QbD-based design and characterization of mucoadhesive microspheres of quetiapine fumarate with improved oral bioavailability and brain biodistribution potential

Komati, Someshwar; Swain, Suryakanta; Rao, Muddana Eswara Bhanoji; Jena, Bikash Ranjan; Sambamoorthy, Unnam; Dasi, Vishali

doi:10.1016/j.bfopcu.2018.09.002

Cited by 21 publications

(18 citation statements)

References 12 publications

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“…To compute the independent variables (CMPs) and their capable effects upon the desired critical quality attributes (CQAs), regarded as independent factors such as peak area, retention time (Rt), and USP plate count. The focal, interactions, and quadratic effects of the influential critical method parameters i.e mobile phase ratio, flow rate, and injection volume upon the dependent factors (responses) peak area (Y1), retention time (Y2), USP plate count (Y3), are analyzed with total 17 experimental runs [24][25][26][27]. A method operable design region (MODR) or appropriate design space was earmarked, providing the best method [20], [26], [27].…”

Section: Methods Development Using Box-benkhen Design (Bbd)mentioning

confidence: 99%

Response Surface Methodology Driven Systematic Development of a Stability- indicating RP-UPLC Method for the Quantification of Aliskiren: A Renin Inhibitor

Jena

Rao

Alavala

et al. 2021

JPRI

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Aims: The current study envisages experimental design enabled rapid, sensitive, and stability-indicating RP-UPLC method to quantify Aliskiren in its pharmaceutical formulations. Study Design: Box-Benkhen experimental Design using Response surface methodology. Place and Duration of Study: Department of Analytical Research and Development, Brawn laboratories ltd., Gurugram, India, and Department of Pharmacy KL College Pharmacy, KL Deemed to be University, Vaddesearam, Guntur, Andhra Pradesh, between May 2021 and September 2021. Methodology: The chromatographic partitioning was achieved on a Waters Acuity H class UPLC system, with BEH 130οA, C18 column (100 x 2.1 mm,1.7 μm) having isocratic elution containing (50:50 %v/v) of 0.2% Glacial acetic acid (GAA) : acetonitrile, at constant flow rate using PDA detection. The optimum conditions were delineated, selecting three influential factors (CMPs), i.e., mobile phase composition, flow rate, and injection volume. Systematic optimization was accomplished by 32 Box-Benkhen design using response surface methodology (RSM). Results: The selected variables are evaluated for obtained responses (CAAs), i.e., peak area, retention time (Rt), USP Plate count. The final optimized method employed, organic phase composition 0.2 % GAA (pH 3.0) and acetonitrile 50:50 (% v/v) with 0.3 mL min-1 flow rate. The injection volume was maintained as 2μL with 2 minutes run time and λmax 280 nm. Conclusion: The method was linear for 5-300 ppm, with regression co-efficient (R2) 0.9995. As per ICH guidelines, forced degradation studies were carried out to analyse the stability profile of drug. The short Rt 1.214, minute implies superior robustness, sensitivity, and cost-effectiveness for routine analysis. The results exhibited that RSM approach of QbD will be competently used to optimize the RP-UPLC method with fewer experimental trials and error-free investigation.

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Section: Methods Development Using Box-benkhen Design (Bbd)mentioning

confidence: 99%

Response Surface Methodology Driven Systematic Development of a Stability- indicating RP-UPLC Method for the Quantification of Aliskiren: A Renin Inhibitor

Jena

Rao

Alavala

et al. 2021

JPRI

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“…Moreover, the linear regression plots between the predicted and observed benefits of the response attribute plotted using MS-Excel, imposing the line through the origin. 15,16…”

Section: Data Analysis and Validation Of The Optimization Modelmentioning

confidence: 99%

“…Still, an increase in the ratio of stearic acid and soya-lecithin exhibited a negative effect on the % EE of the formulations. 16…”

Section: Response Surface Analysis Of Entrapment Efficiencymentioning

confidence: 99%

Acyclovir Loaded Solid Lipid Nanoparticulate Gel for Ocular Delivery: Optimization by using Factorial Design

Majumdar¹,

Swain²,

Rao³

et al. 2021

IJPER

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Background: Acyclovir is a potent antiviral agent primarily used to treat viral infection in the eye, signified as Herpes Simplex Keratitis caused by Herpes Simplex Virus-1. But its applications are limited because of its poor oral bioavailability and permeability caused by significant first-pass metabolism. Objectives: The study is to design the formulation, optimization, in-vitro, ex-vivo and in-vivo characterization of solid lipid nanoparticulate gel (SLNG) of acyclovir and inspect their possibility in ocular applications. Methods: SLNG of acyclovir was prepared by hot homogenization technique and optimized by 2 3 factorial design and evaluated for in-vitro physicochemical characteristics and in-vivo pharmacokinetic study. Response surface methodology estimations and plots for optimization to obtain optimum values for response variables based on desirability criteria was performed using Design-Expert software. Results: The optimized formulation showed a particle size of 193.57±1.14 nm, zeta potential of 35±1.98 mv, drug entrapment efficiency of 82±1.59% and drug loading efficiency of 54.10±0.79%, indicating good physical stability. The transcorneal study showed a significant increase in drug permeation across the cornea as compared with the control. The drug release kinetics of the prepared formulations was best fitted to the first-order kinetic model. In-vivo pharmacokinetic studies revealed a significant enhancement in the drug level in the blood plasma of the optimized formulation as compared to the pure drug suspension. Conclusion: The acyclovir-loaded SLN gel was successfully developed, optimized, evaluated and exhibited enhanced drug permeation as well as systemic bioavailability through excised corneas. Thus, SLNG acts as a favorable approach for ocular applications of acyclovir.

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“…Owing to the advantages offered by nanocrystal, it is proposed to formulate orally disintegrating tablets (ODTs) of VOR to enhance its water solubility as well as the rate of dissolution [16] . Nanosuspension of VOR was prepared by nanoprecipitation method after optimizing various parameters.…”

Section: Introductionmentioning

confidence: 99%

Nanocrystal based orally disintegrating tablets as a tool to improve dissolution rate of Vortioxetine

Ahire

Thakkar

Borade

et al. 2021

Bulletin of Faculty of Pharmacy, Cairo University

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Major depressive disorder (MDD) or depression is a heterogeneous mental illness which have direct effect on patient's behavior and cognition; causing constant feeling of unhappiness and loss of concern in earlier enjoyed events. Vortioxetine (VOR) is a new atypical serotonergic antidepressant reported for the treatment of major MDD and has its use in various psychological disorders. Despite its therapeutic potential, it has poor water solubility which creates problem in delivery. Nanocrystal based orally disintegrating tablets (ODTs) are proposed to enhance water solubility and dissolution rate of VOR. Nanosuspension was prepared by nanoprecipitation method after optimizing various parameters. The formulated nanosuspension was effectively converted to solid powder by the lyophilization technique with emphasis on parameters like nature/concentration of cryoprotectants. Prepared nanocrystals were characterized for solid state of drug present, morphology and size after re-dispersion. The powders were then subsequently compressed into ODTs and dissolution profiles of the tablets were compared. The dissolution profile of the ODTs prepared from nanocrystals showed superior dissolution profile in comparison to ODTs prepared from untreated drug.

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QbD-based design and characterization of mucoadhesive microspheres of quetiapine fumarate with improved oral bioavailability and brain biodistribution potential

Cited by 21 publications

References 12 publications

Response Surface Methodology Driven Systematic Development of a Stability- indicating RP-UPLC Method for the Quantification of Aliskiren: A Renin Inhibitor

Response Surface Methodology Driven Systematic Development of a Stability- indicating RP-UPLC Method for the Quantification of Aliskiren: A Renin Inhibitor

Acyclovir Loaded Solid Lipid Nanoparticulate Gel for Ocular Delivery: Optimization by using Factorial Design

Nanocrystal based orally disintegrating tablets as a tool to improve dissolution rate of Vortioxetine

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