Micelle-like nanoparticles of block copolymer poly(ethylene oxide)-block-poly(methacrylic acid) incorporating fluorescently substituted metallacarboranes designed as HIV protease inhibitor interaction probes.
We prepared nanoparticles differing in morphology from double-hydrophilic block copolymer poly(ethylene oxide)-block-poly(methacrylic acid), PEO-PMA, and two types of fluorescein-[3-cobalt(III) bis(1,2-dicarbollide)] conjugates, GB176 and GB179, in alkaline buffer. GB176 molecule consists of fluorescein attached to the metallacarborane anion. In GB179 molecule, the fluorescein moiety connects two metallacarborane anions. The self-assembly is based on the unusual interaction of metallacarborane clusters with PEO blocks which form insoluble micellar cores. The GB176 containing nanoparticles are loose and irregular, while the GB179 ones are rigid and spherical. The structure of nanoparticles depends to some extent on a procedure of preparation. The micelles were studied by static and dynamic light scattering, fluorometry and atomic force microscopy. Since the metallacarborane conjugates act as potent inhibitors of HIV protease, the presented system is important from the point of view of drug delivery.
Uchman
Mariusz
M
Department of Physical and Macromolecular Chemistry, Faculty of Science, Charles University, Hlavova 2030, 128 40 Prague 2, Czech Republic.
Cígler
Petr
P
Grüner
Bohumír
B
Procházka
Karel
K
Matejícek
Pavel
P
D001896:Boron Compounds; D005453:Fluorescence; D017320:HIV Protease Inhibitors / Q000032:analysis*; D006801:Humans; D008670:Metals; D008689:Methacrylates; D008823:Micelles; D015335:Molecular Probes / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D011091:Polyesters; D011092:Polyethylene Glycols
D001896:Boron Compounds; D017320:HIV Protease Inhibitors; D008670:Metals; D008689:Methacrylates; D008823:Micelles; D015335:Molecular Probes; D011091:Polyesters; C008384:methacrylic acid; D011092:Polyethylene Glycols