Surface charged temoporfin-loaded flexible vesicles: In vitro skin penetration studies and stability

Abstract

In order to increase topical delivery of temoporfin (mTHPC), a highly hydrophobic photosensitizer with low percutaneous penetration, neutral, anionic and cationic flexible liposomes (i.e. flexosomes) were prepared and investigated for their penetration enhancing ability. The in vitro skin penetration study was performed using human abdominal skin mounted in Franz diffusion cells. Besides the effect of surface charge of flexosomes on skin penetration of mTHPC, also its effect on physical properties (particle size, polydispersity index, lamellarity) and physicochemical stability of vesicles was investigated. Photon-correlation spectroscopy revealed that vesicles had after preparation a small particle size and low polydispersity index, while cryo-electron microscopy confirmed that these vesicles were mostly unilamellar and of a spherical shape. Regarding stability, contrasting to anionic flexosomes showing lack of long-term stability, neutral and cationic flexosomes were stable during 9 months storage at 4 °C. As to the penetration enhancing ability, cationic flexosomes possessed the highest, i.e. they delivered the highest mTHPC-amount to stratum corneum and deeper skin layers compared to conventional liposomes, neutral and anionic flexosomes. In conclusion, mTHPC-loaded cationic flexosomes could be a promising tool for delivering mTHPC to the skin, which would be beneficial for the photodynamic therapy of cutaneous malignant or non-malignant diseases.