1,1,2-Trisnorsqualenoic acid was conjugated to paclitaxel to obtain the squalenoyl–paclitaxel prodrugwith the aim to improve the incorporation in phospholipid bilayers. Differential scanning calorimetrytechnique was employed to compare the interaction of squalenoyl–paclitaxel prodrug and free paclitaxelwith phospholipid bilayers. The possibility of using lipid vesicles as carrier for the prodrug was alsoevaluated. An increased encapsulation into phospholipid bilayers of squalenoyl–paclitaxel with respectto the free drug was observed. The ability of lipid vesicles to retain the loaded prodrug was also observedwhich make this system to be considered as carrier for the prodrug.
Squalenoyl prodrug of paclitaxel: synthesis and evaluation of its incorporation in phospholipid bilayers
SARPIETRO, MARIA GRAZIA;CASTELLI, Francesco
2012-01-01
Abstract
1,1,2-Trisnorsqualenoic acid was conjugated to paclitaxel to obtain the squalenoyl–paclitaxel prodrugwith the aim to improve the incorporation in phospholipid bilayers. Differential scanning calorimetrytechnique was employed to compare the interaction of squalenoyl–paclitaxel prodrug and free paclitaxelwith phospholipid bilayers. The possibility of using lipid vesicles as carrier for the prodrug was alsoevaluated. An increased encapsulation into phospholipid bilayers of squalenoyl–paclitaxel with respectto the free drug was observed. The ability of lipid vesicles to retain the loaded prodrug was also observedwhich make this system to be considered as carrier for the prodrug.File | Dimensione | Formato | |
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