International Business Machines Corporation

Agency for Science, Technology and Research

Universidad Del Pais Vasco/euskal Herriko Unibersitatea

Universidad Del París Vasco/euskal Herriko Unibertsitatea

Jeremy P K Tan

James L Hedrick

Yi Yan Yang

Amanda Catherine Engler

Daniel Joseph Coady

Victor W L Ng

Richard Anthony Dipietro

Julian M W Chan

Zhan-Yuin Ong

Haritz Sardon

Jeannette M Garcia

Kazuki Fukushima

Xiyu Ke

Nanoparticles comprise a drug, a first block polymer and a second block polymer. The first block polymer has a poly(ethylene oxide) (PEO) block and a polycarbonate block bearing a side chain aromatic nitrogen-containing heterocycle (N-heterocycle). The N-heterocycle can be in the form of a base, a hydrosalt of the base, a sulfobetaine adduct of the base, or a combination thereof. The second block polymer has a PEO block and a polycarbonate block bearing a side chain catechol group, which can be present as a catechol, oxidized form of a catechol, and/or a polymerized form of a catechol. The nanoparticles can be dispersed in water and are capable of controlled release of the drug.

Polycarbonates bearing aromatic N-heterocycles for drug delivery

A cationic star polymer is disclosed of the general formula (1): wherein w' is a positive number greater than or equal to 3, I&#x2032; is a dendritic polyester core covalently linked to w&#x2032; independent peripheral linear cationic polymer chains P&#x2032;. Each of the chains P&#x2032; comprises a cationic repeat unit comprising i) a backbone functional group selected from the group consisting of aliphatic carbonates, aliphatic esters, aliphatic carbamates, aliphatic ureas, aliphatic thiocarbamates, aliphatic dithiocarbonates, and combinations thereof, and ii) a side chain comprising a quaternary amine group. The quaternary amine group comprises a divalent methylene group directly covalently linked to i) a positive charged nitrogen and ii) an aromatic ring.

Cationic polymers for antimicrobial applications and delivery of bioactive materials

Antimicrobial cationic polymers having one or two cationic polycarbonate chains were prepared by organocatalyzed ring opening polymerization. One antimicrobial cationic polymer has a polymer chain consisting essentially of cationic carbonate repeat units linked to one or two end groups. The end groups can comprise a covalently bound form of biologically active compound such as cholesterol. Other antimicrobial cationic polymers have a random copolycarbonate chain comprising a minor mole fraction of hydrophobic repeat units bearing a covalently bound form of a vitamin E and/or vitamin D2. The cationic polymers exhibit high activity and selectivity against Gram-negative and Gram-positive microbes and fungi.

Antimicrobial cationic polycarbonates

Eight-membered ring cyclic carbonates comprising a ring nitrogen at position 6 (1,3,6-dioxazocan-2-ones) were prepared by reaction of precursor diols with active carbonates. The ring nitrogen is linked to a pendant group Y' via a methylene linking group. The cyclic carbonates undergo organocatalyzed ring opening polymerization to form an initial polycarbonate comprising a backbone tertiary amine group. Quaternization of the initial polycarbonates forms cationic polycarbonates comprising a positive-charged backbone quaternary nitrogen. The cationic polycarbonates can be potent antimicrobial agents.

1,3,6-dioxazocan-2-ones and antimicrobial cationic polycarbonates therefrom

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Singapore, Singapore

Jeremy P K Tan