Preparation of Developing Biotinylated PH-Responsive Glycopolymers as Delivery Nanocarriers for Controlling Release of Bortezomib

Abstract

To develop biotinylated pH-responsive glycopolymers and investigate their performances as anticancer drug delivery nanocarriers, bromide-terminated biotin was synthesized and then used to initiate the polymerization of D-gluconamido ethyl methacrylate (GAMA) and 2-(diethylamino)ethyl methacrylate (DEA) monomers via atom transfer radical polymerization (ATRP). Two biotinylated pH-responsive copolymers with similar degree polymerization (DP) chain segments, Biotin-P(GAMA- b -DEA) and Biotin-P(GAMA- co -DEA), were prepared by block or random architectures, respectively. The chemical compositions and self-assembly behavior of glycopolymers were characterized. The results show that the block glycopolymer self- assembles in water medium into core-shell structure assembly containing PGAMA shell and PDEA core with the 28 nm in diameter, while the random glycopolymer remains water-soluble state above pH 7.4. Both glycopolymers possess the loading ability of the BTZ with encapsulation efficiency (EE %) and loading capacity (LC %) of 83.7% and 8.4%, 78.7% and 7.9%, and the release behavior was kept at low constants with 20% and 26% cumulative amount even after 24 hours at pH 7.4, respectively. The study is expected to give the light to the development of new intelligent drug carrier system with excellent biological compatibility.