Nanoparticulate peptide delivery exclusively to the brain produces tolerance free analgesia
Lisa Godfrey, Antonio Iannitelli, Natalie L. Garrettc, Julian Moger, Ian Imbert, Tamara King, Frank Porreca, Ramesh Soundararajan, Aikaterini Lalats, Andreas G. Schätzlein, Ijeoma F. Uchegbu
Journal of Controlled Release
There is pharmacological evidence of activity of MET enabled enkephalin in morphine-tolerant animals.
We believe the preliminary data from these early animal studies of NES100 support our belief that NES100 may have comparable preclinical activity to morphine in all animal pain models tested without the drug seeking, respiratory depression, and tolerance associated with opioids.
Currently, enkephalins are limited in their therapeutic potential by their pharmacokinetic profiles due to their inability to cross the blood-brain barrier to reach opioid receptors located in the central nervous system.