Nanoparticle encapsulation to target g protein-coupled receptors in endosomes
AssigneeTakeda Pharmaceutical Company Limited
InventorsNigel Bunnett, Thomas Davis, Michael Whittaker, Nicholas Veldhuis
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Abstract
The present invention relates to methods for modulating endosomal GPCR signaling. In particular, the present invention relates to use of polymeric nanoparticles for the targeted delivery of hydrophobic modulators of endosomal GPCRs and their use in the treatment of associated diseases and disorder.
Claims30
An aqueous liquid comprising polymeric nanoparticles of copolymer chains assembled to form a core/shell structure, the copolymer chains having:
- (i) an acid-responsive hydrophobic polymer block that forms the core of the nanoparticles;
- and
- (ii) a hydrophilic polymer block that forms the shell of the nanoparticles and is solvated by the aqueous liquid,
- wherein the nanoparticles contain within their core a hydrophobic modulator of endosomal GPCR signaling, or a pharmaceutically acceptable salt thereof.
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An aqueous liquid comprising polymeric nanoparticles of copolymer chains assembled to form a core/shell structure, the copolymer chains having:
- (i) an acid-responsive hydrophobic polymer block that forms the core of the nanoparticles;
- and
- (ii) a hydrophilic polymer block that forms the shell of the nanoparticles and is solvated by the aqueous liquid,
- wherein the nanoparticles contain within their core:
- a) a first hydrophobic modulator of endosomal GPCR signaling, or a pharmaceutically acceptable salt thereof, and
- b) a second hydrophobic modulator of endosomal GPCR signaling, or a pharmaceutically acceptable salt thereof.
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Dependencies are inferred from the claim text.