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Thermosensitive poly(Nisopropyl acrylamide-co-N,Ndimethyl acryl amide)-blockpoly(d,l-lactide) amphiphilic block copolymer micelles for prednisone drug release
Novel amphiphilic block copolymers consisting of hydrophobic poly(d,l-lactide) segments and
hydrophilic poly(N-isopropylacrylamide-co-N, N-dimethylacrylamide) blocks were designed and
synthesized through a simple free radical copolymerization route based on a bifunctional initiator,
followed by the ring-opening polymerization of d,l-lactide. The copolymers self-assembled into
thermosensitive spherical-nanosized core–shell micelles in aqueous solution in the presence
or the absence of the model drug prednisone. The chemical and physical characterizations of
drug-loaded and unloaded micelles revealed a lower critical solution temperature of 40°C–47°C,
and a critical micelle concentration less than 7.20 mg L−1, a transmission electron microscope
mean particle size from 50 to 75 nm, and a narrow dynamic light scattering diameter below 180
nm. The prepared blank and drug-loaded micellar nanoparticles were thermodynamically stabile
and employed in targeted drug delivery by responding to the higher temperature of the local
microenvironment. Based on prednisone release kinetic studies, structural changes of the selfassembled
micelles as well as temperature- or environment-induced diffusion controlled drug
release and improved bioavailability. The copolymer micelles exhibited good biocompatibility as
established by the MTT cytotoxicity assay. Therefore, an effective target therapy against lesion
tissues is feasible using these polymeric micelles.
Keywords Biomaterials, chemical synthesis, thermosensitivity, copolymer micelles, drug release, cytotoxicity
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