Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2485912 | Journal of Pharmaceutical Sciences | 2010 | 10 Pages |
Abstract
αâTocopheryl succinate (αâTOS) is a semisynthetic analogue of αâtocopherol with selective toxicity to the cancer cells and anticancer activity in vivo. Yet, no suitable formulation of αâTOS for medical application has been reported. Various formulations, for example, solutions in organic solvents, oil emulsions and vesicules prepared by spontaneous vesiculation, polyethylene glycol conjugates and liposomes of various compositions have been tested. We developed and characterised a stable lyophilised liposomeâbased αâTOS formulation. αâTOS (15âmol%) was incorporated into large oligolamellar vesicles (OLVs) composed of soy phosphatidylcholine (SPC) by the method of lipid film hydration followed by extrusion through polycarbonate filters. Stabilised liposomal formulation was prepared by lyophilisation in the presence of sucrose (molar ratio lipid/sucrose, 1:5). The size distribution of the liposomes (130-140ânm, polydispersity index 0.14) as well as the stable lipid and αâTOS contents were preserved during storage in the lyophilised form at 2-8°C for at least 6 months. The data indicate good physical and chemical stability of the lyophilised preparation of αâTOS liposomes that can be used in clinical medicine. © 2009 WileyâLiss, Inc. and the American Pharmacists Association J Pharm Sci 99: 2434-2443, 2010
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Authors
Å tÄpán Koudelka, Josef MaÅ¡ek, Jiri Neuzil, Jaroslav Turánek,