Self-Assembling Nanoparticles Composed of Transmembrane Peptides and Their Application for Specific Intra-Tumor Delivery of Anti
Posted Apr 30 2007 5:00pm
Description of Invention: The current invention discloses peptide based nanoparticles as an alternative to liposomes. The nanoparticles have a diameter of 8-10 nm and are much smaller than a liposome thus providing better tumor penetration. Peptides corresponding to transmembrane domains of a number of integral membrane proteins have been discovered that spontaneously self-assemble in aqueous solutions into stable and remarkably uniform nanoparticles. The nanoparticles of the current invention are fully synthetic, and their surfaces can be functionalized with ligands that provide specific binding to cell surface receptors overexpressed on tumor cells. Thus, they are even more specific for tumor targeting.
Nanoparticles constructed from transmembrane domains of certain receptors and transporters have biological activity of their own and inhibit metastasis or drug resistance thus sensitizing tumors to therapy. Hydrophobic drugs can be easily entrapped inside the nanoparticles, which not only solve the problem of drug insolubility under physiological conditions, but also generate a form of a drug that concentrates in tumors due to enhanced permeability and retention (EPR) effects.
Applications:
Self-assembling nano-particles as an alternative to liposomes, inorganic, dendrimeric or polymeric nanoparticles.
Nanoparticles have biological activity of their own and can inhibit metastasis (CXCR4 receptor antagonists) or drug resistance (inhibitors of ABCG2 transporter and p-glycoprotein) thus sensitizing tumors to therapy.
Advantages:
The nanoparticles are superior in stability, uniformity, ease and reproducibility of preparation compared to conventional liposomes, are much more uniform and less toxic than inorganic, polymeric or dendrimeric nanoparticles.
The nanoparticles are much smaller than a liposome thus providing better tumor penetration.
Synthetic nanoparticles can be easily coated with receptor ligands and loaded with hydrophobic drugs for more specific tumor targeting.
Development Status: The technology is in the pre-clinical stage of development.
NI Tarasova et al. Transmembrane inhibitors of P-glycoprotein, an ABC transporter. J Med Chem. 2005 Jun 2;48(11):3768-3775. [ PubMed abs ]
Licensing Status: Available for exclusive and non-exclusive licensing.
Collaborative Research Opportunity: The NCI Center for Cancer Research is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize self-assembling nanoparticles with intrinsic anti-tumor activity. Please contact John D. Hewes, Ph.D. at 301-435-3121 or hewesj@mail.nih.gov for more information.
Portfolios: Cancer Cancer - Other Nanotechnology
For Additional Information Please Contact: Jennifer Wong NIH Office of Technology Transfer 6011 Executive Blvd. Suite 325, Rockville, MD 20852 United States Email: wongje@mail.nih.gov Phone: 301-435-4633 Fax: 301-402-0220
Description of Invention:
The current invention discloses peptide based nanoparticles as an alternative to liposomes. The nanoparticles have a diameter of 8-10 nm and are much smaller than a liposome thus providing better tumor penetration. Peptides corresponding to transmembrane domains of a number of integral membrane proteins have been discovered that spontaneously self-assemble in aqueous solutions into stable and remarkably uniform nanoparticles. The nanoparticles of the current invention are fully synthetic, and their surfaces can be functionalized with ligands that provide specific binding to cell surface receptors overexpressed on tumor cells. Thus, they are even more specific for tumor targeting.
Nanoparticles constructed from transmembrane domains of certain receptors and transporters have biological activity of their own and inhibit metastasis or drug resistance thus sensitizing tumors to therapy. Hydrophobic drugs can be easily entrapped inside the nanoparticles, which not only solve the problem of drug insolubility under physiological conditions, but also generate a form of a drug that concentrates in tumors due to enhanced permeability and retention (EPR) effects.
Applications:
Advantages:
Development Status:
The technology is in the pre-clinical stage of development.
Inventors:
Nadya I Tarasova (NCI)
Patent Status:
HHS, Reference No. E-256-2006/0
US, Application No. 12/513,950 filed 07 May 2009
Relevant Publication:
Licensing Status:
Available for exclusive and non-exclusive licensing.
Collaborative Research Opportunity:
The NCI Center for Cancer Research is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize self-assembling nanoparticles with intrinsic anti-tumor activity. Please contact John D. Hewes, Ph.D. at 301-435-3121 or hewesj@mail.nih.gov for more information.
Portfolios:
Cancer
Cancer - Other
Nanotechnology
For Additional Information Please Contact:
Jennifer Wong
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Email: wongje@mail.nih.gov
Phone: 301-435-4633
Fax: 301-402-0220
Ref No: 1537
Updated: 05/2007