Practical Liposomal Formulation for Taxanes with Polyethoxylated Castor Oil and Ethanol with Complete Encapsulation Efficiency and High Loading Efficiency

Abstract

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.

Targeting Glioblastoma Cells Expressing CD44 with Liposomes Encapsulating Doxorubicin and Displaying Chlorotoxin-IgG Fc Fusion Protein

“…The M-CTX-Fc or human IgG were coupling to liposome using classical method by employing the maleimide-thiol addition reaction [ 33 ]. Briefly, 2 mol % of Mal–PEG–DSPE were incubated with Dox loaded liposome at 50 °C for 10 min.…”

Cancer stem cell induction from mouse embryonic stem cells

“…Although mouse and human iPSCs are continuously converted into CSCs (3–6,8,9,25,26), the exact inducing factors are not unknown yet. To find them, microarray gene analysis was performed on these CSCs (25,27) and analysis of CM is also ongoing (data not shown).…”

Hyaluronic Acid-Based Nanocapsules as Efficient Delivery Systems of Garlic Oil Active Components with Anticancer Activity

“…Most studies focused on the molecular effects of these compounds report dissolving DADS [13,14] and DATS [15] in dimethyl sulfoxide (DMSO). However, during the last few decades, there have been an increasing number of works considering the delivery of hydrophobic actives using drug-delivery systems (DDSs) based on, e.g., polymers, including e.g., polysaccharides [16][17][18][19][20], liposomes [21], bilosomes [22]. In particular, the nanoscale systems are of high interest for the encapsulation of hydrophobic pharmaceuticals and nutraceuticals [23][24][25].…”