Sustained anti-BCR-ABL activity with pH responsive imatinib mesylate loaded PCL nanoparticles in CML cells

Abstract

Imatinib mesylate (IM) is an inhibitor that targets the tyrosine kinase activity of BCR-ABL present in Chronic Myeloid Leukemia (CML). Here, IM–chitosan complex loaded poly(ε-caprolactone) (PCL) nanoparticles (NPs) are recommended for their potential in supporting controlled release and improving the chemotherapeutic efficiency of IM. The nanoparticles with a size of about 247 nm have a core–shell structure with an IM-containing inner core surrounded by a PCL layer. The presence of chitosan (CH) allows one to modulate the release kinetics in a pH-dependent manner. IM is released from the NPs much more quickly at pH 4.0 and 6.0 than at pH 7.4, which is a desirable characteristic for cancer-targeted drug delivery. Our core–shell PCL NPs could provide a simple and easy way to allow controlled release of IM and improve their chemotherapeutic efficiency, combining the pH sensibility of CH and the slow degradation of PCL.