Surface tension and wettability in transdermal delivery: a study on the in-vitro permeation of haloperidol with cyclodextrin across human epidermis
Article first published online: 10 JUN 2010
© 2010 The Authors Journal compilation © 2010 Royal Pharmaceutical Society of Great Britain
Journal of Pharmacy and Pharmacology
Special Issue: Recent advances in transdermal drug delivery
Volume 62, Issue 6, pages 770–778, June 2010
How to Cite
Azarbayjani, A. F., Lin, H., Yap, C. W., Chan, Y. W. and Chan, S. Y. (2010), Surface tension and wettability in transdermal delivery: a study on the in-vitro permeation of haloperidol with cyclodextrin across human epidermis. Journal of Pharmacy and Pharmacology, 62: 770–778. doi: 10.1211/jpp.62.06.0014
- Issue published online: 10 JUN 2010
- Article first published online: 10 JUN 2010
- Received August 27, 2009Accepted March 03, 2010
- drug–cyclodextrin complexation;
- skin permeability;
- surface tension;
Objectives The aim of this work was to study the effect of surface tension and contact angle on the permeation of haloperidol across human skin using cyclodextrin derivatives.
Methods Surface tension and contact angle of randomly methylated β-cyclodextrin (RM β-CD) and hydroxypropyl β-cyclodextrin (HP β-CD) solutions were measured. Haloperidol solubility and molecular modelling were carried out using the two cyclodextrin derivatives. In-vitro skin permeation was carried out using human skin models.
Key findings The highest increase in drug solubility was observed when the drug was in solution with pH 5 when compared to non-ionised solution, resulting in a 128-fold increase in the intrinsic solubility of the drug. Surface tension measurements indicate a surface-active effect for RM β-CD and HP β-CD. Contact angle measurements showed that vehicles with higher skin wettability increased the contact of the drug with the skin surface and therefore resulted in higher drug permeation across human epidermis.
Conclusions It is concluded that transdermal flux of a drug through the skin may be optimised by controlling surface tension, drug solubility and skin wettability.