Poly(phosphoester)s (PPEs) have the properties of functional adjustability, stealth effect, excellent biodegradability and biocompatibility to have the potential application in biomedical field. To meet more versatile and diverse biomedical applications, multi-arm star-shaped phosphoester copolymer was designed and prepared. Firstly, amphiphilic block copolymer poly(amido amine)-block-poly(2-butenyl phospholane)-block-poly(2-methoxy phospholane) conjugated with folic acid (abbreviated as PAMAM-PBEP-PMP-FA) was synthesized by organo-catalyzed living ring-opening polymerization (ROP) and post-modification. Supramolecular micelles formed by this copolymer via self-assembly exhibited good architectural stability, uniform spherical structures, efficient loading capacity and low protein adsorption in aqueous solution. Afterwards, in vitro drug release experiment showed that anticancer drugs doxorubicin (DOX) could be released from the micelles in a slow and sustained way in the environment of simulated intracellular lysosome (pH 5.0 with phosphodiesterase I). Subsequent research on cytotoxicity and cellular uptake showed that DOX also could enter tumor cells quickly by the enhanced permeability and retention (EPR) effect and FA receptor-medicated active targeting ability, and inhibit tumor cell growth effectively. Therefore, these supramolecular micelles based on multi-arm star-shaped phosphoester copolymers have great potential in controlled drug delivery for tumor treatment.

Supramolecular micelles based on multi-arm star-shaped phosphoester copolymers for controlled drug delivery

256th National Meeting (2018)

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