Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters










Database
Language
Publication year range
1.
Int J Pharm ; 547(1-2): 10-23, 2018 Aug 25.
Article in English | MEDLINE | ID: mdl-29751140

ABSTRACT

Resistance to antiepileptic drugs (AEDs) is a major clinical problem. The overexpression of P-glycoprotein (Pgp), one of the main transporters limiting the entry of xenobiotics into the brain, is among the factors contributing to the AED resistance. Presently, there is no consensus on the interaction of carbamazepine (CBZ) with the Pgp. This study investigates the effect of the Pgp inhibitor verapamil on the anticonvulsant effect of CBZ and its nanoparticulate formulation in the rat model of isoniazid-induced epilepsy. Verapamil significantly increased the anticonvulsant effect of CBZ and reduced its effective dose by at least 30% (from 30 mg/kg to 20 mg/kg). Binding of carbamazepine to the poloxamer 188-coated PLGA nanoparticles enabled a 30-fold increase of its anticonvulsive effect, as compared to the free drug. The inhibition of Pgp did not influence the effectivity of carbamazepine encapsulated in nanoparticles.


Subject(s)
Anticonvulsants/administration & dosage , Carbamazepine/administration & dosage , Drug Resistant Epilepsy/drug therapy , Nanoparticles/administration & dosage , ATP Binding Cassette Transporter, Subfamily B, Member 1/antagonists & inhibitors , Animals , Anticonvulsants/chemistry , Anticonvulsants/pharmacokinetics , Anticonvulsants/therapeutic use , Brain/physiopathology , Carbamazepine/chemistry , Carbamazepine/pharmacokinetics , Carbamazepine/therapeutic use , Dose-Response Relationship, Drug , Drug Delivery Systems , Drug Resistant Epilepsy/chemically induced , Drug Resistant Epilepsy/physiopathology , Electrocorticography , Isoniazid , Lactic Acid/administration & dosage , Lactic Acid/chemistry , Lactic Acid/pharmacokinetics , Lactic Acid/therapeutic use , Male , Nanoparticles/chemistry , Nanoparticles/therapeutic use , Poloxamer/administration & dosage , Poloxamer/chemistry , Poloxamer/pharmacokinetics , Poloxamer/therapeutic use , Polyglycolic Acid/administration & dosage , Polyglycolic Acid/chemistry , Polyglycolic Acid/pharmacokinetics , Polyglycolic Acid/therapeutic use , Polylactic Acid-Polyglycolic Acid Copolymer , Rats, Wistar , Verapamil/pharmacology
SELECTION OF CITATIONS
SEARCH DETAIL
...