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Rapid One-step Enzymatic Synthesis and All-aqueous Purification of Trehalose Analogues
Published on: February 17, 2017
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The interplay between trehalose and dextran as spray drying precursors for cationic liposomes
Anitta Lutta1, Matthias M Knopp2, Matteo Tollemeto3
1Technical University of Denmark, Department of Health Technology, Ørsteds Plads 345C, 2800 Kgs. Lyngby, Denmark; Statens Serum Institut, Department of Infectious Disease and Immunology, Artillerivej 5, 2300 Copenhagen, Denmark.
International Journal of Pharmaceutics
|January 8, 2024
Summary
Spray drying liposomes with trehalose-dextran mixtures enhances oral delivery. This formulation protects liposomes and improves their rehydration, increasing lipid concentration for better drug delivery.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Biomaterials Science
Background:
- Oral delivery of liposomes faces challenges due to harsh gastrointestinal conditions.
- Solid-state formulations and gastro-resistant devices are crucial for successful liposome delivery.
- Spray drying is a key technique for creating stable, solid-state liposome formulations.
Purpose of the Study:
- To evaluate trehalose-dextran mixtures as dehydration precursors for spray-dried liposomes.
- To determine the protective capacity of these excipients during the drying process.
- To optimize liposome concentration and rehydration kinetics in the final dry formulation.
Main Methods:
- Spray drying of CAF®04 liposomes using various trehalose-dextran mixtures.
- Analysis of liposome protection and content in the resulting dry powder.
- Assessment of rehydration kinetics for the optimized formulations.
- Quantification of lipid concentration in the spray-dried liposomes.
Main Results:
- A mixture of 8.5% dextran and 76.5% trehalose effectively protected CAF®04 liposomes during spray drying.
- Liposome content was maintained at 15% of the dry powder formulation.
- Rehydration kinetics showed slight improvement with up to 8.5% dextran.
- A 2.4-fold increase in lipid concentration (from 3 mM to 7.245 mM) was achieved.
Conclusions:
- Trehalose is a significant carrier for spray drying CAF®04 liposomes.
- Incorporating small amounts of dextran can modulate the rehydration properties of spray-dried liposomes.
- This approach enhances liposome stability and lipid concentration for improved oral delivery potential.

