from heuristic algorithms, reducing the design cycle by formulating the surrogates of a design problem. However, the number of required simulations grows exponentially if a full factorial design is used. In this paper, a much more efficient technique is presented to achieve substantial time savings. By using orthogonal fractional experiments, only a small subset of the full factorial design is required, yet the resultant response surface models are still effective. The capability of orthogonal fractional experiments is demonstrated through three examples, including two tag antennas for radio-frequency identification (RFID) applications and one internal antenna for long-term-evolution (LTE) handheld devices. In these examples, orthogonal fractional experiments greatly improve the efficiency of DOE, thereby facilitating the antenna design with less simulation runs.


2021 ◽  
Vol 18 (1) ◽  
pp. 61-67
Author(s):  
Shailendra BHATT ◽  
Jai Bharti SHARMA ◽  
Ruchi KAMBOJ ◽  
Manish KUMAR ◽  
Vipin SAINI ◽  
...  

Polymers ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 772 ◽  
Author(s):  
Hazem Abdul Kader Sabbagh ◽  
Samer Hasan Hussein-Al-Ali ◽  
Mohd Zobir Hussein ◽  
Zead Abudayeh ◽  
Rami Ayoub ◽  
...  

The goal of this study was to develop and statistically optimize the metronidazole (MET), chitosan (CS) and alginate (Alg) nanoparticles (NP) nanocomposites (MET-CS-AlgNPs) using a (21 × 31 × 21) × 3 = 36 full factorial design (FFD) to investigate the effect of chitosan and alginate polymer concentrations and calcium chloride (CaCl2) concentration ondrug loading efficiency(LE), particle size and zeta potential. The concentration of CS, Alg and CaCl2 were taken as independent variables, while drug loading, particle size and zeta potential were taken as dependent variables. The study showed that the loading efficiency and particle size depend on the CS, Alg and CaCl2 concentrations, whereas zeta potential depends only on the Alg and CaCl2 concentrations. The MET-CS-AlgNPs nanocomposites were characterized by X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), thermal gravimetric analysis (TGA), scanning electron microscopy (SEM) and in vitro drug release studies. XRD datashowed that the crystalline properties of MET changed to an amorphous-like pattern when the nanocomposites were formed.The XRD pattern of MET-CS-AlgNPs showed reflections at 2θ = 14.2° and 22.1°, indicating that the formation of the nanocompositesprepared at the optimum conditions havea mean diameter of (165±20) nm, with a MET loading of (46.0 ± 2.1)% and a zeta potential of (−9.2 ± 0.5) mV.The FTIR data of MET-CS-AlgNPs showed some bands of MET, such as 3283, 1585 and 1413 cm−1, confirming the presence of the drug in the MET-CS-AlgNPs nanocomposites. The TGA for the optimized sample of MET-CS-AlgNPs showed a 70.2% weight loss compared to 55.3% for CS-AlgNPs, and the difference is due to the incorporation of MET in the CS-AlgNPs for the formation of MET-CS-AlgNPs nanocomposites. The release of MET from the nanocomposite showed sustained-release properties, indicating the presence of an interaction between MET and the polymer. The nanocomposite shows a smooth surface and spherical shape. The release profile of MET from its MET-CS-AlgNPs nanocomposites was found to be governed by the second kinetic model (R2 between 0.956–0.990) with more than 90% release during the first 50 h, which suggests that the release of the MET drug can be extended or prolonged via the nanocomposite formulation.


2019 ◽  
Vol 0 (0) ◽  
pp. 0-0
Author(s):  
Shailendra Bhatt ◽  
Ruchi Kamboj ◽  
JAI BHARTI SHARMA ◽  
Manish Kumar ◽  
Vipin Saini ◽  
...  

2020 ◽  
Vol 17 (6) ◽  
pp. 523-539
Author(s):  
Jalpa Patel ◽  
Dhaval Mori

Background: Developing a new excipient and obtaining its market approval is an expensive, time-consuming and complex process. Compared to that, the co-processing of already approved excipients has emerged as a more attractive option for bringing better characteristic excipients to the market. The application of the Design of Experiments (DoE) approach for developing co-processed excipient can make the entire process cost-effective and rapid. Objective: The aim of the present investigation was to demonstrate the applicability of the DoE approach, especially 32 full factorial design, to develop a multi-functional co-processed excipient for the direct compression of model drug - cefixime trihydrate using spray drying technique. Methods: The preliminary studies proved the significant effect of atomization pressure (X1) and polymer ratio (microcrystalline cellulose: mannitol - X2) on critical product characteristics, so they were selected as independent variables. The angle of repose, Carr’s index, Hausner’s ratio, tensile strength and Kuno’s constant were selected as response variables. Result: The statistical analysis proved a significant effect of both independent variables on all response variables with a significant p-value < 0.05. The desirability function available in Design Expert 11® software was used to prepare and select the optimized batch. The prepared co-processed excipient had better compressibility than individual excipients and their physical mixture and was able to accommodate more than 40 percent drug without compromising the flow property and compressibility. Conclusion: The present investigation successfully proved the applicability of 32 full factorial design as an effective tool for optimizing the spray drying process to prepare a multi-functional co-processed excipient.


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