Formulation Development of Tamoxifen Loaded Lipid Nanoparticle by Taguchi (L12 (2 11)) Orthogonal Array Design

2020 ◽  
Vol 16 ◽  
Author(s):  
Poovi Ganesan ◽  
N Damodharan
Keyword(s):  
Orthogonal Array ◽  
Drug Loading ◽  
Optimization Technique ◽  
Pharmaceutical Products ◽  
Water Soluble ◽  
Nanostructured Lipid Carrier ◽  
Orthogonal Array Design ◽  
Formulation Development ◽  
Array Design ◽  
Lipid Nanoparticle

Background: A better understanding of the biopharmaceutical and physicochemical properties of drugs and the pharmaco-technical factors would be of great help for developing pharmaceutical products. But, it is extremely difficult to study the effect of each variable and interaction among them through the conventional approach Objective: To screen the most influential factors affecting the particle size (PS) of lipid nanoparticle (LNPs) (solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC)) for poorly water-soluble BCS class-II drug like tamoxifen (TMX) to improve its oral bioavailability and to reduce its toxicity to tolerable limits using Taguchi (L12 (2 11)) orthogonal array design by applying computer optimization technique. Results: The size of all LNPs formulations prepared as per the experimental design varied between 172 nm and 3880 μm, polydispersity index between 0.033 and 1.00, encapsulation efficiency between 70.8% and 75.7%, and drug loading between 5.84% and 9.68%. The study showed spherical and non-spherical as well as aggregated and non-aggregated LNPs. Besides, it showed no interaction and amorphous form of the drug in LNPs formulation. The Blank NLCs exhibited no cytotoxicity on MCF-7 cells as compared to TMX solution, SLNs (F5) and NLCs (F12) suggests that the cause of cell death is primarily from the effect of TMX present in NLCs. Conclusions: The screening study clearly showed the importance of different individual factors significant effect for the LNPs formulation development and its overall performance in an in-vitro study with minimum experimentation thus saving considerable time, efforts, and resources for further in-depth study.

scholarly journals Formulation Development and Evaluation of Hybrid Nanocarrier for Cancer Therapy: Taguchi Orthogonal Array Based Design

2013 ◽  
Vol 2013 ◽  
pp. 1-18 ◽  
Author(s):  
Rakesh K. Tekade ◽  
Mahavir B. Chougule
Keyword(s):  
Aqueous Solution ◽  
Cell Line ◽  
Orthogonal Array ◽  
Solution Concentration ◽  
Orthogonal Array Design ◽  
Formulation Development ◽  
Experimental Conditions ◽  
Array Design ◽  
Taguchi Orthogonal Array

Taguchi orthogonal array design is a statistical approach that helps to overcome limitations associated with time consuming full factorial experimental design. In this study, the Taguchi orthogonal array design was applied to establish the optimum conditions for bovine serum albumin (BSA) nanocarrier (ANC) preparation. Taguchi method with L9 type of robust orthogonal array design was adopted to optimize the experimental conditions. Three key dependent factors namely, BSA concentration (% w/v), volume of BSA solution to total ethanol ratio (v : v), and concentration of diluted ethanolic aqueous solution (% v/v), were studied at three levels 3%, 4%, and 5% w/v; 1 : 0.75, 1 : 0.90, and 1 : 1.05 v/v; 40%, 70%, and 100% v/v, respectively. The ethanolic aqueous solution was used to impart less harsh condition for desolvation and attain controlled nanoparticle formation. The interaction plot studies inferred the ethanolic aqueous solution concentration to be the most influential parameter that affects the particle size of nanoformulation. This method (BSA, 4% w/v; volume of BSA solution to total ethanol ratio, 1 : 0.90 v/v; concentration of diluted ethanolic solution, 70% v/v) was able to successfully develop Gemcitabine (G) loaded modified albumin nanocarrier (M-ANC-G) of size25.07±2.81 nm (ζ=-23.03±1.015 mV) as against to78.01±4.99 nm (ζ=-24.88±1.37 mV) using conventional method albumin nanocarrier (C-ANC-G). Hybrid nanocarriers were generated by chitosan layering (solvent gelation technique) of respective ANC to form C-HNC-G and M-HNC-G of sizes125.29±5.62 nm (ζ=12.01±0.51 mV) and46.28±2.21 nm (ζ=15.05±0.39 mV), respectively. Zeta potential, entrapment,in vitrorelease, and pH-based stability studies were investigated and influence of formulation parameters are discussed. Cell-line-based cytotoxicity assay (A549andH460cells) and cell internalization assay (H460cell line) were performed to assess the influence on the bioperformance of these nanoformulations.

Supercritical CO2 Extraction of Rhizoma Atractylodis macrocephalae

2012 ◽  
Vol 549 ◽  
pp. 60-64
Author(s):  
Zhen Huang ◽  
Xiao Han Shi ◽  
Shao Fang Liu ◽  
Wei Juan Jiang
Keyword(s):  
Particle Size ◽  
Orthogonal Array ◽  
Time Pressure ◽  
Extraction Yield ◽  
Extraction Time ◽  
Time Varying ◽  
Orthogonal Array Design ◽  
Array Design ◽  
Different Sources

An orthogonal array design was employed for optimizing the supercritical CO2 extraction of Rhizoma Atractylodis Macrocephalae. The extraction was performed at temperature from 40 to 60oC, pressure from 15 to 35MPa, extraction time varying from 30 to 90min and particle size spanning from 20 to 80 mesh. The results reflect that the extraction yield is more significantly influenced by the extraction time, pressure and particle size but less by temperature. The experiments show that the extraction yield obviously increases with increasing pressure, different from the literatures. In terms of the sample origin, a comparison shows that outstanding differences exist among the extraction yields from different sources.

scholarly journals Supercritical Fluid Extraction of Pyrrolidine Alkaloid from Leaves of Piper amalago L.

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
V. S. Carrara ◽  
L. C. Filho ◽  
V. A. S. Garcia ◽  
V. S. Faiões ◽  
E. F. Cunha-Júnior ◽  
...  
Keyword(s):  
Carbon Dioxide ◽  
Supercritical Fluid Extraction ◽  
Supercritical Fluid ◽  
Orthogonal Array ◽  
Design Matrix ◽  
Supercritical Carbon Dioxide Extraction ◽  
Orthogonal Array Design ◽  
Fluid Extraction ◽  
Array Design ◽  
Carbon Dioxide Extraction

Supercritical fluid extraction was used to extract the alkaloid N-[7-(3′,4′-methylenedioxyphenyl)-2(Z),4(Z)-heptadienoyl]pyrrolidine from leaves of Piper amalago L. A three-level orthogonal array design matrix, OAD OA9(34), was used for optimization of the parameters of supercritical extraction of the alkaloid, employing supercritical carbon dioxide: extraction time (20, 40, and 60 min), temperature (40, 50, and 60°C), pressure (150, 200, and 250 bar), and the use of cosolvents (ethanol, methanol, and propyleneglycol). All parameters had significant effect on the alkaloid yield. The alkaloid yield after 60 min of extraction without cosolvents at 9 different conditions (32) in terms of temperature (40, 50, and 60°C) and pressure (150, 200, and 250 bar) was also evaluated. The optimal yield (≈3.8 mg g−1) was obtained with supercritical CO2 + methanol (5% v : v) at 40°C and 200 bar for 60 min of extraction.

Hydroxypropylation of 1,2 Galactomannan by Taguchi's L9 Orthogonal Array Design

2021 ◽  
Vol 6 (33) ◽  
pp. 8709-8715
Author(s):  
Rakhi Tyagi ◽  
Vineet Kumar ◽  
Pradeep Sharma ◽  
Raman Nautiyal
Keyword(s):  
Orthogonal Array ◽  
Orthogonal Array Design ◽  
Array Design

Formulation Development and Evaluation of Multiple Unit Pellet System of Tamsulosin Hydrochloride

2021 ◽  
pp. 5319-5324
Author(s):  
Gavaskar Basani ◽  
Madhusudan Rao Yamsani ◽  
Ramya Sri Sura
Keyword(s):  
Extended Release ◽  
Drug Loading ◽  
Prostate Gland ◽  
Water Soluble ◽  
Formulation Development ◽  
Water Soluble Polymer ◽  
Multiple Unit ◽  
Binder Concentration ◽  
Extrusion Spheronization ◽  
Drug Coating

The aim of current work was to grow extended release multiple unit pellets of Tamsulosin Hydrochloride, is an alpha-blocker, used for the healing of the symptoms of a prostate gland condition called BPH (benign prostatic hyperplasia) by extrusion- spheronization (E/S) and solution/suspension layering (S/S) method. In the Extrusion-Spheronization, A ratio of 75:25, 67:33, 64:36 Tamsulosin Hydrochloride and Microcrystalline cellulose were mixed for making drug pellets and extended release (ER) coating was performed in fluidized bed processor (FBP) by solution/suspension layering with Ethyl cellulose (aqueous. dispersion, 4 cps and 7 cps) and Hypromellose (5cps) with different ratios % weight buildups accordingly. In the Solution/suspension layering (S/S) method, Tamsulosin Hydrochloride drug pellets were prepared by layering onto MCC spheres in FBP. These drug pellets were further coated for extended release with HPMC, 5cps and EC, 7cps. In drug coating stage, drug and different binder (Hypromellose, 5 cps) concentrations 8, 10, 12, 14 mg/unit were coated onto the cores for optimization of binder concentration. The weight of MCC spheres were optimized for further formulations. For all the drug coated pellets, ER coating was given with EC, 7cps and HPMC, 5 cps at a coating level of 8% weight by weight. In the extrusion- spheronization (E/S) Optimization of Drug pellets: Among the trials TD3 (Tamsulosin HCl and MCC) showed good mechanical strength with better yield due to increased MCC concentration. Optimization of Extended Release Coating: Optimized TD3 drug pellets were coated with ER coating using water insoluble polymer (Aq.EC 25% dispersion/ EC, 4cps/ EC, 7cps) and water soluble polymer (HPMC, 5cps). Among these polymers, extended release coating was optimized (TD3E14) with the combination of EC, 7cps and HPMC, 5cps at 8% weight build up. In the Solution/Suspension layering: Optimization of binder concentration in drug coating stage: HPMC, 5cps with 12 mg/unit for TF7 was optimized based on %yield. Optimization of MCC spheres in drug coating stage in formulation of ER pellets with different weight drug pellets: The weight of MCC spheres (160, 170, 180, 190 mg/unit) used in the drug coating stage with binder HPMC, 5cps (12 mg/unit). These drug pellets were given with ER coating at 8% weight buildup by using EC, 7cps and HPMC, 5cps. Among these trials, TF7E7 was optimized. Based on the investigations of the present study, conclusions was. formulating low dose, high soluble, BCS class I drug- Tamsulosin Hydrochloride ER formulation by extrusion-spheronization showed flexibility for batch processing and cost effectiveness while solution/suspension layering was process feasible but time consuming due to high drug loading.

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