Local and systemic drug competition in drug-eluting stent tissue deposition properties

Levin, A.; Jonas, Michael; Hwang, Chao Wei; Edelman, Elazer R.

doi:10.1016/j.jconrel.2005.09.041

Cited by 28 publications

(21 citation statements)

References 12 publications

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“…The efficacy of low concentrations may be explained by the uptake of the lipophilic paclitaxel from the culture medium, usually present at large excess, into the cells over time, resulting in much higher intracellular concentrations, that is, 20-to 50-fold as reported by Kuh et al 31 Survival at permanent postmitotic arrest may explain the tolerability of high concentrations of paclitaxel. 32 The distribution of paclitaxel in the arterial wall [7][8][9]33,34 has been the subject of experiments and theoretical considerations. It depends on a large number of parameters, some of which are changed by the effects of the drug, which makes predictions even more difficult.…”

Section: Speck Et Al Pharmacokinetics Explain Restenosis Inhibitionmentioning

confidence: 99%

Do Pharmacokinetics Explain Persistent Restenosis Inhibition by a Single Dose of Paclitaxel?

Speck

Cremers²,

Kelsch³

et al. 2012

Circ: Cardiovascular Interventions

132

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Background-The purpose of this study was to investigate the elimination of paclitaxel from the arterial wall after a single short administration with a coated balloon. Methods and Results-Slightly oversized paclitaxel-coated balloons (dose 3 or 9 g/mm 2 ) without or with premounted stents were inflated in nonatherosclerotic coronary arteries of either young domestic pigs or adult Goettingen minipigs. The paclitaxel content of plasma, arterial segments, and residual hearts (without treated arteries) was measured for up to 180 days using high-performance liquid chromatography/ultraviolet detection or mass spectrometry. Angiograms were evaluated for lumen narrowing. The paclitaxel concentration in plasma remained Ͻ10 ng/mL. In arteries of domestic pigs and minipigs treated with paclitaxel-coated balloons with premounted stents, 10%Ϯ5% or 21%Ϯ8% of dose, respectively, was initially detected and decreased to 3.5%Ϯ3.1% of dose (domestic pig) by Day 7. Within 6 months it fell with a half-life of 1.9 months to 0.40%Ϯ0.35%. After 3 months the concentration in the arterial wall was 17Ϯ11 mol/L. Without a stent, drug transfer to the vessel wall was somewhat reduced and elimination faster. Immediately after treatment up to 26%Ϯ4% of dose was detected in the residual whole hearts. It dropped with a half-life of 45 days to 1.5%Ϯ0.6% of dose (0.3 mol/L) within 6 months. Conclusions-After

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Section: Speck Et Al Pharmacokinetics Explain Restenosis Inhibitionmentioning

confidence: 99%

Do Pharmacokinetics Explain Persistent Restenosis Inhibition by a Single Dose of Paclitaxel?

Speck

Cremers²,

Kelsch³

et al. 2012

Circ: Cardiovascular Interventions

132

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“…42, 43 The transport of free drug has been modelled by reaction-diffusion process and binding of drug by nonlinear saturable reversible chemical reaction. Now the dimensionless governing equations for the model considered may be written as…”

Section: Governing Equations and Boundary Conditionsmentioning

confidence: 99%

Computational Modelling of Three-phase Stent-based Delivery

Mandal¹,

Mandal²

2017

Journal of Exploratory Research in Pharmacology

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Background and Objective: Treatment of arterial lesions using drug-eluting stent is now a gold standard method, however, the mechanisms of drug uptake and its retention is not well understood. In most of the computational studies, only the binding of drug to specific receptor is considered; but it is well established that when the drug binds to the specific receptor, there is also occurrence of non-specific binding caused by the trapping of drug in the extracellular matrix. When non-specific binding is not subtracted from total binding to give receptor-mediated binding, a description of receptor/ligand requires that effects of non-specific binding be considered.

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“…The equations for the rate of uptake of sirolimus to ECM sites and receptors are: are the respective equilibrium dissociation constants. It is certainly true that the drug will bind to binding sites in the tissue and in the cells ( (Levin et al, 2005), (Tzafriri et al, 2012), (Bierer et al, 1990)) although the strength of the affinity will likely vary substantially with the particular drug under consideration. Furthermore, it is not clear how the density of the binding sites could easily be determined.…”

Section: One-dimensional Modelsmentioning

confidence: 99%

Simulating Drug-eluting Stents - Progress Made and the Way Forward

McGinty¹,

McCormick²,

McKee³

et al. 2013

Proceedings of the 3rd International Conference on Simulation and Modeling Methodologies, Technologies and Applications

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Abstract:Drug-eluting stents have significantly improved the treatment of coronary artery disease. Compared with their bare metal predecessors, they offer reduced rates of restenosis and thus represent the current gold standard in percutaneous coronary interventions. Drug-eluting stents have been around for over a decade, and while progress is continually being made, they are not suitable in all patients and lesion types. Furthermore there are still real concerns over incomplete healing and late stent thrombosis. In this paper, some modelling approaches are reviewed and the future of modelling and simulation in this field is discussed.

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Local and systemic drug competition in drug-eluting stent tissue deposition properties

Cited by 28 publications

References 12 publications

Do Pharmacokinetics Explain Persistent Restenosis Inhibition by a Single Dose of Paclitaxel?

Do Pharmacokinetics Explain Persistent Restenosis Inhibition by a Single Dose of Paclitaxel?

Computational Modelling of Three-phase Stent-based Delivery

Simulating Drug-eluting Stents - Progress Made and the Way Forward

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