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US5389378A
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Benzoporphyrin vesicles and their use in photodynamic therapy
Assignee: Elan Pharmaceuticals LLC
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Filing: 1992-12-15
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Granted: 1995-02-14
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Expires: 2012-12-15
Abstract
Abstract This invention relates to benzoporphyrin containing vesicles which are suitable for pharmaceutical application. In particular, the present invention relates to a liposomal preparation of benzoporphyrin (BPD) incorporated into vesicles comprising a liposome forming lipid such as EPC or DMPC at a drug to lipid ratio of greater than 100 mu g/umole lipid which will allow adequate drug dosing with relatively low lipid concentration. In an additional aspect of the present invention, sized liposomes are described which are storage stable. Certain sized BPD-containing vesicles (no greater than about 120 nm in diameter) permit sterilization by terminal filtration. Further, a lyophilized preparation of the BPD-lipid mixture can be obtained from aqueous buffer under conditions which do not result in vesicle fusion/aggregation or BPD precipitation. Liposomes according to the present invention are able to accommodate surprisingly large amounts of BPD within the bilayer of the liposome, rather than in the encapsulated buffer. The advantages of this surprising aspect of the present invention includes the ease of manufacture and the cost savings associated with an efficient use of BPD are also presented.
Inventors
- 👤 Thomas D. Madden
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 04:11
CPC Classifications
A; A61; A61K; A61K41/00; A61K41/0057; A61K41/0071; A61K31/00; A61K31/33; A61K31/395; A61K31/40; A61K9/00; A61K9/10; A61K9/127; Y; Y10; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2984
Claims Analysis
Total Claims: 27
Claim 1
Independent Claim
71 words
A composition for treating cancerous tissue with photodynamic therapy consisting of a photosensitizing effective mount of a benzoporphyrin, which is not complexed to a metal, in liposomes, and a pharmaceutical carrier, wherein said benzoporphyrin is selected from the group consisting of benzoporphyrin monoacid A, monoacid B, diacid A, diacid B and mixtures thereof, and wherein said composition has a benzoporphyrin to lipid ratio greater than 100 μg benzoporphyrin per mole lipid.
Claim 2
Dependent Claim
71 words
A composition for treating cancerous tissue with photodynamic therapy consisting of a photosensitizing effective mount of a benzoporphyrin, which is not complexed to a metal, in liposomes, and a pharmaceutical carrier, wherein said benzoporphyrin is selected from the group consisting of benzoporphyrin monoacid A, monoacid B, diacid A, diacid B and mixtures thereof, and wherein said composition has a benzoporphyrin to lipid ratio greater than 100 μg benzoporphyrin per mole lipid.
Claim 3
Dependent Claim
13 words
The composition according to claim 1 wherein the benzoporphyrin is benzoporphyrin monoacid A.
Claim 4
Dependent Claim
19 words
The composition according to claim 1 wherein the components of said liposome comprise egg phosphatidyl choline or dimyristoylphosphatidyl choline.
Claim 5
Dependent Claim
11 words
The composition according to claim 1 wherein said liposomes are sized.
Claim 6
Dependent Claim
18 words
The composition according to claim 4 wherein said liposomes are no greater than about 120 nm in diameter.
Claim 7
Dependent Claim
17 words
The composition according to claim 1 wherein said benzoporphyrin is inserted substantially within bilayers of said liposomes.
Claim 8
Dependent Claim
12 words
The composition according to claim 1 wherein said liposomes are storage stable.
Claim 9
Dependent Claim
10 words
The composition according to claim 1 adapted for topical administration.
Claim 10
Dependent Claim
10 words
The composition according to claim 1 adapted for parenteral administration.
Claim 11
Dependent Claim
24 words
The composition according to claim 6 having a weight ratio of benzoporphyrin monoacid A to benzoporphyrin monoacid B of about 1:1 to about 4:1.
Claim 12
Dependent Claim
13 words
The composition according to claim 10 wherein the weight ratio is about 1:1.
Claim 13
Dependent Claim
16 words
The composition according to claim 2 wherein the components of the liposome comprise egg phosphatidyl choline.
Claim 14
Dependent Claim
19 words
The composition according to claim 1 wherein the benzoporphyrin is a mixture of benzoporphyrin monoacid A and monoacid B.
Claim 15
Independent Claim
80 words
A method for treating cancerous tissue using photodynamic therapy in a patient comprising administering to said patient a composition consisting of a photosensitizing effective amount of a benzoporphyrin, which is not complexed to a metal, in liposomes, and a pharmaceutical carrier, wherein said benzoporphyrin is selected from the group consisting of benzoporphyrin monoacid A, monoacid B, diacid A,-diacid B and mixtures thereof, and wherein said composition has a benzoporphyrin to lipid ratio greater than 100 μg benzoporphyrin per mole lipid.
Claim 16
Independent Claim
80 words
A method for treating cancerous tissue using photodynamic therapy in a patient comprising administering to said patient a composition consisting of a photosensitizing effective amount of a benzoporphyrin, which is not complexed to a metal, in liposomes, and a pharmaceutical carrier, wherein said benzoporphyrin is selected from the group consisting of benzoporphyrin monoacid A, monoacid B, diacid A,-diacid B and mixtures thereof, and wherein said composition has a benzoporphyrin to lipid ratio greater than 100 μg benzoporphyrin per mole lipid.
Claim 17
Dependent Claim
13 words
The method according to claim 14 wherein the benzoporphyrin is benzoporphyrin monoacid A.
Claim 18
Dependent Claim
19 words
The method according to claim 14 wherein the benzoporphyrin is a mixture of benzoporphyrin monoacid A and monoacid B.
Claim 19
Dependent Claim
19 words
The method according to claim 14 wherein the components of said liposome comprise egg phosphatidyl choline or dimyristoylphosphatidyl choline.
Claim 20
Dependent Claim
11 words
The method according to claim 14 wherein said liposomes are sized.
Claim 21
Dependent Claim
18 words
The method according to claim 18 wherein said liposomes are no greater than about 120 nm in diameter.
Claim 22
Dependent Claim
17 words
The method according to claim 14 wherein said benzoporphyrin is inserted substantially within bilayers of said liposomes.
Claim 23
Dependent Claim
12 words
The method according to claim 14 wherein said liposomes are storage stable.
Claim 24
Dependent Claim
10 words
The method according to claim 14 adapted for topical administration.
Claim 25
Dependent Claim
10 words
The method according to claim 14 adapted for parenteral administration.
Claim 26
Dependent Claim
27 words
The method according to claim 16 wherein the composition has a weight ratio of benzoporphyrin monoacid A to benzoporphyrin monoacid B of about 1:1 to about 4:1.
Claim 27
Dependent Claim
13 words
The method according to claim 24 wherein the weight ratio is about 1:1.
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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) | 1998-02-13 | 1998-08-15 | 1999-02-14 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2002-02-13 | 2002-08-15 | 2003-02-14 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2006-02-13 | 2006-08-15 | 2007-02-14 | $7700.00 | Window Closed / Lapsed |