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Related Concept Videos

Antiepileptic Drugs: Sodium Channel Blockers01:08

Antiepileptic Drugs: Sodium Channel Blockers

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Antiepileptic drugs are specialized medications that prevent seizures in individuals diagnosed with epilepsy. These drugs primarily function by blocking the movement of sodium ions through channels in the neuronal membrane, inhibiting the repetitive firing of action potentials often associated with seizures.
Sodium channel blockers modulate ion channels, particularly voltage-gated sodium channels. They block only sodium ion movement.
Among the most commonly prescribed antiepileptic drugs are...
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Antiepileptic Drugs: Potassium Channel Activators01:20

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Ezocgabine or retigabine, an antiepileptic drug of remarkable efficacy, has revolutionized the management of seizures. It is a potassium channel activator, explicitly targeting the family of Q subtype potassium channels. It enhances the transmembrane potassium currents, regulating neuronal excitability. This action stabilizes the resting membrane potential, a pivotal factor in mitigating the hyperexcitability that characterizes epilepsy.
Ezogabine has gained approval as an adjunctive treatment...
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Antiepileptic Drugs: Calcium Channel Blockers01:17

Antiepileptic Drugs: Calcium Channel Blockers

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Calcium channel blockers, a class of antiepileptic drugs, regulate the flow of calcium ions within neurons.
Calcium channel blockers exert their antiepileptic effects by targeting T-type calcium channels, which are integral to transmitting nerve signals in the central nervous system. These channels allow the passage of calcium ions, which are vital for neuronal communication. By inhibiting T-type calcium channels, calcium channel blockers effectively reduce the release of neurotransmitters and...
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Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
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Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein01:20

Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein

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Antiepileptic drugs, such as levetiracetam (Keppra) and brivaracetam (Briviact), have emerged as crucial tools in managing epilepsy. These medications exert their therapeutic effects by targeting the synaptic vesicle protein SV2A, a transmembrane glycoprotein primarily found in the brain.
SV2A is a transmembrane glycoprotein located predominantly in the brain, modulating the release of neurotransmitters for neuronal communication. Both levetiracetam and brivaracetam exhibit a high affinity for...
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Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

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Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
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Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
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Solid-lipid nanoparticle formulation improves antiseizure action of cryptolepine.

Priscilla Kolibea Mante1, Nana Ofori Adomako2, Paulina Antwi1

  • 1Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.

Biomedicine & Pharmacotherapy = Biomedecine & Pharmacotherapie
|February 9, 2021
PubMed
Summary

This study shows that a solid-lipid nanoparticle formulation of cryptolepine enhances its ability to cross the blood-brain barrier (BBB). This improved delivery significantly boosts its antiseizure activity in a zebrafish model.

Keywords:
Cav1.2 receptorCryptolepisEpilepsyNanoparticlesSigma 2 receptorZebrafish

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Nanotechnology

Background:

  • Epilepsy significantly impacts global health, especially in low- and middle-income countries, with a substantial treatment gap.
  • Cryptolepine, an alkaloid from Cryptolepis sanguinolenta, is being investigated for its potential therapeutic properties.

Purpose of the Study:

  • To evaluate the antiseizure activity of cryptolepine and its solid-lipid nanoparticle formulation (SLN-CRYP).
  • To assess the effect of SLN formulation on cryptolepine's permeability across the blood-brain barrier (BBB).

Main Methods:

  • Isolation of cryptolepine and preparation of its solid-lipid nanoparticle formulation.
  • Evaluation of antiseizure activity using a Pentylenetetrazole (PTZ)-induced seizure model in Zebrafish.
  • Assessment of drug-receptor binding and BBB permeability.

Main Results:

  • SLN formulation significantly increased cryptolepine's BBB permeability from 0.32 × 10-6 cm/s to 10.81 × 10-6 cm/s.
  • SLN-CRYP (2.5 and 5 mg/kg) markedly reduced seizure scores and increased seizure latency in zebrafish.
  • SLN-CRYP administration significantly decreased swimming distance, indicating reduced seizure-like behaviors.

Conclusions:

  • Solid-lipid nanoparticle formulation of cryptolepine enhances its blood-brain barrier permeability.
  • SLN-CRYP demonstrates significant potential as an effective agent for managing epilepsy.