Physical characteristics and in vitro skin permeation of elastic liposomes loaded with caffeic acid-hydroxypropyl-β-cyclodextrin

Abstract

We developed a drug-in-cyclodextrin-in-elastic liposomes (DCEL) system to enhance transdermal delivery of caffeic acid (CA). Hydroxypropyl-β-cyclodextrin (HP-β-CD) was used as a hydrophilic CD. Elastic liposomes (EL) contained polyethylene glycol-free Tego® care 450 as an edge activator. Properties of the CA-HP-β-CD inclusion complex loaded in EL (CD-EL) as DCEL system were compared to characteristics of conventional liposomes (CL), EL, and CD-CL. Particle size, deformability, entrapment efficiency (EE%), stability, and vesicle morphology were characterized in liposome preparations. In addition, in vitro release and skin permeation were analyzed. We found that including Tego® care 450 reduced vesicle size and increased membrane deformability. The addition of HP-β-CD enhanced CA EE% of liposomes almost 1.6-fold that of liposomes without HP-β-CD. Moreover, CD-EL complex showed better controlled release profiles and higher skin permeability than CL and EL. We propose that the DCEL system can be a promising drug delivery vehicle for transdermal delivery of CA.