Tetronic® 904-containing polymeric micelles overcome the overexpression of ABCG2 in the blood-brain barrier of rats and boost the penetration of the antiretroviral efavirenz into the central nervous system

dc.creatorRoma, Martín Ignacio
dc.creatorHocht, Christian
dc.creatorChiappetta, Diego Andrés
dc.creatorDi Gennaro, Stefania S.
dc.creatorMinoia, Juan Mauricio
dc.creatorBramuglia, Guillermo F.
dc.creatorRubio, Modesto Carlos
dc.creatorSosnik, Alejandro Dario
dc.creatorPeroni, Roxana Noemi
dc.date.accessioned2017-03-14T20:52:51Z
dc.date.accessioned2018-11-06T11:26:24Z
dc.date.available2017-03-14T20:52:51Z
dc.date.available2018-11-06T11:26:24Z
dc.date.created2017-03-14T20:52:51Z
dc.date.issued2015-04
dc.identifierRoma, Martín Ignacio; Hocht, Christian; Chiappetta, Diego Andrés; Di Gennaro, Stefania S.; Minoia, Juan Mauricio; et al.; Tetronic® 904-containing polymeric micelles overcome the overexpression of ABCG2 in the blood-brain barrier of rats and boost the penetration of the antiretroviral efavirenz into the central nervous system; Future Medicine; Nanomedicine; 10; 15; 4-2015; 2325-2337
dc.identifier1743-5889
dc.identifierhttp://hdl.handle.net/11336/13856
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1851727
dc.description.abstractAim: To assess the involvement of ABCG2 in the pharmacokinetics of efavirenz in the blood–brain barrier (BBB) and investigate a nanotechnology strategy to overcome its overexpression under a model of chronic oral administration. Materials & methods A model of chronic efavirenz (EFV) administration was established in male Sprague–Dawley rats treated with a daily oral dose over 5 days. Then, different treatments were conducted and drug concentrations in plasma and brain measured. Results: Chronic treatment with oral EFV led to the overexpression of ABCG2 in the BBB that was reverted after a brief washout period. Moreover, gefitinib and the polymeric amphiphile Tetronic® 904 significantly inhibited the activity of the pump and potentiated the accumulation of EFV in CNS. The same effect was observed when the drug was administered within mixed micelles containing TetronicT904 as the main component. Conclusion: Tetronic 904-containing polymeric micelles overcame the overexpression of ABCG2 in the BBB caused by chronic administration of EFV then boosting its penetration into the CNS.
dc.languageeng
dc.publisherFuture Medicine
dc.relationinfo:eu-repo/semantics/altIdentifier/url/http://www.futuremedicine.com/doi/abs/10.2217/nnm.15.77
dc.relationinfo:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.2217/NNM.15.77
dc.rightshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.subjectABCG2 pump inhibition
dc.subjectCNS
dc.subjectdrug-loaded poly(ethylene oxide)-b-poly(propylene oxide) polymeric micelles
dc.subjectefavirenz
dc.subjectHIV
dc.subjectnanotechnology
dc.subjectcentral nervous system
dc.titleTetronic® 904-containing polymeric micelles overcome the overexpression of ABCG2 in the blood-brain barrier of rats and boost the penetration of the antiretroviral efavirenz into the central nervous system
dc.typeArtículos de revistas
dc.typeArtículos de revistas
dc.typeArtículos de revistas


Este ítem pertenece a la siguiente institución