Transdermal delivery of haloperidol: i. effect of vehicles

ABSTRACT

The influence of vehicles on transdermal delivery of haloperidol from five different vehicles, propylene glycol [PG], water, Glycerin, Liquid Paraffin [LP] and polyethelene glycol 400 [PEG 400] was investigated. It was observed that the highest cumulative amount penetrated in 24 hours in presence of PG [506 microg] compared to the cumulative amount penetrated the skin from the other vehicles used. [113, 58, 24, and 13 microg for water, Glycerin, PEG 400 and LP respectively] indicate that PG could be a good and effective vehicle for transdermal delivery of haloperidol studies. This effect may be related to alteration of the barrier property of the stratum cornium and thermodynamic activity of the drug in the different vehicles. The solubility of haloperidol in these vehicles was also determined. In vitro Improved Franz diffusion cell and dorsal rabbit skin were utilized in the permeation study. Analysis of variance [ANOVA] indicates that, the differences in the cumulative amount obtained from different vehicles were significant p < 0.05. This result suggests that the mechanism of permeation of haloperidol is passive diffusion. In order to determine the parameters which control the diffusion of haloperidol across the excised rabbit skin from propylene glycol solution formulation, the formulation containing concentration of the drug [20mg/ml] was used to a chief a steady-state of diffusion which may be characterized by zero-order kinetic