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    • 2. 发明申请
    • CALCIUMPHOSPHATE-BASED NANOPARTICLES AS CARRIER-SYSTEMS FOR PHOTODYNAMIC THERAPY
    • 基于钙磷酸盐的纳米颗粒作为光化学治疗的载体系统
    • WO2010078941A1
    • 2010-07-15
    • PCT/EP2009/009142
    • 2009-12-18
    • BIOLITEC AGUNIVERSITÄT DUISBURG-ESSENSCHWIERTZ, JanineGANESAN, KathirvelEPPLE, MatthiasWIEHE, ArnoGRÄFE, SusannaGITTER, BurkhardALBRECHT, Volker
    • SCHWIERTZ, JanineGANESAN, KathirvelEPPLE, MatthiasWIEHE, ArnoGRÄFE, SusannaGITTER, BurkhardALBRECHT, Volker
    • A61K41/00A61K9/16
    • A61K9/5115A61K41/0057A61K41/0071A61K49/0093Y10S977/773
    • The present invention provides pharmaceutical photosensitizer-loaded nanoparticle formulations and their methods of preparation for photodynamic therapy, comprising a hydrophobic or hydrophilic photosensitizer, nanoparticulate calcium phosphate and in certain cases auxiliary reagents such as stabilizers. The calcium phosphate-based nanoparticle formulations of the present invention provide excellent storage stability and therapeutically effective amounts of photosensitizer for intravenous or topical administration. In a preferred embodiment, tetrapyrrole derivatives such as porphyrins, chlorins and bacteriochlorins, are the preferred hydrophobic photosensitizers to be formulated in calcium phosphate nanoparticle formulations for photodynamic tumor therapy. Additionally, p TPPP is a preferred hydrophilic photosensitizer for photodynamic tumor therapy. In another preferred embodiment, hydrophilic cationic and anionic photosensitizers, especially those of the phenazinium, phenothiazinium and xanthenes series have been found to inactive pathogen bacteria and are the preferred photosensitizers to be formulated in calcium phosphate nanoparticle formulations for antibacterial photodynamic therapy. In another embodiment, photosensitizing nanoparticle formulations are useful to locate cells, tissues or bacteria by using fluorescence imaging methods.
    • 本发明提供负载药物的光敏剂纳米颗粒制剂及其制备光动力疗法的方法,其包括疏水或亲水性光敏剂,纳米颗粒磷酸钙,在某些情况下,辅助试剂如稳定剂。 本发明的基于磷酸钙的纳米颗粒制剂提供优异的储存稳定性和用于静脉内或局部给药的治疗有效量的光敏剂。 在优选的实施方案中,四吡咯衍生物如卟啉,二氢卟酚和细菌二氢卟酚是拟配制在用于光动力学肿瘤治疗的磷酸钙纳米颗粒制剂中的优选的疏水性光敏剂。 另外,pTPPP是用于光动力学肿瘤治疗的优选的亲水性光敏剂。 在另一个优选的实施方案中,亲水性阳离子和阴离子光敏剂,特别是phenazineium,吩噻嗪和呫吨系列的光敏剂已经被发现为无活性的病原体细菌,并且是配制在用于抗菌光动力学治疗的磷酸钙纳米颗粒制剂中的优选光敏剂。 在另一个实施方案中,光敏纳米颗粒制剂可用于通过使用荧光成像方法定位细胞,组织或细菌。
    • 6. 发明专利
    • BR0013304A
    • 2003-01-07
    • BR0013304
    • 2000-07-28
    • BIOLITEC AGBIOLITEC INC
    • RODER BEATEHACKBARTH STEFFENWOEHLECKE GISELA
    • A61K47/30A61K31/409A61K41/00A61K47/42A61K47/48A61N5/06A61P17/00A61P17/06A61P31/12A61P31/22A61P35/00
    • A method for enhanced Photodynamic Therapy (PDT) treatments by applying dendrimer-photosensitizer complexes to bring multiple photosensitizer moieties to a treatment site is provided. The most benefit is derived for treatments using systemic introduction of the photosensitizer formulation. Photosensitizers are covalently coupled to the peripheral bonding places of dendrimers, using labile bonds which are breakable in preference over bonding within either photosensitizer or dendrimer, and the photosensitizers are separated from the complexes in one or more successive cycles. Tetrapyrroles are the photosensitizers employed. In one embodiment the complex is also bound to an antibody or antibody fragment, which aids in targeting the complex to a desired treatment site. After introduction into a patient, the photosensitizers are controllably released, at the treatment site, from the complexes by either light, chemical, or a combined light/chemical effect. Generally the photosensitizers develop their full photodynamic activity as free molecules after being released from the complex. More than one type of photosensitizer may be bound in the complexes. Release and/or activation may be done in a single step or with repeated steps.
    • 10. 发明专利
    • DE19936997B4
    • 2007-06-14
    • DE19936997
    • 1999-08-02
    • BIOLITEC AG
    • ROEDER BEATEHACKBARTH STEFFENWOEHLECKE GISELA
    • A61K41/00A61K47/30A61K31/409A61K47/42A61K47/48A61N5/06A61P17/00A61P17/06A61P31/12A61P31/22A61P35/00
    • A method for enhanced Photodynamic Therapy (PDT) treatments by applying dendrimer-photosensitizer complexes to bring multiple photosensitizer moieties to a treatment site is provided. The most benefit is derived for treatments using systemic introduction of the photosensitizer formulation. Photosensitizers are covalently coupled to the peripheral bonding places of dendrimers, using labile bonds which are breakable in preference over bonding within either photosensitizer or dendrimer, and the photosensitizers are separated from the complexes in one or more successive cycles. Tetrapyrroles are the photosensitizers employed. In one embodiment the complex is also bound to an antibody or antibody fragment, which aids in targeting the complex to a desired treatment site. After introduction into a patient, the photosensitizers are controllably released, at the treatment site, from the complexes by either light, chemical, or a combined light/chemical effect. Generally the photosensitizers develop their full photodynamic activity as free molecules after being released from the complex. More than one type of photosensitizer may be bound in the complexes. Release and/or activation may be done in a single step or with repeated steps.