Cholesteryl-grafted functional amphiphilic poly(N-isopropylacrylamide-co-N- hydroxylmethylacrylamide): Synthesis, temperature-sensitivity, self-assembly and encapsulation of a hydrophobic agent

Abstract

A thermally responsive amphiphilic grafted copolymer comprised of hydroxyl-containing random poly(N-isopropylacrylamide-co-N- hydroxylmethylacrylamide) as the hydrophilic chain and cholesteryl groups as hydrophobic side arms was developed for the controlled release of hydrophobic drugs. The polymer was temperature-sensitive with a lower critical solution temperature of 40.5°C and a critical micelle concentration of 4mg/l. Dynamic light-scattering studies showed that the amphiphilic polymer self-assembled into micelles in aqueous media with their mean sizes in the range of 25-34nm. Transmission electron microscope studies showed that the nanoparticles prepared from the micelle solutions exhibited multiple morphologies including unusual cubic and cuboids-like shapes, and normal spherical shapes, which could be controlled by the formation conditions. Wide-angle X-ray scattering studies showed that these nanoparticles were amorphous in nature but a small crystalline phase existed and the crystallinity of particles increased with the decrease of initial formation concentration. Pyrene was employed as a model hydrophobic agent to examine the encapsulation ability of the polymer with respect to hydrophobic agents in aqueous media. The loading level of the polymer with respect to pyrene was 4.4mg/g, indicating that the thermally responsive amphiphilic polymer would be able to be used for the encapsulation of hydrophobic drugs. © 2003 Elsevier Ltd. All rights reserved.