US5328678A
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Composition and method of use for liposome encapsulated compounds for neutron capture tumor therapy
Assignee: University of Missouri System
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Filing: 1992-12-28
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Granted: 1994-07-12
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Expires: 2012-12-28
Abstract
Abstract Liposomes with hyperosmotic concentration of compounds encapsulated therein are targeted to tumors for neutron capture therapy. The compounds have an element with a large neutron capture cross section and an isotope that emits alpha particles when bombarded with neutrons. A method employing such liposomes for neutron capture therapy is also described.
Inventors
- 👤 Gary Fujii
- 👤 Paul G. Schmidt
- 👤 Ronald C. Gamble
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 20:36
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/12; A61K51/1217; A61K51/1234; A61K41/00; A61K41/009; A61K41/0095; A61K9/00; A61K9/10; A61K9/127; A61K2121/00
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
79 words
Neutron capture therapy agents to deliver a compound to a tumor, comprising small unilamellar liposomes having an average diameter of from about 30 to about 200 nm, said liposomes encapsulating a compound at a concentration of greater than 250 mM, said compound containing an element which has a large neutron cross-section and is capable of forming an isotope which emits an alpha particle from within said liposomes when bombarded with neutrons, which liposomes are stable against leakage and destruction.
Claim 2
Dependent Claim
79 words
Neutron capture therapy agents to deliver a compound to a tumor, comprising small unilamellar liposomes having an average diameter of from about 30 to about 200 nm, said liposomes encapsulating a compound at a concentration of greater than 250 mM, said compound containing an element which has a large neutron cross-section and is capable of forming an isotope which emits an alpha particle from within said liposomes when bombarded with neutrons, which liposomes are stable against leakage and destruction.
Claim 3
Dependent Claim
22 words
The therapy agents of claim 1 wherein said liposomes are comprised of phospholipids having a phase transition temperature greater than 37° C.
Claim 4
Dependent Claim
12 words
The therapy agents of claim 2 wherein said phospholipid is distearoyl phosphatidylcholine.
Claim 5
Dependent Claim
13 words
The therapy agents of claim 1 wherein said compound is a boron compound.
Claim 6
Dependent Claim
19 words
The therapy agents of claim 4 wherein said boron compound contains at least 10 atoms of boron per molecule.
Claim 7
Dependent Claim
46 words
The therapy agents of claim 4 wherein said boron compound is selected from the group consisting of Na 2 B 10 H 10 , Na 2 B 12 H 12 , Na 2 B 12 H 11 SH, or Na 2 B 10 O 16 .
Claim 8
Dependent Claim
19 words
The therapy agents of claim 1 wherein said compound contains the elements 10 B, 235 U, or 6 Li.
Claim 9
Independent Claim
120 words
A method of neutron capture therapy treatment of a tumor comprising introducing into the bloodstream of a subject neutron capture therapy agents comprising small unilamellar liposomes having an average diameter of from about 30 to 200 nm, said liposomes encapsulating a compound at a concentration of greater than 250 mM, said compound containing an element (a) having a large neutron capture cross-section, and (b) being capable of forming an isotope which emits an alpha particle from within said liposomes when bombarded with neutrons, which liposomes are stable against leakage and destruction, and after a time to enable sufficient accumulation of said isotope in the tumor tissue, subjecting the subject to a source that emits neutrons effective for neutron capture therapy.
Claim 10
Independent Claim
120 words
A method of neutron capture therapy treatment of a tumor comprising introducing into the bloodstream of a subject neutron capture therapy agents comprising small unilamellar liposomes having an average diameter of from about 30 to 200 nm, said liposomes encapsulating a compound at a concentration of greater than 250 mM, said compound containing an element (a) having a large neutron capture cross-section, and (b) being capable of forming an isotope which emits an alpha particle from within said liposomes when bombarded with neutrons, which liposomes are stable against leakage and destruction, and after a time to enable sufficient accumulation of said isotope in the tumor tissue, subjecting the subject to a source that emits neutrons effective for neutron capture therapy.
Claim 11
Dependent Claim
12 words
The method of claim 8 wherein said compound is a boron compound.
Claim 12
Dependent Claim
29 words
The method of claim 9 wherein said boron compound is water soluble, has little or no charge at physiological pH, and has no or little toxicity to the subject.
Claim 13
Dependent Claim
34 words
Them method of claim 9 wherein said boron compound is encapsulated in a concentration sufficient to accumulate said isotope in the tumor at a concentration of about 10 μg/g to about 50 μg/g tumor.
Claim 14
Dependent Claim
21 words
The method of claim 8 wherein said liposomes are comprised of phospholipids having a phase transition temperature greater than 37° C.
Claim 15
Dependent Claim
11 words
The method of claim 12 wherein said phospholipid is distearoyl phosphatidylcholine.
Claim 16
Dependent Claim
18 words
The method of claim 9 wherein said boron compound contains at least 10 atoms of boron per molecule.
Claim 17
Dependent Claim
45 words
The method of claim 9 wherein said boron compound is selected from the group consisting of Na 2 B 10 H 10 , Na 2 B 12 H 12 , Na 2 B 12 H 11 SH, or Na 2 B 10 O 16 .
Claim 18
Dependent Claim
17 words
The method of claim 8 wherein said compound contains the elements 10 B, 235 U, 6 Li.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-07-11 | 1998-01-10 | 1998-07-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-07-11 | 2002-01-10 | 2002-07-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-07-11 | 2006-01-10 | 2006-07-12 | $7700.00 | Window Closed / Lapsed |