Optimization and design of an ibuprofen-loaded nanostructured lipid carrier with a 23 full factorial design

Effect of The Surfactant and Liquid Lipid Type in The Physico-chemical Characteristics of Beeswax-based Nanostructured Lipid Carrier (NLC) of Metformin

Pharmaceutical Nanotechnology ◽

10.2174/2211738509666210222143716 ◽

2021 ◽

Vol 09 ◽

Author(s):

Mona Qushawy

Keyword(s):

Drug Release ◽

Factorial Design ◽

Biological Membrane ◽

Entrapment Efficiency ◽

Tween 80 ◽

Full Factorial Design ◽

Nanostructured Lipid Carrier ◽

Class Iii ◽

Scanning Calorimetry ◽

Full Factorial

Background: Metformin (MF) is an antidiabetic drug that belongs to class III of the biopharmaceutical classification system (BCS) which is characterized by high solubility and low permeability. Objective: The study aimed to prepare metformin as nanostructured lipid carriers (MF-NLCs) to control the drug release and enhance its permeability through the biological membrane. Method: 22 full factorial design was used to make the design of MF-NLCs formulations. MF-NLCs were prepared by hot-melt homogenization-ultra sonication technique using beeswax as solid lipid in presence of liquid lipid (either capryol 90 or oleic acid) and surfactant (either poloxamer 188 or tween 80). Results: The entrapment efficiency (EE%) of MF-NLCs was ranged from 85.2±2.5 to 96.5±1.8%. The particle size was in the nanoscale (134.6±4.1 to 264.1±4.6 nm). The value of zeta potential has a negative value ranged from -25.6±1.1 to -39.4±0.9 mV. The PDI value was in the range of (0.253±0.01 to 0.496±0.02). The cumulative drug release was calculated for MF-NLCs and it was found that Q12h ranged from 90.5±1.7 % for MF-NLC1 to 99.3±2.8 for MF-NLC4. Infra-red (IR) spectroscopy and differential scanning calorimetry (DSC) studies revealed the compatibility of the drug with other ingredients. MF-NLC4 was found to the optimized formulation with the best responses. Conclusion: 22 full factorial design succeed to obtain an optimized formulation which controls the drug release and increases the drug penetration.

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Application of 32 Full Factorial Design and Desirability Function for Optimizing The Manufacturing Process for Directly Compressible Multi-Functional Co-Processed Excipient

Current Drug Delivery ◽

10.2174/1567201817666200508094743 ◽

2020 ◽

Vol 17 (6) ◽

pp. 523-539

Author(s):

Jalpa Patel ◽

Dhaval Mori

Keyword(s):

Factorial Design ◽

Spray Drying ◽

Desirability Function ◽

Full Factorial Design ◽

Angle Of Repose ◽

P Value ◽

Independent Variables ◽

Full Factorial ◽

32 Full Factorial Design ◽

Response Variables

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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Formulation of Extended-Release Beads of Lamotrigine Based on Alginate and Cassia fistula Seed Gum by QbD Approach

Current Drug Delivery ◽

10.2174/1567201817666200317124022 ◽

2020 ◽

Vol 17 (5) ◽

pp. 422-437

Author(s):

Dixita Jain ◽

Akshay Sodani ◽

Swapnanil Ray ◽

Pranab Ghosh ◽

Gouranga Nandi

Keyword(s):

Drug Release ◽

Factorial Design ◽

Extended Release ◽

Polymer Concentration ◽

Green Manufacturing ◽

Full Factorial Design ◽

Cassia Fistula ◽

Negative Environmental Impact ◽

Seed Gum ◽

Full Factorial

Aim: This study was focused on the formulation of the multi-unit extended-release peroral delivery device of lamotrigine for better management of epilepsy. Background: The single-unit extended-release peroral preparations often suffer from all-or-none effect. A significant number of multi-unit delivery systems have been reported as a solution to this problem. But most of them are found to be composed of synthetic, semi-synthetic or their combination having physiological toxicity as well as negative environmental impact. Therefore, fabrication and formulation of multi-unit extended-release peroral preparations with natural, non-toxic, biodegradable polymers employing green manufacturing processes are being appreciated worldwide. Objective: Lamotrigine-loaded extended-release multi-unit beads have been fabricated with the incorporation of a natural polysaccharide Cassia fistula seed gum in calcium-cross-linked alginate matrix employing a simple green process and 23 full factorial design. Methods: The total polymer concentration, polymer ratio and [CaCl2] were considered as independent formulation variables with two different levels of each for the experiment-design. The extended-release beads were then prepared by the ionotropic gelation method using calcium chloride as the crosslinkerions provider. The beads were then evaluated for drug encapsulation efficiency and drug release. ANOVA of all the dependent variables such as DEE, cumulative % drug release at 2h, 5h, 12h, rate constant and dissolution similarity factor (f2) was done by 23 full factorial design using Design-Expert software along with numerical optimization of the independent variables in order to meet USP-reference release profile. Results: The optimized batch showed excellent outcomes with DEE of 84.7 ± 2.7 (%), CPR2h of 8.41± 2.96 (%), CPR5h of 36.8± 4.7 (%), CPR12h of 87.3 ± 3.64 (%) and f2 of 65.9. Conclusion: This approach of the development of multi-unit oral devices utilizing natural polysaccharides might be inspiring towards the world-wide effort for green manufacturing of sustained-release drug products by the QbD route.

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