Albumin nanoparticles coated with polysorbate 80 for the targeted delivery of antiepileptic drug levetiracetam into the
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ORIGINAL ARTICLE
Albumin nanoparticles coated with polysorbate 80 for the targeted delivery of antiepileptic drug levetiracetam into the brain Barnabas Wilson 1 & Janani Selvam 1 & Geetha K. Mukundan 2 & Kudumula B. Premakumari 3 & Josephine L. Jenita 1
# Controlled Release Society 2020
Abstract The aim of the study was to target levetiracetam (LEV) into the brain by albumin nanoparticles. The levetiracetam-loaded albumin nanoparticles (LEV-NPs) were formulated by desolvation. The particle size of LEV-NPs was 153.7 ± 44.8 nm and the zeta potential was − 10.8 mV. The in vitro LEV release, in pH 6.8 phosphate buffer, was determined by dialysis and showed a biphasic pattern of drug release and ranged in between 40.42 ± 2.6% w/w and 63.61 ± 2.12% w/w. The biodistribution study was conducted on male Wistar rats. The LEV was given as i.v. injection in tail vein, and the formulations were the free drug, LEVNPs, and levetiracetam-loaded albumin nanoparticles further coated with 1% polysorbate 80 (LEV-NPs-PS 80). A significant increase in LEV concentration was achieved in the brain for LEV-NPs-PS 80 when compared with LEV free drug. The LEV concentration achieved in the brain after administering free drug and LEV-NPs-PS 80 was 5.28 ± 1.79 and 18.54 ± 2.38 μg/gm respectively. The LEV-NPs-PS 80 enhanced LEV concentration in the brain by 3.51-fold when compared with the free drug. Keywords Brain drug targeting . Convulsion . Levetiracetam . Albumin nanoparticles . Blood-brain barrier . Biodistribution
Introduction Epilepsy, a complicated and chronic neurological disorder, is characterized by recurrent seizures and affects all ages but more common in aged population. The seizures are transient signs of abnormal and excessive or hypersynchronous neuronal function in the brain [1]. Epilepsy requires immediate attention to avoid further progression. Approximately 50 million people are suffering from epilepsy worldwide [2]. About 80% of the epileptic patients are found in low- and middleincome countries. Drugs like phenytoin, valproate, carbamazepine, gabapentin, levetiracetam, oxcarbazepine, topiramate, * Barnabas Wilson [email protected] 1
Department of Pharmaceutics, College of Pharmaceutical Sciences, Dayananda Sagar University, Kumaraswamy Layout, Bangalore, Karnataka 560078, India
2
Department of Pharmacology, College of Pharmaceutical Sciences, Dayananda Sagar University, Kumaraswamy Layout, Bangalore, Karnataka 560078, India
3
Department of Pharmaceutical Chemistry, College of Pharmaceutical Sciences, Dayananda Sagar University, Kumaraswamy Layout, Bangalore, Karnataka 560078, India
tiagabine, lamotrigine, and zonisamide are used for controlling epileptic seizures. But the drugs are ineffective to control the epileptic seizures in about 30% of the patients. Further, the antiepileptic drugs are known for their serious side effects, dose-related chronic toxicity, and teratogenicity. Phenytoin and carbamazepine cause ataxia as they activate the sodium channel, and benzodiazepines as well as barbiturates cause s
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