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Details
Inventors: Liu, Daniel;
Assignee: Quadra Logic Technologies Inc. (Vancouver, CA)
Primary Examiner: Raymond; Richard L.
Assistant Examiner:
Attorney, Agent or Firm: Irell & Manella

Porphyrin-type photosensitizers useful in photodynamic therapy can be formulated as water soluble drugs by conjugation of the photosensitizer to a hydrophilic polymer. Conjugation of the photosensitizer in varying ratios to the polymer, such as polyvinyl alcohol, provides compositions which are readily soluble and biodistribute in a fashion equal to or advantageous over that obtained when the photosensitizer is administered alone. In addition, these conjugates which further a contain target specific component provide a mechanism for homing to the desired target tissue, as well as offering a convenient approach to including both target specific component and photosensitizing drug in the same complex.

DETAILED DESCRIPTION I claim: 1.
A pharmaceutical composition useful for photodynamic therapy which composition contains, as active ingredient, a conjugate of a porphyrin-type photosensitizer with a hydrophilic, water soluble, multifunctional polymeric carrier, wherein the ratio of photosensitizer to carrier is 1:1 to 500:1.
2.
The pharmaceutical composition of claim 1 wherein said multifunctional polymeric carrier contains a multiplicity of amino or hydroxyl groups.
3.
The composition of claim 2 wherein said carrier is selected from the group consisting of a polysaccharide, polyallylamine, polyvinyl alcohol, and an esterified polyacrylate.
4.
The composition of claim 1 wherein the carrier is a polyvinyl alcohol.
5.
The composition of claim 1 wherein the porphyrin-type photosensitizer comprises a green porphyrin of formulas 1-6 of FIG.
1 wherein each R.
sup.
1 and R.
sup.
2 is independently selected from the group consisting of carbalkoxy (2-6C), alkyl (1-6C) sulfonyl, aryl (6-10C) sulfonyl, cyano, and --CONR.
sup.
5 CO-- wherein R.
sup.
5 is aryl (6-10C) or alkyl (1-6C); and wherein each R.
sup.
3 is lower alkyl (1-4C) or w-carboxalkyl (2-6C) or the esters or amides thereof.
6.
The composition of claim 5 wherein the green porphyrin is of formula 3 or 5 in FIG.
1 and wherein each R.
sup.
1 and R.
sup.
2 is independently carbalkoxy (2-6C) and each R.
sup.
3 is carbalkoxyethyl or carboxyethyl.
7.
The composition of claim 1 wherein the porphyrin-type photosensitizer is a mixture of porphyrins containing dihematoporphyrin ether.
8.
The composition of claim 1 wherein the ratio of photosensitizer to carrier is 10:1-75:1.
9.
The composition of claim 4 wherein the PVA has a molecular weight of .
about.
10,000 and the ratio of photosensitizer to PVA is 75:1-10:1.
10.
The composition of claim 1 wherein said conjugate further contains a target specific component.
11.
The composition of claim 10 wherein the ratio of target specific component to carrier is between about 5:1-1:1.
12.
The composition of claim 10 wherein said target specific component is an immunoglobulin or an immunoreactive fragment thereof



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