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. Author manuscript; available in PMC: 2018 Oct 1.
Published in final edited form as: Mol Cancer Ther. 2017 Jun 15;16(10):2191–2200. doi: 10.1158/1535-7163.MCT-16-0907

Figure 1. Development of 225Ac labeled αvβ3 targeted liposomes (225Ac-IA-TLs).

Figure 1

(A) PEG-di (carboxylic acid) linker (HOOC(CH2CH2O)n=2-45COOH) was conjugated to 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) and N-hydroxysuccinimide (NHS) to yield pure DiynePE-PEGn-NHS. Monovalent polymerizable IA-lipid was produced by conjugating IA with lipid solution of DiynePE-PEGn-NHS. (B) TLC analysis showing production of pure DiynePE-PEGn-IA along with diagrammatic representation of IA-TLs; prepared liposomes had a mean diameter of ~100 nm. (C) DiynePE was mixed with S-2-(4-Isothiocyanatobenzyl)-1,4,7,10-tetraazacyclododecane tetraacetic acid (pSCN-Bn-DOTA) to produce pure DiynePE-DOTA. For 225Ac labeling, prepared IA-DOTA-TLs were incubated with 225Ac at 70⁰C for 50 minutes. Radio-TLC analysis showed effective radiolabeling of targeted liposomes with a radiochemical purity of 99.6%.