Effect of particle size on the biodistribution of lipid nanocapsules: Comparison between nuclear and fluorescence imaging and counting

Hirsjärvi, Samuli; Sancey, Lucie; Dufort, Sandrine; Belloche, Camille; Vanpouille-Box, Claire; Garcion, Emmanuel; Coll, Jean‐Luc; Hindré, François; Benoı̂t, Jean-Pierre

doi:10.1016/j.ijpharm.2013.05.057

Cited by 58 publications

(46 citation statements)

References 57 publications

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“…On the other hand, the application of nuclear imaging techniques such as single photon emission computed tomography (SPECT) or positron emission tomography (PET) utilizing isotopically labeled EVs hardly can be found in the literature, despite the fact that these techniques have indisputable advantages over fluorescent imaging regarding quantitative measurement of the biodistribution of the labeled compounds. 20 In this paper we report a novel method for radioisotope labeling of EVs using 99m…”

Section: Introductionmentioning

confidence: 99%

Radiolabeling of Extracellular Vesicles with ^99mTc for Quantitative In Vivo Imaging Studies

Varga

Gyurkó

Pálóczi

et al. 2016

Cancer Biotherapy and Radiopharmaceuticals

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The biodistribution of extracellular vesicles (EVs) is a fundamental question in the field of circulating biomarkers, which has recently gained attention. Despite the capabilities of nuclear imaging methods such as single photon emission computed tomography (SPECT), radioisotope labeling of EVs and the use of the aforementioned methods for in vivo studies hardly can be found in the literature. In this paper we describe a novel method for the radioisotope labeling of erythrocyte-derived EVs using the 99m Tctricarbonyl complex. Moreover, the capability of the developed labeling method for in vivo biodistribution studies is demonstrated in a mouse model. We found that the intravenously administered, According to our data, only a minor fraction of the radioactive label became detached from the EVs.

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Section: Introductionmentioning

confidence: 99%

Radiolabeling of Extracellular Vesicles with ^99mTc for Quantitative In Vivo Imaging Studies

Varga

Gyurkó

Pálóczi

et al. 2016

Cancer Biotherapy and Radiopharmaceuticals

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“…[14][15][16][17] Some recent studies have focused on the in vivo fate of nanoparticles using various biosensing tools, such as fluorescent imaging, computed tomography, and magnetic resonance imaging. 18 In this study, we used a noninvasive fluorescence imaging system and microdialysis techniques to analyze the in vivo fate of puerarin (PUE)-scutellarin (SCU) cationic lipid nanoparticles (CLNs).…”

Section: Introductionmentioning

confidence: 99%

Novel cationic lipid nanoparticles as an ophthalmic delivery system for multicomponent drugs: development, characterization, in vitro permeation, in vivo pharmacokinetic, and molecular dynamics studies

Wang¹,

Zhao²,

Li³

et al. 2017

IJN

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The purpose of this study was to prepare, optimize, and characterize a cationic lipid nanoparticle (CLN) system containing multicomponent drugs using a molecular dynamics model as a novel method of evaluating formulations. Puerarin (PUE) and scutellarin (SCU) were used as model drugs. CLNs were successfully prepared using melt-emulsion ultrasonication and low temperature-solidification technique. The properties of CLNs such as morphology, particle size, zeta potential, entrapment efficiency (EE), drug loading (DL), and drug release behavior were investigated. The CLNs were evaluated by corneal permeation, preocular retention time, and pharmacokinetics in the aqueous humor. Additionally, a molecular dynamics model was used to evaluate the formulation. Electron microscopy results showed that the nanoparticles were approximately spherical in shape. The EE (%) and DL (%) values of PUE and SCU in the optimal formulation were 56.60±3.73, 72.31±1.96 and 1.68±0.17, 2.44±1.14, respectively. The pharmacokinetic study in the aqueous humor showed that compared with the PUE and SCU solution, the area under the concentration–time curve (AUC) value of PUE was enhanced by 2.33-fold for PUE-SCU CLNs ( p <0.01), and the SCU AUC was enhanced by 2.32-fold ( p <0.01). In the molecular dynamics model, PUE and SCU passed through the POPC bilayer, with an obvious difference in the free energy well depth. It was found that the maximum free energy required for PUE and SCU transmembrane movement was ~15 and 88 kJ·mol −1 , respectively. These findings indicated that compared with SCU, PUE easily passed through the membrane. The diffusion coefficient for PUE and SCU were 4.1×10 −3 ±0.0027 and 1.0×10 −3 ±0.0006 e −5 cm 2 ·s −1 , respectively. Data from the molecular dynamics model were consistent with the experimental data. All data indicated that CLNs have a great potential for ocular administration and can be used as an ocular delivery system for multicomponent drugs. Moreover, the molecular dynamics model can also be used as a novel method for evaluating formulations.

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“…43 However, 25 nm LNCs quickly disappeared from the blood circulation. 46 As a consequence, 55 nm LNCs were chosen for diffusion studies in a function of their concentration.…”

mentioning

confidence: 99%

Fate of paclitaxel lipid nanocapsules in intestinal mucus in view of their oral delivery

Groo¹,

Saulnier²,

Gimel³

et al. 2013

IJN

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The bioavailability of paclitaxel (Ptx) has previously been improved via its encapsulation in lipid nanocapsules (LNCs). In this work, the interactions between LNCs and intestinal mucus are studied because they are viewed as an important barrier to successful oral delivery. The rheological properties of different batches of pig intestinal mucus were studied under different conditions (the effect of hydration and the presence of LNCs). Fluorescence resonance energy transfer (FRET) was used to study the stability of LNCs in mucus at 37°C for at least 3 hours. Diffusion through 223, 446, and 893 μm mucus layers of 8.4, 16.8, and 42 μg/mL Ptx formulated as Taxol® (Bristol-Myers Squibb, Rueil-Malmaison, France) or encapsulated in LNCs (Ptx-LNCs) were investigated. The effect of the size of the LNCs on their diffusion was also investigated (range, 25–110 nm in diameter). Mucus behaves as a non-Newtonian gel with rheofluidifying properties and a flow threshold. The viscous (G″) and elastic (G′) moduli and flow threshold of the two mucus batches varied with water content, but G′ remained below G″. LNCs had no effect on mucus viscosity and flow threshold. The FRET efficiency remained at 78% after 3 hours. Because the destruction of the LNCs would lead to a FRET efficiency below 25%, these results suggest only a slight modification of LNCs after their contact with mucus. The diffusion of Taxol® and Ptx-LNCs in mucus decreases if the mucus layer is thicker. Interestingly, the apparent permeability across mucus is higher for Ptx-LNCs than for Taxol® for drug concentrations of 16.8 and 42 μg/mL Ptx ( P <0.05). The diffusion of Ptx-LNCs through mucus is not size-dependent. This study shows that LNCs are stable in mucus, do not change mucus rheological properties, and improve Ptx diffusion at low concentrations, thus making these systems good candidates for Ptx oral delivery. The study of the physicochemical interaction between the LNC surface and its diffusion in mucus is now envisioned.

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Effect of particle size on the biodistribution of lipid nanocapsules: Comparison between nuclear and fluorescence imaging and counting

Cited by 58 publications

References 57 publications

Radiolabeling of Extracellular Vesicles with ^99mTc for Quantitative In Vivo Imaging Studies

Radiolabeling of Extracellular Vesicles with ^99mTc for Quantitative In Vivo Imaging Studies

Novel cationic lipid nanoparticles as an ophthalmic delivery system for multicomponent drugs: development, characterization, in vitro permeation, in vivo pharmacokinetic, and molecular dynamics studies

Fate of paclitaxel lipid nanocapsules in intestinal mucus in view of their oral delivery

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Effect of particle size on the biodistribution of lipid nanocapsules: Comparison between nuclear and fluorescence imaging and counting

Cited by 58 publications

References 57 publications

Radiolabeling of Extracellular Vesicles with 99mTc for Quantitative In Vivo Imaging Studies

Radiolabeling of Extracellular Vesicles with 99mTc for Quantitative In Vivo Imaging Studies

Novel cationic lipid nanoparticles as an ophthalmic delivery system for multicomponent drugs: development, characterization, in vitro permeation, in vivo pharmacokinetic, and molecular dynamics studies

Fate of paclitaxel lipid nanocapsules in intestinal mucus in view of their oral delivery

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Radiolabeling of Extracellular Vesicles with ^99mTc for Quantitative In Vivo Imaging Studies

Radiolabeling of Extracellular Vesicles with ^99mTc for Quantitative In Vivo Imaging Studies