Mannose-Conjugated Polymeric Micelles with Different Sizes for Targeted Drug Delivery

Abstract:

The poly（solketal methacrylate）-block-poly（glycidyl methacrylate）（PSA-b-PGMA） copolymer is synthesized by atom transfer radical polymerization（ATRP） and functionalized with mannose by the "click" reaction to yield PSA-b-PGMA-Mannose. These copolymers are used to prepare polymeric micelles，and an anticancer drug，doxorubicin（DOX），is encapsulated into the micelles by oil-water method. Structure of PSA-b-PGMA-Mannose is confirmed by 1H NMR and FT-IR. The size and morphologie of PSA-b-PGMA-Mannose with different block ratios were characterized by transmission electron microscopy and dynamic light scattering. The in vitro cytotoxicity and cellular uptake against MDA-MB-231 cancer cells were evaluated by confocal laser scanning microscopy and MTT assay. The results show a decrease in the average size of micelles upon an increase in the hydrophilic/hydrophobic block ratio. The DOX-loaded micelles are efficiently trapped by MDA-MB-231 cancer cells via receptor-mediated endocytosis and releass loaded DOX into the cells.