To utilize the MNPs as a drug delivery vehicle, it is essential to be coated with hydrophilic or hydrophobic polymer to avoid the aggregation in vivo. Further, these MNPs should also acquire high drug loading capacity, desired release profile, aqueous dispersibility, biocompatibility with cells and tissues along with retention of magnetic properties. Our previous study have demonstrated that coating the MNPs with long chain amphiphilic lipid polymer glyceryl monooleate provides the aqueous dispersibility and permits the incorporation of both hydrophilic and hydrophobic drugs. In different experimental setups, our group has already established the fact that, targeted drug delivery through functionalized drug carriers is an effective strategy to provide higher therapeutic concentrations of anticancer drugs by overcoming the multidrug resistance at the targeted cancer cells thereby reducing the dose and unaffecting the noncancerous tissues. Apart from the therapeutic application, currently significant attention has been laid down for the multifunctional characteristics and complementary role of MNPs as a contrast agent for the magnetic resonance imaging. MRI provides excellent differential soft tissue contrast that helps to discriminate healthy tissues and abnormal tissues like cancer tissues. Thus, magnetic nanoparticles provide an excellent diagnosis tool for the treatment of cancer. In addition, in case of leukemia, T2 weighted MRI has already been established as an efficient diagnostic and management tool. Jaetao et al. have demonstrated that detection of leukemic cells can be enhanced by using MNPs with surface conjugation of receptorspecific ligands. So, here in this study, we have investigated the efficacy of paclitaxel loaded MNPs formulations functionalized with a targeting moiety lectin. The use of specific molecular signatures at the targeted site helps in Staurosporine delivering the appropriate therapeutic PD325901 concentration aiding the advantage of receptor mediated endocytosis. The cellular uptake efficiency of pac-MNPs and lectin conjugated pac-MNPs was compared with native drug in leukemic cell line. The uptake experiment was also studied in lectin negative cell line i.e, HEK293. To elucidae the probable molecular pathways ascribed through pac-MNPs in K562 cells, the levels of different extrinsic and intrinsic apoptotic pathway proteins were studied through immunobloting. Besides the levels of expression of different apoptotic genes and CML specific Bcr-Abl gene were quantified through real time PCR following post treatment of native pac, pac-MNPs and lec-pac-MNPs. In both the cell lines, there was a significant higher uptake of 6- coumarin-MNPs than the native one whereas, the difference in the uptake of 6-couma-MNPs and lec-6-coumarin-MNPs was minimal.