Cyclodextrins — Useful excipients for oral peptide administration?
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CMC Considerations for conventional oral peptide formulations. Scale up and validation
2022, Oral Delivery of Therapeutic Peptides and ProteinsNovel formulations and drug delivery systems to administer biological solids
2021, Advanced Drug Delivery ReviewsCitation Excerpt :Approaches that are commonly used in small-molecule development have been adapted to peptides to improve their solubility. These methods include the use of surfactants, polymer nanoparticles, solid lipid nanoparticles, microemulsions, liposomes, and micelles [154–161]. However, the most challenging obstacle for the oral delivery of peptides is attaining adequate systemic blood circulation levels due to (a) poor permeation across the intestine epithelial layer and (b) high first-pass clearance.
Improvement of pulmonary absorption of poorly absorbable macromolecules by hydroxypropyl-β-cyclodextrin grafted polyethylenimine (HP-β-CD-PEI) in rats
2015, International Journal of PharmaceuticsApproaches for enhancing oral bioavailability of peptides and proteins
2013, International Journal of PharmaceuticsCitation Excerpt :Inclusion of peptides in β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) cavity resulted in increased chemical and enzymatic stability of these peptides besides improving absorption. The reason for improved absorption may be due to impairment of tight junctional integrity which was observed through enhanced permeation of paracellular marker PEG-4000 (Haeberlin et al., 1996). Cyclodextrins have been shown to enhance chemical and physical stability of peptides and proteins through complexation.
Evaluation of protein stability and in vitro permeation of lyophilized polysaccharides-based microparticles for intranasal protein delivery
2011, International Journal of PharmaceuticsCitation Excerpt :HP-β-CD has also been reported for stabilizing protein molecules in the pharmaceutical formulations (Brewster et al., 1991). The stabilizing effect of HP-β-CD is due to the fact that the aromatic phenylalanine, tyrosine and tryptophan residues of proteins could fit in the hydrophobic internal cavity of CD (Haeberlin et al., 1996). Moreover, it was also reported that sugars with HP-β-CD provide better stability in protein formulations than HP-β-CD alone (Iwai et al., 2007).