Radiolabeled methotrexate loaded chitosan nanoparticles as imaging probe for breast cancer: Biodistribution in tumor-bearing mice
Makaleler > Tam Makale · 2022
Yazarlar: Meliha EKİNCİ, Çinel KÖKSAL KARAYILDIRIM, Derya İLEM ÖZDEMİR
Journal of Drug Delivery Science and Technology, SCI Expanded İndekslerine Giren Dergi, Uluslararası, Wos, 2022, cilt 80, ss 104146-104146
DOI: 10.1016/j.jddst.2022.104146
Özet
<p>There is great interest in developing nanoparticle drug delivery systems for the delivery of therapeutics or imaging agents for cancer. In this context, a new radiopharmaceutical was prepared by labeling the methotrexate (MTX) loaded chitosan nanoparticles (CSNPs) with [99mTc]Tc radionuclide, and the breast cancer imaging potential of the radiopharmaceutical was determined by <em>in-vivo</em> biodistribution studies. Within the scope, different amounts of MTX-loaded CSNPs (MTX-CSNPs) (F1–F3) were prepared <em>via</em> an ionotropic gelation process. The physicochemical properties of MTX-CSNPs were evaluated. The mean diameter of MTX-CSNPs was found between 148.8 ± 0.636 nm and 157.0 ± 3.960 nm, the PdI value of between 0.415 ± 0.042 and 0.451 ± 0.036 and the zeta potential of between 15.7 ± 1.17 mV and 18.7 ± 0.27 mV. In addition, the preparation efficiency of MTX-CSNPs was found to be between 64.036 ± 2.054% - 70.234 ± 2.140% and the encapsulation efficiency of CSNPs was found to be between 32.301 ± 1.205–50.304 ± 2.478%. MTX-CSNPs were radiolabeled with [99mTc]Tc, and the radiolabeled nanoparticles ([99mTc]Tc-MTX-CSNPs) were evaluated by both <em>in-vitro</em> cell binding studies and <em>in-vivo</em> biodistribution studies. [99mTc]Tc-MTX-CSNPs showed high labeling efficiency (≥99%) and <em>in-vitro</em> stability up to 6 h at room temperature. According to the cell incorporation study, [99mTc]Tc-MTX-CSNPs (F3) showed significantly higher uptake into 4T1 (breast cancer) cells than R/H-[99mTc]Tc. Biodistribution studies of [99mTc]Tc-MTX-CSNPs (F3) were performed in breast tumor-bearing female Balb/c mice. Compared to [99mTc]Tc-MIBI, [99mTc]Tc-MTX-CSNPs (F3) exhibited significantly higher uptake by breast tumors. This study demonstrates the affinity of [99mTc]Tc-MTX-CSNPs to breast cancer cells and their diagnostic utility.</p>