Modulation of release of paclitaxel from composite cerasomes

Efforts to improve the stability of liposomes have recently led to the development of organic–inorganic liposomal cerasomes. In this study, we explore the potential to modulate the sustained release of paclitaxel from cerasomes by alteration in vesicle composition. Specifically, composite cerasomes have been prepared from mixtures of cerasome-forming lipid (lipid 1) and 1,2-distearoyl-sn-glycero-3-phosphocholine (lipid 2) via one-step construction. The influences of vesicle composition on the physical properties (e.g., particle diameter and surface charge density), physiochemical and long-term storage stability, drug-loading capacity, and release rates of paclitaxel have been investigated. Notably, a wide range of the release profiles of paclitaxel have been achieved by varying the contents of lipid 2, and the composite vesicles display excellent stability when the percentage content of lipid 2 is lower than 50%. Composite vesicles composed of lipids 1 and 2 at a 1:1 molar ratio also exhibited good cytocompatibility and the released paclitaxel effectively inhibit the proliferation of HeLa cancer cells. Together, the development of composite vesicles offers a promising strategy to obtain excellent stability, good drug-loading capacity and cytocompatibility, and enhanced paclitaxel release in single vesicles.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Composite cerasomes (CCs) were constructed from mixtures of cerasome-forming lipid and DSPC lipid via one-step construction. ► The CCs displayed excellent stability when the percentage content of DSPC lipid was lower than 50%. ► Tuning the sustained release of paclitaxel achieved by varying the contents of DSPC lipid. ► The CCs offers a promising strategy to obtain excellent stability, cytocompatibility and tunable drug release in single vesicles.