Compositions and associated methods for radioisotope-binding microparticles
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Publication Number
US-9687573-B2
Publication Date
2017-06-27
Expiration Date
Abstract
The present disclosure relates to polymeric materials that may be labeled with a radioisotope, to processes for producing the labeled polymeric material, and to methods of using the materials in analytical and therapeutic applications. Specifically, the disclosure relates to injectable and implantable microparticles, such as microspheres, which are associated with radioisotopes such that the microparticles are both therapeutic and detectable. The radioisotope-containing microparticles are useful for embolization and other therapeutic medical applications.
Core Innovation
The disclosure describes substantially spherical microspheres and microparticles comprising hydrophilic, non-biodegradable polymeric material with a chelating agent configured to chelate a radioisotope. The polymeric material is provided in polymerized form using one or more polymerized acrylate, acrylamide, acrylic, or vinyl monomers, and the chelating agent is polymerized with the polymerized monomers so that it is incorporated into the polymeric matrix of the microsphere or microparticle.
The chelating agent is defined by a compound of Formula I, and the disclosure further describes additional chelating-agent classes and groups that can be included, including mercaptoacetyltriglycine and derivatives, EDTA and derivatives, DOTA derivatives, crown ether derivatives, iminodiacetic acid, and aminocarboxylic acids such as alkylenediamine-N,N,N',N'-tetraacetic acid-(meth)acrylamide (MAM-EDTA), among others. The chelating agent is configured to chelate a radioisotope and is associated with the polymeric material.
The radioisotope is associated with the chelating agent to provide detectability and therapeutic vascular embolization, including gamma-photon emission and beta emission types. The disclosure identifies specific example radioisotopes associated with the microspheres and microparticles, including technetium-99m, indium-111, gallium-67, iodine-131, holmium-166, rhenium-188, and rhenium-186.
Claims Coverage
The independent claims are clm-00001, clm-00010, and clm-00016. Across these claims, the inventive coverage focuses on two inventive features: hydrophilic, non-biodegradable polymeric microspheres or microparticles with polymerized chelating agents that chelate a radioisotope, including Formula I-defined chelating agents and specified chelating-group sets in Formula II for microparticles.
Hydrophilic non-biodegradable polymer microsphere with polymerized Formula I chelator
A substantially spherical microsphere comprising a hydrophilic and non-biodegradable polymeric material in microsphere form having a diameter ranging from about 1 micrometer to about 2000 micrometers, wherein the polymeric material comprises one or more polymerized acrylate, acrylamide, acrylic, or vinyl monomers; and a chelating agent polymerized with the one or more polymerized monomers, wherein the chelating agent is configured to chelate a radioisotope, and wherein the chelating agent comprises compound of Formula I.
Microparticle of Formula II with polymerized chelating group
A microparticle of Formula II where P is a hydrophilic and non-biodegradable polymer comprising a first polymerized monomer selected from at least one of acrylates, acrylamides, acrylics, vinyls, acetals, allyls, cellulosics, methacrylates, polyamides, polycarbonates, polyesters, polyimides, polyolefins, polyphosphates, polyurethanes, silicones, styrenics, and polysaccharides; X represents a chelating agent comprising Y-Z, wherein the chelating agent is polymerized with at least the first polymerized monomer to form the polymer, wherein the polymer is in the shape of a microparticle; Z is a chelating group selected from at least one of mercaptoacetyltriglycine and multiple named chelating groups; Y comprises a chain of between 1-18 non-hydrogen atoms independently selected from at least one of C, N, O or S; and M is a radioisotope.
Spherical microsphere with Formula I chelating agent and radioisotope
A substantially spherical microsphere comprising a hydrophilic and non-biodegradable polymeric material in microsphere form having a diameter ranging from about 1 micrometer to about 2000 micrometers, wherein the polymeric material comprises one or more polymerized monomers; a chelating agent polymerized with the one or more polymerized monomers, wherein the chelating agent is configured to chelate a radioisotope, and wherein the chelating agent comprises a compound of Formula I with n between 1 and 18 inclusive, Xa and Xb may independently be O, S or N, and R may be alkyl or H; and a radioisotope.
Across clm-00001, clm-00010, and clm-00016, the claims center on polymeric, hydrophilic, non-biodegradable microspheres or microparticles in microsphere form that contain a polymerized chelating agent configured to chelate and associate a radioisotope, including chelating agents defined by Formula I and, for microparticles, chelating-group selection and structure within Formula II.
Stated Advantages
Provides diagnostic/therapeutic detectability through association of radionuclides with the polymeric chelating agent.
Supports therapeutic vascular embolization via radioisotope-chelated microspheres.
Imaging signals are enabled, including gamma-photon emission and beta emission types.
Includes a radioisotope leaching limitation over time for the microsphere.
Documented Applications
Diagnostic/therapeutic use enabled by detectability of radionuclides associated with the polymeric microspheres and microparticles.
Therapeutic vascular embolization using the radioisotope-chelated microspheres.
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