Prescription opioids are a crucial component of modern medicine due to the antinociceptive effects of these compounds. Unfortunately, there has been an increase of mortality in recent years from prescription opioid abuse. Opioid receptor agonists form the backbone of pharmaceutical management of pain. We seek to discover new sustained release methods of delivering mu opioid receptor agonists in an intrinsically abuse deterrent formulation. Therefore we synthesized of a novel opioid polymer delivery system that covalently incorporates novel fentanyl derivatives directly into a polymer’s chain end. Our opioid delivery system can alleviate the addictive reward potential of opioids by slowly releasing them from a polymer while maintain longer circulation times. Fentanyl polymers were synthesized from two novel fentanyl based polymerization initiators, with different analgesic potency, by Ring Opening Polymerization (ROP). We used poly(lactic acid) (PLA) and poly(lactic-co-glycolic acid) (PLGA) to prepare fentanyl chain-end functional biodegradable polymers which were formulated into well-defined biocompatible nanoparticles. The nanoparticles were able to deliver therapeutically relevant doses for up to six days in a mouse model of acute nociception from one subcutaneous dose of nanoparticles. Using our novel chemically functionalized fentanyl polymerization initiators; we could utilize advances in material science, polymer chemistry, and controlled drug release. By controlling the rate that opioids are released from the polymer we may limit abuse potential and control the therapeutic onset, preventing the immediate “high” associated with prescription opioid abuse.

Nanoparticle opioid delivery system that covalently incorporates novel fentanyl derivatives for extended controlled release

254th National Meeting (2017)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.