Ex vivo and in vivo diffusion of ropivacaine through spinal meninges: Influence of absorption enhancers

Brandhonneur, Nolwenn; Dollo, Gilles; Ratajczak-Enselme, Maja; Deniau, Anne Laure; Chevanne, François; Estèbe, Jean Pierre; Legrand, Alain; Corre, Pascal Le

doi:10.1016/j.ijpharm.2010.10.049

Cited by 7 publications

(4 citation statements)

References 26 publications

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“…Coadministration of an anti-hypertensive agent alleviated the high blood pressure, removing mannitol flux inconsistencies among the subject population [139]. Sodium caprate was also shown to increase the arachnoid barrier permeability of local anaesthetic ropivacaine by 1.6-fold upon epidural administration, highlighting sodium caprate as an efficient and robust barrier disruptor [140].…”

Section: Sodium Caprate (C10)mentioning

confidence: 96%

Modulating the Blood–Brain Barrier: A Comprehensive Review

2021

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The highly secure blood–brain barrier (BBB) restricts drug access to the brain, limiting the molecular toolkit for treating central nervous system (CNS) diseases to small, lipophilic drugs. Development of a safe and effective BBB modulator would revolutionise the treatment of CNS diseases and future drug development in the area. Naturally, the field has garnered a great deal of attention, leading to a vast and diverse range of BBB modulators. In this review, we summarise and compare the various classes of BBB modulators developed over the last five decades—their recent advancements, advantages and disadvantages, while providing some insight into their future as BBB modulators.

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Section: Sodium Caprate (C10)mentioning

confidence: 96%

Modulating the Blood–Brain Barrier: A Comprehensive Review

2021

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“…Intracarotid injections of C 10 lead to a transient, reversible and molecular weight-dependent opening of the blood-brain barrier in the rat, beginning 5 min after injection 50 , 51 . After epidural injection of C 10 with the anesthetic ropivacaine, the maximal intrathecal concentration of ropivacaine was elevated 52 . This effect is transient and reversible and limited to the arachnoid barrier.…”

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 97%

“…Possibilities include reincubation with C 10 or coadministration in a liquid or solid form, e.g., tablets by spray freeze-drying 43 , 57 , 68 . Because the uptake of C 10 in vivo is quite fast (t max ~7 min, 48 ) after injection, the drug is injected before and after the application of C 10 52 . C 10 was coadministered with two different size markers combined in tablet or in liquid form.…”

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 99%

Trends in drug delivery through tissue barriers containing tight junctions

2013

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A limitation in the uptake of many drugs is the restricted permeation through tissue barriers. There are two general ways to cross barriers formed by cell layers: by transcytosis or by diffusion through the intercellular space. In the latter, tight junctions (TJs) play the decisive role in the regulation of the barrier permeability. Thus, transient modulation of TJs is a potent strategy to improve drug delivery. There have been extensive studies on surfactant-like absorption enhancers. One of the most effective enhancers found is sodium caprate. However, this modulates TJs in an unspecific fashion. A novel approach would be the specific modulation of TJ-associated marvel proteins and claudins, which are the main structural components of the TJs. Recent studies have identified synthetic peptidomimetics and RNA interference techniques to downregulate the expression of targeted TJ proteins. This review summarizes current progress and discusses the impact on TJs' barrier function.

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“…Similarly, the BAB can be studied using meninges explants by carefully dissecting the meningeal layer, then separating the leptomeninges containing the arachnoid cells from the dura mater [34]. Furthermore, permeability assays can be performed using the whole meningeal layer in a diffusion chamber system [233] or a perfusion system [234].…”

Section: Ex Vivo Modelsmentioning

confidence: 99%

ABC Transporters at the Blood–Brain Interfaces, Their Study Models, and Drug Delivery Implications in Gliomas

et al. 2019

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Drug delivery into the brain is regulated by the blood–brain interfaces. The blood–brain barrier (BBB), the blood–cerebrospinal fluid barrier (BCSFB), and the blood–arachnoid barrier (BAB) regulate the exchange of substances between the blood and brain parenchyma. These selective barriers present a high impermeability to most substances, with the selective transport of nutrients and transporters preventing the entry and accumulation of possibly toxic molecules, comprising many therapeutic drugs. Transporters of the ATP-binding cassette (ABC) superfamily have an important role in drug delivery, because they extrude a broad molecular diversity of xenobiotics, including several anticancer drugs, preventing their entry into the brain. Gliomas are the most common primary tumors diagnosed in adults, which are often characterized by a poor prognosis, notably in the case of high-grade gliomas. Therapeutic treatments frequently fail due to the difficulty of delivering drugs through the brain barriers, adding to diverse mechanisms developed by the cancer, including the overexpression or expression de novo of ABC transporters in tumoral cells and/or in the endothelial cells forming the blood–brain tumor barrier (BBTB). Many models have been developed to study the phenotype, molecular characteristics, and function of the blood–brain interfaces as well as to evaluate drug permeability into the brain. These include in vitro, in vivo, and in silico models, which together can help us to better understand their implication in drug resistance and to develop new therapeutics or delivery strategies to improve the treatment of pathologies of the central nervous system (CNS). In this review, we present the principal characteristics of the blood–brain interfaces; then, we focus on the ABC transporters present on them and their implication in drug delivery; next, we present some of the most important models used for the study of drug transport; finally, we summarize the implication of ABC transporters in glioma and the BBTB in drug resistance and the strategies to improve the delivery of CNS anticancer drugs.

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Ex vivo and in vivo diffusion of ropivacaine through spinal meninges: Influence of absorption enhancers

Cited by 7 publications

References 26 publications

Modulating the Blood–Brain Barrier: A Comprehensive Review

Modulating the Blood–Brain Barrier: A Comprehensive Review

Trends in drug delivery through tissue barriers containing tight junctions

ABC Transporters at the Blood–Brain Interfaces, Their Study Models, and Drug Delivery Implications in Gliomas

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