School of Pharmaceutical Sciences, Liaocheng University, Liaocheng 252059, China.
Molecules. 2023 Mar 31;28(7):3147. doi: 10.3390/molecules28073147.
Antitumor immunity is an essential component of cancer therapy and is primarily mediated by the innate immune response, which plays a critical role in initiating and shaping the adaptive immune response. Emerging evidence has identified innate immune checkpoints and pattern recognition receptors, such as CD47 and Toll-like receptor 7 (TLR7), as promising therapeutic targets for cancer treatment. Based on the fusion protein Fc-CV1, which comprises a high-affinity SIRPα variant (CV1), and the Fc fragment of the human IgG1 antibody, we exploited a preparation which coupled Fc-CV1 to imiquimod (TLR7 agonist)-loaded liposomes (CILPs) to actively target CT26. WT syngeneic colon tumor models. In vitro studies revealed that CILPs exhibited superior sustained release properties and cell uptake efficiency compared to free imiquimod. In vivo assays proved that CILPs exhibited more efficient accumulation in tumors, and a more significant tumor suppression effect than the control groups. This immunotherapy preparation possessed the advantages of low doses and low toxicity. These results demonstrated that a combination of immune checkpoint blockade (ICB) therapy and innate immunity agonists, such as the Fc-CV1 and imiquimod-loaded liposome preparation utilized in this study, could represent a highly effective strategy for tumor therapy.
抗肿瘤免疫是癌症治疗的重要组成部分,主要由先天免疫反应介导,先天免疫反应在启动和塑造适应性免疫反应中起着关键作用。新出现的证据已经确定了先天免疫检查点和模式识别受体,如 CD47 和 Toll 样受体 7(TLR7),作为癌症治疗有前途的治疗靶点。基于由高亲和力 SIRPα 变体(CV1)和人 IgG1 抗体的 Fc 片段组成的融合蛋白 Fc-CV1,我们利用将 Fc-CV1 与咪喹莫特(TLR7 激动剂)负载的脂质体(CILP)偶联的制剂来主动靶向 CT26.WT 同基因结肠肿瘤模型。体外研究表明,CILP 与游离咪喹莫特相比,具有更好的持续释放特性和细胞摄取效率。体内试验证明,CILP 在肿瘤中的积累效率更高,比对照组具有更显著的肿瘤抑制作用。这种免疫治疗制剂具有低剂量和低毒性的优点。这些结果表明,免疫检查点阻断(ICB)治疗与先天免疫激动剂的联合应用,如本研究中使用的 Fc-CV1 和咪喹莫特负载脂质体制剂,可能代表一种治疗肿瘤的高效策略。