Different in vivo investigated peptide delivery systems for subcutaneous delivery
| Technique | Peptide drug | Outcome | References |
|---|---|---|---|
| mPEG-PLGA-mPEG-based thermosensitive in situ forming gel | Salmon calcitonin (mol. mass 3.5 kDa) | Controlled delivery and pharmacologic activity for 20–40 d | Tang and Singh, 2010 |
| Noncovalent Zn-peptide adduct (spray dried) | BMS-686117 (mol. mass 1.5 kDa) | Terminal half-life prolonged by 6 h and Cmax values reduced 6- to 8-fold compared with solution | Qian et al., 2009 |
| Solution | Exenatide | >100% (due to underestimation of i.v. AUC) | http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_Scientific_-_Discussion/human/000698/WC500051842.pdf |
| Thermoresponsive polylactic acid-polyethylene glycol-polylactic acid triblock copolymer | Insulin | Controlled release of bioactive molecule up to 3 mo | Al-Tahami et al., 2011 |
| Aminoacid modification | Insulin lispro | 55–77% absolute bioavailability | Vugmeyster et al., 2012 |
| Solution | Liraglutide | 55% absolute bioavailability | Stevenson, 2009; Perry, 2011 |
| PLGA microspheres | LXT-101 (LHRH antagonist) | Sustained-delivery system, efficacy | Du et al., 2006 |
| Porous silicon microparticles and nanoparticles | PYY3-36 | Controlled-delivery system, increased bioavailability | Kovalainen et al., 2012, 2013 |
DALCE, [D-Ala2, Leu5, Cys6]-enkephalin; LHRH, luteinizing hormone–releasing hormone.