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公开(公告)号：US09765213B2
公开(公告)日：2017-09-19
申请号：US13355910
申请日：2012-01-23
IPC分类号： A61K47/30 , A61P35/00 , C08L53/00 , A61K9/107 , C08F293/00
CPC分类号： C08L53/00 , A61K9/1075 , C08F293/005 , C08L2666/02
摘要： An aqueous composition comprises an amphiphilic block copolymer, having a hydrophilic block comprising pendant zwitterionic groups and a hydrophobic block, and a biologically active compound associated with the polymer. The polymer is preferably in the form of micelles, and preferably the biological active is a hydrophobic drug. The hydrophilic block is preferably formed from acrylic monomer including phosphorylcholine groups. The hydrophobic group is suitably formed from monomer which has groups which can be ionised at useful pH's, especially tertiary amine groups. Micelles may be formed by dissolving the block copolymer in aqueous solvent at a pH at which the amine groups are protonated then raising the pH to a value at which the amine groups are substantially deprotonated, whereupon micelles spontaneously form. The preformed micelles are then contacted with active, under conditions such that solubilisation of the active occurs. The active may be for tumour treatment.
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公开(公告)号：US06852816B2
公开(公告)日：2005-02-08
申请号：US10398400
申请日：2001-10-05
IPC分类号： A61K9/10 , A61K47/32 , C08F4/40 , C08F20/22 , C08F246/00 , C08F293/00 , C08F130/02
CPC分类号： C08F4/40 , C08F246/00 , C08F293/005 , C08F2438/01
摘要： Polymers may be made from zwitterionic monomers having controlled architectures and molecular weights, using living polymerisations such as group or atom transfer radical polymerisation. For instance polymers may be formed by atom transfer radical polymerisation using a copper chloride catalyst, a ligand which is water soluble, and a water soluble tertiary alkyl halide initiator to form homopolymers having controlled polydispersities of less than 1.5 and block copolymers with other hydrophilic or hydrophobic monomers. One suitable zwitterionic monomer is 2-methacryloyloxy-2′-trimethylammoniumethyl phosphate inner salt. The block copolymers may spontaneously form micelles, believed to have zwitterionic, for instance phosphorylcholine, groups at the external surface, which may be useful as drug delivery systems with improved biocompatibility.
摘要翻译： 聚合物可以由具有受控结构和分子量的两性离子单体制备，使用活性聚合如基团或原子转移自由基聚合。 例如聚合物可以通过使用氯化铜催化剂，水溶性配体和水溶性叔烷基卤引发剂的原子转移自由基聚合形成，以形成控制多分散度小于1.5的均聚物和具有其它亲水或疏水性的嵌段共聚物 单体。 一种合适的两性离子单体是2-甲基丙烯酰氧基-2'-三甲基铵乙基磷酸内酯盐。 嵌段共聚物可以自发形成胶束，据信其具有两性离子，例如磷酸胆碱，在外表面的基团，其可用作具有改善的生物相容性的药物递送系统。
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公开(公告)号：US08182802B2
公开(公告)日：2012-05-22
申请号：US10506814
申请日：2003-03-07
CPC分类号： A61K47/6935 , A61K47/60 , A61K47/6907
摘要： Compositions are described comprising a of a block copolymer having an overall ionic charge and in which one of the blocks has pendant zwitterionic groups and a biologically active compound having a charge opposite that of the polymer. The polymer is preferably a linear diablock copolymer, preferably having a low polydispersity, such as a (tertiary amine group containing monomer) block-(zwitterionic monomer) copolymer. Suitable cationic monomers are dialkyl aminoalkyl(alk)acrylates and -acrylamides and suitable zwitterionic monomers are phosphorylcholine group containing acrylate monomers such as 2-methacyloyloxyetyl-21-trimethyl ammonium ethyl phosphate liner salt. The biologically active compound is generally polyionic and is for instance a nucleic acid, such as DNA, especially plasmid DNA.
摘要翻译： 描述了包含具有总离子电荷的嵌段共聚物的组合物，其中一个嵌段具有侧基两性离子基团和具有与聚合物相反的电荷的生物活性化合物。 聚合物优选为线性二嵌段共聚物，优选具有低多分散性，例如（含叔胺基的单体）嵌段 - （两性离子单体）共聚物。 合适的阳离子单体是二烷基氨基烷基（alk）丙烯酸酯和 - 丙烯酰胺，合适的两性离子单体是含有丙烯酸酯单体如2-甲基丙烯酰氧基乙基-2'-三甲基铵乙基磷酸内酯的磷酸胆碱基团。 生物活性化合物通常是聚离子的，并且是例如核酸，例如DNA，特别是质粒DNA。
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公开(公告)号：US07820753B2
公开(公告)日：2010-10-26
申请号：US10544113
申请日：2004-02-05
IPC分类号： C08L31/02
CPC分类号： C08F293/005 , A61K9/1075 , C08L53/00 , C08L2666/02
摘要： Block copolymers comprise a core block formed of hydrophilic monomers and have pendant zwitterionic groups, and at least two terminal blocks, comprising stimulus-responsive groups. The core block has a degree of polymerisation of at least 100, whilst the terminal blocks have an average degree of polymerisation of at least 20. A solution of polymer in a liquid may be caused to change its characteristics, for instance rheology, upon being subjected to a stimulus such as a change in temperature or pH. Examples comprise core blocks formed of 2-methacryloyloxyethyl-2′-trimethylammonium ethylphosphate inner salt (MPC) and terminal blocks formed of 2-(diisopropylamino)ethyl methacrylate. Upon changing the pH from around 2 to around 8, an aqueous solution of the block copolymer gels, the solution becoming mobile again upon lowering the pH. The effect is due to deprotonation of a quaternary ammonium pendant ion to form a non-ionised group and subsequent protonation to form an ionised group. This changes the hydrophilicity of the terminal blocks and allowing formation of a network of micellar structures when the pendant groups are not ionised and relatively hydrophobic and associated in micelles.
摘要翻译： 嵌段共聚物包含由亲水性单体形成的核心嵌段并具有侧基两性离子基团，和包含刺激反应性基团的至少两个末端嵌段。 核心嵌段具有至少100的聚合度，而端嵌段的平均聚合度至少为20.聚合物在液体中的溶液可以在经受流动时改变其特性，例如流变性 到诸如温度或pH变化的刺激。 实例包括由2-甲基丙烯酰氧基乙基-2'-三甲基铵乙基磷酸内酯盐（MPC）形成的核心嵌段和由甲基丙烯酸2-（二异丙基氨基）乙酯形成的端基。 当将pH从约2改变到约8时，嵌段共聚物的水溶液凝胶化，溶液在降低pH后再次变得流动。 该效应是由于季铵离子离子的去质子化而形成非电离基团，随后质子化形成电离基团。 当侧基不被离子化并且相对疏水并且在胶束中缔合时，这改变了端基的亲水性并允许形成胶束结构网络。
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公开(公告)号：US20120157550A1
公开(公告)日：2012-06-21
申请号：US13355910
申请日：2012-01-23
CPC分类号： C08L53/00 , A61K9/1075 , C08F293/005 , C08L2666/02
摘要： An aqueous composition comprises an amphiphilic block copolymer, having a hydrophilic block comprising pendant zwitterionic groups and a hydrophobic block, and a biologically active compound associated with the polymer. The polymer is preferably in the form of micelles, and preferably the biological active is a hydrophobic drug. The hydrophilic block is preferably formed from acrylic monomer including phosphorylcholine groups. The hydrophobic group is suitably formed from monomer which has groups which can be ionised at useful pH's, especially tertiary amine groups. Micelles may be formed by dissolving the block copolymer in aqueous solvent at a pH at which the amine groups are protonated then raising the pH to a value at which the amine groups are substantially deprotonated, whereupon micelles spontaneously form. The preformed micelles are then contacted with active, under conditions such that solubilisation of the active occurs. The active may be for tumour treatment.
摘要翻译： 水性组合物包含具有包含侧基两性离子基团和疏水嵌段的亲水嵌段的两亲性嵌段共聚物和与聚合物缔合的生物活性化合物。 聚合物优选为胶束形式，优选生物活性物质为疏水性药物。 亲水性嵌段优选由包含磷酸胆碱基团的丙烯酸单体形成。 疏水基团适当地由具有可以在有用pH，特别是叔胺基团离子化的基团的单体形成。 胶束可以通过将嵌段共聚物溶解在水性溶剂中，在胺基质子化的pH下将pH升高至胺基基本上去质子化的值，由此胶束自发形成。 然后在预先形成的胶束与活性物质接触的条件下，使活性物发生溶解。 活性物质可用于肿瘤治疗。
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公开(公告)号：US07300990B2
公开(公告)日：2007-11-27
申请号：US11025968
申请日：2005-01-03
IPC分类号： C08F130/02
CPC分类号： C08F4/40 , C08F246/00 , C08F293/005 , C08F2438/01
摘要： Polymers may be made from zwitterionic monomers having controlled architectures and molecular weights, using living polymerisations such as group or atom transfer radical polymerisation. For instance polymers may be formed by atom transfer radical polymerisation using a copper chloride catalyst, a ligand which is water soluble, and a water soluble tertiary alkyl halide initiator to form homopolymers having controlled polydispersities of less than 1.5 and block copolymers with other hydrophilic or hydrophobic monomers. One suitable zwitterionic monomer is 2-methacryloyloxy-2′-trimethylammoniumethyl phosphate inner salt. The block copolymers may spontaneously form micelles, believed to have zwitterionic, for instance phosphorylcholine, groups at the external surface, which may be useful as drug delivery systems with improved biocompatibility.
摘要翻译： 聚合物可以由具有受控结构和分子量的两性离子单体制备，使用活性聚合如基团或原子转移自由基聚合。 例如聚合物可以通过使用氯化铜催化剂，水溶性配体和水溶性叔烷基卤引发剂的原子转移自由基聚合形成，以形成具有小于1.5的受控多分散性的均聚物和具有其它亲水或疏水性的嵌段共聚物 单体。 一种合适的两性离子单体是2-甲基丙烯酰氧基-2'-三甲基铵乙基磷酸内酯盐。 嵌段共聚物可以自发形成胶束，据信其具有两性离子，例如磷酸胆碱，在外表面的基团，其可用作具有改善的生物相容性的药物递送系统。
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