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1. 发明授权

US08153111B2 Photo-triggered release of active substances from dendrimer-photosensitizer complexes 失效
标题翻译：从树枝状大分子光敏剂复合物照片触发释放活性物质
公开(公告)号：US08153111B2
公开(公告)日：2012-04-10
申请号：US10871676
申请日：2004-06-18
申请人： Volker Albrecht , Arno Wiehe , Beate Roeder , Wolfgang Neuberger
发明人： Volker Albrecht , Arno Wiehe , Beate Roeder , Wolfgang Neuberger
IPC分类号： A61K31/00 , A61K9/00
CPC分类号： A61K31/785 , A61K41/00 , A61K47/59 , A61K47/595 , Y10S424/16 , A61K2300/00
摘要： Compositions of dendrimer-photosensitizer complexes including therapeutic molecules, and methods for their synthesis and use are disclosed. The therapeutic molecules and the photosensitizers are each covalently attached to the dendrimer at its end-groups, essentially randomly. Upon exposure to radiation of a suitable wavelength, the photosensitizers are activated to break up the dendrimer structure and thus release the therapeutic molecules. In a preferred embodiment, the end-groups of the dendrimer are replaced with or covalently connected to therapeutic molecules and photosensitizers. In a further preferred embodiment, targeting molecules may also be attached to the dendrimer to create a more accurate treatment. The present invention is especially useful for medical applications, where therapeutic molecules can be delivered to body areas for treatment of a variety of diseases without risk of premature release in the body, due to the strength and stability of the bonds between the end-groups and the photosensitizers and therapeutic molecules.
摘要翻译：公开了包括治疗分子的树枝状大分子光敏剂复合物的组合物及其合成和使用的方法。治疗分子和光敏剂在其端基基本上随机共价连接到树枝状大分子。在暴露于合适波长的辐射下，激活光敏剂以分解树枝状聚合物结构，从而释放治疗分子。在优选的实施方案中，树枝状大分子的端基被治疗分子和光敏剂替代或共价连接。在另一个优选的实施方案中，靶向分子也可以连接到树枝状大分子以产生更准确的处理。本发明特别适用于医疗应用，其中治疗分子可以递送到身体区域以治疗各种疾病，而不会在体内过早释放的风险，这是由于端基之间的键的强度和稳定性光敏剂和治疗分子。

2. 发明申请

US20050281777A1 Photo-triggered release of active substances from dendrimer-photosensitizer complexes 失效
标题翻译：从树枝状大分子光敏剂复合物照片触发释放活性物质
公开(公告)号：US20050281777A1
公开(公告)日：2005-12-22
申请号：US10871676
申请日：2004-06-18
申请人： Volker Albrecht , Arno Wiehe , Beate Roeder , Wolfgang Neuberger
发明人： Volker Albrecht , Arno Wiehe , Beate Roeder , Wolfgang Neuberger
IPC分类号： A61K31/785 , A61K41/00 , A61K47/48
CPC分类号： A61K31/785 , A61K41/00 , A61K47/59 , A61K47/595 , Y10S424/16 , A61K2300/00
摘要： Compositions of dendrimer-photosensitizer complexes including therapeutic molecules, and methods for their synthesis and use are disclosed. The therapeutic molecules and the photosensitizers are each covalently attached to the dendrimer at its end-groups, essentially randomly. Upon exposure to radiation of a suitable wavelength, the photosensitizers are activated to break up the dendrimer structure and thus release the therapeutic molecules. In a preferred embodiment, the end-groups of the dendrimer are replaced with or covalently connected to therapeutic molecules and photosensitizers. In a further preferred embodiment, targeting molecules may also be attached to the dendrimer to create a more accurate treatment. The present invention is especially useful for medical applications, where therapeutic molecules can be delivered to body areas for treatment of a variety of diseases without risk of premature release in the body, due to the strength and stability of the bonds between the end-groups and the photosensitizers and therapeutic molecules.
摘要翻译：公开了包括治疗分子的树枝状大分子光敏剂复合物的组合物及其合成和使用的方法。治疗分子和光敏剂在其端基基本上随机共价连接到树枝状大分子。在暴露于合适波长的辐射下，激活光敏剂以分解树枝状聚合物结构，从而释放治疗分子。在优选的实施方案中，树枝状大分子的端基被治疗分子和光敏剂替代或共价连接。在另一个优选的实施方案中，靶向分子也可以连接到树枝状大分子以产生更准确的处理。本发明特别适用于医疗应用，其中治疗分子可以递送到身体区域以治疗各种疾病，而不会在体内过早释放的风险，这是由于端基之间的键的强度和稳定性光敏剂和治疗分子。

3. 发明申请

US20120101427A1 NOVEL PHOTOSENSITIZER FORMULATIONS FOR ORAL ADMINISTRATION 审中-公开
标题翻译：用于口腔管理的新型光敏剂配方
公开(公告)号：US20120101427A1
公开(公告)日：2012-04-26
申请号：US13266056
申请日：2009-04-28
申请人： Gerard Farmer , Gerhard Wieland , Dietrich Scheglmann , Arno Wiehe , Susanna Gräfe , Nikolay E. Nufantiev , Volker Albrecht , Wolfgang Neuberger
发明人： Gerard Farmer , Gerhard Wieland , Dietrich Scheglmann , Arno Wiehe , Susanna Gräfe , Nikolay E. Nufantiev , Volker Albrecht , Wolfgang Neuberger
IPC分类号： A61M37/00 , A61K31/498 , C07D487/22 , C07D241/46 , A61K9/127 , A61K38/02 , A61K31/7056 , A61K31/706 , A61K31/79 , A61P35/00 , A61P17/00 , A61P9/00 , A61P19/02 , A61P31/04 , A61P33/02 , A61P31/12 , A61P31/00 , A61K31/409 , B82Y5/00
CPC分类号： A61K31/122 , A61K31/40 , A61K31/498 , A61K41/0071
摘要： The present invention provides novel drug formulations for oral administration for diverse medical applications including anticancer, antimetastatic, antibacterial, antifungal, antiprotozoic, antiviral, antiprionic and PDT treatments for diagnostic and therapeutic purposes. In a preferred embodiment the oral drug formulation comprises a photosensitizer and suitable excipients and may be administered in multiple doses over an extended period of time with exposure to activating radiation occurring generally between individual doses or in a light-independent manner. In another preferred embodiment PDT methods for treating hyperplasia and neoplasia, for localizing hyperplasic and neoplasic tissues and pathogen bacteria by fluorescence, for treating infections caused by pathogen bacteria in complex body fluids and for fat reduction, skin disorders and vascular diseases are provided.
摘要翻译：本发明提供用于口服给药以用于各种医学应用的新型药物制剂，包括用于诊断和治疗目的的抗癌，抗转移，抗细菌，抗真菌，抗原生动脉，抗病毒，抗细胞和PDT治疗。在优选的实施方案中，口服药物制剂包含光敏剂和合适的赋形剂，并且可以在延长的时间段内以多个剂量施用，暴露于通常在单独剂量之间或以轻轻独立的方式发生的活化辐射。在另一个优选实施方案中，提供了用于治疗增生和瘤形成的PDT方法，用于通过荧光定位超基质和新生组织和病原体细菌，用于治疗复杂体液中由病原体引起的感染和用于减脂，皮肤病和血管疾病。

4. 发明授权

US08815931B2 Oral formulations for tetrapyrrole derivatives 有权
标题翻译：四吡咯衍生物的口服制剂
公开(公告)号：US08815931B2
公开(公告)日：2014-08-26
申请号：US12768244
申请日：2010-04-27
申请人： Susanna Gräfe , Nikolay Nifantiev , Albrecht Volker , Wolfgang Neuberger , Gerhard Wieland , Dietrich Scheglmann , Alfred Fahr , Arno Wiehe
发明人： Susanna Gräfe , Nikolay Nifantiev , Albrecht Volker , Wolfgang Neuberger , Gerhard Wieland , Dietrich Scheglmann , Alfred Fahr , Arno Wiehe
IPC分类号： A61K31/40 , A61K9/127 , A61K31/498 , A61K9/00 , A61K31/409
CPC分类号： A61K31/409 , A61K9/0065 , A61K9/127 , A61K9/1271 , A61K31/498
摘要： Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles. The oral formulation, in case of a hydrophobic photosensitizer in the present invention, is stabilized using suitable surfactants/solubilizers thus preventing aggregation of the drug in the stomach and until it is absorbed in the duodenum and the small intestine. Oral formulations can be administered in the form of liquid, capsule, tablet, powder, paste or gel. Formulated drugs can be administered orally as one single dose or in multiple doses before administering PDT. In one embodiment Temoporfin (m-THPC) is used as a photosensitizer in the oral formulations. Temoporfin like many hydrophobic photosensitizers are especially suitable to be administered orally because there is no known enzyme system in the mammalian body which can metabolize Temoporfin or similar photosensitizers. Temoporfin can reach the blood system unchanged and fully active after absorption of the formulation in the gastrointestinal tract.
摘要翻译：提出了在光动力治疗（PDT）和抗微生物光动力疗法（APDT）治疗中配制口服光敏剂的口服制剂和方法。口服配制的光敏剂显示增加的溶解度和渗透性，从而提高光敏剂在治疗部位的生物利用度。口服给药的光敏剂适于配制用于通过胃肠粘膜进行粘膜粘附和吸收。本文提供的口服制剂通过口服途径使用脂质和已知蛋白质作为光敏剂的载体。用于封装预选光敏剂的载体包括常规脂质体，聚乙二醇化脂质体，纳米乳剂，纳米胶体，纳米颗粒，脂肪乳剂，脂质制剂，水溶胶，SMEDDS，α-铁蛋白（AFP）和牛血清白蛋白（BSA），脂肪乳剂，热熔融挤出物和纳米颗粒。在本发明的疏水性光敏剂的情况下，使用合适的表面活性剂/增溶剂稳定口服制剂，从而防止药物在胃中的聚集，直到其被吸收到十二指肠和小肠中。口服制剂可以以液体，胶囊，片剂，粉末，糊剂或凝胶的形式施用。配制药物可以在给予PDT之前以一次剂量或多次剂量口服给药。在一个实施方案中，Temoporfin（m-THPC）用作口服制剂中的光敏剂。类似于许多疏水性光敏剂的Temoporfin特别适合于口服给药，因为哺乳动物体内没有已知的可以代谢Temoporfin或类似光敏剂的酶系统。 Temoporfin可以在胃肠道吸收制剂后达到血液系统不变和充分活性。

5. 发明申请

US20100273803A1 Oral Formulations for Tetrapyrrole Derivatives 有权
标题翻译：四吡咯衍生物的口服制剂
公开(公告)号：US20100273803A1
公开(公告)日：2010-10-28
申请号：US12768244
申请日：2010-04-27
申请人： Susanna Gräfe , Nikolay Nifantiev , Albrecht Volker , Wolfgang Neuberger , Gerhard Wieland , Dietrich Scheglmann , Alfred Fahr , Arno Wiehe
发明人： Susanna Gräfe , Nikolay Nifantiev , Albrecht Volker , Wolfgang Neuberger , Gerhard Wieland , Dietrich Scheglmann , Alfred Fahr , Arno Wiehe
IPC分类号： A61K31/498 , C07D241/46 , A61K31/409 , C07D487/22 , A61P35/00 , A61P31/00 , A61K8/49 , A61Q19/00 , A61Q9/00
CPC分类号： A61K31/409 , A61K9/0065 , A61K9/127 , A61K9/1271 , A61K31/498
摘要： Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles. The oral formulation, in case of a hydrophobic photosensitizer in the present invention, is stabilized using suitable surfactants/solubilizers thus preventing aggregation of the drug in the stomach and until it is absorbed in the duodenum and the small intestine. Oral formulations can be administered in the form of liquid, capsule, tablet, powder, paste or gel. Formulated drugs can be administered orally as one single dose or in multiple doses before administering PDT. In one embodiment Temoporfin (m-THPC) is used as a photosensitizer in the oral formulations. Temoporfin like many hydrophobic photosensitizers are especially suitable to be administered orally because there is no known enzyme system in the mammalian body which can metabolize Temoporfin or similar photosensitizers. Temoporfin can reach the blood system unchanged and fully active after absorption of the formulation in the gastrointestinal tract.
摘要翻译：提出了在光动力治疗（PDT）和抗微生物光动力疗法（APDT）治疗中配制口服光敏剂的口服制剂和方法。口服配制的光敏剂显示增加的溶解度和渗透性，从而提高光敏剂在治疗部位的生物利用度。口服给药的光敏剂适于配制用于通过胃肠粘膜进行粘膜粘附和吸收。本文提供的口服制剂通过口服途径使用脂质和已知蛋白质作为光敏剂的载体。用于封装预选光敏剂的载体包括常规脂质体，聚乙二醇化脂质体，纳米乳剂，纳米胶体，纳米颗粒，脂肪乳剂，脂质制剂，水溶胶，SMEDDS，α-铁蛋白（AFP）和牛血清白蛋白（BSA），脂肪乳剂，热熔融挤出物和纳米颗粒。在本发明的疏水性光敏剂的情况下，使用合适的表面活性剂/增溶剂稳定口服制剂，从而防止药物在胃中的聚集，直到其被吸收到十二指肠和小肠中。口服制剂可以以液体，胶囊，片剂，粉末，糊剂或凝胶的形式施用。配制药物可以在给予PDT之前以一次剂量或多次剂量口服给药。在一个实施方案中，Temoporfin（m-THPC）用作口服制剂中的光敏剂。类似于许多疏水性光敏剂的Temoporfin特别适合于口服给药，因为哺乳动物体内没有已知的可以代谢Temoporfin或类似光敏剂的酶系统。 Temoporfin可以在胃肠道吸收制剂后达到血液系统不变和充分活性。

6. 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。

7. 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。

8. 发明申请

US20120263625A1 GLYCO-SUBSTITUTED DIHYDROXY-CHLORINS AND ß-FUNCTIONALIZED CHLORINS FOR ANTI-MICROBIAL PHOTODYNAMIC THERAPY 有权
标题翻译：用于抗微生物光化学治疗的GLYCO取代的二羟基氯和ß-功能氯化物
公开(公告)号：US20120263625A1
公开(公告)日：2012-10-18
申请号：US13189113
申请日：2011-07-22
申请人： Daniel Aicher , Volker Albrecht , Burkhard Gitter , Christian B. W. Stark , Arno Wiehe
发明人： Daniel Aicher , Volker Albrecht , Burkhard Gitter , Christian B. W. Stark , Arno Wiehe
IPC分类号： C07H15/26 , A61L2/08
CPC分类号： A61K31/185 , A61K31/19 , A61K31/409 , A61K31/7056 , A61K41/0071 , A61K47/549 , C07H15/26
摘要： Antimicrobial molecular conjugates for the treatment and prevention of infectious diseases caused by pathogenic microorganisms in human and animals are provided. The key to these conjugates is connecting dihydroxychlorins or β-functionalized chlorins to carbohydrate moieties. These conjugates are found to be very effective in combating bacterial infections caused by Gram-positive and Gram-negative bacteria, including their resistant strains. Significantly, they are also effective in complex environments, including blood, serum, and other body fluids which are present in patient's body. A method of use to control pathogenic microorganisms in human and animals is also provided.
摘要翻译：提供了用于治疗和预防人和动物中致病微生物引起的感染性疾病的抗微生物分子缀合物。这些缀合物的关键是将二羟基二氢卟酚或二官能化的二氢卟酚连接到碳水化合物部分。发现这些缀合物对抗革兰氏阳性和革兰氏阴性细菌（包括其抗性菌株）引起的细菌感染是非常有效的。值得注意的是，它们在复杂的环境中也是有效的，包括血液，血清和患者体内存在的其他体液。还提供了用于控制人和动物中的病原微生物的方法。

9. 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。

10. 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。

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