Intestinal uptake and biodistribution of novel polymeric micelles after oral administration

Mathot, Frédéric; Beijsterveldt, Ludy van; Préat, Véronique; Brewster, Marcus E.; Ariën, Albertina

doi:10.1016/j.jconrel.2005.11.012

Cited by 96 publications

(33 citation statements)

References 28 publications

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“…For instance, Préat and coworkers have investigated the potential of polymeric micelles prepared from methoxypoly(ethylene glycol)-poly(ε-caprolactone/trimethylene carbonate) [PEG-p(CLco-TMC)] (Molecular weight ~ 5,000 g/mol) for oral administration utilizing risperidone as a model drug (24,25). They used an in vitro model of the intestine (Caco-2 cells) to assess the intestinal permeability of [ 14 C]-radiolabeled PEG750-P(CL-co-TMC) micelles.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of Orally Administered Poly(Ethylene Oxide)-block-Poly(ε-Caprolactone) Micelles of Cyclosporine A in Rats: Comparison with Neoral®

et al. 2018

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of Orally Administered Poly(Ethylene Oxide)-block-Poly(ε-Caprolactone) Micelles of Cyclosporine A in Rats: Comparison with Neoral®

et al. 2018

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“…Third, due to their small size, these NRs will have a high permeability, thus enabling effective transport through the intestinal wall. [26][27][28] Finally, compared to spheres or other shapes, the NR drugs are expected to penetrate tumors or atherosclerotic plaque more efficiently and much faster than individual NPs. This should lead to better bioavailability of the drug as well as reduced toxicity and side effects.…”

Section: Dielectrophoretic Assembly Of Nanoparticlesmentioning

confidence: 99%

Novel Nanoprinting for Oral Delivery of Poorly Soluble Drugs

Yilmaz

Sarısözen

Torchilin

et al. 2016

Methodist DeBakey Cardiovascular Journal

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Many of the newly developed drugs for cancer, and some of those for cardiovascular disease, are poorly soluble in water and cannot be taken orally. This can be overcome by employing a new and effective delivery system utilizing nanotechnology. We present a new method for oral preparation of poorly soluble drugs that entails assembling (printing) drug-loaded polymeric micelles into sub-100 nm orally acceptable nanorods (NRs). Due to their small size, these NRs will have a high permeability through cells and thus should transport through the intestine to allow for drug delivery in the blood. These NRs drugs are expected to penetrate tumors more efficiently and much faster than individual nanoparticles and may also be useful for drug delivery to atherosclerotic plaque. This should lead to better bioavailability of the drug with reduced toxicity and side effects. Currently used micellar formulations are administered intravenously, which is invasive and could be toxic due to high doses and interaction with normal healthy tissues. Oral drug administration is the easiest and most desirable way to deliver most drugs, including those that are poorly soluble.MDCVJ | XII (3) 2016 158 houstonmethodist.org/debakey-journal absorption, enhance circulation time, avoid immune surveillance mechanisms, and promote delivery to the site of disease. Recent advances in nanotechnology have increased the flexibility of design and enhanced quality control of nanoparticles (NPs) such as nanotubes, NRs, nanowires, nanocages and nanodisks. Among these, NRs attract more attention due to their favorable properties over spherical particles. Ghandehari et al. demonstrated that circulation time of PEGylated NRs is higher than PEGylated gold nanospheres.12 Moreover, NRs were taken up by macrophages to a lesser extent than spherical NPs, which explains their increased circulation time and lower accumulation in the liver compared to spherical particles. Another important finding is that the serum proteins interacted strongly with spherical-shaped particles but not with NRs, which lead to less opsonization and up to 2-fold more tumor accumulation of NRs over spheres. Chauhan et al. compared PEGylated quantum-dot structures of nanospheres and NRs with equal hydrodynamic size and found that both could diffuse through 5-μm pores at the same rate. However, when the pore size decreased to the 100 nm to 400 nm range (the range of pores in tumor vasculature or the neovessels of atherosclerotic plaque), NRs diffused through the pores up to an order of magnitude faster than the nanospheres. Chauhan et al. also showed in vivo that NRs penetrated into the tumors four times as rapidly as the nanospheres. 13 More recently, Dasgupta et al. reported a systematic approach to understanding how the shape of an NP affects its cellular internalization after finding that rod-like particles assumed stable endocytotic states.14 Their summarized data suggests that rod-shaped nanotherapeutics may be far more effective for cancer therapy than currently approved sph...

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“…In this study, the centrifugation method was used to determine D EE (Mathot et al, 2006). The PLGA concentration has a marked influence on drug loading capacity of NPs.…”

Section: Ee and Drug Loadingmentioning

confidence: 99%

“…It was observed that liver and kidneys accumulated major portion of the administered OPT-FTC NPs. Nevertheless, liver is one of the major organs of reticuloendothelial system (RES), which is known to accumulate and metabolize NPs (Mathot et al, 2006). The in vivo biodistribution data revealed initial rapid uptake and showed significantly higher concentrations of FTC by liver and kidneys, which were 0.582 AE 2.16 mg/g and 363.34 AE 1.79 mg/g, respectively, for OPT-FTC NPs than those observed in groups treated with pure drug, on 1 day of oral administration ( Figure 5A).…”

Section: In Vivo Biodistributionmentioning

confidence: 99%

Pharmacokinetics andin vivobiodistribution of optimized PLGA nanoparticulate drug delivery system for controlled release of emtricitabine

Singh

Pai

2013

Drug Delivery

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The objective of this study was to develop systematically optimized (OPT) nanoparticles (NPs) providing a controlled release using PLGA of emtricitabine (FTC) employing Formulation by Design (FbD), and evaluate their in vitro and in vivo performance. FTC generates severe adverse effects with risks of toxicity. Thus, NPs were prepared to reduce these drawbacks in this study. The NPs were prepared by water-in-oil-in-water (w/o/w) emulsion method, followed by high-pressure homogenization. The FTC NPs were systematically OPT using 3 2 central composite design and the OPT formulation located using overlay plot. The pharmacokinetics and in vivo biodistribution of OPT-FTC NPs were investigated in male Wistar rats via the oral administration. Transmission electron microscopy studies on OPT-FTC NPs demonstrated uniform shape and size of particles. In vitro release was sustained up to 15 days in PBS pH 7.4. Augmentation in the values of C max (1.63 fold) and AUC 0-1 (5.39 fold) indicated significant enhancement in the rate and extent of bioavailability by the OPT-FTC NPs compared to pure drug. OPT-FTC NPs showed 2.325 fold increase in the values of FTC concentrations in liver. The OPT-FTC NPs was found to be quite stable during 6 months of study period. Hence, the developed OPT-FTC NPs can be used as drug carrier for sustained/prolonged drug release and/or to reduce toxic effects.

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Intestinal uptake and biodistribution of novel polymeric micelles after oral administration

Cited by 96 publications

References 28 publications

Pharmacokinetics of Orally Administered Poly(Ethylene Oxide)-block-Poly(ε-Caprolactone) Micelles of Cyclosporine A in Rats: Comparison with Neoral®

Pharmacokinetics of Orally Administered Poly(Ethylene Oxide)-block-Poly(ε-Caprolactone) Micelles of Cyclosporine A in Rats: Comparison with Neoral®

Novel Nanoprinting for Oral Delivery of Poorly Soluble Drugs

Pharmacokinetics andin vivobiodistribution of optimized PLGA nanoparticulate drug delivery system for controlled release of emtricitabine

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