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Critical Reviews™ in Therapeutic Drug Carrier Systems
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ISSN Druckformat: 0743-4863
ISSN Online: 2162-660X

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Critical Reviews™ in Therapeutic Drug Carrier Systems

DOI: 10.1615/CritRevTherDrugCarrierSyst.2015010903
pages 149-180

Ligand-Appended BBB-Targeted Nanocarriers (LABTNs)

Ankit Jain
Institute of Pharmaceutical Research, GLA University, 17km Stone, NH-2, Mathura-Delhi Road P.O. Chaumuhan, Mathura, Uttar Pradesh 281406, India
Sanjay Kumar Jain
Pharmaceutics Research Projects Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Central University, Sagar (M.P.), India


Delivering therapeutics across the blood brain barrier (BBB) remains the rate-limiting step in brain medicine research. Three main categories of endogenous transportation at BBB that can be used for targeting brain are carrier-mediated transport, active efflux transport, and receptor-mediated transport. Various approaches using nanocarriers such as liposomes, niosomes, micelles, and nanoparticles with manifested surface modifications using either covalent or noncovalent methods to append suitable ligands are being intensively explored to achieve drug delivery to the brain. Harvested ligands include peptide, glutathione, transferrin, and transferrin antibody, lectins, lactic acid, cholera toxin B, etc. In this review, we present recent insights into the development of safe and efficient brain drug delivery as well as recent advances in BBB targeting tactics including antibody-directed enzyme prodrug therapy, a biotin-avidin conjugated system, and chimeric peptides. This review serves as an excellent source of knowledge for budding brain researchers.