Please cite this article in press as: Mishra, V., Kesherwani, P. Dendrimer technologies for brain tumor, Drug Discov Today (2016), http://dx.doi.org/10.1016/j.drudis.2016.02.006 Drug Discovery Today  Volume 00, Number 00  February 2016 REVIEWS Ligand-anchored dendrimers have great potential for acceptance in the biomedical field in terms of better brain tumor management. Dendrimer technologies for brain tumor Vijay Mishra Q1 1,3 and Prashant Kesherwani 2,3 1 Pharmaceutical Nanotechnology Research Laboratory, Adina Institute of Pharmaceutical Sciences, Sagar, M.P. 470002, India 2 Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, USA Despite low prevalence, brain tumors are one of the most lethal forms of cancer. Unfortunately the blood–brain barrier (BBB), a highly regulated, well coordinated and efficient barrier, checks the permeation of most of the drugs across it. Hence, crossing this barrier is one of the most significant challenges in the development of efficient central nervous system therapeutics. Surface-engineered dendrimers improve biocompatibility, drug-release kinetics and aptitude to target the BBB and/or tumors and facilitate transportation of anticancer bioactives across the BBB. This review sheds light on different aspects of brain tumors and dendrimers based on different approaches for treatment including recent research, opportunities and challenges encountered in development of novel and efficient dendrimer-based therapeutics for the treatment of brain tumors. Introduction Q2 Around the world, brain cancer remains one of the most important causes of morbidity and mortality. Conventional therapy consists of regimens that include surgical debulking, radiation therapy and systemic chemotherapy. There are several factors underlying the disappointing results in brain cancer therapeutics including limited tumor cell drug uptake, intracellular drug metabolism, inherent tumor sensitivity to chemotherapy and cellular mechanisms of resistance [1]. Poor bioavailability of current therapeutics and imaging agents is a significant obstacle in the treatment and imaging of brain tumors. The greatest obstacle is frequently not drug potency but the physical barriers present at distinct interfaces including the blood vessels of the brain (blood– brain barrier; BBB), the choroid plexus (blood–cerebrospinal-fluid barrier; BCSFB) and the arachnoid layer of the meninges (blood–arachnoid layer), rendering the typical circulatory routes of delivery ineffective [2,3]. The prognosis of malignant glioma is generally poor. The median survival rate could be as low as 14.6 months for the advanced stages of disease [4]. When used alone, the clinical benefit of chemotherapy for brain cancer treatment is very disappointing. Many chemotherapeutic drugs Reviews  FOUNDATION REVIEW Vijay Mishra earned his doctoral degree in ‘pharmaceutical sciences from Dr Hari Singh Gour Central University, Sagar (Madhya Pradesh), India. He received an AICTE Junior Research Fellowship (New Delhi, India) and UGC-BSR Senior Research Fellowship (New Delhi, India). He has co-authored more than 17 international publications and one book on pharmaceutical dosage. His current research interests encompass surface- engineered dendrimers, siRNA delivery, carbon nanotubes and controlled and novel drug delivery systems. Dr Prashant Kesharwani grew up in Sagar, Madhya Pradesh, India. He obtained his PhD in pharmaceutics from Dr Hari Singh Gour Central University, Sagar (Madhya Pradesh), India, in 2014. Dr Kesharwani currently works as a Postdoctoral Fellow in the Department of Pharmaceutical Sciences at Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, USA. His major research expertise lies in the field of nanoengineered drug delivery systems for cancer, with a key focus on dendrimer and polymeric bionanoconjugates. He has received an ICMR Senior Research Fellowship and AICTE Junior Research Fellowship, as well as many honors and awards. Dr Kesharwani is a co-author on more than 40 publications in international journals. Corresponding author: Kesherwani, P. (prashantdops@gmail.com), (prashant_pharmacy04@rediffmail.com) 3 These authors contributed equally to this work. 1359-6446/ß 2016 Published by Elsevier Ltd. http://dx.doi.org/10.1016/j.drudis.2016.02.006 www.drugdiscoverytoday.com 1