The effect of lipid composition and liposome size on the release properties of liposomes-in-hydrogel

Abstract

To study the release of liposome-associated drugs into hydrogels, we designed and synthesized two pH-sensitive rhodamine derivatives to use as model compounds of different lipophilicities. The dyes were fluorescent when in the free form released from liposomes into the chitosan hydrogel, but not when incorporated within liposomes. The effect of liposomal composition, surface charge and vesicle size on the release of those incorporated dyes was evaluated. The lipophilicity of the rhodamine derivatives affected both the amount and rate of release. While liposome size had only a minor effect on the release of dyes into the hydrogel, the surface charge affected the release to a greater extent. By optimizing the characteristics of liposomes we could develop a liposomes-in-hydrogel system for application in wound therapy. We further characterized liposomes-in-hydrogel for their rheological properties, textures and moisture handling, as well as their potential to achieve a controlled release of the dye. The polymer-dependent changes in the hydrogel properties were observed upon addition of liposomes. The charged liposomes exhibited stronger effects on the textures of the chitosan hydrogels than the neutral ones. In respect to the ability of the system to handle wound exudates, chitosan-based hydrogels were found to be superior to Carbopol-based hydrogels.

Keywords: Chitosan; Hydrogels; In vitro release; Liposomes; PC; PC ns; PC s; PC/PG; PC/PG ns; PC/PG s; PC/SA; PC/SA ns; PC/SA s; PG; PI; SA; Skin therapy; non-sonicated; non-sonicated phosphatidylcholine liposomes; non-sonicated phosphatidylcholine/octadecylamine; non-sonicated phosphatidylcholine/phosphatidylglycerol liposomes; ns; octadecylamine (=stearylamine); phosphatidylcholine; phosphatidylcholine/octadecylamine; phosphatidylcholine/phosphatidylglycerol; phosphatidylglycerol; polydispersity index; s; sonicated; sonicated phosphatidylcholine liposomes; sonicated phosphatidylcholine/octadecylamine; sonicated phosphatidylcholine/phosphatidylglycerol liposomes.