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Abstract
Background: Malignant brain tumors are among the most challenging to treat and at present there are no uniformly successful treatment strategies. Standard treatment regimens consist of maximal surgical resection followed by radiotherapy and chemotherapy. The limited survival advantage attributed to chemotherapy is partially due to low CNS penetration of antineoplastic agents across the blood–brain barrier (BBB). Objective: The objective of this paper is to review recent approaches to delivering anticancer drugs into primary brain tumors. Methods: Both preclinical and clinical strategies to circumvent the BBB are considered that include chemical modification and colloidal carriers. Conclusion: Analysis of the available data indicates that new approaches may be useful for CNS delivery, yet an appreciation of pharmacokinetic issues and improved knowledge of tumor biology will be needed to affect significantly drug delivery to the target site.