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TTBZ-APEG-PCL nanoparticles
- Development stage
- Preclinical
- Lead developer
- Sun Yat-sen University
- Modality
- Nanoparticles → Drug Delivery Systems, Peptides, Small Molecules
- Administration
- Intravenous
01
Overview
TTBZ-APEG-PCL nanoparticles are an experimental, brain-targeted nanomedicine designed for the treatment of Huntington's disease. The formulation consists of the small molecule drug tetrabenazine (TTBZ) encapsulated within a biodegradable polymeric matrix composed of poly(epsilon-caprolactone) (PCL) and poly(ethylene glycol) (PEG). The surface of the nanoparticle is functionalized with Angiopep-2 (APEG), a peptide ligand that specifically binds to the low-density lipoprotein receptor-related protein 1 (LRP1) expressed on the blood-brain barrier. This targeting mechanism facilitates the transport of the nanoparticles into the central nervous system via receptor-mediated transcytosis. Once in the brain, the sustained release of tetrabenazine inhibits the vesicular monoamine transporter 2 (VMAT2), thereby reducing the chorea symptoms associated with Huntington's disease while potentially minimizing peripheral side effects and improving the drug's pharmacokinetic profile.
- Other names
- Tetrabenazine-loaded Angiopep-2-PEG-PCL nanoparticlesANG-PEG-PCL-TTBZ
02
Targets
PIAS1 (Protein inhibitor of activated STAT 1)VMAT2 (Vesicular monoamine transporter 2)LRP1 (Prolow-density lipoprotein receptor-related protein 1)
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