Development of ErbB2-Targeting Liposomes for Enhancing Drug Delivery to ErbB2-Positive Breast Cancer
Development of ErbB2-Targeting Liposomes for Enhancing Drug Delivery to ErbB2-Positive Breast Cancer
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DOI：
10.3390/pharmaceutics12060585
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发表时间：
2020-06
期刊：
影响因子：
5.4
通讯作者：
S. Ueno;Min Woo Kim;Gibok Lee;Yong Il Park;T. Niidome;Ruda Lee
中科院分区：
文献类型：
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作者：
S. Ueno;Min Woo Kim;Gibok Lee;Yong Il Park;T. Niidome;Ruda Lee
ErbB2 是一种受体酪氨酸激酶，已知其参与肿瘤发生、肿瘤侵袭性和临床结果。使用治疗性抗体的 ErbB2 靶向疗法在乳腺癌治疗中取得了成功。然而，需要重复治疗和高成本是单克隆抗体疗法的主要缺点。与抗体相比，肽价格便宜、相对稳定、免疫原性低。我们开发了一种高度特异性的癌症靶向药物递送系统，使用靶向肽来最大限度地提高雷帕霉素的治疗效率，并帮助预防 ErbB2 阳性乳腺癌的耐药性。理化表征证实了 ErbB2 靶向脂质体 (ErbB2Lipo) 的成功构建。乱序肽 (ScrErbB2) 与 ErbB2 靶向肽的比较证实，除了靶向能力外，这些肽具有相似的特性。 ErbB2Lipo 在 ErbB2 阳性 BT-474 细胞中表现出比与 ScrErbB2 缀合的非靶向脂质体 (ScrErbB2Lipo) 更高的递送效率。这种肽靶向策略有可能提高 ErbB2 阳性癌症的化疗疗效。
ErbB2 is a type of receptor tyrosine kinase, which is known to be involved in tumorigenesis, tumor aggressiveness, and clinical outcome. ErbB2-targeting therapy using therapeutic antibodies has been successful in breast cancer treatment. However, the need for repeated treatments and the high cost are major disadvantages with monoclonal antibody therapies. Compared with antibodies, peptides are cheap, relatively stable, and have low immunogenicity. We have developed a highly specific cancer-targeting drug delivery system using a targeting peptide to maximize the therapeutic efficiency of rapamycin and to help prevent drug resistance in ErbB2-positive breast cancer. Physicochemical characterization confirmed the successful construction of ErbB2-targeting liposomes (ErbB2Lipo). A comparison of a scrambled peptide (ScrErbB2) with the ErbB2-targeting peptide confirmed that these peptides had similar properties except for the targeting ability. The ErbB2Lipo exhibited higher delivery efficiency in ErbB2 positive BT-474 cells than non-targeting liposomes conjugated with ScrErbB2 (ScrErbB2Lipo). This peptide-targeting strategy has the potential to improve the efficacy of chemotherapy in ErbB2-positive cancers.