Preparation and optimization of controlled release nanoparticles containing cefixime using Central Composite design: An attempt to enrich its antimicrobial activity

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohammad Ali Mahjoub ◽  
Pedram Ebrahimnejad ◽  
Fatemeh Shahlaee ◽  
Pouneh Ebrahimi ◽  
Zaynab Sadeghi-Ghadi
Keyword(s):  
Central Composite Design ◽  
Dissolution Rate ◽  
Ex Vivo ◽  
Chitosan Nanoparticles ◽  
Amorphous State ◽  
Scanning Tunneling ◽  
Release Kinetic ◽  
Calorimetric Analysis ◽  
Cell Culture Study ◽  
Central Composite

Background: Due to the increased resistance against existing antibiotics, research is essential to discover new and alternative ways to control infections induced by resistant pathogens. Objective: The goal of the current scrutinization was to enrich the dissolution rate and antibacterial property of cefixime (CEF) orally. Methods: To achieve the desired results, chitosan nanoparticles (NPs) containing CEF were fabricated using the ionic gelation method. Central Composite design has been applied to get the optimal formulation for the delivery of CEF. The effect of three variables such as the concentration of chitosan, tripolyphosphate, and tween 80 on the characteristics of NPs was evaluated. Results: The optimized NPs were a relatively monodispersed size distribution with an average diameter of 193 nm and a zeta potential of about 11 mV. The scanning tunneling microscope confirmed the size of NPs. The surface morphology of NPs was observed by scanning electron microscopy. The calorimetric analysis indicated the amorphous state of cefixime in the formulation. The dissolution rate of NPs in aqueous media was acceptable and the model of release kinetic for CEF from NPs followed the Peppas model. The potency of CEF in NPs against various types of bacteria was hopefully efficient. The ex- vivo release study demonstrated higher penetration of NPs from the rat intestine compared to free drug. The cell culture study showed the safety of the optimized formulation. Conclusion: It was concluded that CLN could be considered as a prospering system for the controlled delivery of CEF with advantaging its antibacterial effectiveness.

Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design

2018 ◽  
Vol 11 (6) ◽  
pp. 4337-4348
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas I
Keyword(s):  
Central Composite Design ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Release Mechanism ◽  
Solvent Evaporation Method ◽  
Onset Of Action ◽  
Evaporation Method ◽  
Central Composite

Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.

Formulation and Optimization of 5-Fluorouracil Loaded Chitosan Nanoparticles Employing Central Composite Design

2012 ◽  
Vol 2 (4) ◽  
pp. 281-289
Author(s):  
Rattan Lal ◽  
Rakesh Kumar Marwaha ◽  
Deepti Pandita ◽  
Harish Dureja
Keyword(s):  
Central Composite Design ◽  
Chitosan Nanoparticles ◽  
Central Composite

scholarly journals ATENOLOL MICROPARTICLES BY TWO-FACTOR TWO-LEVEL CENTRAL COMPOSITE DESIGN

2020 ◽  
pp. 192-201
Author(s):  
ARTI SHARMA ◽  
SUNIL K BATRA
Keyword(s):  
Drug Release ◽  
Central Composite Design ◽  
Release Kinetics ◽  
Liquid Paraffin ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Size Analysis ◽  
Release Kinetic ◽  
New Delhi ◽  
Central Composite

Objective: The objective of this research was to formulation, optimization, and evaluation of gastric-mucoadhesive microparticles which contains selective β1 receptor antagonist atenolol. Methods: The following chemicals were used, atenolol (Gangwal Chemicals Pvt. Ltd., Mumbai), ethyl cellulose (EC) (Loba Chemie Pvt. Ltd., Mumbai), Carbopol 940 (Loba Chemie Pvt. Ltd., Mumbai), liquid paraffin (Arora Pharmaceuticals Pvt. Ltd., New Delhi), and Span 80 (Central Drug House (P) Ltd., New Delhi). Microparticles were prepared by the emulsification solvent evaporation technique using polymers of Carbomer 934p (CP) and EC. Disc formulations were prepared by direct compression technique from microparticles. Microparticles of combined polymers were designed according to 22 factorial central composite design (CCD), taking EC concentration and surfactant concentration as the independent variables. A total of 13 batches were prepared. The dependent variables were percentage of % drug released and % entrapment efficiency. Results and Discussion: All evaluation tests were done for the prepared 13 formulations, such as percentage entrapment efficiency, percentage drug release, swelling index, percentage yield, and particle size analysis. The entrapment efficiency of optimized formulation was found to be 72.02%. The entrapment efficiency increases with increase in EC concentration and stirring speed. Optimized formulation was further subjected to study of drug release kinetics based on the R2 value; it was observed that Korsmeyer Peppas release kinetic model was found to be best suited for formulation of atenolol with EC: carbopol 934 by solvent evaporation method. Conclusion: The optimized formulation of microparticles containing atenolol was found to be homogeneous, good appearance and had well flow properties and better release kinetics.

Development and Optimization of Atorvastatin Calcium-Cyclodextrin Inclusion Complexed Orally-Disintegrating Tablets with Enhanced Pharmacokinetic and Pharmaco-dynamic Profile

1970 ◽  
Vol 9 (2) ◽  
pp. 3170-3180
Author(s):  
Palem Chinna Reddy ◽  
Narendar Reddy Dudhipala ◽  
Satyanarayana Goda ◽  
Varsha B. Pokharkar
Keyword(s):  
Central Composite Design ◽  
Dissolution Rate ◽  
In Vivo Studies ◽  
Drying Methods ◽  
Phase Solubility ◽  
Dissolution Profile ◽  
Atorvastatin Calcium ◽  
Central Composite ◽  
Spray Dried

The content of the investigation was to study the influence of hydroxy propyl-b-cyclodextrin (HPβCD) complexed oral disintegrating tablets (ODTs) on enhancement of solubility, dissolution rate, pharmacodynamic activity and bioavailability of atorvastatin calcium (AT) by central composite design. Based on preliminary phase solubility studies, solubility was linearly increased and followed AL-type profile. Solid complexes were prepared by physical mixing, kneading, freeze and spray drying methods. Spray-dried product showed higher solubility and dissolution rate than other complexes. Amount of drug (X1), amount of HPβCD (X2) and amount of supradisintegrant (X3) as independent and solubility (Y1), disintegration time (Y2) and percent drug release in 15 min (Q15, Y3) as dependent responses. Drug- HPβCD complex formation was confirmed by FTIR, DSC and XRD. AT-HPβCD ODTs were developed and evaluated for physico-chemical properties, stability and dissolution rate. Further, in vivo pharmacokinetic and pharmacodynamic studies were performed in rat model. The statistically optimized formulation showed 0.817 ± 0.06 mg/ml of solubility, 54 ± 2 sec of DT and 69 ± 2.4 % of Q15. The physical stability was studied for 6 months. No significant changes were detected in dissolution profile and drug content of tablets after 6 months during the stability studies. The in vivo studies of spray dried complexed tablets compared to AT in rats revealed that 3.3-folds improvement in oral bioavailability and there was significant reduction (p<0.01) in cholesterol and triglyceride levels and significant improvement (p<0.01) in HDL level. The results conclusively demonstrated that the AT-HPbCD-ODT could be prepared with improved solubility and hypolipidemic activity by using central composite design.

Development of Sertaconazole Nitrate Loaded Nanostructured Lipid Carriers Gel Using Central Composite Design: In-vitro and Ex-vivo Evaluation

2020 ◽  
Vol 10 ◽  
Author(s):  
Moreshwar Patil ◽  
Pallavi Bhagade ◽  
Meghana Amale ◽  
Sandeep Sonawane ◽  
Sanjay Kshirsagar
Keyword(s):  
Drug Release ◽  
Central Composite Design ◽  
Total Lipid ◽  
High Speed ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Topical Formulation ◽  
Central Composite

Aim: The aim of this study was to develop effective topical antifungal formulation containing sertaconazole nitrate. Background: Sertaconazole nitrate, topical antifungal was incorporated in solid-liquid lipid nanostructures and gelled further for topical application. Objective: The objective of this investigation was to develop a topical formulation containing sertaconazole nitrate which was incorporated in the solid state of matrix to prolong the release in deep skin infection and hence reduce the application frequency. Methods: The nanostructured lipid carriers of sertaconazole nitrate were developed by high speed homogenization followed by ultrasonication using Estosoft-GTS® (glyceryl tristearate) as a solid lipid, oleic acid as liquid lipid and Tween 80 as an emulsifier. Central composite design was used to optimize total lipid concentration and fraction of liquid lipid in the total lipid and its effect on entrapment efficiency and drug release was determined. Results: The carrier particles had an average size of 366.3 nm; entrapment efficiency in between 50.66% to 87.36%; cumulative drug release up to 92.90% and zeta potential of 7.43 mV. Characterization by FTIR indicated no negative interaction between drug and excipients, XRD showed disappearance of crystalline peaks of the encapsulated drug while DSC revealed complete solubilization of the drug. About 99.6% of drug was estimated by HPLC method. The drug release from gel and cream was 25.04% and 72.97% respectively. The lipid and gel excipients did not interfere with antifungal activity of the drug. Conclusion: The developed nanocarriers loaded gel were stable. It prolonged the drug release (for 24 hours) than marketed cream. It could be a promising concept for topical delivery of antifungal and anti-inflammatory materials.

Development and optimization of solid lipid nanoparticles of amikacin by central composite design

2009 ◽  
Vol 00 (00) ◽  
pp. 090721051030036-8
Author(s):  
Jaleh Varshosaz ◽  
Solmaz Ghaffari ◽  
Mohammad Reza Khoshayand ◽  
Fatemeh Atyabi ◽  
Shirzad Azarmi ◽  
...  
Keyword(s):  
Central Composite Design ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Central Composite
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