The purpose of this study was to assess and compare the in vivo stability, shelf stability, cargo protection and to control of drug loading and drug release profiles of polymeric drug delivery systems (DDSs) based on interfacially-engineered PEG-PCL block copolymers. These novel polymeric micelle DDSs were expected to safely transport the toxic chemotherapeutic drug docetaxel and selectively deliver it to the tumor site with an elevated percent of the injected dose reaching the solid tumors and eliciting enhanced tumor killing in an orthotopic model of triple negative breast cancer in female SCID mice. We will present experimental results confirming the efficiency of the novel polymeric micelles, together with structure-property relationships. Specifically, docetaxel was loaded in micelles using co-nanoprecipitation method. Encapsulation efficiency was evaluated using LC-MS while in vitro drug release profile was obtained in sink conditions and was evaluated via HPLC. The stability of the self-assembled nanosystems in blood serum, and in the tumor environment was determined via NMR, GPC, fluorescence spectroscopy and via DLS. Results to be presented confirmed that the engineered interface of the triblock copolymers allows simplification and better control of the DDS formulation and drug loading process, higher drug loading capacity, superior enzymatic stability en-route to tumor and a controlled, focused release of docetaxel into the tumors, translating into an efficient tumor growth control doubled by an excellent toxicity profile, as proved by in vivo results in experimental animals.<br/>

Self-assembled block copolymer micelles with tuned hydrolytic stability as efficient docetaxel delivery systems for breast cancer therapy

256th National Meeting (2018)

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