- The challenge of providing effective relief for chronic pain persists, as opioids encounter issues of tolerance and contribute to the ‘opioid epidemic’ through their impact on the central nervous system (CNS).
- Ongoing efforts are directed towards the development of opioids with restricted blood-brain barrier (BBB) penetration, achieved through peripheralization. This involves modifying the hydrophilic group at the C-6 position.
- The addition of polar groups, such as zwitterionic moieties at C-6, serves to prevent entry into the CNS, ensuring selective targeting of the peripheral nervous system.
- A nano carrier-based strategy, utilizing hyperbranched polyglycerols (PG), facilitates the delivery of morphine specifically to peripheral inflammatory tissues. This approach prevents BBB penetration and enhances targeted relief.
- In conclusion, opioid receptors have been identified in the CNS, peripheral nervous system (PNS), and peripheral tissues. Stimulating peripheral opioid receptors results in potent analgesia. Various chemical and pharmacological methods are currently under development to deliver the selective pain-relieving properties of morphine.
Summary of "Peripheralization Strategies Applied to Morphinans and Implications for Improved Treatment of Pain"
Summary published January 10, 2024
