Loading and release of the anti cancer drug paclitaxel in liposome preparations studied in-situ by X-ray diffraction and calorimetry measurements

摘要

Loading and release of the hydrophobic anti-cancer drug paclitaxel in liposome preparations was investigated by X-ray diffraction and differential scanning calorimetry (DSC) measurements. Indication for high solubility of the drug in liposome membranes from lipids with unsaturated (oleic acid) acyl chains in the liquid crystalline phase was found. Together with other parameters, like the liposomewater partition coefficient and the solubility in either phase, the results provide a valuable basis for the assessment of fundamental stability limits of paclitaxel formulations. Lipids with oleic acid chains appear to be particularly suitable for manufacturing of paclitaxel liposome formulations.