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1. 发明授权

US08956648B2 Calciumphosphate-based nanoparticles as carrier-systems for photodynamic therapy 有权
标题翻译：基于磷酸钙的纳米粒子作为光动力疗法的载体系统
公开(公告)号：US08956648B2
公开(公告)日：2015-02-17
申请号：US13140855
申请日：2009-12-18
申请人： Burkhard Gitter , Susanna Gräfe , Arno Wiehe , Volker Albrecht , Matthias Epple , Janine Schwiertz , Kathirvel Ganesan
发明人： Burkhard Gitter , Susanna Gräfe , Arno Wiehe , Volker Albrecht , Matthias Epple , Janine Schwiertz , Kathirvel Ganesan
IPC分类号： A61P35/00 , A61P31/04 , A61K9/14 , A61K31/5415 , B82Y5/00 , A61K9/51 , A61K41/00 , A61K49/00
CPC分类号： A61K9/5115 , A61K41/0057 , A61K41/0071 , A61K49/0093 , Y10S977/773
摘要： 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, 5,10,15,20-tetrakis(4-phosphonooxyphenyl)porphine (pTPPP) 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.
摘要翻译：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，5,10,15,20-四（4-膦酰氧基苯基）卟吩（pTPPP）是用于光动力学肿瘤治疗的优选亲水性光敏剂。在另一个优选的实施方案中，已经发现亲水性阳离子和阴离子光敏剂，特别是吩嗪鎓，吩噻嗪和呫吨系列的亲水性阳离子和阴离子光敏剂是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的光敏剂。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。

2. 发明申请

US20110257586A1 CALCIUMPHOSPHATE-BASED NANOPARTICLES AS CARRIER-SYSTEMS FOR PHOTODYNAMIC THERAPY 审中-公开
标题翻译：基于钙磷酸盐的纳米颗粒作为光化学治疗的载体系统
公开(公告)号：US20110257586A1
公开(公告)日：2011-10-20
申请号：US13140855
申请日：2009-12-18
申请人： Burkhatd Gitter , Susanna Grafe , Arno Wiehe , Volker Albrecht , Matthias Epple , Janine Schwiertz , Kathirvel Ganesan
发明人： Burkhatd Gitter , Susanna Grafe , Arno Wiehe , Volker Albrecht , Matthias Epple , Janine Schwiertz , Kathirvel Ganesan
IPC分类号： A61M37/00 , A61K31/409 , A61K31/675 , A61P35/00 , A61P31/04 , A61K9/14 , A61K31/5415 , B82Y5/00
CPC分类号： A61K9/5115 , A61K41/0057 , A61K41/0071 , A61K49/0093 , Y10S977/773
摘要： 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, 5,10,15,20-tetrakis(4-phosphonooxyphenyl)porphine (pTPPP) 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.
摘要翻译：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，5,10,15,20-四（4-膦酰氧基苯基）卟吩（pTPPP）是用于光动力学肿瘤治疗的优选亲水性光敏剂。在另一个优选的实施方案中，已经发现亲水性阳离子和阴离子光敏剂，特别是吩嗪鎓，吩噻嗪和呫吨系列的亲水性阳离子和阴离子光敏剂是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的光敏剂。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。

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