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Potential usage of thermosensitive liposomes for macromolecule delivery
1Department of Radiobiochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Japan.
Biochimica Et Biophysica Acta
|May 11, 1994
Summary
Thermosensitive liposomes with a hyper-osmotic internal phase effectively deliver large molecules like dextran. These liposomes swell and release contents at 40-42°C, showing stability in serum.
Area of Science:
- Biotechnology
- Drug Delivery Systems
- Lipid Bilayer Research
Background:
- Liposomes are versatile nanocarriers for drug delivery.
- Transient swelling of liposomes during phase transitions can facilitate macromolecule permeation.
- Hyper-osmotic internal aqueous phases in liposomes can enhance this swelling effect.
Purpose of the Study:
- To investigate the potential of thermosensitive liposomes with a hyper-osmotic internal phase for macromolecule delivery.
- To evaluate the release kinetics of encapsulated macromolecules under specific temperature conditions.
- To assess the stability of these liposomes in the presence of serum.
Main Methods:
- Preparation of thermosensitive liposomes with an internal osmotic pressure twofold higher than physiological levels.
- Sizing of liposomes to approximately 200 nm using a 200-nm pore size filter.
- Incubation of liposomes containing dextran (M(r) 144,000) at temperatures between 40-42°C.
- Assessment of liposome stability in serum-containing media.
Main Results:
- Thermosensitive liposomes effectively released encapsulated macromolecules, including dextran (M(r) 144,000), at 40-42°C.
- Liposomes with a twofold higher internal osmotic pressure demonstrated enhanced macromolecule release.
- These liposomes exhibited greater stability in serum compared to those with an internal osmotic pressure threefold higher than physiological levels.
Conclusions:
- Thermosensitive liposomes with a carefully controlled hyper-osmotic internal phase are effective for delivering macromolecules.
- The temperature-induced swelling mechanism facilitates the release of large molecules through the lipid bilayer.
- Optimized liposome formulations offer improved stability in biological environments like serum, enhancing their therapeutic potential.