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.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Zybina A,Anshakova A,Malinovskaya J,Melnikov P,Baklaushev V,Chekhonin V,Maksimenko O,Titov S,Balabanyan V,Kreuter J,Gelperina S,Abbasova Kdoi
10.1016/j.ijpharm.2018.05.023subject
Has Abstractpub_date
2018-08-25 00:00:00pages
10-23issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(18)30321-1journal_volume
547pub_type
杂志文章abstract：:Hexamidine diisethionate (HEX D) has been used in the personal care industry and in a number of over-the-counter (OTC) drug products as an antimicrobial agent since the 1950's. Recently, the compound has also been investigated for its beneficial effects on skin health. Surprisingly, there is only limited information d...
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