Transdermal permeation of trimetazidine from nerodilol-based HPMC gel drug reservoir system across rat epidermis

ABSTRACT

To study the in vitro transdermal permeation of trimetazidine from hydroxypropylmethyl cellulose [HPMC] gel drug reservoir system using nerodilol as a penetration enhancer. An HPMC gel containing selected concentrations of nerodilol [0, 2, 4 or 5% w/v] and 2.5% w/v of trimetazidine was prepared, and subjected to in vitro permeation studies across rat epidermis. The amount of trimetazidine permeated at different time intervals [1, 2, 4, 8, 12, 18 and 24 h] was estimated, and the data were analyzed to calculate various permeation parameters. There was an increase in the amount of trimetazidine [8,719.7 +/- 153.3 micro g/cm[2]] permeated across the rat epidermis up to 24 h [Q[24]] with an increase in nerodilol concentration [5% w/v] in HPMC gel drug reservoir. However, no significant difference [p > 0.05] was observed in the amount of drug permeated [Q[24]] with 5% w/v of nerodilol when compared to that obtained with 4% w/v of nerodilol [8,484.5 +/- 165.8 micro g/ cm[2]]. Nerodilol, at a concentration of 4% w/v enhanced the flux of trimetazidine across rat epidermis by about 1.96 times when compared to control. The HPMC gel drug reservoir containing 4% w/v of nerodilol showed optimal transdermal permeation of trimetazidine