Quetiapine Fumarate Loaded Solid Lipid Nanoparticles for Improved Oral Bioavailability

Aboti, Pooja; Shah, Payal; Patel, Dhaiwat; Dalwadi, Sonali

doi:10.2174/221030310402140805105127

Cited by 12 publications

(6 citation statements)

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“…The statistical analysis of variables was done using the analysis of variance (ANOVA). The DoE software was utilized to select the best fit model based on sequential p -value, predicted R 2 , and adjusted R 2 and lack of fit p -value (Aboti et al, 2014 ). Each factor showed their significant contribution based on F-value > 0.05 and P -value < 0.05 (Marto et al, 2016 ).…”

Section: Methodsmentioning

confidence: 99%

RETRACTED: QbD-based rivastigmine tartrate-loaded solid lipid nanoparticles for enhanced intranasal delivery to the brain for Alzheimer's therapeutics

Arora

Bhatt²,

Kumar³

et al. 2022

Front. Aging Neurosci.

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Alzheimer's disease (AD) is a neurodegenerative disease that affects a wide range of populations and is the primary cause of death in various countries. The treatment of AD is still restricted to oral conventional medicines that act only superficially. Fabrication of intranasal solid lipid nanoparticulate system for the uptake of therapeutic agents will act as a convincing approach with limited off-site toxicity and increased pharmacological activity. The objective of this study was to formulate, optimize, and evaluate the efficiency of rivastigmine tartrate (RT)-loaded intranasal solid lipid nanoparticles (SLNs) employing the solvent-evaporation diffusion method. To optimize the formulation parameters, the central composite design (CCD) was used. Lipid concentration (X1) and surfactant concentration (X2) were considered to be independent variables, while particle size (Y1), percentage entrapment efficiency (Y2), and percentage drug release (Y3) were considered as responses. The solid lipid was glyceryl monostearate, while the surfactant was polysorbate 80. The optimized formulation has a particle size of 110.2 nm, % entrapment efficiency of 82.56%, and % drug release of 94.86%. The incompatibility of drug excipients was established by differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). Nasal histopathology tests on sheep mucosa revealed that the developed SLNs were safe to utilize for intranasal delivery with no toxicity. Ex vivo permeation investigations revealed that the flux and diffusion coefficients for RT solid lipid nanoparticles and RT solution were 3.378 g/cm2 /h and 0.310–3 cm2 /h, respectively. Stability studies demonstrated that the developed SLNs were stable when stored under various storage conditions. The viability and vitality of adopting a lipid particle delivery system for improved bioavailability via the intranasal route were also established in the in vivo pharmacokinetic investigations. According to the histopathological and pharmacokinetic investigations, the developed formulations were safe, non-lethal, efficient, and robust. These results suggest the potentiality provided by rivastigmine tartrate-loaded solid lipid nanoparticles for nasal delivery.

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Section: Methodsmentioning

confidence: 99%

RETRACTED: QbD-based rivastigmine tartrate-loaded solid lipid nanoparticles for enhanced intranasal delivery to the brain for Alzheimer's therapeutics

Arora

Bhatt²,

Kumar³

et al. 2022

Front. Aging Neurosci.

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“…Quetiapine Fumarate (QF) is an atypical antipsychotic drug belonging to the 2 nd generation of antipsychotics [1]. It is frequently used for the treatment of chronic or intermittent psychotic diseases mainly schizophrenia and bipolar disorders in adults and adolescents.…”

Section: Introductionmentioning

confidence: 99%

“…The novelty of the present work lies in the use of a simple method requiring simple and easy to use equipment which has been optimised using Quality by Design (QbD) approach. The method used for the preparation of SLN does not involve the use of any organic solvent and is therefore safe as no traces of organic solvent would be left behind in the SLN, making it a better method over previously used and reported methods of QF SLN [1,3,4]. The developed SLN can be potentially used for lymphatic transport via the intestinal route for bypassing the hepatic first-pass metabolism which can result in enhanced bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Quality by Design Approach for Development and Characterisation of Solid Lipid Nanoparticles of Quetiapine Fumarate

Agarwal

Murthy

Harikumar

et al. 2020

CAD

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Background: Quetiapine fumarate, a 2nd generation anti-psychotic drug has oral bioavailability of 9% because of hepatic first pass metabolism. Reports suggest that co-administration of drugs with lipids affects their absorption pathways, enhances lymphatic transport thus bypassing hepatic first-pass metabolism resulting in enhanced bioavailability. Objective: The present work aimed at developing, and characterising potentially lymphatic absorbable Solid Lipid Nanoparticles (SLN) of quetiapine fumarate by Quality by Design approach. Method: Hot emulsification followed by ultrasonication was used as a method of preparation. Precirol ATO5, Phospholipon 90G and Poloxamer 188 were used as a lipid, stabilizer and surfactant respectively. A32 Central Composite design optimised the 2 independent variables, lipid concentration and stabilizer concentration and assessed their effect on percent Entrapment Efficiency (%EE: Y1). The lyophilized SLNs were studied for stability at 5 ±3οC and 25 ± 2οC/60 ± 5% RH for 3 months. Results: The optimised formula derived for SLN had 270mg Precirol ATO5 and 107mg of Phospholipon 90G giving %EE of 76.53%. Mean particle size was 159.8nm with polydispersity index 0.273 and zeta potential -6.6mV. In-vitro drug release followed Korsmeyer-Peppas kinetics (R2=0.917) with release exponent n=0.722 indicating non-Fickian diffusion. Transmission electron microscopy images exhibited particles to be spherical and smooth. Fourier-transform infrared spectroscopy, differential scanning calorimetry and X-ray diffraction studies ascertained drug-excipient compatibility. Stability studies suggested 5οC as appropriate temperature for storage and preserving important characteristics within acceptable limits. Conclusion: Development and optimisation by Quality by Design were justified as it yielded SLN having acceptable characteristics and potential application for intestinal lymphatic transport.

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“…Quetiapine fumarate (QF) undergoes extensive first pass metabolism with a plasma half‐life of 6 h and hence shows low oral bioavailability. Aboti et al formulated QF‐loaded SLNs using glyceryl trimyristate through double W/O/W emulsion to prepare spherical nanoparticle size ∼ 174 nm and EE of 92% [Aboti et al, ]. Constant in vitro Higuchi model release was observed for the first 12 h. In vivo studies in rats showed a prolonged peak concentration and a greater than 10‐fold increase in bioavailability for QF.…”

Section: Atypical Antipsychotic Deliverymentioning

confidence: 99%

Delivery of Antipsychotics with Nanoparticles

Sun

Chen

Liu

et al. 2016

Drug Development Research

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Preclinical Research Psychosis remains one of the most challenging health problems for society, affecting hundreds of millions of people worldwide. Although current antipsychotics can alleviate the symptoms of psychosis, they are still far away from being perfect, often causing significant and even fatal side effects such as involuntary movement disorders and metabolic syndrome. With the lack of precise knowledge of the underlying mechanisms of psychosis, a rational approach to improve the efficiency of current antipsychotics is by nanoparticle-based administration. Nanoparticles with the size of 1-500 nm can be used in drug formulations to pass through many biological barriers including the blood-brain barrier, which makes them excellent candidates for the delivery of antipsychotics. Besides that, nanoparticles loaded with antipsychotics can solve the common aqueous solubility issues for most brain targeting drugs, and enable a slow-release profile for the encapsulated drugs. This research overview provides a brief summary and discussion of the progress and development in the delivery of antipsychotics with nanoparticle formulations over the past five years (2011-2016). Drug Dev Res 77 : 393-399, 2016. © 2016 Wiley Periodicals, Inc.

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Quetiapine Fumarate Loaded Solid Lipid Nanoparticles for Improved Oral Bioavailability

Cited by 12 publications

References 0 publications

RETRACTED: QbD-based rivastigmine tartrate-loaded solid lipid nanoparticles for enhanced intranasal delivery to the brain for Alzheimer's therapeutics

RETRACTED: QbD-based rivastigmine tartrate-loaded solid lipid nanoparticles for enhanced intranasal delivery to the brain for Alzheimer's therapeutics

Quality by Design Approach for Development and Characterisation of Solid Lipid Nanoparticles of Quetiapine Fumarate

Delivery of Antipsychotics with Nanoparticles

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