Pulmonary delivery of a GLP-1 receptor agonist, BMS-686117

Development of inhalable dry powder formulation of basic fibroblast growth factor

“…The inactive excipients should satisfy two distinct requirements simultaneously: they should not only be able to provide desirable aerodynamic properties but also be compatible with bFGF. While there are a few known excipients suitable for formation of inhalable dry powders, such as disaccharides (Qian et al, 2009), phospholipids (Codrons et al, 2003), amino acids (Lucas et al, 1999;Li et al, 2003;Seville et al, 2007), or proteins (Codrons et al, 2003), it is unknown whether bFGF is stable in their presence, especially in the solid state.…”

Site of action of a pentapeptide agonist at the glucagon-like peptide-1 receptor. Insight into a small molecule agonist-binding pocket

“…Recently, a smaller peptide consisting of 11 amino acids has been shown to have similar potency to full-length GLP1, and can potentially be delivered via inhalation. 19 The current project is focused on another small molecule lead compound, NRTFD, representing the fragment from the GLP1 receptor that was shown to possess full agonist activity. 9 …”

Pulmonary delivery of dry powders to rats: Tolerability limits of an intra-tracheal administration model

“…Particle size of powder aerosol obtained with the DP device ranges between 1 and 14 m according to the compound (Alcock et al, 2002;Grainger et al, 2004;Koushik et al, 2004;Qian et al, 2009;Ungaro et al, 2009). However, large particle sizes, comparable with those obtained in our study (47-59 m for lactose, about 20 m for magnesium stearate), have also been reported: powder aerosol containing insulin mannitol (5-21 m) (Todo et al, 2003), lipid-based microparticles (4-20 m) (Dellamary et al, 2004), chitosan microparticles (20-150 m) (Huang et al, 2005) and azithromycin loading powders (4.7-52.1 m) (Zhang et al, 2010).…”