DRUG CARRIERS COMPRISING AMPHILPHILIC BLOCK COPOLYMERS
    3.
    发明申请
    DRUG CARRIERS COMPRISING AMPHILPHILIC BLOCK COPOLYMERS 审中-公开
    包含AMPHILPHILIC嵌段共聚物的药物载体

    公开(公告)号:US20120157550A1

    公开(公告)日:2012-06-21

    申请号:US13355910

    申请日:2012-01-23

    IPC分类号: A61K47/30 A61P35/00

    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。