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    • 1. 发明申请
    • ENCAPSULATION OF CHEMICAL COMPOUNDS IN FLUOROUS-CORE AND FLUOROUS-INNER-SHELL MICELLES FORMED FROM SEMIFLUORINATED-BLOCK OR FLUORINATED-BLOCK COPOLYMERS
    • 从半球形或氟化嵌段共聚物形成的氟核心和荧光细胞内细胞中化学化合物的封装
    • WO2005067517A2
    • 2005-07-28
    • PCT/US2005000100
    • 2005-01-03
    • WISCONSIN ALUMNI RES FOUND
    • MECOZZI SANDROHOANG KHANH CONG
    • A61K9/00A61K9/107A61K9/127A61K9/16A61K9/50A61K9/51A61K47/34C08F293/00C08F297/00C08K5/00C08L53/00
    • A61K9/0019A61K9/1075A61K9/1273A61K9/1274A61K31/075A61K47/34C08F293/005C08F297/00C08K5/0008C08L53/00C08L53/005C08L2666/02
    • In one embodiment of the present invention, a block copolymer with a hydrophilic region and a semifluorinated region is synthesized and mixed, below a critical micellar concentration, with a fluorinated drug, and the temperature then lowered, or the block-copolymer concentration then increased, or other solution conditions changed, in order to form fluorous-core, drug-encapsulating micelles. Alternatively, a drug may be taken up by already formed micelles in solution. A suspension of the fluorous-core, fluorinated-drug-encapsulating micelles is injected into the bloodstream to deliver the fluorinated drug to target tissues and organs. In an alternative embodiment of the present invention, a block copolymer with a hydrophilic block, a hydrophobic block, and a semifluorinated block is used to form fluorous-core, drug-encapsulating micelles. In a third embodiment, a block copolymer with a hydrophilic block, a semifluorinated block, and a hydrophobic block is used to form hydrophobic-core, drug-encapsulating micelles. In additional embodiments, block copolymers with various types of blocks are synthesized and employed to form micelles with interior shell and core regions suitable for encapsulating specific target compounds for a variety of purposes.
    • 在本发明的一个实施方案中,合成具有亲水区域和半氟化区域的嵌段共聚物,并在低于临界胶束浓度的情况下与氟化药物混合,然后降低温度,或者嵌段共聚物浓度增加, 或其他溶液条件改变,以形成氟核心,药物封装胶束。 或者,药物可以通过已经形成的溶胶中的胶束吸收。 将含氟的含氟药物包封的胶束的悬浮液注射到血液中以将氟化药物递送至靶组织和器官。 在本发明的另一个实施方案中,使用具有亲水嵌段,疏水嵌段和半氟化嵌段的嵌段共聚物来形成氟核,药物封装胶束。 在第三个实施方案中,使用具有亲水嵌段,半氟化嵌段和疏水嵌段的嵌段共聚物来形成疏水核心的药物封装胶束。 在另外的实施方案中,合成具有各种类型嵌段的嵌段共聚物并且用于形成胶束,其具有适于封装特定目标化合物用于各种目的的内壳和芯区。