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Immunomicelles: Targeted pharmaceutical carriers for poorly soluble drugs

机译:免疫球蛋白:针对难溶性药物的靶向药物载体

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摘要

To prepare immunomicelles, new targeted carriers for poorly soluble Pharmaceuticals, a procedure has been developed to chemically attach mAbs to reactive groups incorporated into the corona of polymeric micelles made of polyethylene glycol-phosphati-dylethanolamine conjugates. Micelle-attached antibodies retained their ability to specifically interact with their antigens. Immunomi-celles with attached antitumor mAb 2C5 effectively recognized and bound various cancer cells in vitro and showed an increased accumulation in experimental tumors in mice when compared with nontargeted micelles. Intravenous administration of tumor-specific 2C5 immunomicelles loaded with a sparingly soluble antican-cer agent, taxol, into experimental mice bearing Lewis lung carcinoma resulted in an increased accumulation of taxol in the tumor compared with free taxol or taxol in nontargeted micelles and in enhanced tumor growth inhibition. This family of pharmaceutical carriers can be used for the solubilization and enhanced delivery of poorly soluble drugs to various pathological sites in the body.
机译:为了制备免疫胶束(难溶性药物的新的靶向载体),已经开发了一种程序,可将mAb化学连接到由聚乙二醇-磷脂-二乙醇胺共轭物制成的聚合物胶束的电晕中并入的反应性基团。附着胶束的抗体保留了与其抗原特异性相互作用的能力。与非靶向胶束相比,带有抗肿瘤单抗2C5的免疫细胞在体外能有效识别并结合各种癌细胞,并在小鼠实验肿瘤中显示出增加的积累。与携带游离紫杉醇或紫杉醇的非靶向胶束相比,向带有Lewis肺癌的实验小鼠静脉内注射载有微溶性抗癌剂紫杉醇的肿瘤特异性2C5免疫胶束可导致紫杉醇在肿瘤中的积累增加,而在非靶向胶束和增强的肿瘤中生长抑制。该系列药物载体可用于将难溶性药物溶解和增强向体内各种病理部位的递送。

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