Penetration enhancing effect of menthol on the percutaneous flux of nicardipine hydrochloride through excised rat epidermis from hydroxypropyl cellulose gels.
The aim of the present investigation is to study the penetration enhancing effect of menthol on the percutaneous flux of nicardipine hydrochloride through the excised rat epidermis from 2% w/w hydroxypropyl cellulose (HPC) gel system. The HPC gel formulations containing nicardipine hydrochloride and selected concentrations of menthol (0-12% w/w) were prepared, and evaluated for in vitro permeation of the drug through excised rat abdominal epidermis. The percutaneous flux of nicardipine hydrochloride across rat epidermis was enhanced markedly by the addition of menthol to the HPC gels. A maximum flux of nicardipine hydrochloride (227.70 +/- 1.30 micrograms cm-2 hr-1) was observed with an enhancement ratio of 7.12 when menthol was incorporated at a concentration of 8% w/w in a reservoir HPC system. The differential scanning calorimetry and Fourier transform-infrared spectroscopy data indicated that menthol increased the percutaneous flux of nicardipine hydrochloride through the rat skin by partial extraction of lipids in the stratum corneum. The results suggest that menthol may be useful for increasing the skin permeability of nicardipine hydrochloride from transdermal therapeutic system containing HPC gel as a reservoir.
Krishnaiah
Y S R
YS
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam-530003, India. krishnaysr112@rediffmail.com
Satyanarayana
V
V
Karthikeyan
R S
RS
D000465:Algorithms; D000818:Animals; D002121:Calcium Channel Blockers / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000031:analogs & derivatives*; D002851:Chromatography, High Pressure Liquid; D005782:Gels; D066298:In Vitro Techniques; D008297:Male; D008610:Menthol / Q000494:pharmacology*; D009529:Nicardipine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D051381:Rats; D012869:Skin Absorption / Q000187:drug effects*; D017550:Spectroscopy, Fourier Transform Infrared
D002121:Calcium Channel Blockers; D005782:Gels; D008610:Menthol; D002482:Cellulose; C008079:hydroxypropylcellulose; D009529:Nicardipine