Carboxymethyl cellulose microgels as promising multifunctional carriers of bismuth radionuclides and drugs

Abstract

Ternary microgels CMC-Bi(²¹³Bi, ²⁰⁷Bi)-L obtained by crosslinking of bismuth ions with carboxymethylcellulose (CMC) and physicochemically characterized. Here L is AP = 2-aminopyrimidine / L¹ = N-(5,6-dihydro-4H-1,3-thiazin-2-yl)benzamide / L² = N-(4-isopropyl—phenyl)–N-(1 -iminoethyl) piperidine–1-carbothioamide hydrobromide. Ligands L¹ and L² are NO synthase effectors (inhibitor and activator, respectively), possessing antileukemic properties. The sizes of ternary microgels containing L¹ and L² were 160–180 nm in PBS and 110–160 nm in PBS + BSA compared to 400 nm for the native CMC. Cytotoxicity tests revealed the most promising microgel compositions (c TW = 625) for further research for medical purposes. The distribution and elimination of ternary microgels in vivo in the body studied on a mouse model and for most organs it was approximately 24 h.