Opioid Peptides: Pharmaceutical Significance and Formulation Approaches

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Engin D., TİMUR S. S., Muçaj S., GÜRSOY R. N.

Hacettepe University Journal of the Faculty of Pharmacy, vol.43, no.3, pp.243-260, 2023 (Scopus) identifier


Opioids have been used in pain management for thousands of years due to the pain relief effects that they show by binding to their own receptors. Nowadays, their use continues in a more controlled manner because they have various side effects and a potential for dependence. Researchers have found substances that are naturally synthesized and cause opioid-like effects in the human body. These substances are known as endogenous opioid peptides. Synthetic analogs of these peptides are also synthesized. These compounds are hydrophilic due to their structure, they are charged molecules and their oral administration is limited. There are several approaches to the formulation of opioid peptides. Synthesis of peptide-based hydrogels and conjugation of the compound to a hydrogel, conversion of the peptide into a coumarinic acid-based cyclic prodrug are some of the approaches that protect unstable opioid peptides from enzyme degradation. Nanotechnology has also been used to encapsulate peptides in nanocarriers such as; nanoparticles and liposomes. In this context, research shows that it is possible to administer peptide-based drugs in post-surgical pain management using multivesicular liposomes (DepoFoam). A wide variety of technologies are used in the formulation of these peptides and promising results have been obtained from these studies.