The peptide-based products that are currently in development in a wide range of diseases are highly promising therapeutic candidates because of their high potency and specificity. However, fast clearance associated with metabolic instability has hampered development and commercialisation. Transiently stable entrapment of peptides in CriPec® nanoparticles might prevent burst release and undesired peak levels, protect peptides against degradation, and enable sustained systemic levels that allow for convenient dosing schedules.
Proof of Concept (PoC) studies have shown the excellent applicability of CriPec for a range of therapeutic peptides, such as leuprolide, octreotide, exenatide and an undisclosed 20+ amino acid peptide. Upon linker-derivatisation, the various peptides were successfully entrapped within CriPec nanoparticles of approximately 60 nm.
Pharmacokinetic studies demonstrated a 50-fold increase of systemic peptide levels upon a single intravenous administration of CriPec peptide, providing clear evidence for the sustained therapeutics levels of the entrapped peptide.
Prolonged systemic levels of free peptide (approx. 1.2 kDa) upon single intravenous administration of either the conventional peptide or CriPec peptide, administered to rats at different doses.