Formulation of radiolabeled solid lipid nanoparticles for paclitaxel delivery and determination of radiopharmaceutical potential

In current study, it is aimed to synthesize paclitaxel (PTX) loaded solid lipid nanoparticles, to radiolabel these nanoparticles with technetium-99m tricarbonyl core and to evaluate its biological behaviour utilizing in vitro and in vivo methods. Solid lipid nanoparticles (SLN) were synthesized by solvent diffusion method. Structural characterization of SLN was performed by Zeta Potential Analysis, Dynamic Light Scattering (DLS) method, Transmission Electron Microscope (TEM) and Scanning Electron Microscope (SEM) imaging. Nanoparticles were modified with folate derivative polyethylene glycol-cholesterol hemisuccinate (Fol-PEG-CHEMS) molecule to target folate receptors. Characterization of targeting molecule was performed by proton Nuclear Magnetic Resonance Spectroscopy (1H-NMR). Radiolabeling of PTX loaded solid lipid nanoparticles with technetium (I) tri carbonyl core [99mTc(CO)3(H2O)3]+ accomplished with 90 % efficiency. Thin Layer Radiochromatography (TLRC) and High Performance Liquid Radiochromatography (HPLRC) methods were used for quality control of paclitaxel loaded radiolabeled solid lipid nanoparticles (99mTc(CO)3-SLN-PTX). In vitro biological behavior of 99mTc(CO)3-SLN-PTX investigated with incorporation studies on folate receptor positive breast (MCF7), cervix (HeLa) and folate receptor negative lung (A549) carcinoma cell lines. Higher uptake values of 99mTc(CO)3-SLN-PTX were determined on MCF7 and HeLa cell lines according to A549 cell line. Biodistribution and imaging studies were conducted to investigate in vivo behaviour of 99mTc(CO)3-SLN-PTX on female Wistar Albino rats. According to results of in vivo studies, it was observed that 99mTc(CO)3-SLN-PTX have higher uptake in folate receptor positive kidney tissue considering other sites. According to obtained data from in vitro and in vivo studies, it is seen that the improved system (paclitaxel loaded radiolabeled solid lipid nanoparticles) is specific to folate receptors. It is concluded that the system improved in present study will make contribution to improve an easy prepared, target specific and biocompatible diagnostic agent with therapy potential.