Solid-lipid nanoparticle formulation improves antiseizure action of cryptolepine
Following the high treatment gap and massive impact of epilepsy on global health particularly in low- and middle-income countries, our study aims to investigate cryptolepine, the major alkaloid of Cryptolepis sanguinolenta as well as its solid-lipid nanoparticle formulation for potential antiseizure...
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doaj-7ff0bafe19b94c6ead3885b359a33b9e2021-07-15T04:26:45ZengElsevierBiomedicine & Pharmacotherapy0753-33222021-05-01137111354Solid-lipid nanoparticle formulation improves antiseizure action of cryptolepinePriscilla Kolibea Mante0Nana Ofori Adomako1Paulina Antwi2Nana Kofi Kusi-Boadum3Newman Osafo4Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana; Corresponding author.Department of Pharmacy Practice, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, GhanaDepartment of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, GhanaDepartment of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, GhanaDepartment of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, GhanaFollowing the high treatment gap and massive impact of epilepsy on global health particularly in low- and middle-income countries, our study aims to investigate cryptolepine, the major alkaloid of Cryptolepis sanguinolenta as well as its solid-lipid nanoparticle formulation for potential antiseizure activity. Cryptolepine was isolated and a solid-lipid formulation was prepared. Antiseizure activity of Solid-Lipid Nanoparticle formulation of cryptolepine (SLN-CRYP) was investigated using Pentylenetetrazole (PTZ)-induced model of seizure-like behaviors in Zebrafish with 2.5 and 5 mg/kg each of cryptolepine and SLN-CRYP. Drug receptor binding and permeability of the compound across the Blood Brain Barrier (BBB) were also assessed. SLN formulation of cryptolepine increased its permeability to the BBB from 0.32 × 10−6 cm/s to 10.81 × 10−6 cm/s. 2.5 and 5 mg/kg of SLN-CRYP significantly reduced mean seizure score (P = 0.0018; F(6, 63) = 23.52) and significantly increased (P < 0.0001; F(6, 63) = 65.41) latency to onset of seizures. The total distance swam by fish administered with 2.5 and 5 mg/kg of SLN-CRYP was significantly (P < 0.000; F(6, 63) = 161.9) decreased. 5 mg/kg of cryptolepine also significantly decreased swimming distance. Cryptolepine exhibited inhibitory modulation of human voltage-gated calcium channels (Cav1.2), H1-receptor, Peripheral Benzodiazepine Receptor and Sigma 2 receptor with a high Ki values of 6133.38 nM and 2945.0 nM, indicating less potent antagonism on Cav1.2 and Sigma 2 receptors compared to Nifedipine and Haloperidol respectively. This study reveals that the solid-lipid nanoparticle formulation of cryptolepine improves its BBB permeability and hence antiseizure activity.http://www.sciencedirect.com/science/article/pii/S0753332221001396NanoparticlesCav1.2 receptorSigma 2 receptorZebrafishEpilepsyCryptolepis |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Priscilla Kolibea Mante Nana Ofori Adomako Paulina Antwi Nana Kofi Kusi-Boadum Newman Osafo |
spellingShingle |
Priscilla Kolibea Mante Nana Ofori Adomako Paulina Antwi Nana Kofi Kusi-Boadum Newman Osafo Solid-lipid nanoparticle formulation improves antiseizure action of cryptolepine Biomedicine & Pharmacotherapy Nanoparticles Cav1.2 receptor Sigma 2 receptor Zebrafish Epilepsy Cryptolepis |
author_facet |
Priscilla Kolibea Mante Nana Ofori Adomako Paulina Antwi Nana Kofi Kusi-Boadum Newman Osafo |
author_sort |
Priscilla Kolibea Mante |
title |
Solid-lipid nanoparticle formulation improves antiseizure action of cryptolepine |
title_short |
Solid-lipid nanoparticle formulation improves antiseizure action of cryptolepine |
title_full |
Solid-lipid nanoparticle formulation improves antiseizure action of cryptolepine |
title_fullStr |
Solid-lipid nanoparticle formulation improves antiseizure action of cryptolepine |
title_full_unstemmed |
Solid-lipid nanoparticle formulation improves antiseizure action of cryptolepine |
title_sort |
solid-lipid nanoparticle formulation improves antiseizure action of cryptolepine |
publisher |
Elsevier |
series |
Biomedicine & Pharmacotherapy |
issn |
0753-3322 |
publishDate |
2021-05-01 |
description |
Following the high treatment gap and massive impact of epilepsy on global health particularly in low- and middle-income countries, our study aims to investigate cryptolepine, the major alkaloid of Cryptolepis sanguinolenta as well as its solid-lipid nanoparticle formulation for potential antiseizure activity. Cryptolepine was isolated and a solid-lipid formulation was prepared. Antiseizure activity of Solid-Lipid Nanoparticle formulation of cryptolepine (SLN-CRYP) was investigated using Pentylenetetrazole (PTZ)-induced model of seizure-like behaviors in Zebrafish with 2.5 and 5 mg/kg each of cryptolepine and SLN-CRYP. Drug receptor binding and permeability of the compound across the Blood Brain Barrier (BBB) were also assessed. SLN formulation of cryptolepine increased its permeability to the BBB from 0.32 × 10−6 cm/s to 10.81 × 10−6 cm/s. 2.5 and 5 mg/kg of SLN-CRYP significantly reduced mean seizure score (P = 0.0018; F(6, 63) = 23.52) and significantly increased (P < 0.0001; F(6, 63) = 65.41) latency to onset of seizures. The total distance swam by fish administered with 2.5 and 5 mg/kg of SLN-CRYP was significantly (P < 0.000; F(6, 63) = 161.9) decreased. 5 mg/kg of cryptolepine also significantly decreased swimming distance. Cryptolepine exhibited inhibitory modulation of human voltage-gated calcium channels (Cav1.2), H1-receptor, Peripheral Benzodiazepine Receptor and Sigma 2 receptor with a high Ki values of 6133.38 nM and 2945.0 nM, indicating less potent antagonism on Cav1.2 and Sigma 2 receptors compared to Nifedipine and Haloperidol respectively. This study reveals that the solid-lipid nanoparticle formulation of cryptolepine improves its BBB permeability and hence antiseizure activity. |
topic |
Nanoparticles Cav1.2 receptor Sigma 2 receptor Zebrafish Epilepsy Cryptolepis |
url |
http://www.sciencedirect.com/science/article/pii/S0753332221001396 |
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