Self-assembling Nanofibril Particles for Controlled Release of IV and SUBQ Therapeutics



    • Clinically approved methods for the controlled release of oral therapies have demonstrated their efficacy in reducing required dosage, administration frequency, and side effects, thereby boosting patient compliance. Despite these successes, no solution is available for the controlled release of intravenously and subcutaneously administered therapies.
    • The inventors synthesized copolymers composed of hydrophilic PEG and hydrophobic oligo(ethyl sulfide) (OES) blocks which self-assemble in aqueous solution to form two or three dimensional high aspect ratio nanofibril structures. Drug cargo can either be dissolved within the polymer, or covalently attached. The specific fibril structure and conditions that induce its disassembly can be tuned by altering the copolymer composition. 
    • The inventors injected various mouse models with the nanoparticles conjugated with fluorophore. They showed that the particles formed a depot at the injection site, are delivered to the lymph nodes via flow and cellular methods and are delivered to tumor tissue and tumor associated immune cells. This demonstration emphasizes the applicability of the invention in cancer therapeutics and vaccines. 



    In vivo proof-of-concept experiment showing that nanoparticles can either remain at the injection site and form a depot or target cargo to the lymph nodes depending on functionalization. Mice were injected with 100ug fluorescent nanoparticle with or without 10ug of Toll-like receptor ligand CpG-B. Only CpG-B conjugated nanoparticles targeted the lymph nodes and the unfunctionalized nanoparticles remained at the injection site.





    • Programmable release conditions
    • Programmable size and shape
    • More control over depot formation than standard formulations



    • Intravenous and subcutaneous drug formulation
    • Oncology therapeutics
    • Vaccines
    • Research tool (immunology, oncology, pharmacokinetics)


    • PCT/US2014/048009



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