Polycarbonates Bearing Aromatic N-Heterocycles for Drug Delivery

Strategic Insights -

A team of researchers has developed a new class of polycarbonates that can be used for drug delivery, according to a patent application published by the United States Patent and Trademark Office. The inventors have designed a nanoparticle system that incorporates polycarbonates bearing aromatic N-heterocycles, which can be used to deliver drugs in a controlled and targeted manner.

The patent application describes a system in which a drug is encapsulated within a nanoparticle composed of two block polymers. The first block polymer is a polycarbonate that contains an aromatic N-heterocycle, while the second block polymer is a polycarbonate that contains a catechol group. The two block polymers are linked through non-covalent interactions, allowing the nanoparticle to be dispersible in water and capable of controlled release of the drug.

The researchers have conducted a series of experiments to evaluate the toxicity and efficacy of the nanoparticle system. The results show that the system is non-toxic and capable of delivering the drug to target cells in a controlled manner.

Key Takeaways:

  • The nanoparticle system is composed of two block polymers, one containing an aromatic N-heterocycle and the other containing a catechol group.
  • The two block polymers are linked through non-covalent interactions, allowing the nanoparticle to be dispersible in water and capable of controlled release of the drug.
  • The system is non-toxic and capable of delivering the drug to target cells in a controlled manner.
  • The nanoparticle system shows promise for use in drug delivery applications, particularly for delivering hydrophobic drugs.
  • The system has been shown to be effective in delivering the drug Doxorubicin, which is commonly used in cancer chemotherapy.
  • The nanoparticle system has the potential to overcome the deficiencies of existing drug delivery systems, including unchecked particle growth and premature release of the drug.

Statistics:

  • The nanoparticle system is composed of two block polymers, each with a molecular weight of between 2,000 and 50,000.
  • The aromatic N-heterocycle in the first block polymer is present as a free base, hydrosalt, or sulfobetaine adduct.
  • The catechol group in the second block polymer is present as a free catechol or catechol ester.
  • The nanoparticle system has been shown to maintain its structure and function for up to 120 hours.
  • The system has been shown to release the drug Doxorubicin at a rate of approximately 10% per hour.
  • The nanoparticle system has been shown to be effective in delivering the drug to target cells in a controlled manner, with a cell viability of 80% or greater.

Sources:

  • Chan, Julian M. W.; Engler, Amanda C.; Hedrick, James L.; Ke, Xiyu; Ng, Victor W.L.; Sardon, Haritz; Tan, Jeremy P. K.; Yang, Yi Yan. Polycarbonates Bearing Aromatic N-Heterocycles for Drug Delivery. Filed December 5, 2013 and posted June 18, 2015. Patent URL: http://appft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&u=%2Fnetahtml%2FPTO%2Fsearch-adv.html&r=6264&p=126&f=G&l=50&d=PG01&S1=20150611.PD.&OS=PD/20150611&RS=PD/20150611

Note: The date on which the patent application was posted is June 18, 2015.