US5879713A
Expired / Lapsed
US
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Targeted delivery via biodegradable polymers
Assignee: Genzyme Corp
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Filing: 1997-01-23
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Granted: 1999-03-09
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Expires: 2017-01-23
Abstract
Abstract Delivery of bioactive molecules such as nucleic acid molecules encoding a protein can be significantly enhanced by immobilization of the bioactive molecule in a polymeric material adjacent to the cells where delivery is desired, where the bioactive molecule is encapsulated in a vehicle such as liposomes which facilitates transfer of the bioactive molecules into the targeted tissue. Targeting of the bioactive molecules can also be achieved by selection of an encapsulating medium of an appropriate size whereby the medium serves to deliver the molecules to a particular target. For example, encapsulation of nucleic acid molecules or biologically active proteins within biodegradable, biocompatible polymeric microparticles which are appropriate sized to infiltrate, but remain trapped within, the capillary beds and alveoli of the lungs can be used for targeted delivery to these regions of the body following administration to a patient by infusion or injection.
Inventors
- 👤 Laurence A. Roth
- 👤 Stephen Jack Herman
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 05:50
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K9/0024; A61K9/10; A61K9/127; A61P; A61P43/00
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
220 words
A method for delivery of biologically active molecules to a targeted site in the vascular system of an animal where treatment is needed, the method comprising selecting microparticles comprising a synthetic biodegradable polymer and biologically active molecules and having a diameter that causes the microparticles to lodge at the targeted site, wherein the diameter is between one and 100 microns and administering the microparticles to the animal so that the microparticles selectively lodge at the targeted site within the vascular system of the animal where release is desired for a sufficient amount of time to permit controlled release of a therapeutically effective amount of the biologically active molecules, wherein the biologically active molecules are selected from the group consisting of growth factors, cytokines, angiogenesis factors, immunosuppressant molecules, peptide fragments thereof, and nucleic acid constructs capable of synthesizing these compounds and wherein the synthetic polymer is biodegradable and is made from a polymerizable macromer having a solubility of at least about 1 g/100 ml in an aqueous solution comprising at least one water soluble region, at least one degradable region which is hydrolyzable under in vivo conditions, and free radical polymerizable end groups having the capacity to form additional covalent bonds resulting in macromer interlinking, wherein the polymerizable end groups are separated from each other by at least one degradable region.
Claim 2
Independent Claim
220 words
A method for delivery of biologically active molecules to a targeted site in the vascular system of an animal where treatment is needed, the method comprising selecting microparticles comprising a synthetic biodegradable polymer and biologically active molecules and having a diameter that causes the microparticles to lodge at the targeted site, wherein the diameter is between one and 100 microns and administering the microparticles to the animal so that the microparticles selectively lodge at the targeted site within the vascular system of the animal where release is desired for a sufficient amount of time to permit controlled release of a therapeutically effective amount of the biologically active molecules, wherein the biologically active molecules are selected from the group consisting of growth factors, cytokines, angiogenesis factors, immunosuppressant molecules, peptide fragments thereof, and nucleic acid constructs capable of synthesizing these compounds and wherein the synthetic polymer is biodegradable and is made from a polymerizable macromer having a solubility of at least about 1 g/100 ml in an aqueous solution comprising at least one water soluble region, at least one degradable region which is hydrolyzable under in vivo conditions, and free radical polymerizable end groups having the capacity to form additional covalent bonds resulting in macromer interlinking, wherein the polymerizable end groups are separated from each other by at least one degradable region.
Claim 3
Dependent Claim
38 words
The method of claim 1 wherein the microparticles are administered in a pharmaceutically acceptable carrier by a route of administration selected from the group consisting of intravenous, intraarterial, percutaneous, intramuscular, subcutaneous, direct lavage, aerosol, and via surgical incision.
Claim 4
Dependent Claim
22 words
The method of claim 1 wherein the microparticles are administered intravascularly and release the biologically active molecules after the microparticle selectively lodges.
Claim 5
Dependent Claim
65 words
The method of claim 1 wherein the targeted site is an area where vascularization or revascularization is needed, and wherein the growth factor is selected from the group consisting of vascular endothelial growth factor (VEGF), endothelial cell growth factor (ECGF), basic fibroblast growth factor (bFGF), bone morphogenic protein (BMP), platelet derived growth factor (PDGF), peptides thereof, and nucleic acid constructs capable of expressing the same.
Claim 6
Dependent Claim
15 words
The method of claim 1 wherein the route of administration of the composition is intravascular.
Claim 7
Dependent Claim
25 words
The method of claim 1 wherein the targeted site is an area of a blood vessel where abnormal accumulation of smooth muscle cells has occurred.
Claim 8
Dependent Claim
23 words
The method of claim 1 wherein the targeted site is an area of a blood vessel where restenosis has occurred following balloon angioplasty.
Claim 9
Dependent Claim
16 words
The method of claim 1 wherein the targeted site is an area where atherosclerosis has occurred.
Claim 10
Dependent Claim
16 words
The method of claim 8 wherein the atherosclerosis is present in the lower limbs causing claudication.
Claim 11
Dependent Claim
16 words
The method of claim 1 wherein the targeted site is an area where ischemia has occurred.
Claim 12
Dependent Claim
29 words
The method of claim 1, wherein the microparticles are administered into a region or organ so as to lodge or adhere at a locus within the region or organ.
Claim 13
Dependent Claim
15 words
The method of claim 1 wherein the microparticles are in the form of a hydrogel.
Claim 14
Dependent Claim
16 words
The method of claim 12, in which the hydrogel is composed predominantly of a polyalkylene oxide.
References Cited (Backward Citations)
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| 7.5 Years (Year 8) | 2006-03-08 | 2006-09-07 | 2007-03-09 | $3760.00 | Window Closed / Lapsed |
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