# US 2012/0070371 A1 · Low-Density Magnesium-Aluminum-Silicate (MAS) Microparticles for Radiotherapy and/or Radioimaging

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- Number: US 2012/0070371 A1
- Document ID: US20120070371A1
- Status: Published application
- Kind: A1
- Application number: 12/883,813
- Filed: 2010-09-16
- Published: 2012-03-22
- Earliest claimed: 2010-09-16
- Assignees: Mo-Sci Corporation
- Inventors: Delbert E. Day; Yiyong He
- Web page: https://patentgrep.com/patent/US20120070371A1

## CPC

- A61K 51/1255: {Granulates, agglomerates, microspheres}
- A61B 6/037: {Emission tomography}
- A61B 6/4057: {by using radiation sources located in the interior of the body (A61B6/037 takes precedence)}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 51/025: {inorganic Tc complexes or compounds}
- A61K 51/1244: {microparticles or nanoparticles, e.g. polymeric nanoparticles}
- A61N 5/1001: {using radiation sources introduced into or applied onto the body; brachytherapy}
- A61P 35/00: Antineoplastic agents
- A61N 2005/1021: {Radioactive fluid}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61B: DIAGNOSIS; SURGERY; IDENTIFICATION (usefulness limited to only animals A61D)
- A61N: ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY (measurement of bioelectric currents A61B; surgical instruments, devices or methods for transferring non-mechanical forms of energy to or from the body A61B18/00; anaesthetic apparatus in general A61M; incandescent lamps H01K; infrared radiators for heating H05B)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

This invention relates to low density radioactive magnesium-aluminum-silicate (MAS) microparticles that contain either samarium-yttrium, samarium, or lutetium as medical isotopes for radiotherapy and/or radioimaging.

## Claims

### Claim 1

A radioactive low density microsphere for radiation therapy of a mammal comprising a biologically compatible magnesium-alumina-silicate glass microparticle having a density of about 3.0 g/ml or less, a size range from about 20-40 um, said microparticle containing at least one beta or gamma radiation emitting isotope distributed substantially throughout the MAS glass which emits a therapeutic intensity and amount of beta or gamma radiation, and a balance of elements selected from the group consisting of elements that do not become radioactive upon neutron irradiation and elements that have a half-like that is sufficiently short so that the elements do not emit a significant amount of beta or gamma radiation at the time of administration, the microsphere having a chemical durability such that subsequent to administration of the microsphere to the mammal, the microsphere will not release a significant amount of the radiation emitting radioisotope into the mammal's system.

### Claim 2 (depends on 1)

The radioactive low density microsphere of claim 1, wherein the isotope is at least one medical isotope selected from the group consisting of Samarium-153, Yttrium-90, and Lutetium-177.

### Claim 3 (depends on 1)

The radioactive low density microsphere of claim 1, wherein the isotope is a combination of Samarium-153 and Yttrium-90.

### Claim 4 (depends on 1)

The radioactive low density microsphere of claim 1, wherein the density is about 2.8 g/ml or less.

### Claim 5 (depends on 1)

The radioactive low density microsphere of claim 1, wherein the isotope is 90Y (Yttrium-90) and has specific activity of 162 mCi per 107 microparticles for therapy.

### Claim 6 (depends on 5)

The radioactive low density microsphere of claim 5, further comprising a second radiation emitting isotope consisting of177Lu (Lutetium-177), wherein the 177Lu has specific activity of 32 mCi per 107 microparticles for imaging.

### Claim 7 (depends on 5)

The radioactive low density microsphere of claim 5, further comprising a second radiation emitting isotope consisting of 153Sm (Samarium-153), wherein the 153Sm has a specific activity of 12 mCi per 250,000 microparticles for imaging.

### Claim 8 (depends on 1)

A method of administering radioactive magnesium-alumina-silicate glass microparticles to a patient in need thereof, comprising delivering by catheter to an artery that feeds an organ or a tumor of a patient a composition comprising the radioactive low density microspheres of claim 1, and a physiologically acceptable carrier.

### Claim 9 (depends on 8)

The method of claim 8, further comprising wherein the isotope is a combination of samarium-153 and yttrium-90.

### Claim 10 (depends on 8)

The method of claim 8, further comprising wherein the isotope is lutetium-177.

### Claim 11 (depends on 8)

The method of claim 8, further comprising wherein the isotope is samarium-153.

### Claim 12 (depends on 8)

The method of claim 8, further comprising wherein the magnesium-alumina-silicate glass is a composition having an approximate chemical formula of 2(MgO)-2(Al2O3)-5(SiO2).

### Claim 13 (depends on 8)

The method of claim 8, further comprising wherein the aluminum-magnesium-silica glass core has the approximate weight percent ranges of magnesium-alumina-silicate glass comprising: MgO 8-14%; Al2O3 32-35%; and SiO2 47-52%.

### Claim 14 (depends on 8)

The method of claim 8, wherein the organ or tumor is selected from the group consisting of liver, spleen, brain, kidney, head & neck, uterine, and prostate.

### Claim 15

A method of obtaining a radiologic image of a patient's organ, comprising administering by catheter to an artery that feeds an organ of a patient a composition containing radioactive magnesium-alumina-silicate glass microparticles that contain samarium-153 or lutetium-177 as the medical isotope in a physiologically acceptable carrier, and obtaining the radiologic image of the patient's organ by capturing the radiation emitted by the samarium-153 or lutetium-177 using a suitable radionuclide imaging technique.

### Claim 16 (depends on 15)

The method of claim 15, further comprising wherein the radionuclide imaging technique is single photon emission computed tomography (SPECT).

### Claim 17 (depends on 15)

The method of claim 15, wherein the organ or tumor is selected from the group consisting of liver, spleen, brain, kidney, head & neck, uterine, and prostate.

### Claim 18

A method of administering radioactive magnesium-alumina-silicate glass microparticles that contain both samarium-153 as a radiodiagnostic medical isotope and yttrium-90 as a radiotherapeutic medical isotope to a patient in need thereof, comprising delivering by catheter to the hepatic artery of a patient a composition comprising radioactive magnesium-alumina-silicate glass microparticles that contain a radiodiagnostic amount of samarium-153 and a radiotherapeutic amount of yttrium-90, and a physiologically acceptable carrier, wherein the magnesium-alumina-silicate glass microparticles are about 25 to about 38 um in diameter.