The positively-charged peptide antp derived from Antennapedia transcription protein is demonstrated to mediate the liposome translocation across the cell membrane. In the current investigation, we prepared a stable liposomal doxorubicin (Dox) formulation and targeted it with the antp peptide from 0 to 200 ligand/liposome. These antp-containing liposomes were investigated in terms of physical stability on storage in the refrigerator and upon incubation in blood. Also, other features like cell binding, uptake, biodistribution, and treatment efficiency were evaluated in C26 colon carcinoma BALB/c mice. The Antp in liposomes resulted in enhanced particle growth with the development of the enormously large liposomes from 2000 to 6000 nm. Upon incubation in blood, these large liposomes were removed. The antp also enhanced the cell binding affinity and cell uptake rate of the liposomes and resulted in the restriction of the cancer cell proliferation, but it failed to improve the chemotherapeutic property of the Dox-liposome. The i.v. injection of antp-liposomes (15 mg Dox/kg) caused severe body weight loss and early death incidence due to probably increased toxicity. The antp targeting offered no advantage to the Dox-liposome in the delivery of Dox to the tumor, and failed to enhance the treatment efficiency of the liposomes.

中文翻译：

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触角衍生的带正电荷肽在用作脂质体多柔比星的靶向配体时面临多个问题

来自 Antennapedia 转录蛋白的带正电荷的肽 antp 被证明可介导脂质体跨细胞膜的易位。在目前的研究中，我们制备了一种稳定的脂质体多柔比星 (Dox) 制剂，并用 antp 肽从 0 到 200 个配体/脂质体靶向它。研究了这些含有 antp 的脂质体在冰箱中储存和在血液中孵育时的物理稳定性。此外，在 C26 结肠癌 BALB/c 小鼠中评估了其他特征，如细胞结合、摄取、生物分布和治疗效率。随着超大脂质体从 2000 到 6000 nm 的发展，脂质体中的 Antp 导致颗粒生长增强。在血液中孵育后，这些大脂质体被去除。antp还增强了脂质体的细胞结合亲和力和细胞摄取率，导致癌细胞增殖受到限制，但未能改善Dox-脂质体的化疗性能。由于毒性可能增加，静脉注射 antp-脂质体 (15 mg Dox/kg) 导致严重的体重减轻和早期死亡发生率。antp靶向对Dox-脂质体在将Dox递送至肿瘤方面没有提供任何优势，并且未能提高脂质体的治疗效率。