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CGP 55 847 liposome-delivered zinc(II)-phthalocyanine as a phototherapeutic agent for tumors

机译:CGP 55847脂质体递送的锌(II)-酞菁锌作为肿瘤的光疗剂

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Abstract: Zinc(II)-phthalocyanine (Zn-Pc) was chosen for development as a second-generation photosensitizer for photodynamic therapy (PDT) of tumors and for benign conditions because of its advantageous chemical and photophysical properties. Zn-Pc displayed good selectivity for malignant tissue in pharmacokinetic studies with Meth-A-sarcoma-bearing BALB/c mice when injected in a dose of 0.125 mg/kg, delivered by CGP 55 847. Intravenous doses of Zn-Pc ranging from 0.032 to 0.375 mg/kg caused tumor necrosis and, subsequently, cure of Meth-A-sarcoma-bearing mice when phototreatment was performed 48 hours after injection of CGP 55 847. Intravenous injection of Zn-Pc into hairless mice in doses ranging from 0.1 to 1.0 mg/kg caused dose- and time-dependent phototoxicity. We conclude that the promising pharmacological properties of liposomally delivered Zn-Pc, along with its advantageous chemical and photophysical properties, warrant the development of CGP 55 847 as a candidate drug for photodynamic therapy of tumors in humans. !16
机译:摘要:锌(II)-酞菁(Zn-Pc)具有良好的化学和光物理特性,因此被选作第二代光敏剂,用于肿瘤的光动力疗法(PDT)和良性疾病。在由CGP 55847注射的0.125 mg / kg剂量的含Meth-A肉瘤的BALB / c小鼠的药代动力学研究中,Zn-Pc对恶性组织表现出良好的选择性。静脉注射Zn-Pc的范围为0.032,范围为0.032剂量为0.375 mg / kg会导致肿瘤坏死,随后在注射CGP 55 847后48小时进行光疗时会治愈带有Meth-A肉瘤的小鼠。将Zn-Pc静脉注射到无毛小鼠中的剂量范围为0.1到0.375 mg / kg。 1.0 mg / kg引起剂量和时间依赖性光毒性。我们得出的结论是,脂质体递送的Zn-Pc的有前途的药理性质,以及其有利的化学和光物理性质,保证了CGP 55847的发展,它可以作为人类肿瘤光动力疗法的候选药物。 !16

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