Development of fluorescent- and radio-traceable T1307-polymeric micelles as biomedical agents for cancer diagnosis: biodistribution on 4T1 tumor-bearing mice

Abstract

In recent years, nanocarriers have been studied as promising pharmaceutical tools for controlled drug-delivery, treatment-efficacy follow-up and disease imaging. Among them, X-shaped amphiphilic polymeric micelles (Tetronic®, poloxamines) display great potential due to their biocompatibility and non-toxic effects, among others. In the present work, polymeric micelles based on the T1307 copolymer were initially decorated with a 4,4-difluoro-4-bora-3a,4a-diazas-indacene (BODIPY)-fluorophore in order to determinate its in vivo biodistribution on 4T1 tumor-bearing mice. However, unfavorable results with this probe led to two different strategies. On the one hand, the BODIPY-loaded micelles, L-T1307-BODIPY, and on the other hand, the 99m Tc-radiolabeled micelles, L-T1307-99m Tc, were analyzed separately in vivo. The results indicated that T1307 accumulates mainly in the stomach, the kidneys, the lungs and the tumor, reaching the maximum organ-accumulation 2 hours after intravenous injection. Additionally, and according to the results obtained for L-T1307-99m Tc, the capture of the polymeric micelles in organs could be observed up to 24 hours after injection. The results obtained in this work were promising towards the development of new radiotracer agents for breast cancer based on X-shaped polymeric micelles.

Molecular insights into the aggregation and solubilizing behavior of biocompatible amphiphiles Gelucire® 48/16 and Tetronics® 1304 in aqueous media

“…Similarly, Puig-Rigall et al 34 developed formulations of miltefosine (MF), an alkylphospholipid for breast cancer treatment, using TPGS, T1107 and T904 and noted improved activity of MF with T904 against intracellular amastigotes. Lecot et al 35 in a recent study used T1307 modified with a 4,4-difluoro-4-bora-3a,4a-diaza- s -indacene fluorophore for assessing it's in vivo biodistribution on 4T1 tumor-bearing mice and attained results revealing promising role of T1307 micelles as radio tracer agents for breast cancer imaging. Castelli et al 36 observed the co-association of aptamer Sgc8-c-Alexa647, a biomarker in cancer with different nanostructures like F127, T1307 and pegylated liposomes.…”