Assessment of the percutaneous penetration of cisplatin: The effect of monoolein and the drug skin penetration pathway

• Published in: European journal of pharmaceutics and biopharmaceutics 2009-09, Vol.73 (1), p.90-94
• Main Authors: Simonetti, Leonardo D.D., Gelfuso, Guilherme M., Barbosa, Julie C.R., Lopez, Renata F.V.
• Format: Article
• Language: English
• Subjects: Administration, Cutaneous; Animals; Barrier function; Biological and medical sciences; Cisplatin; Cisplatin - administration & dosage; Cisplatin - metabolism; Drug Synergism; General pharmacology; Glycerides - administration & dosage; Glycerides - metabolism; In Vitro Techniques; Medical sciences; Monoolein; Permeability - drug effects; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Signal Transduction - drug effects; Signal Transduction - physiology; Skin - drug effects; Skin - metabolism; Skin Absorption - drug effects; Skin Absorption - physiology; Skin penetration; Stratum corneum; Swine
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2009.04.016

It was intended to examine the in vitro penetration of cisplatin (CIS) through porcine skin in the presence of different concentrations of monoolein (MO) as well as to verify the main barrier for CIS skin penetration. In vitro skin penetration of CIS was studied from propylene glycol (PG) solutions containing 0%, 5%, 10%, and 20% of MO using Franz-type diffusion cell and porcine ear skin. Pretreatment experiments with MO and experiments with skin without stratum corneum (SC) were also carried out. Skin penetration studies of CIS showed that the presence of MO doubled the drug permeation through the intact skin. However, permeation studies through the skin without SC caused only a small enhancement of CIS permeation compared to intact skin. Moreover, pretreatment of skin with MO formulations did not show any significant increase in the flux of the drug. In conclusion, MO did not act as a real penetration enhancer for CIS, but it increased the drug partition to the receptor solution improving CIS transdermal permeation. The absence of improvement in drug permeation by MO pretreatment and by the removal of SC indicates that the SC is not the main barrier for the permeation of the metal coordination compound.