In Vivo Imaging of the Stability and Sustained Cargo Release of an Injectable Amphipathic Peptide-Based Hydrogel

Abstract

Hydrogels are promising materials for biomedical applications such as tissue engineering and controlled drug release. In the past two decades, the peptide hydrogel subclass has attracted an increasing level of interest from the scientific community because of its numerous advantages, such as biocompatibility, biodegradability, and, most importantly, injectability. Here, we report on a hydrogel consisting of the amphipathic hexapeptide H-FEFQFK-NH, which has previously shown promising in vivo properties in terms of releasing morphine. In this study, the release of a small molecule, a peptide, and a protein cargo as representatives of the three major drug classes is directly visualized by in vivo fluorescence and nuclear imaging. In addition, the in vivo stability of the peptide hydrogel system is investigated through the use of a radiolabeled hydrogelator sequence. Although it is shown that the hydrogel remains present for several days, the largest decrease in volume takes place within the first 12 h of subcutaneous injection, which is also the time frame wherein the cargos are released. Compared to the situation in which the cargos are injected in solution, a prolonged release profile is observed up to 12 h, showing the potential of our hydrogel system as a scaffold for controlled drug delivery. Importantly, this study elucidates the release mechanism of the peptide hydrogel system that seems to be based on erosion of the hydrogel providing a generally applicable controlled release platform for small molecule, peptide, and protein drugs.

Acupoint nanocomposite hydrogel for simulation of acupuncture and targeted delivery of triptolide against rheumatoid arthritis

“…Then, we chose an amphipathic self-assembling peptide FEFQFK to form hydrogel for its favorable biocompatibility and biodegradation which is confirmed to be a potent depot to control the release of different therapeutic agents [ 38 , 39 ]. The mass of peptide is 844.5 Da and the purity is 94.85% (Additional file 1 : Fig.…”

Supramolecular Hydrogels for Protein Delivery in Tissue Engineering

“…In vivo release studies were conducted for a peptide-based supramolecular hydrogel [75]. The hydrogel was formed by self-assembly of the amphipathic hexapeptide H-FEFQFK-NH 2 , and three kinds of model cargos were encapsulated including a small molecule, a 15-residue peptide and a small protein.…”

Advances and Perspectives of Peptide and Polypeptide‐Based Materials for Biomedical Imaging

“…In addition to targeted tumor localization, targeting peptide functionalization of imaging platforms for SPECT and SPECT/CT are widely used to evaluate biodistribution, targeting efficiency, and therapeutic effect. [ 125–129 ]…”

“…www.advancedsciencenews.com www.advnanobiomedres.com peptide functionalization of imaging platforms for SPECT and SPECT/CT are widely used to evaluate biodistribution, targeting efficiency, and therapeutic effect. [125][126][127][128][129] Polypeptide imaging platforms with radionuclides loading are promising for SPECT and SPECT/CT imaging with improved biocompatibility and potential combination of treatment. Recently, Du and co-workers reported a bone-targeting polypeptide-based polymer vesicle for simultaneous imaging and effective malignant bone-tumor treatment (Figure 11).…”