The Effects of oil-in-Water Nanoemulsion Polyethylene Glycol Surface Density on Intracellular Stability, Pharmacokinetics, and Biodistribution in Tumor Bearing Mice

Hak, Sjoerd; Garaiova, Zuzana; Olsen, Linda Therese; Nilsen, Asbjørn Magne; Davies, Catharina de Lange

doi:10.1007/s11095-014-1553-6

Cited by 18 publications

(11 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Preclinical studies have shown that BBR has a very limited oral bioavailability (BA) (< 5% in plasma), largely due to its poor aqueous solubility, combined with low gastrointestinal absorption, and rapid metabolism [ 48 ]. However, novel self-nanoemulsion system is an emerging area of science and includes material application on the nanometre scale in various domains, including biology, chemistry, medicine, and engineering [ 49 ]. It is likely to improve the solubility stability and selectivity of drugs, improving the permeability of drugs while treating solid tumours through the enhanced permeability and retention effect, even for the blood brain barrier, which is high correlated with leukemia metastasis of the bone borrow [ 50 ].…”

Section: Discussionmentioning

confidence: 99%

Self-nanoemulsifying system improves oral absorption and enhances anti-acute myeloid leukemia activity of berberine

Yang

Shen

et al. 2018

J Nanobiotechnol

View full text Add to dashboard Cite

BackgroundRecently, we found that berberine (BBR) exerts anti-acute myeloid leukemia activity, particularly toward high-risk and relapsed/refractory acute myeloid leukemia MV4-11 cells in vitro. However, the poor water solubility and low bioavailability observed with oral BBR administration has limited its clinical use. Therefore, we design and develop a novel oil-in-water self-nanoemulsifying system for BBR (BBR SNE) to improve oral bioavailability and enhance BBR efficacy against acute myeloid leukemia by greatly improving its solubility.ResultsThis system (size 23.50 ± 1.67 nm, zeta potential − 3.35 ± 0.03 mV) was prepared with RH40 (surfactant), 1,2-propanediol (co-surfactant), squalene (oil) and BBR using low-energy emulsification methods. The system loaded BBR successfully according to thermal gravimetric, differential scanning calorimetry, and Fourier transform infrared spectroscopy analyses. The release profile results showed that BBR SNE released BBR more slowly than BBR solution. The relative oral bioavailability of this novel system in rabbits was significantly enhanced by 3.41-fold over that of BBR. Furthermore, Caco-2 cell monolayer transport studies showed that this system could help enhance permeation and prevent efflux of BBR. Importantly, mice with BBR SNE treatment had significantly longer survival time than BBR-treated mice (P < 0.001) in an MV4-11 engrafted leukemia murine model.ConclusionsThese studies confirmed that BBR SNE is a promising therapy for acute myeloid leukemia.Electronic supplementary materialThe online version of this article (10.1186/s12951-018-0402-x) contains supplementary material, which is available to authorized users.

show abstract

Section: Discussionmentioning

confidence: 99%

Self-nanoemulsifying system improves oral absorption and enhances anti-acute myeloid leukemia activity of berberine

Yang

Shen

et al. 2018

J Nanobiotechnol

View full text Add to dashboard Cite

show abstract

“…To our knowledge, only a few studies have investigated how to prolong the half-life of PEGylated NEs [ 30 , 51 , 52 ]. Cheng et al studied how different molecular weights and different concentrations of lipid–PEG affected NE size but did not analyze their pharmacokinetic profiles [ 52 ].…”

Section: Discussionmentioning

confidence: 99%

“…PEGylation of liposomes [ 27 ], micelles [ 28 ], and nanoparticles [ 29 ] has been widely investigated, but only a few works have focused on NE surface modification with PEG. Hak et al [ 30 ] studied the impact of PEG surface density on NE half-life by blood sampling at different time points after administration in mice. Here, the effect of NE surface modification by PEG layers of different molecular weights (PEG 2000 and/or PEG 3400 ) on liver uptake was studied by dynamic MRI.…”

Section: Introductionmentioning

confidence: 99%

A Nano-Emulsion Platform Functionalized with a Fully Human scFv-Fc Antibody for Atheroma Targeting: Towards a Theranostic Approach to Atherosclerosis

Bonnet

Prévot

Mornet

et al. 2021

IJMS

View full text Add to dashboard Cite

Atherosclerosis is at the onset of the cardiovascular diseases that are among the leading causes of death worldwide. Currently, high-risk plaques, also called vulnerable atheromatous plaques, remain often undiagnosed until the occurrence of severe complications, such as stroke or myocardial infarction. Molecular imaging agents that target high-risk atheromatous lesions could greatly improve the diagnosis of atherosclerosis by identifying sites of high disease activity. Moreover, a “theranostic approach” that combines molecular imaging agents (for diagnosis) and therapeutic molecules would be of great value for the local management of atheromatous plaques. The aim of this study was to develop and characterize an innovative theranostic tool for atherosclerosis. We engineered oil-in-water nano-emulsions (NEs) loaded with superparamagnetic iron oxide (SPIO) nanoparticles for magnetic resonance imaging (MRI) purposes. Dynamic MRI showed that NE-SPIO nanoparticles decorated with a polyethylene glycol (PEG) layer reduced their liver uptake and extended their half-life. Next, the NE-SPIO-PEG formulation was functionalized with a fully human scFv-Fc antibody (P3) recognizing galectin 3, an atherosclerosis biomarker. The P3-functionalized formulation targeted atheromatous plaques, as demonstrated in an immunohistochemistry analyses of mouse aorta and human artery sections and in an Apoe−/− mouse model of atherosclerosis. Moreover, the formulation was loaded with SPIO nanoparticles and/or alpha-tocopherol to be used as a theranostic tool for atherosclerosis imaging (SPIO) and for delivery of drugs that reduce oxidation (here, alpha-tocopherol) in atheromatous plaques. This study paves the way to non-invasive targeted imaging of atherosclerosis and synergistic therapeutic applications.

show abstract

“…Target, distribution, and metabolism of contrast agents in vivo can be observed by small animals living optical imaging [ 31 ]. The tendency of the accumulated fluorescence at tumor site consistent with the tumor ultrasound imaging suggested that the NPs remained at the tumor tissue.…”

Section: Discussionmentioning

confidence: 99%

Carboxyl of Poly(D,L-lactide-co-glycolide) Nanoparticles of Perfluorooctyl Bromide for Ultrasonic Imaging of Tumor

Luo

Ding

Wang

et al. 2018

Contrast Media & Molecular Imaging

View full text Add to dashboard Cite

Perfluorooctyl bromide (PFOB) enclosed nanoparticles (NPs) as ultrasonic contrasts have shown promising results in the recent years. However, NPs display poor contrast enhancement in vivo. In this work, we used the copolymers poly(lactide-co-glycolide) carboxylic acid (PLGA-COOH) and poly(lactide-co- glycolide) poly(ethylene glycol) carboxylic acid (PLGA-PEG-COOH) as a shell to encapsulate PFOB to prepare a nanoultrasonic contrast agent. The NPs were small and uniform (210.6 ± 2.9 nm with a polydispersity index of 0.129 ± 0.016) with a complete shell nuclear structure under the transmission electron microscopy (TEM). In vitro, when concentration of NPs was ≥10 mg/ml and clinical diagnostic frequency was ≥9 MHz, NPs produced intensive enhancement of ultrasonic gray-scale signals. NPs could produce stable and obvious gray enhancement with high mechanical index (MI) (MI > 0.6). In vivo, the NPs offered good ultrasound enhancement in tumor after more than 24 h and optical imaging also indicated that NPs were mainly located at tumor site. Subsequent analysis confirmed that large accumulation of fluorescence was observed in the frozen section of the tumor tissue. All these results caused the conclusion that NPs encapsulated PFOB has achieved tumor-selective imaging in vivo.

show abstract

The Effects of oil-in-Water Nanoemulsion Polyethylene Glycol Surface Density on Intracellular Stability, Pharmacokinetics, and Biodistribution in Tumor Bearing Mice

Abstract: Optimal PEG surface density of lipid-based nanoparticles for tumor targeting was found to be below 10 mol%.

Cited by 18 publications

References 33 publications

Self-nanoemulsifying system improves oral absorption and enhances anti-acute myeloid leukemia activity of berberine

Self-nanoemulsifying system improves oral absorption and enhances anti-acute myeloid leukemia activity of berberine

A Nano-Emulsion Platform Functionalized with a Fully Human scFv-Fc Antibody for Atheroma Targeting: Towards a Theranostic Approach to Atherosclerosis

Carboxyl of Poly(D,L-lactide-co-glycolide) Nanoparticles of Perfluorooctyl Bromide for Ultrasonic Imaging of Tumor

Contact Info

Product

Resources

About