|
| Delivery carriers | Therapeutic material | Modified peptide | Characterizations | Applications | In vivo injection route | Glycemic effect period | Diabetes type | Ref |
|
| ReGel | GLP-1 | ZnGLP-1 in ReGel | Sustained release of zinc-complexed GLP-1 formulated in ReGel (triblocopolymers) | In vitro and in vivo (ZDF rats) | s.c. (1x) | 2 weeks | T2D | [42] |
| VAP and alginate | GLP-1 | VAPG | Rat islets and VAPG macroencapsulated in alginate | In vitro | — | Insulinotropic effect | | [43] |
| PLGA | Exendin-4 | Palmityl-acylated exendin-4 | palmityl-acylated exendin-4 adsorbed onto porous PLGA microparticle | In vitro and in vivo (db/db mice) | Pulmonary (1x) | 5 days | T2D | [44] |
|
| PEG | GLP-1 | mPEG-Lys-GLP-1 | PEGylated GLP-1 peptide with 2 k mPEG at free amine function groups in C-terminal (Lys26 and Lys34) | In vitro and in vivo (SD rats) | i.v. or s.c. (1x) | Pharmaco-kinetics (2 h) | T2D | [45] |
| Exendin-4 and glucagon agonist | Dual-acting hybrid peptide with several mutations | PEGylated either GLP-1 or exendin-4 and a glucagon receptor antagonist peptide with 22 or 43 kDa PEG | In vitro and in vivo (Wistar rats) | s.c. (1x) | 17 h (IPTGT) | T2D | [46] |
| Albumin | GLP-1 | CJC-1131 | GLP-1 with a short covalent reactive chemical linker that interacts with a specific cysteine residue in the albumin molecule | In vitro and in vivo (db/db mice) | i.p. or s.c. (2x daily for 4 weeks) | 6 weeks | T2D | [47] |
| Albumin-PEG | Exendin-4 | HAS-PEG-exendin-4 | Exendin-4-conjugated with human serum albumin via heterobifunctional PEG | In vitro and in vivo (db/db mice) | i.p. (1x) | 120 h | T2D | [48] |
|
| — | GLP-1 | GLP-1 containing disulfide bond | Cysteine residue mutated at position of 10, 23, and 30 in wild-type GLP-1 | In vivo (SD or ZDF rats) | s.c. (7x) | 35 days | T2D | [49] |
| — | GLP-1 or Exexdin-4 | GLP-1 or exendin-4 containing additional disulfide bond and glycine residues | Several cysteine residues mutations in native GLP-1 and insertion of one or more glycine residues at C-terminal | In vitro and in vivo (SD or ZDF rats) | s.c. (7x) | 35 days | T2D | [50] |
|
