Radiolabeled trastuzumab (TRZ) loaded solid lipid nanoparticles
(SLNs) were prepared by high shear homogenization and sonication techniques.
The apoptosis mechanism of TRZ-SLNs was studied only with the MCF-7
cell line, while the cytotoxicity and cell binding capacity were investigated
using breast cancer cells (MCF-7 and MDA-MB-231) and the human keratinocyte
cell line (HaCaT). The particle sizes of TRZ-SLNs were found to be
below 100 nm, and they possessed a negative charge. The high radiolabeling
efficiency and good radiolabeling stability in saline and a cell culture
medium were obtained in the results of radiolabeling studies. According
to the in vitro studies, TRZ-SLNs were found to be biocompatible,
and they effectively induced apoptosis in MCF-7 cells. After the parenteral
injection of TRZ-SLNs into rats, a sustained release profile in blood
circulation was achieved compared with free drug solution by the evaluation
of pharmacokinetic parameters. As a conclusion, the study reveals
that Technetium-99m (
99m
Tc radiolabeled) TRZ loaded SLN
formulations could be promising theranostic agents based on their
characterization profiles, in vitro cellular uptake and apoptosis
induction capacity, and in vivo pharmacokinetic profiles.
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