Studies on optimizing in vitro transdermal permeation of ondansetron hydrochloride using nerodilol, carvone, and limonene as penetration enhancers.
The present investigation was carried out to formulate a terpene-based hydroxypropyl cellulose (HPC) gel drug reservoir system for its optimal transdermal permeation of ondansetron hydrochloride. The HPC gel formulations containing ondansetron hydrochloride (3% w/w) and selected concentrations of either nerodilol (0% w/w, 1% w/w, 2% w/w, 3% w/w, and 4% w/w), carvone (0% w/w, 2% w/w, 4% w/w, 8% w/w, and 10% w/w), or limonene (0% w/w, 2% w/w, 3% w/w, and 4% w/w) were prepared and subjected to in vitro permeation of the drug across rat epidermis. All the 3 terpene enhancers increased the transdermal permeation of ondansetron hydrochloride. The optimal transdermal permeation was observed with 3% w/w of nerodilol (175.3 +/- 3.1 microg/cm(2.)h), 8% w/w of carvone (87.4 +/- 1.6 microg/cm(2.)h), or 3% w/w of limonene (181.9 +/- 0.9 microg/cm(2.)h). The enhancement ratio (ER) in drug permeability with 3% w/w nerodilol, 8% w/w carvone, and 3% w/w limonene were 21.6, 10.8, and 22.5, respectively, when compared with that obtained without a terpene enhancer (control). However, there was 1.04-, 2.09-, and 2.17-fold increase in the optimal drug flux obtained with carvone, nerodilol, and limonene, respectively, when compared with the desired drug flux (84 microg/cm(2.)h). It was concluded that the HPC gel drug reservoir systems containing either 3% w/w nerodilol or 3% w/w limonene act as optimal formulations for use in the design of membrane-controlled transdermal therapeutic system (TTS) of ondansetron hydrochloride.
Krishnaiah
Yellela S R
YS
Department of Pharmaceutics, Faculty of Pharmacy, Kuwait University, Kuwait City, Kuwait. ysrkrishnaiah@hsc.edu.kw
Raju
Vengaladasu
V
Shiva Kumar
Mantri
M
Rama
Bukka
B
Raghumurthy
Vanambattina
V
Ramana Murthy
Kolapalli V
KV
D000279:Administration, Cutaneous; D000818:Animals; D000932:Antiemetics / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D000081005:Cyclohexane Monoterpenes; D053138:Cyclohexenes / Q000494:pharmacology*; D004817:Epidermis / Q000187:drug effects; D005079:Excipients; D005782:Gels; D066298:In Vitro Techniques; D000077222:Limonene; D008297:Male; D039821:Monoterpenes / Q000494:pharmacology*; D017294:Ondansetron / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D051381:Rats; D012869:Skin Absorption / Q000187:drug effects*; D013729:Terpenes / Q000494:pharmacology*
D000932:Antiemetics; D000081005:Cyclohexane Monoterpenes; D053138:Cyclohexenes; D005079:Excipients; D005782:Gels; D039821:Monoterpenes; D013729:Terpenes; C508312:nerodilol; D017294:Ondansetron; C006923:carvone; D000077222:Limonene