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    • 1. 发明申请
    • NOVEL NANOPARTICLES
    • 新型纳米材料
    • US20100009001A1
    • 2010-01-14
    • US12438591
    • 2007-09-05
    • Steven ArmesJian-Jun Yuan
    • Steven ArmesJian-Jun Yuan
    • A61K9/14A61P43/00
    • A61K9/5089A61K9/501C08K3/36C08K9/00C08K9/02C08K9/12C08K2201/011C08K2201/013C08L53/00C08L2207/53C09D7/70G02B1/111Y10T428/254Y10T428/2998
    • The invention provides a composition comprising core-shell nanoparticles, the nanoparticles comprising (a) cationic core material comprising polymer; and (b) a shell material comprising silica. Preferred core materials comprise diblock copolymer micelles comprising one block of dialkylaminoethyl methacrylate units which are partially or fully quaternised and one block of dialkylaminoethyl methacrylate units that remain non-quaternised. The invention also provides a method for the preparation of the said composition, the method involving (a) preparing a cationic core material comprising polymer; and (b) coating the core material with a shell comprising silica by treating the polymer with a silica precursor under ambient conditions. The invention also envisages a composition comprising core-shell nanoparticles which is adapted to facilitate controlled delivery of at least one active agent into a system in response to controlled changes in the pH of the system.
    • 本发明提供包含核 - 壳纳米颗粒的组合物,所述纳米颗粒包含(a)包含聚合物的阳离子核心材料; 和(b)包含二氧化硅的壳材料。 优选的核心材料包括二嵌段共聚物胶束,其包含部分或全部季铵化的一个二烷基氨基乙基甲基丙烯酸酯单元和一个保持非季铵化的一个二烷基氨基乙基甲基丙烯酸酯单元。 本发明还提供了一种制备所述组合物的方法,所述方法包括(a)制备包含聚合物的阳离子核心材料; 和(b)在环境条件下用二氧化硅前体处理聚合物,用包含二氧化硅的壳涂覆芯材。 本发明还设想包含核 - 壳纳米颗粒的组合物,其适于响应于系统的pH的受控变化而促进至少一种活性剂被控制递送到系统中。
    • 6. 发明申请
    • Drug carriers comprising amphiphilic block copolymers
    • 包含两亲性嵌段共聚物的药物载体
    • US20050220880A1
    • 2005-10-06
    • US10506805
    • 2003-03-07
    • Andrew LewisSteven ArmesAndrew LloydJonathan Salvage
    • Andrew LewisSteven ArmesAndrew LloydJonathan Salvage
    • A61K9/107A61K9/51C08F4/40C08F293/00C08L53/00A61K9/14
    • C08L53/00A61K9/1075C08F293/005C08L2666/02
    • 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, for instance having a calculated or experimentally determined logP of at least 1.0, where P is the octanol:water partition coefficient. The hydrophilic block is preferably formed from acrylic monomer including phosphoryicholine 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 a water-insoluble drug, for instance for tumour treatment.
    • 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,优选地,生物活性剂是疏水性药物,例如具有至少1.0的计算或实验测定的logP,其中P是辛醇:水分配系数。 亲水性嵌段优选由包括磷酰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。 活性物质可以是水不溶性药物,例如用于肿瘤治疗。
    • 7. 发明申请
    • Composition of polymers
    • 聚合物的组成
    • US20050163743A1
    • 2005-07-28
    • US10506814
    • 2002-03-07
    • Andrew LewisSteven Armes
    • Andrew LewisSteven Armes
    • A61K47/48A61K48/00A61K31/785C12N15/88
    • A61K47/6935A61K47/60A61K47/6907
    • 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.
    • 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。