Hydroxypropyl β cyclodextrins effects on self-assembly of cyclic peptide, lanreotide acetate, in water and subsequent release rate from an in vitro emulator of subcutaneous delivery
Year: 2024
Type: article
Abstract: Most of the peptide drugs are often delivered subcutaneously. The significant barrier in this type of peptide administration is the high concentration of formulation, which can lead to self-assembly and aggregation. These phenomena can negatively impact the peptide drug's bioavailability, manufacturing, and injectability. This study investigated the self-assembly behavior of Lanreotide acetate at high concentrations in water using Hydroxypropyl β- Cyclodextrins (HPβCyD) to mitigate the self-assembly and enhance release rate during subcutaneous administration. Our finding demonstrated that the lanreotide/ HPβCyD inclusion complex effectively prevents aromatic-aromatic interactions of lanreotide, thereby controlling self-assembly. This complexation also alters the viscosity behavior of lanreotide from non-Newtonian under low shear rates to Newtonian solution. Furthermore, the lanreotide/ HPβCyD inclusion complex reduces interactions with hyaluronic acid in the subcutaneous environment, leading to significant improvement in the release rate of lanreotide acetate at high concentrations (above 3 % w/w in water).
Authors: Negar Jafari, Camille Addison, Hao Lou, Michael J. Hageman
Institution: University of Kansas
Language: English
Subfield: Pharmaceutical Science
Domain: Life Sciences
Open Access status: hybrid
Estimated APC paid: $3,620
OpenAlex ID: W4404870216
