In vitro–in vivo and pharmacokinetic evaluation of solid lipid nanoparticles of furosemide using Gastroplus™

Ali, Hasan; Verma, Priya Ranjan Prasad; Dubey, Sunil Kumar; Venkatesan, Jayachandran; Seo, Youngwan; Kim, Se‐Kwon; Singh, Sandeep Kumar

doi:10.1039/c7ra04038e

Cited by 17 publications

(9 citation statements)

References 50 publications

(56 reference statements)

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“…The products of this process are denoted SLN-PVP-GTS (generated from the spray dried PVP/GTS formulation), SLN-IMC and SLN-5FU (formed from the IMC and 5-FU-loaded formulations respectively). These are SLNs, and the images very closely resemble those previously reported in the literature (Ali et al, 2017;Kumar and Randhawa, 2015;Vieira et al, 2016;Yuan et al, 2014). From the images, the SLNs appear to be monolithic in nature, with no evidence for any core/shell morphology or phase separation.…”

Section: Sln Self-assemblysupporting

confidence: 86%

Solid lipid nanoparticles self-assembled from spray dried microparticles

Sanchez-Vazquez

Lee

Štrimaite

et al. 2019

International Journal of Pharmaceutics

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We report the self-assembly of anti-cancer drug-loaded solid lipid nanoparticles (SLNs) from spray dried microparticles comprising poly(vinylpyrrolidone) (PVP) loaded with glyceryl tristearate (GTS) and either indomethacin (IMC) or 5-fluorouracil (5-FU). When the spray dried microparticles are added to water, the PVP matrix dissolves and the GTS and drug self-assemble into SLNs. The SLNs provide a non-toxic delivery platform for both hydrophobic (indomethacin) and hydrophilic (5-fluorouracil) drugs. They show extended release profiles over more than 24 h, and in permeation studies the drug cargo is seen to accumulate inside cancer cells. This overcomes major issues with achieving local intestinal delivery of these active ingredients, in that IMC permeates well and thus will enter the systemic circulation and potentially lead to side effects, while 5-FU remains in the lumen of the small intestine and will be secreted without having any therapeutic benefit. The SLN formulations are as effective as the pure drugs in terms of their ability to induce cell death. Our approach represents a new and simple route to the fabrication of SLNs: by assembling these from spraydried microparticles on demand, we can circumvent the low storage stability which plagues SLN formulations.

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Section: Sln Self-assemblysupporting

confidence: 86%

Solid lipid nanoparticles self-assembled from spray dried microparticles

Sanchez-Vazquez

Lee

Štrimaite

et al. 2019

International Journal of Pharmaceutics

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“…Furthermore, different pharmacokinetic compartment models, including 1C, 2C, and 3C, were statistically analyzed, and the best-fit model was selected considering high R 2 and low SC and AIC values. 22 2.6. In Vitro−In Vivo Correlation Determination.…”

Section: Pharmacokinetic Studiesmentioning

confidence: 99%

Liquid Chromatography–Electrospray Ionization Tandem Mass Spectrometry Estimation of Quercetin-Loaded Nanoemulsion in Rabbit Plasma: In Vivo–In Silico Pharmacokinetic Analysis Using GastroPlus

Das

Verma

Sekarbabu³

et al. 2023

ACS Omega

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In the present study, we developed and validated a rapid, specific, sensitive, and reproducible liquid chromatography–electrospray ionization tandem mass spectrometry method for quantifying quercetin (QT) in rabbit plasma using hydrochlorothiazide as the internal standard. Animals were orally administered with optimized QT-loaded nanoemulsion (QTNE) and QT suspension (QTS), equivalent to 30 mg/kg, to the test and control group, respectively. The blood samples were collected at pre-determined time points up to 48 h. The linearity range was from 5 to 5000 ng mL–1 with R 2 = 0.995. Further, we analyzed the various pharmacokinetic parameters and established the in vitro–in vivo correlation (IVIVC) of QTNE using GastroPlus software. The method was successfully developed and validated, and when applied for the determination of QT in rabbit plasma, it exhibited an increase in C max from 122.56 ng mL–1 (QTS) to 286.51 ng mL–1 (QTNE) (2.34-fold) and AUC0–48 from 976 ng h mL–1 (QTS) to 4249 ng h mL–1 (QTNE) (4.35-fold), indicating improved oral bioavailability QT when administered as QTNE. Statistical analysis revealed that the Loo–Riegelman method (two-compartmental method) best fitted the deconvolution approach (R 2 = 0.998, SEP = 4.537, MAE = 2.759, and AIC = 42.38) for establishing the IVIVC. In conclusion, the established bioanalytical method and IVIVC studies revealed that QTNE is a potential carrier for the effective delivery of QT with enhanced oral bioavailability.

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“…in the development of complex PBPK models of NPs [ 26 ]. However, GastroPlus has been applied for simulation and in silico prediction of pharmacokinetics and absorption of NPs [ 120 , 121 , 122 , 123 ].…”

Section: Main Pbpk Modeling Softwarementioning

confidence: 99%

Physiologically Based Pharmacokinetic Modeling of Nanoparticle Biodistribution: A Review of Existing Models, Simulation Software, and Data Analysis Tools

Kutumova

Akberdin

Kiselev

et al. 2022

IJMS

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Cancer treatment and pharmaceutical development require targeted treatment and less toxic therapeutic intervention to achieve real progress against this disease. In this scenario, nanomedicine emerged as a reliable tool to improve drug pharmacokinetics and to translate to the clinical biologics based on large molecules. However, the ability of our body to recognize foreign objects together with carrier transport heterogeneity derived from the combination of particle physical and chemical properties, payload and surface modification, make the designing of effective carriers very difficult. In this scenario, physiologically based pharmacokinetic modeling can help to design the particles and eventually predict their ability to reach the target and treat the tumor. This effort is performed by scientists with specific expertise and skills and familiarity with artificial intelligence tools such as advanced software that are not usually in the “cords” of traditional medical or material researchers. The goal of this review was to highlight the advantages that computational modeling could provide to nanomedicine and bring together scientists with different background by portraying in the most simple way the work of computational developers through the description of the tools that they use to predict nanoparticle transport and tumor targeting in our body.

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In vitro–in vivo and pharmacokinetic evaluation of solid lipid nanoparticles of furosemide using Gastroplus™

Abstract: In this work, we conducted pharmacokinetic studies and established the in vitro and in vivo correlation (IVIVC) of furosemide (FRS) loaded solid lipid nanoparticles (FSLN).

Cited by 17 publications

References 50 publications

Solid lipid nanoparticles self-assembled from spray dried microparticles

Solid lipid nanoparticles self-assembled from spray dried microparticles

Liquid Chromatography–Electrospray Ionization Tandem Mass Spectrometry Estimation of Quercetin-Loaded Nanoemulsion in Rabbit Plasma: In Vivo–In Silico Pharmacokinetic Analysis Using GastroPlus

Physiologically Based Pharmacokinetic Modeling of Nanoparticle Biodistribution: A Review of Existing Models, Simulation Software, and Data Analysis Tools

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