Increase of the duration of the anticonvulsive activity of a novel NMDA receptor antagonist using poly(butylcyanoacrylate) nanoparticles as a parenteral controlled release system

Friese, Andreas; Seiller, Erhard; Quack, G.; Lorenz, B.; Kreuter, Jörg

doi:10.1016/s0939-6411(99)00073-9

Cited by 134 publications

(43 citation statements)

References 13 publications

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“…administration of a novel non-competitive NMDA receptor antagonist MRZ 2/576 (potent but rather short-acting anticonvulsant, rapidly discharged from the central nervous system by transport processes that are sensitive to probenecid) bound to PBCA NPs coated with PS-80; this formulation prolonged the length of the anticonvulsive effect up to 210 min and after probenecid pretreatment up to 270 min compared to 150 min with probenecid and MRZ 2/576 alone. 36 Reasonably, the NPs operated as drug delivery systems, able to protect and to prolong the release of drugs to the CNS. Moreover, the coating of NPs with PS-80 seems to be necessary to target and to achieve an uptake of the particles into the brain.…”

Section: Epilepsymentioning

confidence: 99%

Nanoparticle transport across the blood brain barrier

et al. 2016

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While the role of the blood-brain barrier (BBB) is increasingly recognized in the (development of treatments targeting neurodegenerative disorders, to date, few strategies exist that enable drug delivery of non-BBB crossing molecules directly to their site of action, the brain. However, the recent advent of Nanomedicines may provide a potent tool to implement CNS targeted delivery of active compounds. Approaches for BBB crossing are deeply investigated in relation to the pathology: among the main important diseases of the CNS, this review focuses on the application of nanomedicines to neurodegenerative disorders (Alzheimer, Parkinson and Huntington's Disease) and to other brain pathologies as epilepsy, infectious diseases, multiple sclerosis, lysosomal storage disorders, strokes.

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Section: Epilepsymentioning

confidence: 99%

Nanoparticle transport across the blood brain barrier

et al. 2016

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“…Beyond the ongoing controversy about their mechanism of action, polysorbate 80-coated PBCA nanoparticles should be evaluated in term of benefit/risk ratio and of innovative therapeutics. In addition to the toxicity issue, the short duration of the pharmacological effect observed after administration of drugs formulated with this carrier (210 min at the best 39 ) would probably necessitate daily intravenous administrations, a perspective not suitable for the treatment of chronic brain diseases.…”

Section: General Considerationsmentioning

confidence: 99%

Drug transport to brain with targeted nanoparticles

2005

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Summary: Nanoparticle drug carriers consist of solid biodegradable particles in size ranging from 10 to 1000 nm (50 -300 nm generally). They cannot freely diffuse through the bloodbrain barrier (BBB) and require receptor-mediated transport through brain capillary endothelium to deliver their content into the brain parenchyma. Polysorbate 80-coated polybutylcyanoacrylate nanoparticles can deliver drugs to the brain by a still debated mechanism. Despite interesting results these nanoparticles have limitations, discussed in this review, that may preclude, or at least limit, their potential clinical applications. Long-circulating nanoparticles made of methoxypoly(ethylene glycol)-polylactide or poly(lactide-co-glycolide) (mPEG-PLA/ PLGA) have a good safety profiles and provide drug-sustained release. The availability of functionalized PEG-PLA permits to prepare target-specific nanoparticles by conjugation of cell surface ligand. Using peptidomimetic antibodies to BBB transcytosis receptor, brain-targeted pegylated immunonanoparticles can now be synthesized that should make possible the delivery of entrapped actives into the brain parenchyma without inducing BBB permeability alteration. This review presents their general properties (structure, loading capacity, pharmacokinetics) and currently available methods for immunonanoparticle preparation.

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“…Drugs delivered to CNS in these constructs included, analgesics (Dalargin, Loperamide), anti-cancer agents (Doxorubicin), anti-convulsants (NMDA receptor antagonist, MRZ 2/576), and peptides (Ddalargin and Kytorphin) [196,197]. For example, nanoparticles prolonged anticonvulsive activity of MRZ 2/576 compared to the free drug [199]. In another study, Doxorubicin-laden nanoparticles increased survival in rats with aggressive glioblastoma [197].…”

Section: Nanoparticlesmentioning

confidence: 99%

Nanomedicine in the diagnosis and therapy of neurodegenerative disorders

Kabanov

Gendelman

2007

Progress in Polymer Science

242

138

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Neurodegenerative and infectious disorders including Alzheimer's and Parkinson's diseases, amyotrophic lateral sclerosis, and stroke are rapidly increasing as population's age. Alzheimer's disease alone currently affects 4.5 million Americans, and more than $100 billion is spent per year on medical and institutional care for affected people. Such numbers will double in the ensuing decades. Currently disease diagnosis for all disorders is made, in large measure, on clinical grounds as laboratory and neuroimaging tests confirm what is seen by more routine examination. Achieving early diagnosis would enable improved disease outcomes. Drugs, vaccines or regenerative proteins present "real" possibilities for positively affecting disease outcomes, but are limited in that their entry into the brain is commonly restricted across the blood-brain barrier. This review highlights how these obstacles can be overcome by polymer science and nanotechnology. Such approaches may improve diagnostic and therapeutic outcomes. New developments in polymer science coupled with cell-based delivery strategies support the notion that diseases that now have limited therapeutic options can show improved outcomes by advances in nanomedicine.

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Increase of the duration of the anticonvulsive activity of a novel NMDA receptor antagonist using poly(butylcyanoacrylate) nanoparticles as a parenteral controlled release system

Cited by 134 publications

References 13 publications

Nanoparticle transport across the blood brain barrier

Nanoparticle transport across the blood brain barrier

Drug transport to brain with targeted nanoparticles

Nanomedicine in the diagnosis and therapy of neurodegenerative disorders

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