One-Pot Synthesis of Linear-Hyperbranched Amphiphilic
Block Copolymers Based on Polyglycerol Derivatives and Their Micelles
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Abstract
This paper describes the one-pot
synthesis of a polyglycidol (PG)-based
polymer, poly(ethoxyethyl glycidyl ether) (PEEGE)-<i>b</i>-[<i>hyperbranched</i> polyglycerol (<i>hb</i>PG)-<i>co</i>-PEEGE]<sub><i>x</i>/<i>y</i></sub>, its micelle formulation, and the ability to encapsulate a
model therapeutic molecule. Amphiphilic block copolymers were prepared
by the sequential addition of ethoxyethyl glycidyl ether (EEGE) to
glycidol. The composition of the block copolymers varied from 62:38
to 92:8. Block copolymers with composition <i>x</i>:<i>y</i> ≥ 66:34 were soluble only in organic solvents.
Micelles were formulated by injection of deionized water into a tetrahydrofuran
block copolymer solution with or without pyrene as a model hydrophobic
molecule. The critical micelle concentration was 18.2–30.9
mg/L, and the micelle size was 100–250 nm. The pyrene-containing
micelle rapidly collapsed on acidic exposure, allowing conversion
of hydrophobic PEEGE to hydrophilic PG, thus, facilitating the release
of the encapsulated pyrene. Cytotoxicity data showed high biocompatibility
of PG-based block copolymers, suggesting their potential as a drug
delivery carrier