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Arsenic trioxide liposomes: encapsulation efficiency and in vitro stability
Paraskevi Kallinteri1, Dimitrios Fatouros, Pavlos Klepetsanis
1Laboratory of Pharmaceutical Technology, Department of Pharmacy, University of Patras, Rio, Greece.
Journal of Liposome Research
|October 6, 2004
Summary
Researchers developed liposomes to encapsulate arsenic trioxide (ATO) for cancer therapy. DSPC/Chol liposomes, particularly DRV types, showed superior ATO retention compared to PC/Chol liposomes, suggesting improved drug delivery potential.
Area of Science:
- Pharmaceutical Nanotechnology
- Drug Delivery Systems
- Cancer Therapeutics
Background:
- Arsenic trioxide (ATO) shows promise in cancer treatment, evidenced by its approval for relapsed promyelocytic leukemia.
- Minimizing ATO's toxicity requires advanced drug delivery systems, such as liposomes, to control its release and reduce side effects.
Purpose of the Study:
- To prepare and characterize liposomes encapsulating arsenic trioxide (ATO) as a potential cancer therapy carrier.
- To evaluate the encapsulation efficiency and in vitro stability of ATO-loaded liposomes with different lipid compositions and types.
Main Methods:
- Preparation of three liposome types: large multilamellar vesicles (MLV), small unilamellar vesicles (SUV), and dried reconstituted vesicles (DRV).
- Utilized thin film hydration, sonication, and DRV methods for liposome preparation with EggPC/Chol or DSPC/Chol lipid compositions.
- Assessed ATO encapsulation using energy-dispersive X-ray fluorescence spectroscopy or atomic absorption, and evaluated drug retention after incubation at 37°C.
Main Results:
- ATO encapsulation efficiency varied from 0.003 to 0.506 mol/mol of lipid, with DRV vesicles showing the highest and SUV the lowest.
- PC/Chol liposomes exhibited poor ATO retention (>70% release within 24 hours), while DSPC/Chol liposomes demonstrated significantly better retention (54% retained in DRV after 24 hours).
- Temperature influenced ATO release in PC/Chol MLV liposomes but had a minimal, statistically insignificant effect on DSPC/Chol liposomes.
Conclusions:
- DSPC/Chol liposomes, especially DRV, offer superior in vitro stability for encapsulating arsenic trioxide compared to PC/Chol liposomes.
- These findings suggest that DSPC/Chol-based liposomes are promising candidates for developing safer and more effective arsenic trioxide drug delivery systems in cancer therapy.