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    • 8. 发明申请
    • NANOPARTICLE CARRIER SYSTEMS BASED ON POLY(DL-LACTIC-CO-GLYCOLIC ACID) (PLGA) FOR PHOTODYNAMIC THERAPY (PDT)
    • 基于聚合(DL-LACTIC-CO-GLYCOLIC ACID)(PLGA)用于光化学治疗(PDT)的纳米载体系统
    • WO2011071970A2
    • 2011-06-16
    • PCT/US2010/059367
    • 2010-12-08
    • BIOLITEC, INC.LANGER, KlausKNOBLOCH, ThomasRÖDER, BeatePREUSS, AnnegretALBRECHT, VolkerGRÄFE, SusannaWIEHE, Arnovon BRIESEN, HagenLÖW, KarinWAGNER, Sylvia
    • LANGER, KlausKNOBLOCH, ThomasRÖDER, BeatePREUSS, AnnegretALBRECHT, VolkerGRÄFE, SusannaWIEHE, Arnovon BRIESEN, HagenLÖW, KarinWAGNER, Sylvia
    • A61K47/30A61K33/20A61K9/127A61P35/00A61P27/02A61P29/00
    • A61K9/5153A61K33/20A61K41/0071
    • Compositions, which are stable in storage, and a method of production of pharmaceutical based nanoparticutate formulations for clinical use in photodynamic therapy comprising a hydrophobic photosensitizer, poly(lactic-co-glycolic) acid and stabilizing agents are provided. These nanoparticulate pharmaceutical formulations provide therapeutically effective amounts of photosensitizer for parenteral administration. In particular, tetrapyrrole derivatives can be used as photosensitizers, whose efficacy and safety are enhanced by such nanoparticulate formulations. It also leaches the method of preparing PLGA-based nanoparticles under sterile conditions. In one of the preferred embodiments of the present invention PLGA-based nanoparticles have a mean particle size less than 500nm and the photosensitizer is temoporfϊn, 5,10,15,20-tetrakis(3-hydroxyphenyl)-chlorin ( m THPC). In another embodiment, the photosensitizer 2,3-dihydroxy-5,10,15,20-tetrakis(3- hydroxyphenyl)-chlorin ( m THPD-OH) is formulated as a nanoparticle for parenteral administration. Yet, in another embodiment preferred photosensitizer is 5,10,15,20-tetrakis(3- hydroxyphenyl)-porphyrin ( m THPP). The formulations can be used for treating hyperptasic and neoplasia conditions, inflammatory problems, and more specifically to target tumor cells.
    • 提供了在储存中稳定的组合物以及用于临床用于光动力疗法的基于药物的纳米颗粒制剂的方法,其包括疏水性光敏剂,聚(乳酸 - 共 - 乙醇酸)酸和稳定剂。 这些纳米颗粒药物制剂提供治疗有效量的用于肠胃外给药的光敏剂。 特别地,四吡咯衍生物可以用作光敏剂,其功效和安全性通过这种纳米颗粒制剂增强。 它还浸出了在无菌条件下制备基于PLGA的纳米颗粒的方法。 在本发明的一个优选实施方案中,基于PLGA的纳米颗粒具有小于500nm的平均粒度,并且光敏剂是temoporf TM,5,10,15,20-四(3-羟基苯基) - 氯化物(mTHPC)。 在另一个实施方案中,将光敏剂2,3-二羟基-5,10,15,20-四(3-羟基苯基) - 青霉素(mTHPD-OH)配制成用于肠胃外给药的纳米颗粒。 然而,在另一个实施方案中,优选的光敏剂是5,10,15,20-四(3-羟基苯基) - 卟啉(mTHPP)。 该制剂可用于治疗高血压和瘤形成症状,炎症问题,更具体地用于靶向肿瘤细胞。