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

INTERNATIONAL JOURNAL OF PHARMACEUTICS(2024)

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摘要
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 (R) 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 (R) 04 liposomes. Ultimately, this study demonstrates the significance of trehalose as a primary carrier during spray drying of CAF (R) 04 liposomes and highlights the advantage of incorporating small amounts of dextran to tune rehydration kinetics of spray-dried liposomes.
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关键词
Liposomes,Spray drying,Trehalose,otran,Solid solubility,Rehydration kinetics
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