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1. 发明申请

US20110142948A1 Nanoparticle Carrier Systems based on Human Serum Albumin for Photodynamic Therapy 有权
标题翻译：基于人血清白蛋白的纳米粒子载体系统用于光动力疗法
公开(公告)号：US20110142948A1
公开(公告)日：2011-06-16
申请号：US12941350
申请日：2010-11-08
申请人： Klaus Langer , Matthias Wacker , Beate Röder , Annegret Preuss , Volker Albrecht , Susanna Gräfe , Arno Wiehe , Hagen von Briesen , Karin Löw , Sylvia Wagner
发明人： Klaus Langer , Matthias Wacker , Beate Röder , Annegret Preuss , Volker Albrecht , Susanna Gräfe , Arno Wiehe , Hagen von Briesen , Karin Löw , Sylvia Wagner
IPC分类号： A61K31/409 , A61K9/00 , A61K9/14 , A61P35/00 , A61P17/00 , A61P27/02 , A61P13/00 , A61P19/02 , A61P29/00 , A61P31/04 , B82Y5/00
CPC分类号： A61K31/409 , A61K9/5169 , A61K41/0071
摘要： Compositions, which are stable in storage, and a method of production of pharmaceutical based nanoparticulate formulations for photodynamic therapy comprising a hydrophobic photosensitizer, human serum albumin (HSA) and stabilizing agent are provided. These nanoparticulate formulations provide therapeutically effective amounts of photosensitizer (PS) for parenteral administration. In particular, tetrapyrrole derivatives can be used as photosensitizers whose efficacy and safety are enhanced by such nanoparticulate formulations. A method of preparing the HSA-based nanoparticles under sterile conditions is also provided. In one of the preferred embodiments of the present invention temoporfin, a hydrophobic PS, is formulated as a nanoparticle for parenteral administration. The formulations are useful for treating hyperplasic and neoplasic conditions, inflammatory problems, and more specifically to target tumor cells.
摘要翻译：提供了在储存中稳定的组合物以及用于光动力疗法的药物基纳米颗粒制剂的制备方法，其包括疏水性光敏剂，人血清白蛋白（HSA）和稳定剂。这些纳米颗粒制剂提供用于胃肠外给药的治疗有效量的光敏剂（PS）。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样的纳米颗粒制剂增强。还提供了在无菌条件下制备基于HSA的纳米颗粒的方法。在本发明的一个优选实施方案中，一种疏水性PS被配制成用于肠胃外给药的纳米颗粒。该制剂可用于治疗过度和肿瘤状况，炎症问题，更具体地涉及靶向肿瘤细胞。

2. 发明授权

US09211283B2 Nanoparticle carrier systems based on human serum albumin for photodynamic therapy 有权
标题翻译：基于人血清白蛋白的纳米粒子载体系统进行光动力学治疗
公开(公告)号：US09211283B2
公开(公告)日：2015-12-15
申请号：US12941350
申请日：2010-11-08
申请人： Klaus Langer , Matthias Wacker , Beate Röder , Annegret Preuss , Volker Albrecht , Susanna Gräfe , Arno Wiehe , Hagen von Briesen , Karin Löw , Sylvia Wagner
发明人： Klaus Langer , Matthias Wacker , Beate Röder , Annegret Preuss , Volker Albrecht , Susanna Gräfe , Arno Wiehe , Hagen von Briesen , Karin Löw , Sylvia Wagner
IPC分类号： A61K9/51 , A61K31/409 , A61K33/20 , A61K41/00
CPC分类号： A61K31/409 , A61K9/5169 , A61K41/0071
摘要： Compositions, which are stable in storage, and a method of production of pharmaceutical based nanoparticulate formulations for photodynamic therapy comprising a hydrophobic photosensitizer, human serum albumin (HSA) and stabilizing agent are provided. These nanoparticulate formulations provide therapeutically effective amounts of photosensitizer (PS) for parenteral administration. In particular, tetrapyrrole derivatives can be used as photosensitizers whose efficacy and safety are enhanced by such nanoparticulate formulations. A method of preparing the HSA-based nanoparticles under sterile conditions is also provided. In one of the preferred embodiments of the present invention temoporfin, a hydrophobic PS, is formulated as a nanoparticle for parenteral administration. The formulations are useful for treating hyperplasic and neoplasic conditions, inflammatory problems, and more specifically to target tumor cells.
摘要翻译：提供了在储存中稳定的组合物以及用于光动力疗法的药物基纳米颗粒制剂的制备方法，其包括疏水性光敏剂，人血清白蛋白（HSA）和稳定剂。这些纳米颗粒制剂提供用于胃肠外给药的治疗有效量的光敏剂（PS）。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样的纳米颗粒制剂增强。还提供了在无菌条件下制备基于HSA的纳米颗粒的方法。在本发明的一个优选实施方案中，一种疏水性PS被配制成用于肠胃外给药的纳米颗粒。该制剂可用于治疗过度和肿瘤状况，炎症问题，更具体地涉及靶向肿瘤细胞。

3. 发明申请

US20110275686A1 NANOPARTICLE CARRIER SYSTEMS BASED ON POLY(DL-LACTIC-CO-GLYCOLIC ACID) (PLGA) FOR PHOTODYNAMIC THERAPY (PDT) 审中-公开
标题翻译：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
公开(公告)号：US20110275686A1
公开(公告)日：2011-11-10
申请号：US12941447
申请日：2010-11-08
申请人： Klaus Langer , Thomas Knobloch , Beate Röder , Annegret Preuß , Volker Albrecht , Susanna Gräfe , Arno Wiehe , Hagen von Briesen , Karin Löw , Sylvia Wagner
发明人： Klaus Langer , Thomas Knobloch , Beate Röder , Annegret Preuß , Volker Albrecht , Susanna Gräfe , Arno Wiehe , Hagen von Briesen , Karin Löw , Sylvia Wagner
IPC分类号： A61K31/409 , A61P35/00 , A61K9/113 , A61K9/14 , A61P29/00 , B82Y5/00
CPC分类号： A61K9/5153 , A61K33/20 , A61K41/0071
摘要： Compositions, which are stable in storage, and a method of production of pharmaceutical based nanoparticulate 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 teaches 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 500 nm and the photosensitizer is temoporfin, 5,10,15,20-tetrakis(3-hydroxyphenyl)-chlorin (mTHPC). In another embodiment, the photosensitizer 2,3-dihydroxy-5,10,15,20-tetrakis(3-hydroxyphenyl)-chlorin (mTHPD-OH) is formulated as a nanoparticle for parenteral administration. Yet, in another embodiment preferred photosensitizer is 5,10,15,20-tetrakis(3-hydroxyphenyl)-porphyrin (mTHPP). The formulations can be used for treating hyperplasic and neoplasic conditions, inflammatory problems, and more specifically to target tumor cells.
摘要翻译：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制备方法，其包括疏水性光敏剂，聚（乳酸 - 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。它还教导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，光敏剂是temoporfin，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）。制剂可用于治疗过度和肿瘤的病症，炎症问题，更具体地用于靶向肿瘤细胞。

4. 发明申请

US20120263739A1 ANTI INTEGRIN ANTIBODIES LINKED TO NANOPARTICLES LOADED WITH CHEMOTHERAPEUTIC AGENTS 审中-公开
标题翻译：与用化学药剂负载的纳米颗粒连接的抗体整合抗体
公开(公告)号：US20120263739A1
公开(公告)日：2012-10-18
申请号：US13509492
申请日：2010-10-21
申请人： Klaus Langer , Marion Anhorn , Joerg Kreuter , Florian Rothweiler , Hagen von Briesen , Sylvia Wagner , Martin Michaelis , Jindrich Cinatl
发明人： Klaus Langer , Marion Anhorn , Joerg Kreuter , Florian Rothweiler , Hagen von Briesen , Sylvia Wagner , Martin Michaelis , Jindrich Cinatl
IPC分类号： C07K19/00 , A61P35/00 , A61K39/44
CPC分类号： B82Y5/00 , A61K47/6935
摘要： The invention relates to anti-integrin antibodies which are covalently linked to nanoparticles, wherein these nanoparticles were prior loaded with chemotherapeutic/cytotoxic agents. The antibody-chemotherapeutic agent-nanoparticle conjugates according to the invention, especially wherein the antibody is MAb DI17E6 and the cytotoxic agent is doxorubicin show a significant increase of tumor cell toxicity.
摘要翻译：本发明涉及与纳米颗粒共价连接的抗整联蛋白抗体，其中这些纳米颗粒之前已经加载有化学治疗/细胞毒性剂。根据本发明的抗体 - 化学治疗剂 - 纳米颗粒缀合物，特别是其中抗体是MAb DI17E6，细胞毒性剂是多柔比星显示肿瘤细胞毒性的显着增加。

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