Taxanes including
paclitaxel and
docetaxel are effective
anticancer agents preferably sufficient for liposomal drug delivery. However, the encapsulation of these drugs with effective amounts into conventional
liposomes is difficult due to their high hydrophobicity. Therefore, an effective encapsulation strategy for liposomal
taxanes has been eagerly anticipated. In this study, the mixture of
polyethoxylated castor oil (
Cremophor EL) and
ethanol containing
phosphate buffered saline termed as CEP was employed as a
solvent of the inner hydrophilic core of
liposomes where
taxanes should be incorporated.
Docetaxel-,
paclitaxel-, or 7-oxacetylglycosylated
paclitaxel-encapsulating
liposomes were successfully prepared with almost 100% of encapsulation efficiency and 29.9, 15.4, or 29.1 mol% of loading efficiency, respectively. We then applied the
docetaxel-encapsulating
liposomes for targeted drug delivery.
Docetaxel-encapsulating
liposomes were successfully developed HER2-targeted drug delivery by coupling HER2-specific binding
peptide on
liposome surface. The HER2-targeting
liposomes exhibited HER2-specific internalization and enhanced anticancer activity in vitro. Therefore, we propose the sophisticated preparation of liposomal
taxanes using CEP as a promising formulation for effective
cancer therapies.