Solubilization of poorly soluble PDT agent, meso-tetraphenylporphin, in plain or immunotargeted PEG-PE micelles results in dramatically improved cancer cell killing in vitro
Solubilization of poorly soluble PDT agent, meso-tetraphenylporphin, in plain or immunotargeted PEG-PE micelles results in dramatically improved cancer cell killing in vitro
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DOI：
10.1016/j.ejpb.2005.09.010
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发表时间：
2006-04-01
影响因子：
4.9
通讯作者：
Torchilin, VP
中科院分区：
文献类型：
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作者：
Roby, A;Erdogan, S;Torchilin, VP
用聚乙二醇/磷脂酰乙醇胺偶联物（PEG-PE）制备的非靶向和肿瘤靶向聚合物胶束，有效地溶解了难溶性光动力治疗（PDT）药物中四苯基卟啉（TPP）。将TPP包封在peg - pe基胶束和免疫胶束中（含有抗癌单克隆2C5抗体），在PDT条件下对小鼠（LLC, b16）和人（MCF-7, BT20）癌细胞的体外抗癌作用显著提高。为此，将细胞与TPP或TPP负载的PEG-PE胶束/免疫胶束孵育6或18小时，然后光照射30分钟。光毒性作用取决于TPP浓度和免疫胶束的特异性靶向。在pdt处理的培养中，细胞凋亡水平增加。将抗癌2C5抗体附着在装载tpp的胶束上，在给定时间内提供了最大水平的细胞杀伤。本研究结果表明，含ppp的PEG-PE胶束可能是一种实用的PDT光敏剂配方。(c) 2006 Elsevier B.V.版权所有
Poorly soluble photodynamic therapy (PDT) agent, meso-tetratphenylporphine (TPP), was effectively solubilized using non-targeted and tumor-targeted polymeric micelles prepared of polyethylene glycol/phosphatidyl ethanolamine conjugate (PEG-PE). Encapsulation of TPP into PEG-PE-based micelles and inimunomicelles (bearing an anti-cancer monoclonal 2C5 antibody) resulted in significantly improved anticancer effects of the drug at PDT conditions against murine (LLC, B 16) and human (MCF-7, BT20) cancer cells in vitro. For this purpose, the cells were incubated for 6 or 18 h with the TPP or TPP-loaded PEG-PE micelles/immunomicelles and then light-irradiated for 30 min. The phototoxic effect depended on the TPP concentration and specific targeting by immunomicelles. An increased level of apoptosis was shown in the PDT-treated cultures. The attachment of the anti-cancer 2C5 antibodies to TPP-loaded micelles provided the maximum level of cell killing at a given time. The results of this study showed that TPP-containing PEG-PE micelles may represent a useful formulation of the photosensitizer for practical PDT. (c) 2006 Elsevier B.V. All rights reserved.