Biocompatible Dendritic Polypeptides for Delivery of Multiple Small-Molecule Therapeutics and siRNAs

Kibum Lee (Inventor), Prasad Subramaniam (Inventor), Dipti Barman (Inventor)

Research output: Innovation

Abstract

Invention Summary: Over the past decade, there has been a tremendous interest in the development of nanoparticle-based drug delivery systems. Among them, dendrimers and polypeptide-based systems have been the most prominent. Dendrimers have certain unique characteristics such as monodispersity, modifiable surface functionality, highly defined size and structure, and efficient cellular translation. However, the use of dendrimers is severely limited by their inherent toxicity and high immunogenicity. Polypeptides are generally biodegradable and biocompatible, but they require multistep synthetic processes or amplification. Polypeptides also have demonstrated limited success with the loading and effective release of multiple drugs. Further, micelles are formed only at high molecular weights, which lead to higher cytotoxicity and greater immune response. Rutgers scientists have synthesized a low-molecular-weight dendritic polypeptide-based carrier for the delivery of multiple therapeutics with synergistic therapeutic effects. The structure of the three-armed polypeptide can be accurately controlled, and conjugation of drugs can be done in a simple manner.Co-delivery of the histone deacetylase inhibitor (HDACi) SAHA and topoisomerase inhibitor Doxorubicin has been demonstrated in vitro to result in remarkable tumor cell killing. Its ability to deliver siRNAs is also tested in brain cancer cells. Overall, the ease of synthesis, biocompatibility, biodegradability and the ability to deliver multiple therapeutics to cells provides an attractive alternative over conventional drug delivery platforms. Market Applications: Delivery of multiple therapeutics including small molecules and nucleic acids for cancer and other diseases. Advantages: Ability to delivery multiple therapeutics for synergistic effect leading to potential reduction of drug dosage, side effects, and likelihood of drug resistance. Biodegradability High biocompatibility (low toxicity and immunogenicity) Ease of synthesis Intellectual Property & Development Status: US Patent 9,943,606. Available for licensing and/or research collaboration.
Original languageEnglish (US)
StatePublished - Jun 2019
Externally publishedYes

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