The interplay between trehalose and dextran as spray drying precursors for cationic liposomes

• Published in: International journal of pharmaceutics Vol. 652; p. 123798
• Main Authors: Lutta, Anitta, Knopp, Matthias M., Tollemeto, Matteo, Pedersen, Gabriel K., Schmidt, Signe T., Grohganz, Holger, Hagner Nielsen, Line
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 05.03.2024
• Subjects: Dextran; Liposomes; Rehydration kinetics; Solid solubility; Spray drying; Trehalose; Dextran; Spray drying; Rehydration kinetics; Liposomes; Trehalose; Solid solubility
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2024.123798

[Display omitted] Successful oral delivery of liposomes requires formulations designed to withstand harsh gastrointestinal conditions, e.g., by converting to solid-state followed by loading into gastro-resistant delivery devices. The hypothesis was that the use of dextran-trehalose mixtures for spray drying would improve the rehydration kinetics of dried liposomes. The objectives were to determine the protective capacity of trehalose-dextran dehydration precursors and to increase the concentration of liposomes in the dry formulation volume. The study successfully demonstrated that 8.5% dextran combined with 76.5% trehalose protected CAF®04 liposomes during drying, with the liposome content maintained at 15% of the dry powder. Accordingly, the rehydration kinetics were slightly improved in formulations containing up to 8.5% dextran in the dry powder volume. Additionally, a 2.4-fold increase in lipid concentration (3 mM vs 7.245 mM) was achieved for spray dried CAF®04 liposomes. Ultimately, this study demonstrates the significance of trehalose as a primary carrier during spray drying of CAF®04 liposomes and highlights the advantage of incorporating small amounts of dextran to tune rehydration kinetics of spray-dried liposomes.