Method of drug formulation based on increasing the affinity of active agents for crystalline microparticle surfaces

摘要

Methods are provided for promoting the adsorption of an active agent to microparticles by modifying the structural properties of the active agent in order to facilitate favorable association to the microparticle.

主权项

1. A process for preparing a drug delivery composition comprising an active agent and a crystalline diketopiperazine microparticle comprising the steps in the sequence set forth of:
i) providing an active agent solution comprising a protein, polypeptide or peptide active agent molecule and providing a preformed crystalline diketopiperazine microparticle in a suspension or powder; next ii) combining said active agent solution with said preformed crystalline diketopiperazine microparticle suspension or powder to form a fluid phase; and iii) then modifying the chemical potential of the active agent in the fluid phase; wherein said modifying step causes adsorption of said active agent onto a surface of said preformed crystalline diketopiperazine microparticle to provide a coating of said active agent on said preformed crystalline diketopiperazine microparticle.