Transdermal permeation of trimetazidine from nerodilol-based HPMC gel drug reservoir system across rat epidermis.
OBJECTIVE
To study the in vitro transdermal permeation of trimetazidine from hydroxypropylmethyl cellulose (HPMC) gel drug reservoir system using nerodilol as a penetration enhancer.


METHODS
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.


RESULTS
There was an increase in the amount of trimetazidine (8,719.7 +/- 153.3 microg/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 microg/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.


CONCLUSIONS
The HPMC gel drug reservoir containing 4% w/v of nerodilol showed optimal transdermal permeation of trimetazidine.
Krishnaiah
Yellela S
YS
Department of Pharmaceutics, Faculty of Pharmacy, Kuwait University, Kuwait. ysrkrishnaiah@hsc.edu.kw
Al-Saidan
Saleh M
SM
D000279:Administration, Cutaneous; D000818:Animals; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems / Q000295:instrumentation* / Q000379:methods; D005782:Gels; D066298:In Vitro Techniques; D007785:Lactose / Q000031:analogs & derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives; D023421:Models, Animal; D051381:Rats; D012869:Skin Absorption; D013729:Terpenes / Q000008:administration & dosage*; D014292:Trimetazidine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D014665:Vasodilator Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*
D005782:Gels; D013729:Terpenes; D014665:Vasodilator Agents; C509290:hydroxypropylmethylcellulose-lactose matrix; C508312:nerodilol; D008747:Methylcellulose; D007785:Lactose; D014292:Trimetazidine