Nose-to-brain transport of imatinib mesylate: A pharmacokinetic evaluation

Hada, Nobuko; Netzer, William J.; Belhassan, Fanny; Wennogle, Lawrence P.; Gizurarson, Sveinbjörn

doi:10.1016/j.ejps.2017.02.032

Cited by 28 publications

(13 citation statements)

References 43 publications

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“…The high expression of P-gp in the BBB, nasal membranes, and olfactory bulb will greatly limit the transport of drugs which are P-gp substrates. Several studies have shown that transport of verapamil, a P-gp substrate, to the brain can be increased by either the addition of a P-gp inhibitor, e.g., rifampin or cyclosporin A, or the use of P-gp-deficient mice [ 74 , 91 , 92 , 93 ]. For drugs which are substrates for P-gp, this evidence is very encouraging.…”

Section: Preparation and Evaluation Of Intranasal Drug Delivery Systemsmentioning

confidence: 99%

Evaluation of Recent Intranasal Drug Delivery Systems to the Central Nervous System

Crowe

Hsu

2022

Pharmaceutics

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Neurological diseases continue to increase in prevalence worldwide. Combined with the lack of modifiable risk factors or strongly efficacious therapies, these disorders pose a significant and growing burden on healthcare systems and societies. The development of neuroprotective or curative therapies is limited by a variety of factors, but none more than the highly selective blood-brain barrier. Intranasal administration can bypass this barrier completely and allow direct access to brain tissues, enabling a large number of potential new therapies ranging from bioactive peptides to stem cells. Current research indicates that merely administering simple solutions is inefficient and may limit therapeutic success. While many therapies can be delivered to some degree without carrier molecules or significant modification, a growing body of research has indicated several methods of improving the safety and efficacy of this administration route, such as nasal permeability enhancers, gelling agents, or nanocarrier formulations. This review shall discuss promising delivery systems and their role in expanding the clinical efficacy of this novel administration route. Optimization of intranasal administration will be crucial as novel therapies continue to be studied in clinical trials and approved to meet the growing demand for the treatment of patients with neurological diseases.

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Section: Preparation and Evaluation Of Intranasal Drug Delivery Systemsmentioning

confidence: 99%

Evaluation of Recent Intranasal Drug Delivery Systems to the Central Nervous System

Crowe

Hsu

2022

Pharmaceutics

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“…In another study, the use of rifampin, which is a Pgp inhibitor, in Pgp-competent and Pgp-deficient mice increased the use of verapamil in the brain [44,45]. Coadministration of two Pgp inhibitors pantoprazole and elacridar with imatinib mesylate also raised the later brain concentration [47].…”

Section: Inhibitors Of P-glycoproteinmentioning

confidence: 99%

Nose-to-Brain Drug Delivery: An Update to the Alternative Path to Successful Targeted Anti-Migraine Drugs

Chattopadhyay¹,

Das

Sarma

2021

Int J App Pharm

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The Blood-Brain Barrier (BBB) limits transportation to the brain of possible treatment moieties. Specific stimulation of the brain through olfactory and trigeminal neural pathways by BBB has been taken into consideration for the development of a wide spectrum of brain therapeutics. The intranasal delivery path delivers the drugs through the brain, eliminating any side effects and increasing neurotherapeutics performance. Diverse drug delivery systems (DDDss) for reaching the brain via the nasal route have been researched over the past few decades. Large-scale molecular biologics, such as Deoxyribonucleic acid (DNA), gene vectors, and stem cells, can be administered intranasally, as a method for the management of a range of CNS illnesses, including stroke, Parkinson's diseases, multiple sclerosis, Migraine, Alzheimer's diseases, epilepsy, and mental disorders. New DDSs, including nanoparticles, liposomes, and polymeric micelles, have acquired potentials in the nasal mucosa and central nervous system (CNS), as effective means of concentrating the brain without toxicity. Differential nasal cavity structures posed a significant obstacle in ineffective drugs beyond the nasal valve. Pharmaceutical firms have increasingly used emerging techniques for the production of new nasal pharmaceutical drugs to overcome these obstacles. This review aims to identify the new advances in the nasal administration of brain-based DDSs for Migraines.

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“…By contrast, the extracellular transport of molecules from the nasal cavity to the brain is a much more rapid process. Rapid delivery, almost immediately or up to one hour after intranasal administration [23][24][25][26], has been reported for many molecules, hence an extracellular pathway is the most likely mode of transport in those instances. Extracellular transport may play a role in the movement of peptide-loaded nanoparticles within the brain [27].…”

Section: Introductionmentioning

confidence: 99%

Gene Targeting to the Cerebral Cortex Following Intranasal Administration of Polyplexes

Kubajewska

Vaideanu²,

Schätzlein

et al. 2022

Pharmaceutics

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Gene delivery to the cerebral cortex is challenging due to the blood brain barrier and the labile and macromolecular nature of DNA. Here we report gene delivery to the cortex using a glycol chitosan—DNA polyplex (GCP). In vitro, GCPs carrying a reporter plasmid DNA showed approximately 60% of the transfection efficiency shown by Lipofectamine lipoplexes (LX) in the U87 glioma cell line. Aiming to maximise penetration through the brain extracellular space, GCPs were coated with hyaluronidase (HYD) to form hyaluronidase-coated polyplexes (GCPH). The GCPH formulation retained approximately 50% of the in vitro hyaluronic acid (HA) digestion potential but lost its transfection potential in two-dimensional U87 cell lines. However, intranasally administered GCPH (0.067 mg kg−1 DNA) showed high levels of gene expression (IVIS imaging of protein expression) in the brain regions. In a separate experiment, involving GCP, LX and naked DNA, the intranasal administration of the GCP formulation (0.2 mg kg−1 DNA) resulted in protein expression predominantly in the cerebral cortex, while a similar dose of intranasal naked DNA led to protein expression in the cerebellum. Intranasal LX formulations did not show any evidence of protein expression. GCPs may provide a means to target protein expression to the cerebral cortex via the intranasal route.

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Nose-to-brain transport of imatinib mesylate: A pharmacokinetic evaluation

Cited by 28 publications

References 43 publications

Evaluation of Recent Intranasal Drug Delivery Systems to the Central Nervous System

Evaluation of Recent Intranasal Drug Delivery Systems to the Central Nervous System

Nose-to-Brain Drug Delivery: An Update to the Alternative Path to Successful Targeted Anti-Migraine Drugs

Gene Targeting to the Cerebral Cortex Following Intranasal Administration of Polyplexes

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