Particles comprising polyesteramide copolymers for drug delivery

    公开(公告)号:US09873764B2

    公开(公告)日:2018-01-23

    申请号:US14128731

    申请日:2012-06-25

    摘要: 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.

    PARTICLES COMPRISING POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY

    公开(公告)号:US20140120170A1

    公开(公告)日:2014-05-01

    申请号:US14128731

    申请日:2012-06-25

    IPC分类号: A61K47/34

    摘要: The present invention relates to micro- or nanoparticles comprising a polyesteramide (PEA) having a chemical formula described by structural formula (IV), 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, (C1C6)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); 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 whereby a is at least 0.05 and b is at least 0.05 and a+b=1.

    METHOD TO ACTIVATE SILICONE RUBBER SURFACES
    3.
    发明申请
    METHOD TO ACTIVATE SILICONE RUBBER SURFACES 有权
    激活硅橡胶表面的方法

    公开(公告)号:US20120322954A1

    公开(公告)日:2012-12-20

    申请号:US13518131

    申请日:2010-12-23

    摘要: A method for activating silicone rubber surfaces comprising steps of: i) swelling at least the surface of the silicone rubber matrix with a silicone rubber swelling solvent; ii) treating the silicone rubber matrix during or after the swelling with a solution comprising at least a reactive silane, the reactive silane comprising: a) at least one Si—C bond and; b) at least one hydrolytically labile bond linked to at least one of the Si atoms present in the reactive silane and; c) at least one functional group F1 connected via a Si—C bond to the same or an other Si atom present in the reactive silane, the functional group comprising electrophilic and/or nucleophilic moieties, and/or at least one functional group F2 connected via a Si—C bond to the same or an other Si atom present in the reactive silane comprising moieties which become electrophilic or nucleophilic moieties by a mechanism selected from the group consisting of ring opening of a cyclic structure, hydrolysis, displacement or by a migration reaction; iii) drying and/or heat treating of the treated silicone rubber matrix.

    摘要翻译: 一种活化硅橡胶表面的方法,包括以下步骤:i)用硅橡胶溶胀溶剂至少使硅橡胶基体的表面膨胀; ii)在溶胀期间或之后用含至少一种反应性硅烷的溶液处理该硅橡胶基质,该反应性硅烷包含:a)至少一个Si-C键;和 b)与反应性硅烷中存在的至少一种Si原子连接的至少一个水解不稳定键; c)至少一个通过Si-C键连接到存在于反应性硅烷中的相同或另一个Si原子的官能团,所述官能团包括亲电子和/或亲核部分,和/或至少一个官能团F2连接 通过Si-C键与存在于反应性硅烷中的相同或另一个Si原子,其包含通过选自环状结构的开环,水解,置换或通过迁移的机制而成为亲电子部分或亲核部分 反应; iii)处理的硅橡胶基质的干燥和/或热处理。

    Method to activate silicone rubber surfaces
    4.
    发明授权
    Method to activate silicone rubber surfaces 有权
    激活硅橡胶表面的方法

    公开(公告)号:US09221999B2

    公开(公告)日:2015-12-29

    申请号:US13518131

    申请日:2010-12-23

    摘要: A method for activating silicone rubber surfaces comprising steps of: i) swelling at least the surface of the silicone rubber matrix with a silicone rubber swelling solvent; ii) treating the silicone rubber matrix during or after the swelling with a solution comprising at least a reactive silane, the reactive silane comprising: a) at least one Si—C bond and; b) at least one hydrolytically labile bond linked to at least one of the Si atoms present in the reactive silane and; c) at least one functional group F1 connected via a Si—C bond to the same or an other Si atom present in the reactive silane, the functional group comprising electrophilic and/or nucleophilic moieties, and/or at least one functional group F2 connected via a Si—C bond to the same or an other Si atom present in the reactive silane comprising moieties which become electrophilic or nucleophilic moieties by a mechanism selected from the group consisting of ring opening of a cyclic structure, hydrolysis, displacement or by a migration reaction; iii) drying and/or heat treating of the treated silicone rubber matrix.

    摘要翻译: 一种活化硅橡胶表面的方法,包括以下步骤:i)用硅橡胶溶胀溶剂至少使硅橡胶基体的表面膨胀; ii)在溶胀期间或之后用含至少一种反应性硅烷的溶液处理该硅橡胶基质,该反应性硅烷包含:a)至少一个Si-C键;和 b)与反应性硅烷中存在的至少一种Si原子连接的至少一个水解不稳定键; c)至少一个通过Si-C键连接到存在于反应性硅烷中的相同或另一个Si原子的官能团,所述官能团包括亲电子和/或亲核部分,和/或至少一个官能团F2连接 通过Si-C键与存在于反应性硅烷中的相同或另一个Si原子,其包含通过选自环状结构的开环,水解,置换或通过迁移的机制而成为亲电子部分或亲核部分 反应; iii)处理的硅橡胶基质的干燥和/或热处理。