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AssigneeAlkermes Controlled Therapeutics, Inc.
InventorsMark Tracy, David Scher
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The present invention relates to a sustained release composition for the targeted delivery of biologically active agents to specific tissues and cells. The composition comprises microparticles containing a biocompatible polymer, a water-soluble polymer and a biologically active agent. In one embodiment, the biologically active agent is an antigen or an immunomodulator. In another embodiment, the biologically is a labile agent. The microparticles have a number median diameter of greater than 20 microns upon administration. The water-soluble polymer is present in the sustained released composition in at least about 20% of the dry weight of the microparticle. the sustained release composition provides for the dissolution of the water-soluble polymer of the composition upon hydration, at a much greater rate than the degradation of the biocompatible polymer. This variance is solubility generates pseudo-microparticles which have a number median diameter which is substantially smaller than the size of the administered microparticles. The pseudo-microparticles can be engulfed by antigen presenting cells of the immune system, or absorbed by the Peyer's patches in the gut.
A method for stimulating a systemic immune response to an antigen in a mammal comprising administering to the mammal an effective amount of a sustained release composition comprising microparticles containing an antigen, a biocompatible polymer, and a water soluble polymer wherein, the microparticles have a number median diameter of greater than 20 microns, the water soluble polymer represents at least about 20% of the dry weight of the microparticles and the microparticles generate pseudo-microparticles upon hydration whereby sufficient pseudo-microparticles are taken up by antigen presenting cells to stimulate a systemic immune response.
A method for the systemic delivery of an effective amount of a labile agent to a mammal comprising orally administering to the mammal an effective amount of a sustained release composition comprising microparticles containing a labile agent, a biocompatible polymer, and a water soluble polymer wherein, the microparticles have a number median diameter of greater than 20 microns, the water soluble polymer represents at least about 20% of the dry weight of the microparticles and the microparticles generate pseudo-microparticles upon hydration, whereby sufficient pseudo-microparticles are absorbed into the Peyer's patches of the gastrointestinal tract.
A method for modulating an immune response in a mammal comprising administering to the mammal an effective amount of a sustained release composition comprising microparticles containing an immunomodulator, a biocompatible polymer, and a water soluble polymer wherein, the microparticles have a number median diameter of greater than 20 microns, the water soluble polymer represents at least about 20% of the dry weight of the microparticles and the microparticles generate pseudo-microparticles upon hydration whereby sufficient pseudo-microparticles are taken up by antigen presenting cells to modulate an immune response.
A sustained release composition for administration to a mammal capable of stimulating a systemic immune response comprising an effective amount of microparticles containing an antigen, a biocompatible polymer, and a water soluble polymer wherein, the microparticles have a number median diameter of greater than 20 microns upon administration, the water soluble polymer represents at least about 20% of the dry weight of the microparticles and the microparticles generate pseudo-micropaticles upon hydration having a number median diameter of less than about 20 microns.
The sustained release composition of claim 71 wherein the poloxamer is poloxamer 188, poloxamer 407 or any combination thereof.
The sustained release composition of claim 73 wherein the polysorbate is polysorbate 80, polysorbate 20 or any combination thereof.
A sustained release composition for oral administration to a mammal capable of delivering an effective amount of a labile agent comprising an effective amount of microparticles containing a labile agent, a biocompatible polymer, and a water soluble polymer wherein, the microparticles have a number median diameter of greater than 20 microns upon administration, the water soluble polymer represents at least about 20% of the dry weight of the microparticles and the microparticles hydrate in vivo to generate pseudo-micropaticles having a number median diameter of less than about 20 microns.
Dependencies are inferred from the claim text.