Methods for micronization of hydrophobic drugs

A method for micronizing a hydrophobic agent, comprising:

• dissolving a hydrophobic agent in an effective amount of a first solvent, with a polymer, wherein the hydrophobic agent and the first solvent form a mixture having a continuous phase, introducing a second solvent into the mixture, and introducing an aqueous solution into the mixture wherein the aqueous solution causes precipitation of the hydrophobic agent to produce a composition of micronized hydrophobic agent having an average particle size of 1 micron or less.

A composition, comprising a preparation of micronized hydrophobic agent having an average particle size of less than 1 micron, wherein the preparation is composed of less than 5% polymer carrier and is free of surfactant.

A composition, comprising a preparation of micronized hydrophobic agent having an average particle size of less than 1 micron, wherein the preparation is free of polymer carrier and wherein the crystallinity of the micronized hydrophobic agent is at least 50% of the crystallinity of the non-micronized hydrophobic agent.

A method for delivering an agent to a subject, comprising:

• orally administering a solid preparation of micronized hydrophobic agent having an average particle size of less than 1 micron, wherein the preparation is composed of less than 5% polymer and is free of surfactant.

A method for delivering an agent to a subject, comprising:

• administering microparticles of a micronized hydrophobic agent encapsulated by phase inversion nanoencapsulation having an average particle size of less than 1 micron, wherein the preparation is composed of less than 5% polymer and is free of surfactant.

A method for achieving 100% bioactivity comprising:

• orally administering to the subject a solid preparation of micronized hydrophobic agent having an average particle size of less than 1 micron and wherein 100% of the orally administered agent is bioactive.