Nanoparticulate system for brain delivery of drug is a challenging area, and there are pulsating changes happening almost every day. The blood-brain barrier (BBB) is a vital element in the regulation of the constancy of the internal environment of the brain. The BBB represents an insurmountable obstacle for a large number of drugs, including antibiotics, antineoplastic agents. Despite the certain progress in this area, development of drug targeting technology that enables safe and noninvasive access to the brain remains a challenge, resulting in the emergence of novel strategies. Recently, it was shown that the drugs normally unable to cross the BBB could be delivered to the brain after binding to the surface modified nanoparticles. This book is an attempt to cover the recent trends and emerging technologies in the area of nanoparticulate system for brain delivery of drug. It is our hope that this book will assist and enrich the readers in understanding the brain targeted nanoparticulate drug delivery systems. This book is equally relevant to academic, industrial, as well as scientists working in pharmaceutical drug delivery worldwide.