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    • 43. 发明授权
    • Stabilization and acoustic activation of polymeric micelles for drug delivery
    • 用于药物递送的聚合胶束的稳定和声学活化
    • US06649702B1
    • 2003-11-18
    • US09979481
    • 2002-08-07
    • Natalya RapoportWilliam G. Pitt
    • Natalya RapoportWilliam G. Pitt
    • C08L5300
    • A61K9/5138A61K9/0009A61K9/1075A61K9/5146C08G65/32C08G2650/58C08L71/02C08L2666/04
    • Methods are disclosed in which a micelle is stabilized against degradation upon dilution. The micelle comprises molecules of a block polymer having a hydrophobic block and a hydrophilic block. The hydrophobic block forms a core of the micelle with corona from the hydrophilic block. The methods for stabilizing the core are (1) by chemically cross-linking, (2) incorporating a hydrophobic oil (vegetable oil) in the core to render it more hydrophobic and stable, and (3) incorporating a cross-linked interpenetrating network of a stimuli-responsive hydrogel into the core. The hydrogel is responsive to any stimuli, but preferably temperature or pH. A substance such as, drugs, can be incorporated into the dense inner core of the micelles. When subjected to ultrasound, the micelles release the substance, and then reversibly revert to a stable dense core and re-encapsulating the substance when the ultrasound is turned off. By pulsing the ultrasound, it is therefore, to controllably release the substance in a pulsed manner corresponding to the ultrasound signal.
    • 公开了在稀释时胶束稳定以免降解的方法。 胶束包括具有疏水嵌段和亲水嵌段的嵌段聚合物的分子。 疏水嵌段由亲水嵌段形成具有电晕的胶束核心。 用于稳定核心的方法是(1)通过化学交联,(2)在核心中加入疏水性油(植物油)以使其更具疏水性和稳定性,和(3)结合交联的互穿网络 刺激性反应性水凝胶进入核心。 水凝胶对任何刺激都有响应,但优选温度或pH。 药物等物质可以并入胶束的致密内核中。当进行超声波处理时,胶束释放物质,然后当超声波转动时,可逆地还原成稳定的致密核心并重新封装物质 关闭 通过脉冲超声波,因此可以以对应于超声信号的脉冲方式可控地释放物质。