Abstract
Glioma has been considered to be the most frequent primary tumor within the central nervous system (CNS). The complexity of glioma, especially the existence of the blood-brain barrier (BBB), makes the survival and prognosis of glioma remain poor even after a standard treatment based on surgery, radiotherapy, and chemotherapy. This provides a rationale for the development of some novel therapeutic strategies. Among them, receptor-mediated drug delivery is a specific pattern taking advantage of differential expression of receptors between tumors and normal tissues. The strategy can actively transport drugs, such as small molecular drugs, gene medicines, and therapeutic proteins to glioma while minimizing adverse reactions. This review will summarize recent progress on receptor-mediated drug delivery systems targeting to glioma, and conclude the challenges and prospects of receptor-mediated glioma-targeted therapy for future applications.
Highlights
Glioma, which arises from glial cells, is by far the most frequent and lethal brain tumor, accounting for approximately 80% of malignant tumors in the central nervous systems (CNS) [1,2]
The results showed that the peptide itself was a drug delivery system which could cross the blood-brain barrier (BBB) and target to the glioma via the transferrin receptor (TfR)-binding peptide, and further lead to cancer cell death via lysis by the lytic peptide
What’s more, the cell killing effect could be significantly inhibited by suramin, a low-density lipoprotein receptor (LDLR) inhibitor. These results suggested the LDLR-mediated mechanism of nLDL. Some targeting moieties such as ApoB, apolipoprotein E (ApoE), or some peptides corresponding to the LDLR-binding domain of ApoE or ApoB have been proven to be effective in LDLR-targeted therapy of neoplastic diseases [71,72]
Summary
Glioma, which arises from glial cells, is by far the most frequent and lethal brain tumor, accounting for approximately 80% of malignant tumors in the central nervous systems (CNS) [1,2]. Even in combination of currently most effective therapies such as surgery, radiotherapy, and chemotherapy, median survival for high-grade glioma still remains gloomy (14.6 months) [4,5]. This might be attributed to specific properties of glioma, such as the highly infiltrative nature and lack of clear margins. It has been reported that the BBB dysfunction is related to the increasing histological grade of glioma, which implies that the BBB is grossly intact at the early stage, and gradually disrupted with the progress of glioma [14] Based on this occasion, the glioma-targeted drug delivery systems are mainly divided into two categories. Recent progress on receptor-mediated drug delivery systems targeting glioma is summarized according to the amount and type of the targeting moieties
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