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In vivo stability of ester- and ether-linked phospholipid-containing liposomes as measured by perturbed angular
J T Derksen1, J D Baldeschwieler, G L Scherphof
1Laboratory of Physiological Chemistry, University of Groningen, The Netherlands.
Summary
Liposome composition impacts drug delivery. Ether-linked phospholipids in multilamellar vesicles (MLVs) enhance stability against degradation, suggesting improved intracellular drug depot potential.
Area of Science:
- Biochemistry
- Materials Science
- Pharmacology
Background:
- Liposomes are crucial for drug delivery, acting as carriers for sustained release.
- Understanding liposome degradation is key to optimizing intracellular drug depot formulations.
Purpose of the Study:
- To compare the uptake and degradation of various liposome formulations in rat liver and spleen.
- To evaluate liposome compositions for intracellular sustained-release drug depots.
Main Methods:
- Utilized perturbed angular correlation spectroscopy to assess liposome integrity.
- Injected 111In-labeled liposomes (MLVs and SUVs) of diverse compositions intravenously into rats.
- Quantified liposome recovery and intact percentage in blood, liver, and spleen over time.
Main Results:
- Multilamellar vesicles (MLVs) with dihexadecylglycerophosphorylcholine (DHPC) showed enhanced resistance to lysosomal degradation compared to other phospholipids.
- High phase-transition temperature phospholipids (DSPC, DPPC) in MLVs also slowed degradation but reduced liver uptake.
- Small unilamellar vesicles (SUVs) showed no significant difference in degradation resistance across tested compositions.
Conclusions:
- Ether-linked phospholipids, specifically DHPC in MLVs, offer superior stability for intracellular drug depots.
- Liposome size and phospholipid type significantly influence degradation rates and organ uptake.
- Optimized liposome design is critical for effective sustained drug delivery.