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热词
    • 4. 发明授权
    • Drug delivery system for the simultaneous delivery of drugs activatable
by enzymes and light
    • 用于同时递送通过酶和光激活的药物的药物递送系统
    • US5258453A
    • 1993-11-02
    • US822924
    • 1992-01-21
    • Jindrich KopecekNancy L. Krinick
    • Jindrich KopecekNancy L. Krinick
    • A61K41/00A61K47/48C08F20/04C08F20/52C08F20/56C08F120/04C08G63/48C08G63/91A61L9/01
    • A61K47/48176A61K41/0071Y10S530/811Y10S530/812Y10S530/815Y10S530/816
    • Compositions for the treatment of cancerous tissues in warm-blooded animals containing both an anticancer drug and a photoactivatable drug attached to copolymeric carriers are made up of a member selected from the group consisting of (a) a copolymeric carrier having attached thereto both an anticancer drug and a photoactivatable drug, (b) a mixture of copolymeric carriers wherein one copolymeric carrier has attached an anticancer drug and the other copolymeric carrier has attached a photoactivatable drug and (c) a combination of (a) and (b). The anticancer drug is attached to the polymeric carrier by side-chains which are stable in the blood stream of the warm-blooded animal but susceptible to hydrolysis by lysosomal enzymes intracellularly. The photoactivatable drug is attached by either the same degradable side-chain or by a non-degradable attachment. The polymer carrier may optionally contain a targeting moiety. Upon administration polymeric macromolecules enter targeted cancer cells by pinocytosis which reduces the side effects normally elicited by the free drugs. A time lag is allowed following administration for optimal uptake of the copolymers in the cancerous tissue for the anticancer agent to begin to take effect. Then a light sources of the appropriate wavelength and energy is to activate the photoactivatable drug. The combined effect of the anticancer agent and photoactivatable drug provides greater cell destruction at reduced dosages and side effects.
    • 用于治疗包含附着在共聚载体上的抗癌药物和可光活化药物的温血动物中的癌组织的组合物由选自以下的成员组成:(a)与抗癌药物 和可光活化药物,(b)共聚载体的混合物,其中一种共聚载体已经附着有抗癌药物,另一种共聚载体附着有可光活化药物,和(c)(a)和(b)的组合。 抗癌药物通过在温血动物的血液中稳定但易于细胞内溶酶体酶水解的侧链的侧链连接到聚合物载体上。 可光活化药物通过相同的可降解侧链或不可降解的附着物连接。 聚合物载体可任选地含有靶向部分。 在施用聚合物大分子时,通过胞饮作用进入靶向的癌细胞,其减少通常由游离药物引起的副作用。 给药后允许时间延迟以使抗癌剂的癌组织中的共聚物的最佳摄取开始起作用。 那么合适的波长和能量的光源就是激活可光活化的药物。 抗癌剂和可光活化药物的组合效果在降低的剂量和副作用下提供更大的细胞破坏。