Therapeutic Nanoparticles Comprising a Therapeutic Agent and Methods of Making and Using Same
AssigneeBIND Therapeutics, Inc.
InventorsMaria Figueiredo, Erick Peeke, David Dewitt, Christina Van Geen Hoven, Greg Troiano, James Wright, Young-Ho Song, Hong Wang
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Abstract
The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid, a basic therapeutic agent having a protonatable nitrogen, and a polymer. Other aspects include methods of making and using such nanoparticles.
Claims44
A therapeutic nanoparticle comprising:
- about 0.05 to about 30 weight percent of a substantially hydrophobic acid;
- about 0.2 to about 20 weight percent of a basic therapeutic agent having a protonatable nitrogen;
- wherein the pKa of the basic therapeutic agent is at least about 1.0 pKa units greater than the pKa of the hydrophobic acid;
- and
- about 50 to about 99.75 weight percent of a diblock poly(lactic) acid-poly(ethylene)glycol copolymer or a diblock poly(lactic acid-co-glycolic acid)-poly(ethylene)glycol copolymer, wherein the therapeutic nanoparticle comprises about 10 to about 30 weight percent poly(ethylene)glycol.
A therapeutic nanoparticle comprising:
- a substantially hydrophobic acid, wherein the molar ratio of the substantially hydrophobic acid to the basic therapeutic agent is about 0.25:1 to about 2:1;
- about 0.2 to about 20 weight percent of a basic therapeutic agent having a protonatable nitrogen;
- wherein the pKa of the basic therapeutic agent is at least about 1.0 pKa units greater than the pKa of the hydrophobic acid;
- and
- about 50 to about 99.75 weight percent of a diblock poly(lactic) acid-poly(ethylene)glycol copolymer or a diblock poly(lactic acid-co-glycolic acid)-poly(ethylene)glycol copolymer, wherein the therapeutic nanoparticle comprises about 10 to about 30 weight percent poly(ethylene)glycol.
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A therapeutic nanoparticle comprising:
- a hydrophobic ion-pair comprising a substantially hydrophobic acid and a therapeutic agent having at least one ionizable amine moiety;
- wherein difference between the pKa of the basic therapeutic agent and the hydrophobic acid is at least about 1.0 pKa units;
- and
- about 50 to about 99.75 weight percent of a diblock poly(lactic) acid-poly(ethylene)glycol copolymer, wherein the poly(lactic) acid-poly(ethylene)glycol copolymer has a number average molecular weight of about 15 kDa to about 20 kDa poly(lactic acid) and a number average molecular weight of about 4 kDa to about 6 kDa poly(ethylene)glycol.
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A therapeutic nanoparticle prepared by:
- emulsification of a first organic phase comprising a first polymer, a basic therapeutic agent having a protonatable nitrogen, and a substantially hydrophobic acid, thereby forming an emulsion phase;
- quenching of the emulsion phase thereby forming a quenched phase;
- and
- filtration of the quenched phase to recover the therapeutic nanoparticles.
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Dependencies are inferred from the claim text.