Department of Pharmaceutical Technology, School of Pharmacy, International Medical University, 57000, Kuala Lumpur, Malaysia.
School of Pharmacy, International Medical University, 57000, Kuala Lumpur, Malaysia.
Drug Deliv Transl Res. 2018 Oct;8(5):1545-1563. doi: 10.1007/s13346-018-0552-2.
Treatment of glioblastoma multiforme (GBM) is a predominant challenge in chemotherapy due to the existence of blood-brain barrier (BBB) which restricts delivery of chemotherapeutic agents to the brain together with the problem of drug penetration through hard parenchyma of the GBM. With the structural and mechanistic elucidation of the BBB under both physiological and pathological conditions, it is now viable to target central nervous system (CNS) disorders utilizing the presence of transferrin (Tf) receptors (TfRs). However, overexpression of these TfRs on the GBM cell surface can also help to avoid restrictions of GBM cells to deliver chemotherapeutic agents within the tumor. Therefore, targeting of TfR-mediated delivery could counteract drug delivery issues in GBM and create a delivery system that could cross the BBB effectively to utilize ligand-conjugated drug complexes through receptor-mediated transcytosis. Hence, approach towards successful delivery of antitumor agents to the gliomas has been making possible through targeting these overexpressed TfRs within the CNS and glioma cells. This review article presents a thorough analysis of current understanding on Tf-conjugated nanocarriers as efficient drug delivery system.
多形性胶质母细胞瘤（GBM）的治疗是化疗中的主要挑战，这是由于血脑屏障（BBB）的存在限制了化疗药物向大脑的输送，以及药物穿透 GBM 硬实质的问题。随着 BBB 在生理和病理条件下的结构和机制的阐明，现在可以利用转铁蛋白（Tf）受体（TfRs）来靶向中枢神经系统（CNS）疾病。然而，这些 TfRs 在 GBM 细胞表面的过度表达也有助于避免 GBM 细胞在肿瘤内输送化疗药物的限制。因此，TfR 介导的递药靶向可以对抗 GBM 中的药物递药问题，并创建一个能够有效穿过 BBB 的递药系统，通过受体介导的胞吞作用利用配体偶联的药物复合物。因此，通过靶向 CNS 和神经胶质瘤细胞中这些过表达的 TfRs，使抗肿瘤药物递送到神经胶质瘤成为可能。本文综述了 Tf 结合纳米载体作为有效的药物递药系统的最新研究进展。
