To investigate the percutaneous absorption of naproxen (NPX), used as model anti-inflammatory drug, included in liposomes composed of different lipids, namely stratum corneum lipids (SCL) and phosphatidylcholine/cholesterol (PC/CHOL). Liposomes were produced using reverse-phase evaporation (REV) or thin layer evaporation (TLE). Cryo-TEM showed spherical vesicles and bigger irregular elongated nanoparticles for TLE SCL liposomes. REV resulted in spherical and elongated multilamellar vesicles. X-ray diffraction evidenced La or Lb multilamellar vesicles for PC/CHOL and SCL liposome, respectively. The in vitro study showed a lower NPX flux for SCL with respect to PC/CHOL liposome. Tape stripping corroborates the in vitro findings regarding SCL, suggesting that liposomes create a drug reservoir mixing with SC lipids, whilst PC/CHOL liposome promoted NPX permeation through the skin. Liposome lipid composition seems to affect NPX permeation through the skin. The results of our work outlined how lipid composition of liposomal vesicles could modify the permeation profile of a well-known NSAID, such as NPX. In particular, SCL liposomes demonstrated drug penetration reduction due to the formation of a drug depot in the stratum corneum. On the other hand PC/CHOL liposomes promoted drug permeation in vivo, probably modifying the skin permeability properties. The obtained results may be of value in a rational design and development of dermal formulations.
Liposomal formulations for percutaneous absorption of naproxen: a comparative study
CORTESI, Rita;RAVANI, Laura;ESPOSITO, Elisabetta
2011
Abstract
To investigate the percutaneous absorption of naproxen (NPX), used as model anti-inflammatory drug, included in liposomes composed of different lipids, namely stratum corneum lipids (SCL) and phosphatidylcholine/cholesterol (PC/CHOL). Liposomes were produced using reverse-phase evaporation (REV) or thin layer evaporation (TLE). Cryo-TEM showed spherical vesicles and bigger irregular elongated nanoparticles for TLE SCL liposomes. REV resulted in spherical and elongated multilamellar vesicles. X-ray diffraction evidenced La or Lb multilamellar vesicles for PC/CHOL and SCL liposome, respectively. The in vitro study showed a lower NPX flux for SCL with respect to PC/CHOL liposome. Tape stripping corroborates the in vitro findings regarding SCL, suggesting that liposomes create a drug reservoir mixing with SC lipids, whilst PC/CHOL liposome promoted NPX permeation through the skin. Liposome lipid composition seems to affect NPX permeation through the skin. The results of our work outlined how lipid composition of liposomal vesicles could modify the permeation profile of a well-known NSAID, such as NPX. In particular, SCL liposomes demonstrated drug penetration reduction due to the formation of a drug depot in the stratum corneum. On the other hand PC/CHOL liposomes promoted drug permeation in vivo, probably modifying the skin permeability properties. The obtained results may be of value in a rational design and development of dermal formulations.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
