Abstract
Nanotechnology has opened up a world of possibilities for the treatment of brain disorders. Nanosystems can be designed to encapsulate, carry, and deliver a variety of therapeutic agents, including drugs and nucleic acids. Nanoparticles may also be formulated to contain photosensitizers or, on their own, serve as photothermal conversion agents for phototherapy. Furthermore, nano-delivery agents can enhance the efficacy of contrast agents for improved brain imaging and diagnostics. However, effective nano-delivery to the brain is seriously hampered by the formidable blood–brain barrier (BBB). Advances in understanding natural transport routes across the BBB have led to receptor-mediated transcytosis being exploited as a possible means of nanoparticle uptake. In this regard, the oligopeptide Angiopep-2, which has high BBB transcytosis capacity, has been utilized as a targeting ligand. Various organic and inorganic nanostructures have been functionalized with Angiopep-2 to direct therapeutic and diagnostic agents to the brain. Not only have these shown great promise in the treatment and diagnosis of brain cancer but they have also been investigated for the treatment of brain injury, stroke, epilepsy, Parkinson’s disease, and Alzheimer’s disease. This review focuses on studies conducted from 2010 to 2021 with Angiopep-2-modified nanoparticles aimed at the treatment and diagnosis of brain disorders.
Highlights
The blood–brain barrier (BBB) is a selectively permeable network of capillary endothelial cells, astroglia, pericytes, and perivascular mast cells, which stringently regulates the exchange of molecules between the blood and the cerebral tissue
Angiopep-2 has been appended to a wide variety of nanostructures for the delivery of therapeutic agents to treat brain disorders, which include cancer, brain injury, stroke, of therapeutic agents to treat brain disorders, which include cancer, brain injury, stroke, epilepsy, fungal infections, Alzheimer’s disease (AD), and Parkinson’s disease (PD)
Angiopep-2 NPs have been applied to the delivery of small interfering RNA (siRNA) against genes involved in brain cancer progression and survival
Summary
The blood–brain barrier (BBB) is a selectively permeable network of capillary endothelial cells, astroglia, pericytes, and perivascular mast cells, which stringently regulates the exchange of molecules between the blood and the cerebral tissue. Understanding the natural routes of transport, such as receptor-mediated transcytosis (RMT), across the BBB has led to the ‘trojan horse’ concept being widely investigated This strategy involves modifying nanoparticles (NPs) with ligands that can bind specific receptors at the apical membrane of brain endothelial cells and promote endocytosis. Angiopep-2 (TFFYGGSRGKRNNFKTEEY, molecular weight 2.4 kDa) is a 19-aminoacid-long oligopeptide that binds to the low-density lipoprotein receptor-related protein-1. Angiopep-2 (TFFYGGSRGKRNNFKTEEY, molecular weight 2.4 kDa) is a 19-aminoacid-long oligopeptide that binds to the low-density lipoprotein receptor-related protein (LRP1) [5]. II sists of three paclitaxel residues linked to Angiopep-2, showed patient benefits in a phase study of adults with recurrent brain metastases arising from breast cancer [14].
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