Abstract

Rationale & aim: Imatinib mesylate (IM), a selective tyrosine kinase inhibitor of the oncoprotein BCR-ABL,is the 'gold standard' for patients with chronic myeloid leukemia (CML) but the drug does not eliminateCML stem cells, leading to disease relapse on drug discontinuation. At present, much effort is focused ondelivery carriers that can increase the intracellular retention and antileukemic impact of IM. We previouslyvalidated IM-loaded polyelectrolyte microcapsules as effective purging agents to eradicate BCR-ABL+ cellsfrom CML patient autografts. The aim is to develop controlled release carriers that can increase theintracellular retention and functionality of IM in leukemia cells. Materials & methods: Herein, novelpolyelectrolyte complexes were used as model carriers for IM in a CML cell line (KU812) and CD34+ cellsfreshly isolated from patients. Results & discussion: Polyelectrolyte complexes promoted a long-actingBCR-ABL kinase inactivation that was necessary to promote apoptosis at approximately twofold lowerintracellular IM dose compared with the microscale formulation polyelectrolyte microcapsules.Conclusion: IM-loaded polyelectrolyte complexes can be used as more efficient delivery devices forovercoming drug resistance of BCR-ABL+ leukemic cells.

Autore Pugliese

• Palama' Ilaria Elena

Tutti gli autori

• I.E. Palamà; A.M.L. Coluccia; G. Gigli

Titolo volume/Rivista

Nanomedicine

Anno di pubblicazione

2014

ISSN

1743-5889

ISBN

Non Disponibile

Numero di citazioni Wos

Nessuna citazione

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

Non Disponibile

Ultimo Aggiornamento Citazioni

Non Disponibile

Settori ERC

Non Disponibile

Codici ASJC

Non Disponibile