Loadable polymeric particles for therapeutic and/or diagnostic applications and methods of preparing and using the same

• US 9,511,153 B2
• Filed: 09/20/2012
• Issued: 12/06/2016
• Est. Priority Date: 10/25/2004
• Status: Active Grant

• Current Assignee: Varian Medical Systems Incorporated (Siemens AG)
• Original Assignee: CeloNova Biosciences Germany GmbH (Boston Scientific Corporation)
• Inventors: Harder, Philipp, Fritz, Olaf, Fritz, Ulf
• Primary Examiner(s): Dickinson, Paul
• Application Number:
  US13/623,151
• Publication Number:
  US 20130052142A1
• Time in Patent Office: 1,538 Days
• Field of Search: None
• US Class Current: 1/1
• CPC Class Codes: A61K 49/0404 containing barium sulfate
• CPC Class Codes: A61K 49/0419 Microparticles, microbeads, microcapsules, microspheres, i.e. having a size or diameter higher or equal to 1 micrometer
• CPC Class Codes: A61K 9/1641 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
• CPC Class Codes: A61K 9/1694 resulting in granules or microspheres of the matrix type containing more than 5% of excipient
• CPC Class Codes: A61K 9/5031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/5073 having two or more different coatings optionally including drug-containing subcoatings
• CPC Class Codes: A61K 9/5078 with drug-free core
• CPC Class Codes: A61K 9/5089 Processes
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid

Abstract

Particles are provided for use in therapeutic and/or diagnostic procedures. The particles include poly[bis(trifluoroethoxy)phosphazene] and/or a derivatives thereof which may be present throughout the particles or within an outer coating of the particles. The particles can also include a core having a hydrogel formed from an acrylic-based polymer. Barium sulfate may also be provided to the core of the particles as a coating or absorbed within the core of the particles. The particles can be used to minimize blood flow to mammalian tissues by occluding at least a portion of a blood vessel of the mammal, or to deliver an active agent to a localized area within a body of a mammal by contacting a localized area with at least one of the particles. Further, the particles are useful in sustained release formulations including active agent(s) for oral administration, as tracer particles for injection into the bloodstream of a mammal or for use in enhanced ultrasound imaging. The particles may include agents for increasing density for achieving useful buoyancy levels in suspension.

Claims

1. A method of tracing the passage of a particle through a blood vessel in a mammal, the method comprising injecting into the bloodstream of a mammal at least one tracer particle, the tracer particle comprising poly[bis(trifluoroethoxy)phosphazene] and/or a derivative thereof and a contrast agent, and imaging the route of the particle.

2. The method according to claim 1, wherein the tracer particle comprises a core and a coating surrounding the core, wherein the coating comprises poly[bis(trifluoroethoxy)phosphazene] and/or a derivative thereof and the core comprises an acrylic-based polymer hydrogel.

3. The method according to claim 2, wherein the particle core further comprises barium sulfate as coating and/or diffused within the core.

4. The method according to claim 1, wherein the contrast agent is selected from the group consisting of barium sulfate, tantalum compounds, gadolinium compounds and iodine-containing compounds.