Particles comprising polyesteramide copolymers for drug delivery
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-047/34
C08G-069/44
A61K-047/69
C08L-077/12
C08J-005/18
A61K-031/165
출원번호
US-0128731
(2012-06-25)
등록번호
US-9873764
(2018-01-23)
우선권정보
EP-11171191 (2011-06-23)
국제출원번호
PCT/EP2012/062267
(2012-06-25)
§371/§102 date
20131223
(20131223)
국제공개번호
WO2012/175748
(2012-12-27)
발명자
/ 주소
Mihov, George
Zupancich, John Andrew
출원인 / 주소
DSM IP ASSETS, B.V.
대리인 / 주소
Bull, Kevin M.
인용정보
피인용 횟수 :
0인용 특허 :
83
초록▼
The present disclosure relates to microparticles or nanoparticles comprising a polyesteramide (PEA) having a chemical formula described by structural formula (IV), wherein m+p varies from 0.9-0.1 and q varies from 0.1 to 0.9; m+p+q=1 whereby m or p could be 0; n is about 5 to about 300; (pref. 50-2
The present disclosure relates to microparticles or nanoparticles comprising a polyesteramide (PEA) having a chemical formula described by structural formula (IV), wherein m+p varies from 0.9-0.1 and q varies from 0.1 to 0.9; m+p+q=1 whereby m or p could be 0; n is about 5 to about 300; (pref. 50-200); R1 is independently selected from the group consisting of (C2-C20) alkylene, (C2-C20) alkenylene, —(R9—CO—O—R10—O—CO—R9)—, —CHR11—O—CO—R12—COOCR11— and combinations thereof; R3 and R4 in a single backbone unit m or p, respectively, are independently selected from the group consisting of hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C6-C10)aryl, (C1-C6)alkyl, —(CH2)SH, —(CH2)2S(CH3), —CH2OH, —CH(OH)CH3, —(CH2)4NH3+, —(CH2)3NHC(═NH2+)NH2, —CH2COOH, —(CH2)COOH, —CH2—CO—NH2, —CH2CH2—CO—NH2, —CH2CH2COOH, CH3—CH2—CH(CH3)—, (CH3)2—CH—CH2—, H2N—(CH2)4—, Ph-CH2—, CH═C—CH2—, HO-p-Ph-CH2—, (CH3)2—CH—, Ph-NH—, NH—(CH2)3—C—, NH—CH═N—CH═C—CH2—; R5 is selected from the group consisting of (C2-C20)alkylene, (C2-C20)alkenylene, alkyloxy or oligoethyleneglycol; R6 is selected from bicyclic-fragments of 1,4:3,6-dianhydrohexitols of structural formula (III); R7 is (C6-C10)aryl (C1-C6)alkyl; R8 is —(CH2)4—; R9 or R10 are independently selected from C2-C12 alkylene or C2-C12 alkenylene; and R11 or R12 are independently selected from H, methyl, C2-C12 alkylene or C2-C12 alkenylene; whereby a is at least 0.05 and b is at least 0.05 and a+b=1.
대표청구항▼
1. Microparticles with an average diameter of from 1 to 100 μm or nanoparticles with an average diameter of from 10 to less than 1000 nm comprising a bioactive agent and a biodegradable polyesteramide copolymer (PEA) according to the following formula: wherein m+p is from 0.9-0.1 and q is from 0.1 t
1. Microparticles with an average diameter of from 1 to 100 μm or nanoparticles with an average diameter of from 10 to less than 1000 nm comprising a bioactive agent and a biodegradable polyesteramide copolymer (PEA) according to the following formula: wherein m+p is from 0.9-0.1 and q is from 0.1 to 0.9;m+p+q=1 whereby one of m or p could be 0;n is about 5 to about 300;a is at least 0.05, b is at least 0.05, a+b=1, qa=q*a, and qb=q*b; wherein units of m (if present), units of p (if present), units of qa, and units of qb are all randomly distributed throughout the copolymer;R1 is independently selected from the group consisting of (C2-C20) alkylene, (C2-C20) alkenylene, —(R9—CO—O—R10—O—CO—R9)—, —CHR11—O—CO—R12—COOCR11—, and combinations thereof;R3 and R4 in a single backbone unit m or p, respectively, are independently selected from the group consisting of hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C6-C10)aryl, (C1-C6)alkyl, —(CH2)SH, —(CH2)2S(CH3), —CH2OH, —CH(OH)CH3, —(CH2)4NH3+, —(CH2)3NHC(═NH2+)NH2, —CH2COOH, —(CH2)COOH, —CH2—CO—NH2, —CH2CH2—CO—NH2, —CH2CH2COOH, CH3—CH2—CH(CH3)—, (CH3)2—CH—CH2—, H2N—(CH2)4—, Ph-CH2—, CH═C—CH2—, HO-p-Ph-CH2—, (CH3)2—CH—, Ph-NH—, NH—(CH2)3—C—, NH—CH═N—CH═C—CH2—;R5 is selected from the group consisting of (C2-C20)alkylene, (C2-C20)alkenylene, alkyloxy or oligoethyleneglycol;R6 is selected from bicyclic-fragments of 1,4:3,6-dianhydrohexitols of structural formula (III); R7 is selected from the group consisting of (C6-C10) aryl (C1-C6)alkyl;R8 is —(CH2)4—;R9 or R10 are independently selected from C2-C12 alkylene or C2-C12 alkenylene;R11 or R12 are independently selected from H, methyl, C2-C12 alkylene or C2-C12 alkenylene. 2. The microparticles or nanoparticles according to claim 1, wherein a is at least 0.5. 3. The microparticles or nanoparticles according to claim 1, wherein a is at least 0.75. 4. The microparticles or nanoparticles according to claim 1, wherein p=0, m=0.75, and a=0.5;wherein the m, qa, and qb units are randomly distributed;R1 is —(CH2)8—, R3 is (CH3)2—CH—CH2—, R5 is hexyl, and R7 is benzyl. 5. The microparticles or nanoparticles according to claim 1, wherein m=0.3, p=0.45, q=0.25, and a=0.5;wherein the m, p, qa, and qb units are randomly distributed;R1 is —(CH2)8—; R3 and R4 respectively, are (CH3)2—CH—CH2—; R5 is (C2-C20)alkylene; and R7 is benzyl. 6. The microparticles or nanoparticles according to claim 1, wherein m=0.3, p=0.45, q=0.25, and a=0.75;wherein the m, p, qa, and qb units are randomly distributed;R1 is —(CH2)8—; R4 is (CH3)2—CH—CH2—; and R7 is benzyl. 7. The microparticles or nanoparticles according to claim 1, wherein m=0.6, p=0.30, q=0.1, and a=0.5;wherein the m, p, qa, and qb units are randomly distributed;R1 —(CH2)4—; R3 and R4 respectively, are (CH3)2—CH—CH2—; and R7 benzyl. 8. The microparticles or nanoparticles according to claim 1, wherein R1 is independently selected from (C2-C20)alkylene. 9. The microparticles or nanoparticles according to claim 1, wherein R5 is (C2-C20)alkylene. 10. The microparticles or nanoparticles according to claim 8, wherein R5 is (C2-C20)alkylene. 11. The microparticles or nanoparticles according to claim 1, wherein the bioactive agent is a small molecule drug, or prodrug or metabolite thereof. 12. The microparticles or nanoparticles according to claim 5, wherein the bioactive agent is a small molecule drug, or prodrug or metabolite thereof. 13. The microparticles or nanoparticles according to claim 10, wherein the bioactive agent is a small molecule drug, or prodrug or metabolite thereof. 14. The microparticles or nanoparticles according to claim 1, comprising an inner core and an outer shell structure. 15. A composition comprising the microparticles or nanoparticles according to claim 11. 16. A composition comprising the microparticles or nanoparticles according to claim 12. 17. A composition comprising the microparticles or nanoparticles according to claim 13. 18. An article or device comprising the microparticles or nanoparticles according to claim 11. 19. An article or device comprising the microparticles or nanoparticles according to claim 12. 20. An article or device comprising the microparticles or nanoparticles according to claim 13.
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