Nanotechnology-based medicine (Nanomedicine) has received progressive interest for the treatment of intractable diseases, such as cancer, as well as for the non-invasive diagnosis through various imaging modalities. Engineered polymeric nanosystems with smart functions play a key role in nanomedicine as drug carriers, gene vectors, and imaging probes. This presentation focuses present status and future trends of self-assembled nanosystems from block copolymers for the therapy and the non-invasive diagnosis of intractable diseases.<br/>Nanosystems with 10 to 100 nm in size can be prepared by programmed self-assembly of block copolymers in aqueous entity. Most typical example is polymeric micelles with distinctive core-shell architecture. Several micellar formulations of antitumor drugs have been intensively studied in preclinical and clinical trials, and their utility has been demonstrated. Compared with conventional formulations, such as liposomes, polymeric micelles have several advantages, including controlled drug release, tissue penetrating ability and stimuli-sensitivity. The development of smart polymeric micelles that dynamically change their properties due to sensitivity to chemical or physical stimuli is the most promising trend toward nanomedicines, directing to the targeting therapy with high efficacy and ensured safety. Notable anti-tumor efficacy against intractable and metastatic cancer, including pancreatic and brain cancers, of antitumor drug-incorporated polymeric micelles with pH-responding property was demonstrated to emphasize a promising utility of nanomedicines for cancer treatment.<br/>Versatility in drug incorporation is another feasibility of polymeric micelles. Polymeric micelles loaded with siRNA and mRNA have been successfully formulated with relevant properties for nanotherapeutics. Furthermore, loading of imaging reagents makes polymeric micelles with theranostic functions. Appealing enough, our recent result revealed that by installing proper ligands polymeric micelles can effectively crossing the blood-brain barrier to send various therapeutic compounds directly into neural cells in brain parenchyma.

Self-assembled supramolecular nanosystems for smart diagnosis and targeted therapy of intractable diseases

253rd National Meeting (2017)

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