Oral peptide delivery by tetraether lipid liposomes

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

“…Many efforts have been undertaken to increase the stability and integrity of liposomes in the GIT either by coating the vesicles with polymers, such as chitosan, polyethylene glycol and pectin (Immordino et al, 2006;Nguyen et al, 2011;Parmentier et al, 2011;Kowapradit et al, 2012), or by inclusion of tetraether lipids or gangliosides within their structures (Torchilin, 2005). Recently, BS-liposomes have been investigated as stable carriers for delivering sensitive therapeutic agents and proteins by replacing a fraction of the CH in the lipid bilayers with bile salts (Guan et al, 2011;Niu et al, 2011Niu et al, , 2012Niu et al, , 2014.…”

Liposomes containing lipids from Sulfolobus islandicus withstand intestinal bile salts: An approach for oral drug delivery?

“…Three formulations were prepared: (A) pure egg lecithin (egg PC), (B) egg PC: cholesterol (ratio 80:20, mol%) and (C) egg PC:TLE:cholesterol (70:18:12, mol%) (Parmentier et al, 2011b). The assumed molar mass for the TLE was 1400 g/mol.…”

“…Here, the function of the liposomes is to protect therapeutic agents from premature degradation in the acidic and proteolytic environment of the stomach and upper intestine. In the lower intestine and colon absorption of a range of peptides and even small proteins in therapeutically relevant amounts appears feasible (Hamman et al, 2005;Parmentier et al, 2011b). A key requirement for a successful oral delivery system is thus reasonable stability of the carrier in the gastrointestinal (GI) tract, in order to offer protection to the encapsulated peptide/protein (Sprott et al, 1996).…”

“…Different attempts have been undertaken to improve the liposome-based oral delivery e.g., through incorporation of membrane stabilizing additives and/or absorption enhancers, yet with variable success (Iwanaga et al, 1997;Katayama et al, 2003;Okada et al, 1995;Parmentier et al, 2010;Patel et al, 1982;Ravily et al, 1996). One class of membrane stabilizers, however, has been successfully employed by several groups: membrane lipids isolated from Archaea (Choquet et al, 1994;Li et al, 2011;Parmentier et al, 2014;Parmentier et al, 2011b). Archaea represent a domain of life with good adoptability to survive in hostile environments such as hot springs.…”

Emerging oral controlled-release technology for optimal therapy

“…For better patient compliance to substitute parenteral administration of protein drugs for chronic diseases, several pharmaceutical strategies for oral delivery have been suggested, such as the use of absorption enhancers such as surfactants and small-molecule carriers, enzyme inhibitors, chemical modifications and use of particulate delivery systems (e.g., liposomes, polymeric nanoparticles or poly(ethylene glycol)-chitosan nanoparticles) [21].…”