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(?-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. This journal is
Sustained anti-BCR-ABL activity with pH responsive imatinib mesylate loaded PCL nanoparticles in CML cells
Cortese Barbara;Gigli Giuseppe;Palamà Ilaria Elena
2015
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(?-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. This journal isI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.


