Alnemeh-Al Ali H, Bejaud J, Lautram N, Dupont A, Eyer J
Univ Angers, Inserm, CNRS, MINT, SFR ICAT, F-49000 Angers, France.
Univ Rennes, CNRS, Inserm, BIOSIT-UMS 3480, US_S 018 Rennes, France.
Int J Pharm X. 2025 Aug 26;10:100382. doi: 10.1016/j.ijpx.2025.100382. eCollection 2025 Dec.
Peptide conjugated-nanodrug is one of the most studied new treatment options in the field of cancer, including glioblastoma (GBM). This tumour, GBM, is a difficult to treat brain tumour mainly due to its location and the complexity of targeting tumour cells. A promising GBM-targeting peptide (NFL-TBS.40-63) is a cell penetrating peptide (CPP) that has previously demonstrated selectivity against GBM cells and also a capacity to damage their microtubule network at appropriate concentrations. Here, a potential nano-based delivery system was developed by coupling the biotinylated-NFL-peptide (BIOT-NFL) with lipid nanocapsules (LNCs) loaded with Colchicine (Col), an anti-microtubule agent with potent anticancer activity. The effect of BIOT-NFL and free Colchicine was first evaluated on GBM cells. Colchicine was then loaded in lipid nanocapsules (Col-loaded LNCs) and the obtained nanocapsules were characterized for particle size, morphology, encapsulation efficiency and release, and then coupled with the BIOT-NFL-peptide. Interestingly, a potential nanosystem composed of peptide-nanofibers (formed from BIOT-NFL) decorated with Col-LNCs was observed by electron microscopic examination. Finally, the effects of this BIOT-NFL coupled to Col-LNCs were evaluated on GBM cells. This new nanosystem may offer a promising strategy for GBM targeted therapy.
肽偶联纳米药物是癌症领域(包括胶质母细胞瘤,即GBM)研究最多的新型治疗选择之一。这种GBM肿瘤是一种难以治疗的脑肿瘤,主要是由于其位置以及靶向肿瘤细胞的复杂性。一种有前景的GBM靶向肽(NFL-TBS.40-63)是一种细胞穿透肽(CPP),它先前已证明对GBM细胞具有选择性,并且在适当浓度下能够破坏其微管网络。在此,通过将生物素化的NFL肽(BIOT-NFL)与负载秋水仙碱(Col)的脂质纳米胶囊(LNCs)偶联,开发了一种潜在的基于纳米的递送系统,秋水仙碱是一种具有强大抗癌活性的抗微管剂。首先评估了BIOT-NFL和游离秋水仙碱对GBM细胞的作用。然后将秋水仙碱负载到脂质纳米胶囊中(负载Col的LNCs),并对获得的纳米胶囊进行粒径、形态、包封率和释放特性的表征,然后与BIOT-NFL肽偶联。有趣的是,通过电子显微镜检查观察到了一种由用Col-LNCs修饰的肽纳米纤维(由BIOT-NFL形成)组成的潜在纳米系统。最后,评估了这种与Col-LNCs偶联的BIOT-NFL对GBM细胞的作用。这种新的纳米系统可能为GBM靶向治疗提供一种有前景的策略。