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Saposin C (SapC) is a multifunctional lysosomal protein known to activate lysosomal enzymes and induce membrane fusion.We have investigated the antituinor efficacy of SapC-lipid nanovesicles in preclinical cancer models.SapClipid nanovesicles, with a mean diameter of ~190 nm, demonstrated specific tumor-targeting and tumor-homing activities by in vivo imaging.Paramagnetic iron oxide (USPIO) nanoparticles are magnetic resonance (MR) contrast agents used to label cells.In this study, we have incorporated SapC and USPIO in lipid nanovesicles and demonstrated in vivo the combined delivery of USPIO to tumors using high resolution MR imaging.SapC-lipid nanovesicles with Tumor-targeting activity could potentially be used to deliver USPIO to cancer tissues, aiding in earlier detection and better visualization using MRI.Tumor-homing delivery and uptake of drugs can also be estimated using contrast enhanced MR micro-imaging by using SapC-lipid nanovesicles as dual carriers for the drug and the contrast agent.Biophotonic IVIS(R) imaging and immunofluorescence analysis confirmed that SapC and fluorescent lipophilic probe delivered by SapC-lipid nanovesicles were preferentially accumulated in tumor vessels and cells.Tumor-accumulation of SapC-lipid results from its selective targeting and homing to tumor sites in an acidic micro-enviroument.Preclinical toxicity studies suggest a high clinical safety margin for use of SapC-lipid nanovesicles.Therefore, SapC-lipid nanovesicles have the potential to offer a targeted potent, broad and safe agent for cancer imaging and diagnosis.