在全球范围内，非小细胞肺癌（NSCLC）对人类健康构成重大威胁，占肺癌病例的 80% 以上。顺铂（CDDP）是临床治疗中常用的药物，一直是研究的焦点，旨在通过封装在脂质体中减轻其潜在的毒性。然而，药物装载效率降低和非特异性释放等挑战已成为障碍。本研究旨在通过预先制备CDDP并通过掺入花生凝集素（PNA）作为配体修饰脂质体表面来提高CDDP在脂质体中的包封率[CDDP负载PNA修饰脂质体（CDDP-PNA-Lip） )]。该策略旨在增强 CDDP 向肿瘤组织的递送，从而减少相关的副作用。通过体外研究阐明了 CDDP-PNA-Lip 对高 MUC1 表达的 NSCLC 细胞系增殖和迁移的影响。此外，通过异种移植肿瘤实验评估了 PNA 修饰增强脂质体靶向抗肿瘤功效的能力。结果表明，在体外摄取测定中，与游离 RhB 相比，细胞摄取负载罗丹明 B (RhB) 的 PNA 修饰脂质体的效率高约 50%。此外，与游离 CDDP 相比，CDDP-PNA-Lip 体内肿瘤抑制效果增强了 2.65 倍。这些发现表明，将CDDP封装在配体修饰的脂质体中可以显着提高其肿瘤靶向能力，为临床药物开发提供有价值的见解。

Globally, non‑small cell lung cancer (NSCLC) is a significant threat to human health, and constitutes >80% of lung cancer cases. Cisplatin (CDDP), a commonly used drug in clinical treatment, has been the focus of research aiming to mitigate its potent toxicity through encapsulation within liposomes. However, challenges, such as a reduced drug loading efficiency and nonspecific release, have emerged as obstacles. The present study aimed to improve the encapsulation efficiency of CDDP within liposomes by pre‑preparation of CDDP and modifying the liposome surface through the incorporation of peanut agglutinin (PNA) as a ligand [CDDP‑loaded PNA‑modified liposomes (CDDP‑PNA‑Lip)]. This strategy was designed to enhance the delivery of CDDP to tumour tissues, thereby reducing associated side effects. The effect of CDDP‑PNA‑Lip on the proliferation and migration of NSCLC cell lines with high MUC1 expression was elucidated through in vitro studies. Additionally, the capacity of PNA modification to augment the targeted anti‑tumour efficacy of liposomes was assessed through xenograft tumour experiments. The results indicated that in an in vitro uptake assay Rhodamine B (RhB)‑loaded PNA‑modified liposomes were taken up by cells with ~50% higher efficiency compared with free RhB. In addition, CDDP‑PNA‑Lip resulted in a 2.65‑fold enhancement of tumour suppression in vivo compared with free CDDP. These findings suggested that the encapsulation of CDDP within ligand‑modified liposomes may significantly improve its tumour‑targeting capabilities, providing valuable insights for clinical drug development.