Doxorubicin-loaded polymeric nanoparticles containing ketoester-based block and cholesterol moiety as specific vehicles to fight estrogen-dependent breast cancer.

The presented research concerns the preparation of polymer nanoparticles (PNPs) for the delivery of doxorubicin. Several block and statistical copolymers, composed of ketoester derivative, N-isopropylacrylamide, and cholesterol, were synthesized. In the nanoprecipitation process, doxorubicin (DOX) molecules were kept in spatial polymeric systems. DOX-loaded PNPs show high efficacy against estrogen-dependent MCF-7 breast cancer cell lines despite low doses of DOX applied and good compatibility with normal cells. Research confirms the effect of PNPs on the degradation of the biological membrane, and the accumulation of reactive oxygen species (ROS), and the ability to cell cycle arrest are strictly linked to cell death. Highlights: DDS based on cholesterol, ketoester, and NIPAAm, designed for the delivery of DOX. The ketoester and arrangement of blocks are crucial for anticancer activity. PNPs not only act as transporters but also sensitize the cell to DOX. High cytotoxicity of DOX-loaded PNPs was achieved despite low doses of the drug. PNPs have the proper size, shape, and ζ potential for efficient drug delivery. [ABSTRACT FROM AUTHOR]