School of Pharmacy, Fudan University, Shanghai, P.R. China.
Curr Pharm Biotechnol. 2012 Sep;13(12):2380-7. doi: 10.2174/138920112803341798.
Treatment of malignant gliomas remains a challenge irrespective of the recent improvements. Chemotherapeutic agents for malignant gliomas have been particularly inefficient for the existence of blood-tumor barrier (BTB), which hampers the accumulation and uptake in tumor. Moreover, even though blood-brain barrier (BBB) is compromised to some extent under the situation of malignant gliomas, it remains to be the obstacle influencing the therapeutic efficacies via systemic administration. Fortunately, there are many receptors over-expressed on the BTB (glioma cells and/or tumor microvessels) that can mediate ligand modified drug delivery systems targeting to gliomas and enhance tumor uptake. On the other hand, numerous routes have also been explored to circumvent the BBB. In this manuscript, we elucidate the BBB/BTB status under the situation of malignant gliomas and review the receptors over-expressed on BTB and the malignant gliomas targeted drug delivery strategies. We also discuss the perspective of malignant gliomas targeted drug delivery systems with new concepts.
无论最近有何进展,恶性脑胶质瘤的治疗仍然是一个挑战。用于恶性脑胶质瘤的化疗药物由于血脑肿瘤屏障(BTB)的存在而特别低效,这阻碍了药物在肿瘤中的积累和摄取。此外,尽管在恶性脑胶质瘤的情况下,血脑屏障(BBB)在某种程度上受到了损害,但它仍然是通过全身给药影响治疗效果的障碍。幸运的是,BTB 上有许多过度表达的受体(胶质瘤细胞和/或肿瘤微血管),可以介导配体修饰的药物传递系统靶向胶质瘤,增强肿瘤摄取。另一方面,也已经探索了许多途径来绕过 BBB。在本文中,我们阐明了恶性脑胶质瘤情况下的 BBB/BTB 状态,并综述了 BTB 上过度表达的受体和针对恶性脑胶质瘤的药物传递策略。我们还讨论了具有新概念的恶性脑胶质瘤靶向药物传递系统的前景。