Jump to main content
Jump to site search

Issue 3, 2016
Previous Article Next Article

Injectable peptide hydrogels for controlled-release of opioids

Author affiliations

Abstract

Herein, a family of hydrogel-forming peptides was designed starting from the short, tunable and amphipathic hexapeptide hydrogelator H-Phe-Glu-Phe-Gln-Phe-Lys-OH (1). The hydrophobic side chains as well as the nature of both N- and C-termini were modified in order to obtain suitable gelation conditions and drug release profiles for in vivo application. To potentially increase the enzymatic stability, an all-D analogue was prepared as well. After their macroscopic and microscopic characterization by rheology and transmission electron microscopy (TEM) analysis, opioid drugs were encapsulated into the hydrogels and sustained release experiments were carried out. Hydrogel toxicity was assessed in cell viability assays. Based on the physicochemical, mechanical, and noncytotoxic properties, H-Phe-Glu-Phe-Gln-Phe-Lys-NH2 (2) was further investigated for in vivo release of morphine. The antinociceptive effects following subcutaneous injection of the morphine-containing hydrogel 2 was evaluated in a model of thermal nociception using the mouse tail-flick test. Sustained antinociceptive effects over extended periods of time (up to 24 h) for morphine co-formulated with hydrogel 2, compared to morphine injection in solution (effects up to 2 h), were observed.

Graphical abstract: Injectable peptide hydrogels for controlled-release of opioids

Back to tab navigation

Supplementary files

Publication details

The article was received on 30 Sep 2015, accepted on 02 Dec 2015 and first published on 17 Feb 2016


Article type: Research Article
DOI: 10.1039/C5MD00440C
Author version available: Download Author version (PDF)
Citation: Med. Chem. Commun., 2016,7, 542-549
  •   Request permissions

    Injectable peptide hydrogels for controlled-release of opioids

    C. Martin, E. Oyen, J. Mangelschots, M. Bibian, T. Ben Haddou, J. Andrade, J. Gardiner, B. Van Mele, A. Madder, R. Hoogenboom, M. Spetea and S. Ballet, Med. Chem. Commun., 2016, 7, 542
    DOI: 10.1039/C5MD00440C

Search articles by author

Spotlight

Advertisements