Hydrophobic Drug Delivery by Self-Assembling Triblock Copolymer-Derived Nanospheres

We describe the synthesis and characterization of a family of biocompatible ABA-triblock copolymers that comprised of hydrophilic A-blocks of poly(ethylene glycol) and hydrophobic B-blocks of oligomers of suberic acid and desaminotyrosyl−tyrosine esters. The triblock copolymers spontaneously self-as...

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Bibliographic Details
Published in:Biomacromolecules 2005-09, Vol.6 (5), p.2726-2731
Main Authors: Sheihet, Larisa, Dubin, Robert A, Devore, David, Kohn, Joachim
Format: Article
Language:English
Subjects:
Antineoplastic Agents - administration & dosage
Applied sciences
Biocompatible Materials - chemistry
Biological and medical sciences
Caprylates - chemistry
Chemical modifications
Chemical reactions and properties
Chromatography
Chromatography, Gel
Dicarboxylic Acids - chemistry
Dose-Response Relationship, Drug
Drug Delivery Systems
Esters
Exact sciences and technology
Fluorescein - pharmacology
Fluoresceins - pharmacology
General pharmacology
Humans
Medical sciences
Models, Chemical
Molecular Weight
Nanotechnology
Nanotubes - chemistry
Neoplasms - therapy
Organic polymers
Paclitaxel - pharmacology
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Phosphates - chemistry
Physicochemistry of polymers
Polyethylene Glycols - chemistry
Polymers - chemistry
Time Factors
Tyrosine - chemistry
Ultracentrifugation
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Summary:We describe the synthesis and characterization of a family of biocompatible ABA-triblock copolymers that comprised of hydrophilic A-blocks of poly(ethylene glycol) and hydrophobic B-blocks of oligomers of suberic acid and desaminotyrosyl−tyrosine esters. The triblock copolymers spontaneously self-assemble in aqueous solution into nanospheres, with hydrodynamic diameters between 40 and 70 nm, that do not dissociate under chromatographic and ultracentrifugation conditions. These nanospheres form strong complexes with hydrophobic molecules, including the fluorescent dye 5-dodecanoylaminofluorescein (DAF) and the antitumor drug, paclitaxel, but not with hydrophilic molecules such as fluorescein and Oregon Green. The nanosphere−paclitaxel complexes retain in vitro the high antiproliferative activity of paclitaxel, demonstrating that these nanospheres may be useful for delivery of the hydrophobic drugs.
ISSN:1525-7797
1526-4602
DOI:10.1021/bm050212u