Nanostructured lipid carriers (NLCs) are the new generation of solid lipid drug delivery systems. Their suitability as contrast agents for gamma scintigraphy is an attracting major attention. The aim of current study was to prepare surface modified nanostructured lipid carrier system for paclitaxel (PTX) with active targeting and imaging functions. In accordance with the purpose of study, PTX loaded nanostructured lipid carriers (NLCs) prepared, modified with a folate derivative and radiolabeled with technetium-99 m tricarbonyl complex (Tc-99 m(CO)(3)(+)). Cellular incorporation ratios of radiolabeled nanoparticles (Tc-99 m(CO)(3)-PTX-NLC) were investigated in vitro on three cancer cell lines. Additionally in vivo animal studies conducted to evaluate biological behavior of Tc-99 m(CO)(3)-PTX-NLC on female Wistar Albino rats. Biodistribution results showed that the folate derivative modified Tc-99 m(CO)(3)-PTX-NLC had considerably higher uptake in folate receptor positive organs. The data obtained from present study could be useful in the design of biodegradable drug carriers of PTX and folate receptor based tumor imaging agents.