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1. CA2653811 - FILMS AND PARTICLES

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[ EN ]
We Claim
1. An oligomer or polymer having a repeat unit represented by formula XX:
Wherein:
Q is selected from among O, S, Se or NH
G is selected from among the following structures:
R2 is selected from among hydrogen, a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, or fluorocarbon chain of 1-50 carbons, wherein each alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, or fluorocarbon chain is optionally substituted internally or terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono- or di-substituted amino, thiol, thioester, sulfate, phosphate, phosphonate, or halogen substituents;
R3 is selected from among hydrogen, methoxy, ethoxy, amino, a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, or arylalkyl chain of 1-10 carbons;
R4 R5 and R6 are each independently selected from among a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, or arylalkyl chain of 1- carbons; and
R7 and R8 are each independently selected from among hydrogen, a straight or branched alkyl, cycloalkyl, aryl, olefin, alkylaryl, or arylalkyl chain of 150 carbons, wherein each alkyl, cycloalkyl, aryl, olefin, alkylaryl or arylalkyl chain is optionally substituted internally or terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono- or di-substituted amino, thiol, thioester, sulfate, phosphate, phosphonate, or halogen-substituents.
2. The oligomer or polymer of claim 1, wherein the oligomer or polymer is represented by Formula XX':
Wherein: n is an integer from 2-750, and wherein each oligomeric or polymeric chain has
terminal group, the terminal goup being selected from among amined, thiols, amides, phosphates, sulphated, hydroxides, alkenes, and alkynes.
3. The oligomer or polymer of claim 1, wherein R2 is hydrogen or methyl.
4. The oligomer or polymer of claim 1, wherein Q is oxygen.
5. A composition comprising the oligomer or polymer of claim 1.
6. A polymer film or particle comprising an oligomer or polymer of claim 1.
7. A polymer particle of claim 6, comprising a microparticle or nanoparticle.
8. A polymeric particle of claim 7, wherein the particle has a diameter between about 2 nm and 1 micron.
9. The polymeric particle of claim 7 comprising a first volume at a first pH, and a second volume at a second pH, different from the from the first pH.
10. The polymeric particle of claim 9, wherein the second volume is 1X or more
greater than the first volume when the second pH is lower than the first pH.
11. The polymeric particle of claim 9, wherein the second volume is 4X or more
greater than the first volume when the second pH is lower the the first pH.
12. The polymeric particle of claim 9, wherein the second volume is 8X or more
greater than the first volume when the second pH is lower than the first pH.
13. The polymeric particle of claim 9, wherein the second volume is greater than the first volume and the change in volume is sufficient that the particle when within a cell during the volume change ruptures the cell or a cellular compartment.
14. The polymeric particle of claim 9, wherein the second volume is greater than the first volume and the change in volume is sufficient to cause the particle to become lodged, embedded, or immobilized in an anatomic location, such as a lymph node, airway, cavity, capillary, or other tissue.
15. The polymeric film or particle of claim 6, further comprising an agent.
16. The polymeric film or particle of claim 15, wherein the agent is a biologically active agent comprising one or more of an anti-cancer agent, an anti-biotic, an anti- neoplastic agent, an analgesic, an angiogenic, or an agent that promotes wound healing.
17. The polymeric film or particle of claim 15, wherein the biologically active agent comprise one or more of asparaginase; bleomycin; busulfan; capecitabine; carboplatin; carmustine; chlorambucil; cisplatin; cyclophosphamide; cytarabine; dacarbazine; dactinomycin; daunorubicin; dexrazoxane; docetaxel; doxorubicin; etoposide; floxuridine; fludarabine; fluorouracil; gemcitabine; hydrozyurea; idarubicin; ifosfamine; irinotecan; lomustine; mechlorethamine; melphalan; mercaptopurine;
methotrexate; mitomycin; mitotane; mitoxantrone; paclitaxel; pemetrexed; pentostatin; plicamycin; procarbazine; rituximab; streptozocin; teniposide; thioguamine; thiotepa; vinblastine; vincristine; and vinorelbine.
18. A method of using the particle of film of claim 6, the method comprising applying to one or more of the following: (i) a surgical resection margin, (ii) within a treated or untreated tumor or cavity, (iii) a target site of disease away from a surgical margin, and (iv) a lymph node.
19. The film of claim 6, wherein the film is a single layered film.
20. The film of claim 15, further comprising two or more layers to form a multi- layered film.
21. The film of claim 15, comprising a first layer comprising a first polymer of
Formula XX, and a second layer comprising a second polymer different from
Formula
XX.
22. The film of claim 21, wherein the second polymer comprises one or more of poly(lactic acid), poly(glycolic acid), poly(lactic-co-glycol acid), polycaprolactone, poly)trimethelene carbonate), polyester, polycarbonate, and polyamide.
23. An oligomer or polymer, or portion thereof, represented by Formula XXI,
XXII,
XXIII, XXIV, XXV, XXVI, XXVII, XXVIII, XXIX, XXX, XXXI, XXXII, XXXIII,
XXXIV, XXXV, XXXVI or XXXVII:
wherein:
Q' is independently selected from among O, S, Se or NH;
G', G1', and G2' are each independently selected from among the following structures:
or R1; wherein G1' and G2' are not the same;
R1' is selected from among a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, or fluorocarbon chain of 3-50 carbons, wherein each alkyl, cycloalkyl, aryl, olefin, silyl, alkysilyl, arylsilyl, alkylaryl, arylalkyl or fluorocarbon chain is optionally substituted internally or terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono- or di- substituents; or
R1' is selected from among poly(ethylene glycol), poly(ethylene oxide), poly(hydroxyacid)), a carbohydrate, a protein, a polypeptide, an amino acid, a nucleic acid, a nucleotide, a polynucleotide, any DNA or RNA segment, a lipid, a polysaccharide, and antibody, a pharmaceutical agent, or any epitope for a biological receptor; or
R1' is selected from among a photocrosslinkable or ionically crosslinkable group;
R2' is selected from among hydrogen, a straight or branched alkyl, cycloalkyl,
aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, or fluorocarbon chain of 1-50 carbons, wherein each alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, or fluorocarbon chain is optionally substituted internally or terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono- or di-substituted amino, thiol, thioester, sulfate, phosphate, phosphonate, or halogen substituents; x and y are each independently selected from an integer of 2-750; a is selected from an integer of 1-25; b is selected from an integer of 1-14;
c is selected from an integer of 1-14; and each polymeric terminal group is selected from among amines, thiols, amides, phosphated, sulphates, hydroxides, metals, alkanes, alkenes, and alkynes.
24. An oligomer or polymer, or portion thereof, presented by Formula XXXVIII:
wherein:
Q' is independently selected from among O, S, Se or NH;
G' is selected from among
R1' is selected from among a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, arylalkyl, or fluorocarbon chain of 3-50 carbons, wherein each alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, or fluorocarbon, chain is optionally substituted internally or terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono- or di- substituted amino, thiol, thioester, sulfate, phosphate, phosphonate, or halogen substituents; or
R1' is selected from among poly(ethylene glycol), poly(ethylene oxide), poly)hydroxyacid)), a carbohydrate, a protein, a polypeptide, an amino acid, a nucleic acid, a nucleotide, a polynucleotide, any DNA or RNA segment, a lipid, a polysaccharide, an antibody, pharmaceutical agent, or any epitope for a biological receptor; or
R1' is selected from among photocrosslinkable or ionically crosslinkable group; x and y are each independently selected from an integer of 2-750;
e is selected from an integer of 1-8; and each polymeric terminal group is selected from among amines, thiols, amides, phosphated, sulphates, hydroxides, metals, alkanes, alkenes and alkynes.
25. The oligomer or polymer of claim 24, wherein R1' is selected from among a straight or branched alkyl, cycloalkyl, aryl, olefin, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, or fluorocarbon chain of 3-50 carbons, wherein each alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, or fluorocarbon chain is optionally substituted internally of terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyseter, carboxiamide, amino, mono- or di-substituted amino, thiol, thioester, sulfate, phosphate, phosphonate, or halogen substituents.
26. The oligomer or polymer of claim 24, wherein R1' is selected from among a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, or fluorocarbon chain of 3-50 carbons.
27. The oligomer or polymer of claim 24, wherein R1' is selected from among a straight or branched alkyl chain of 3-50 carbons.
28. A polymeric film or particle comprising a polymer or claim 23 or 24.
29. A polymeric particle of claim 28, comprising a microparticle or nanoparticle.
30. A polymeric particle of claim 29, wherein the particle comprises a diameter of between about 1 nm and 2 microns.
31. A polymeric particle of claim 29, wherein the particle comprises a diameter between about 10 nm and 1 microns.
32. The polymeric film or particle of claim 28, further comprising an agent.
33. The polymeric film or particle of claim 32, wherein the agent is a biologically active agent comprising one or more of an anti-cancer, an anti-biotic, antineoplastic, an analgesic, and angiogenic, or agent that promotes healing.
34. The polymeric film or particle of claim 32, wherein the biologically active agent comprise one or more of asparaginase; bleomycin; busulfan; capecitabine; carboplatin; carmustine chlorambucil; cisplatin; cyclophosphamide; cytarabine; dacarbazine;
dactinomycin; daunorubicin; dexrazoxane; docetaxel; doxorubicin; etoposide; floxuridine; fludarabine; fluorouracil; gemcitabine; hydroxyurea; idarubicin; ifosfamide; irinotecan; lomustine; mechlorethamine; melphalan; mercaptopurine;
methotrexate; mitomycin; mitotane; mitoxantrone; paclitaxel; premetrexed, pentostatin; plicamycin; procarbazine; rituximab; streptozocin; teniposide; thioguanine; thiotepa; vinblastine; vincristine; and vinorelbine.
35. A method of using the particle of film of claim 32, the method comprising applying to one or more of the following: (i) a surgical resection margin, (ii) within a treared or untreated tumor or cavity, (iii) a target site of disease away from a surgical margin, and (iv) a lymph node.
35. The film of claim 32, wherein the film is a single layered film.
36. The film of claim 32, further comprising two or more layers to form a multi- layered film.
37. The film of claim 32, comprising a first layer comprising a first polymer of
Formula XX, and a second layer comprising a second polymer different from
Formula
XX.
38. The film of claim 33, wherein the second polymer comprises one or more of poly(lactic acid), poly(glycolic acid), poly(lactid0co-glycolic acid), polycaprolactone, poly(trimethlene carbonate), polyester, polycarbonate, and polyamide.
39. An oligomer or polymer having a repeat unit represented by Formula XX:
wherein:
G comprise a first group that is convertible to a second group different from the first group at a pH at or below about 6.0;
R2 is selected from among hydrogen, a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylalryl, arylalkyl, or fluorocarbon chain of 1-50 carbons, wherein each alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl or fluorocarbon chain is optionally substituted internally or terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono or di-substituted amino, thiol, thioester, sulfate, phosphate, phosphonate, or halogen substituents; and
Q is selected from among O, S, Se, or NH.
40. The oligomer or polymer of claim 39, wherein G is selected from among the following structures:
41. A particle having a first volume and comprising and oligomer or polymer having a repeat unit represented by Formula XX:
wherein:
G comprises a first group that is convertible to a second group different from the first group at a pH at or below about 6.0;
R2 is selected from among hydrogen, a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, or fluorocarbon chain of 1-50 carbons, wherein, each alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, or fluorocarbon chain is optionally substituted internally or terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono- or di-substituents; and
Q is selected from among O, S, Se, or NH; and wherein when the particles is placed in an environment having a pH at or below about 6.0, the particle increases in
volume from the first volume to a second volume that is more than two time the first volume after equilibrium is established.