ABSTRACT
We describe herein the assembly and in vivo evaluation of a tailor-made micellar carrier system designed for the optimized encapsulation of a superfluorinated MRI probe and further targeting of solid tumors. The in vivo validation was carried out on MC38 tumor-bearing mice which allowed the confirmation of the efficient targeting properties of the nano-carrier, as monitored by 19F-MRI.
Subject(s)
Fluorine-19 Magnetic Resonance Imaging , Neoplasms , Animals , Magnetic Resonance Imaging , Mice , MicellesABSTRACT
In this study, a "click and hybridization" strategy was developed for the functionalization of polydiacetylene micelles with a targeting aptamer ligand. Decoration of the nanocarriers with an anti-Annexin A2 sequence efficiently triggered enhanced internalization of the functionalized micelles in the MCF-7 cell line, with a marked increase compared to control micelles.
Subject(s)
Annexin A2/genetics , Aptamers, Nucleotide/administration & dosage , Drug Carriers/administration & dosage , Micelles , Polyacetylene Polymer/administration & dosage , Biological Transport , Humans , MCF-7 CellsABSTRACT
Polydiacetylene micelles were functionalized with controlled amounts of biotin using bioorthogonal click chemistry. The biotinylated micelles were evaluated in the selective targeting of the MCF-7 cancerous cell line and were shown to be readily internalized. The efficiency of the cellular uptake was correlated to the density of grafted biotin.
Subject(s)
Biotin/analogs & derivatives , Micelles , Polymers/chemistry , Polyynes/chemistry , Biotin/metabolism , Biotinylation , Click Chemistry , Humans , MCF-7 Cells , Polyacetylene Polymer , Polymerization , Polymers/chemical synthesis , Polymers/metabolism , Polyynes/chemical synthesis , Polyynes/metabolism , Receptors, Growth Factor/metabolismABSTRACT
Compact polymerized polydiacetylene-micelles with "stealth" zwitterionic surface coating were assembled and tested in a murine xenograft model of breast cancer. In vivo fluorescence imaging indicated accumulation in the tumor area and histological studies revealed predominant uptake of the micelles at the margins of the tumor, thereby allowing the delineation of its volume.
