Targeted Blood-to-Brain Drug Delivery – 10 Key Development Criteria

Author(s): Pieter J. Gaillard, Corine C. Visser, Chantal C.M. Appeldoorn, Jaap Rip

Journal Name: Current Pharmaceutical Biotechnology

Volume 13 , Issue 12 , 2012

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Drug delivery to the brain remains challenging due to the presence of the blood-brain barrier. In this review, 10 key development criteria are presented that are important for successful drug development to treat CNS diseases by targeted drug delivery systems. Although several routes of delivery are being investigated, such as intranasal delivery, direct injections into the brain or CSF, and transient opening of the blood-brain barrier, the focus of this review is on physiological strategies aiming to target endogenous transport mechanisms. Examples from literature, focusing on targeted drug delivery systems that are being commercially developed, will be discussed to illustrate the 10 key development criteria. The first four criteria apply to the targeting of the blood-brain barrier: (1) a proven inherently safe receptor biology, (2) a safe and human applicable ligand, (3) receptor specific binding, and (4) applicable for acute and chronic indications. Next to an efficient and safe targeting strategy, as captured in key criteria 1 to 4, a favorable pharmacokinetic profile is also important (key criterion 5). With regard to the drug carriers, two criteria are important: (6) no modification of active ingredient and (7) able to carry various classes of molecules. The final three criteria apply to the development of a drug from lab to clinic: (8) low costs and straightforward manufacturing, (9) activity in all animal models, and (10) strong intellectual property (IP) protection. Adhering to these 10 key development criteria will allow for a successful brain drug development.

Keywords: Blood-brain barrier, brain diseases, CNS, drug targeting, receptor-mediated endocytosis, transport/transcytosis, Drug delivery, physiological strategies, blood-brain barrier, Alzheimer’s disease, central nervous system, neurological targets, gene-based medicine, physiological strategies

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Article Details

Year: 2012
Published on: 04 October, 2012
Page: [2328 - 2339]
Pages: 12
DOI: 10.2174/138920112803341815
Price: $65

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