Self-Assembly of Therapeutic-Agent Nanostructures

An improved delivery mechanism has been developed for hydrophobic drugs such as camptothecin which will increase chemotherapeutic efficacy.

The Need

Many cancer therapeutics exhibit extremely toxic side effects or have limited efficacy due to low bio-availability. Existing drug delivery technologies can add excessive mass to the therapeutic, grossly expanding the dosage necessary for response. Camptothecin (CPT) is a naturally occurring compound which has chemotherapeutic applications. However, clinical trials utilizing CPT are limited by several of the compound's properties. CPT is highly insoluble in aqueous solutions and is hydrolytically unstable in blood due to its affinity to bind to the human serum protein albumin, which increases equilibrium concentration of the toxic carboxylate form. CPT is poorly absorbed by cancerous cells after oral or intravenous ingestion, which means that large doses must be administered with deleterious side effects for the patient. To optimize CPT's chemotherapeutic effects on cancerous cells and minimize these negative, synthetic CPT derivatives must circumvent such molecular behaviors of unmodified CPT.

The Technology

Dr. Parquette and his team of researchers at The Ohio State University developed a novel method in which peptides self-assemble into well-defined nanotubes and nanofibers.

  • CPT-peptide assemblies tested in vitro were more effective at killing human colorectal cancer cells than clinically used Irinotecan drug, at lower concentrations
  • Improved water solubility for intravenous clinical treatments
  • Greater lactone stability and decreased cytotoxicity in comparison to unmodified CPT
  • Efficacy at lower doses, resulting in less toxicity to the patient

Commercial Applications

  • Pharmaceuticals
    • Cancer Therapy

Benefits/ Advantages

  • Potential for tumor targeting due to nanometer dimensions
  • High drug loadings possible
  • Increased ability to induce cell death of human colorectal cells
  • Greater hydrolytic stability in PBS


Patent # Title Country
10098967 Self-Assembly of Therapeutic Agent-Peptide Nanostructures United States of America

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