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1. WO2007140483 - FILMS AND PARTICLES

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[ EN ]

We Claim:
1. An oligomer or polymer having a repeat, unit represented by Formula XX:



XX
"wrserem:
Q is selected from among CX S, Se, or NH;
G is selected from anions; th«_ fol lowing structures:



R> is selected from among hydrogen, a straight or branched alky!, cycloalkyl. aryl, olefin, silyi alkylsilyi, arylsilyj, alkylaryl, aryklkyi, or fiuorocarboii chairs, of 1-50 carbons, wherein each alkyl. cycloalkyl, aryl, olefin, siiyl, alkylsilyi, arylsilyi, alkylaryl, arylalkyl, or liuorocarbon chain is optionally substituted internally or teπninaliy by one or more hydroxy!, hydroxyether, carboxyi, carboxyesier, carboxyamide, amino, mono- or di-subsiituied amino, thiol thioester, sulfate, phosphate, phosphonate, or halogen
Bobsfituents;

R:; is selected from among hydrogen., methoxy, othoxy, amino, a straight or branched aikyl. eycloalkyl aryl, olefin, silyl, aϊkyMlyl, arylsiiyl aikylaryi, or sryialkyl chain of 1-10 carbons;
Rij, R-Ϊ, &t\ά Rb are each independently selected from among a straight or branched alky), cydosikyi, aryl, olefin, silyl, alkylsilyl, arylsiiyi, aikylaryi, or arylalkyi chain of 1-10 carbons; ami
R7 ami Rj5 are each independently selected from among hydrogen, a straight or branched alky!, eycloalkyl aryl olefin, aikylaryi, or arylalkyi chain of 1 -50 carbons, wherein each aikyl. cycioalkyi, aryi, olefin, aikylaryi, or arylalkyi cham is optionally substituted internally or tcπninaliy by one or more hydroxy]., hydroxyether, carboxy], carboxyestcr, carboxyamide, amino, mono- or di-subsπtυted amino, thiol, ihioester, sulfate, phosphate, phtosphonate, or halogen substituents.

2. The oligomer or polymer of claim 1 , wherein the oligomer or polymer is represented by Forraukt XX';



XX:
wherein:
n is an integer from 2-750, and wherein each oiigαmεrk or polymeric chain has a terminal group, the terminal gαup being selected from among amines, thiols, amides, phosphates, sulphates, hydroxides, alkenes. and alkynes.

3. The oligomer or polymer of claim 1 , wherein R; is hydrogen or methyl.

4. The oligomer or polymer of claim 1 , wherein Q is oxygen.

5. A composition comprising fee oligomer or polymer of claim ! .

6. A polymeric film or particle comprising an oligomer or polymer of claim 1 - ?. A polymeric panicle ϋf claim 6, comprising a microparticie or uanopartic'ie.

8. A polymeric particle of claim 7, wherein die particle has a diameter between about 2 mϊi and I micron.

9. The polymeric particle of claim 7 comprising a first volume at a first pϊi, ami a second volume at a second pfl, different from the from the first pH,

10. The polymeric particle of claim 9, wherein the second volume is 1 X or .more greater ihaxs the first volume when the second pH is lower than the Brst pll

1 1. The polymeric particle of claim 9, wherein the second volume is 4 X or .more greater than the first volume when the second pH is lower than the first pi L

12. The polymeric particle of claim 9, wherein the second volume- is SX or more greater thars the first volume when the second pH is lower than the lirsi pH.

! 3. 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 titan the first volume and the change in volume is sufficient to cause the particle to become lodged, embedded, or immobilized in an anatomic location, sueh 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 anii-biotk, an antineoplastic agent, an analgesic, mi angiogenic, or an agent that promotes wound healing.

17. The polymeric film or particle of claim 15, wherein the biologically active agent comprises one or more of asparaginase; bleomycin; husuHan; capedtabirie; earbopktin; earmusiine chlorambucil; cisplatm; cyclophosphamide; eytarab-ine; dacariwhie;
dactinomycin; daunorubicm; dexr&εoxane; docetaxel; doxorubicin; etσposide;
fioxuridiπe; fiudarabine; iluorourøcil; gemcHabine; hydroxyurea; idarubi.cin;
ifosfanikk; irinotecan; iomustiae; mechloreth&røine; rnelphalaπ: mercaptopurine:
methotrexate; mitomycin; mitotane; mitoxantrone; paciitaxel; pemetrexed; pemostatin; pHeamycin; procarbazine; ritisxiraab; streptozocin; tenipoaidc; ihiαguaranc: thiotepa; vinblasiiϊie; vincristine; and vinαrelbine.

1 S. A method of -using the particle or 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 fϋrn 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 Elm.

21. The iϊiπi of claim 15, comprising a first layer comprising a first polymer of Formula XX5 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 poiyijactie acid), poly(giyco!ic acid), polyfjaetio-α>glyccmc acid}, polycaproiactoπe, ρoly(triirieth!ene carbonate), polyester, polycarbonate, and polyamide.

An. oligomer or polymer, or portion thereof, represeined by Formula XXL, XXII,

XXlil. XXiV, XXV, XXVI, XXViJ5 XXVIIl XXlX, XXX XXXI, XXXIi, XXXIII, XXXFV, XXXV, XXXVi or XXXVIf:





wherein:

Q' is independently selected from among O, S, Se, or NH;
Q\ (V, and GV are each independently selected from among the following structures:


and GV are not ihe same;
R/ is selected from among a straight or branched alkyls eyeloalkyi, aryl, olefin, silyK alkylsilyl, arylsilyi, alkylaryl, arylalkyi, or iϊuorocarhon chairs of 3-50 carbons, wherein each alky!, eyeloalkyi, aryl, olefin, silyl, alkylsilyl, arylsϋyl, alkylaryl, arylalkyl or fmoraearbon chain is optionally substituted internally or terminally by one or more hydroxy!, hydroxyethsr, earboxyi, carboxyester, earboxyarπide, amino, mono- or di-substituted ammo, thiol, thioester, sυl&te, phosphate, phosphorate, or halogen substituents; or
Ri/ is selected from aixsong ρoly(ethy!ene glycol), ρoiy(ethy!ene oxide), poly(hydroxyacid)), a carbohydrate, a protein,, a polypeptide, an amino acid, a αudde acid, a nucleotide, a polynucleotide, any DNA or RNA segment, a !φid, a
polysaccharide, aτi antibody, a pharmaceutical agent, or any epitope for a biological receptor; or
R;' is selected from among & photocrosslmkable or iorαcalry erossliαkable group;

Ra' is selected ifom among hydrogen, a straight or branched ιύky\, eyeloalkyl, aryl, oS dm, silyl, alkylsilyl, arylsilyi alkylaryl, arylalkyl, or ilυorocarbon chain of 1-50 carbons, wherein each aikyl, eyeloalkyi aryL olefin, silyi, alkylsilyi, arylsilyi, alkylaryK arylalkyK or flυorocarbon chain is optionally substituted internally or terminally by one or more hydroxy!, hydroxyether, carboxyl, carboxyester, carboxyaπude, amino, mono- or di-suhstiiυtei amino, thiol, thioe.ster, sulfate, phosphate, phosphonatc, QΪ halogen substituεnts;
x and y are each independently selected from an integer of 2-750;
a is selected from an integer of I -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, phosphates, sulphates, hydroxides, metals, alkanes, alkenes and alkynes.

24, An oligomer or polymer, or portion thereof, represented by Formula XXXV"



wherein;
Q' is independently selected from among O, S, Se, or KH;


G' b selected from among 1^ or Rj';
Rj' is selected from among a straight or branched alkyi, cycloalkyk aryl, olefin. silyi, ajkylsiiyl, arylsilyi, alkylaryl, arylalkyl, or lluoroearbon chairs of 3-50 carbons, wherein each aikyl, cycioalkyi, aryl, olefin, silyi, alkyLsilyl, arylsilyi, alkylaryi, aryiaikyϊ, or iluorocarboB chain is optionally substituted internally or terminally by one or more hydroxy], hydrαxyedier, carboxyl, c-arboxyester, carboxyamide, amino, mono- or di-siibstituted amino, thiol thioester, sulfate, phosphate, phosphonate, or halogen substituents; or
R{ is selected from among poiy(elhylene glycol), poiy( 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, a pharmaceutical agent, or any epitope for a biological receptor; or
Rj' is selected from among a photocrosslinkable or ionically erossiisikahie group; x. and y are each independently selected from an integer of 2-750;

e is selected from an integer of i -S; and
each polymeric terminal group Is selected from among amines, thiols, amides, phosphates, sulphates, hydroxides, metals, alkar.es, alkenes and alkynes.

25. The oligomer or polymer of claim 2.4, wherein Ry' is selected from among a straight or branched aikyL cycloalkyL ary!, olefin, silyi, alkyisiiyi, arylsiiyl, alkylaryl, arylalkyl, or iluotoearbon chain of 3-50 carbons, wherein each alkyl cydoalkyL aryl, olefin, silvi, alkyisiiyi, arylsilyi, alkylaryl, aiylalkyl. or fiuorocarbon chain is optionally substituted inteπialiy or terminally by one or more hydroxy!, hydroxy ether, carboxyl earboxyester, carboxyamide, amino, mono- or di-substituted amino. thiol, thioester, sulfate, phosphate, phosphorate, or halogen substituents.

26. 'flic oligomer or polymer of claim 24, wherein IV is selected from, among a straight or branched alky!, cycloalkyl, aryl, olefin, silyi, aikylsilyl, aryisifyi, ai'kyiaryl ary! alky 1. or fhjorocarboTi chain of 3-50 carbons.

27. The oligomer or polymer of daini 24, wherein R,' is selected from among a straight or branched aikyl chain of 3-50 carbons.

28. A polymeric film or particle comprising a polymer of claim 23 or 24.

29. A polymeric particle of claim 28, comprising a πύcroparticie or .nanøpaitide.

30. A polymeric particle of claim 29, wherein the particle comprises a diameter of between about 1 urn and 2 microns.

3 i . A polymeric particle of claim 29, wherein the particle comprises a diameter between about 10 am and 1 microns.

32. The polymeric film or particle of claim 28, farther comprising an agent.

33, The polymeric film or particle of claim 32, wherein the agent is a biologically active agerst comprising one or more of an anti-cancer, an aαti-blotic, anti-neopfastic. an analgesic, an angiogenic, or agent that promotes healing,

34, The polymeric film or particle of claim 32, wherein the biologically active agent comprises one or more of asparaginase; bleomycin; busυifan; capeciiabtne; earbtφiatin; earmustme chlorambucil; cisplatin; cyclophosphamide; eytarabine: dacarbazine;
dactinomyciiv. daunorubiem; dexrazox&πε; doceiaxel; doxorubicin; etoposidε;
fiox uridine; fJud&rabme; tlisorouracil; gemcitabine; hydroxyurea; idarubicin;
ifosfamide; irinoteean; lomustine; mechlorethaiuine; meiphaian; mercaptopurine; methotrexate; mitomycin; mitotane; rnitoxantroπe; paclitaxel; prcmetrcxed; pcntostatin; plicamycin; procarbazine; ritiiximab; streptozocin; teniposide; thiogiianine; thiotepa; vinblastine; vincristine; and vinorelbine.

35, A .method of using the panicle or film of claim 32, the method comprising applying to one or more of the following: (i) a surgical resection margin. (U) within a treated 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- film.

3?.. The film of claim 32, comprising a first layer comprising a first polymer of Formula XX, asd 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 ρo!y(laetic acid), poiyCglyeolie acid), poiy(Iactie-co-gtycoiic acid), polycaproJsctone. polyCtrimethiene carbonate), polyester, polycarbonate, and polyamide.

39. An oligomer or polymer having a repeal 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 pli at or below about 6.0;
R^ is selected from among hydrogen, a straight or branched aikyl, eydoai&yi, aryl, olefin, silyl, alkylsilyi, arylsihi, alkylaryl, arylaikyl, or fluorocarbon chain of 1-50 carbons., wherein each alky], cycloalkyl, aryl. olefin, silyj. alkvisiiyL arylsily!, alkylaryl, arylalkyi or Suorocarborj chain is optionally substituted internally or terminally by one or more hydroxy!, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono- or di-substivuted amino, thiol, Ihioester, sulfate, phosphate, phosphαnaie, or halogen substHuents; and
Q is selected from among O, S1 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 an 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 h selected from among hydrogen, a straight or branched alkyi, cydoalkyl aryl, olefin, sllyl, aikylailyl, arylsilyi, alkylaryl, arylalkyL or iiuorocarbon chain csf 1 -50 carbons, wherein each aikyl cycloalkyl, aryl, olefin, si Iy L alkylsilyl, arylsilyi, alkylaryl, aryialkyl. or thiorocarbon chain is optionally substituted iotemaHy or terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono- or di-substituted amino, thiol, thioester, sulfate, phosphate, phosphorate, or halogen substituenls; and
Q is selected from among O, S5 Sc, or NH; and wherein when the panicle is pkcαl in an environment having a pf i at or below about 6.0, the particle increases in volume from the first volume to a second volume thai is more than two limes the first volume alter equilibrium is established.