Transdermal delivery of imipramine hydrochloride: development and evaluation (in vitro and in vivo) of reservoir gel formulation.
The in vitro permeation studies of imipramine hydrochloride (IMH) reported earlier from our laboratory showed that a combination of menthol (2.5% w/v) and oleic acid (2.5% w/v) worked well in terms of safety and efficacy. The main objective of this study was to evaluate the in vivo performance of this combination; in order to do that, penetration enhancers were incorporated in a hydro-alcoholic gel of hydroxypropylmethyl cellulose along with IMH and used as the drug matrix in a reservoir transdermal patch. A stability study of IMH gel was performed at 40 degrees C/75% RH for 2 months. The results of this study indicate that gels of IMH stored at 40 degrees C/75% RH turned yellow brown in 2 months and the small change in viscosity of gel at 40 degrees C/75% RH had an insignificant effect on the release rate of IMH from the gel (p>0.05). The in vivo performance of the gel was tested in rats using a reservoir transdermal patch, which consisted of a backing membrane, drug matrix and retaining membrane with an area of 12.5 cm2. Plasma concentrations of 3 microg/ml of IMH were achieved and in a histopathological study 24 h occlusion was found to be safe.
Jain
Amit Kumar
AK
Department of Pharmaceutics, National Institute of Pharmceutical Education and Research (NIPER), Sector 67, Phase-X, Mohali-160062, Punjab, India.
Panchagnula
Ramesh
R
D000279:Administration, Cutaneous; D000818:Animals; D000929:Antidepressive Agents, Tricyclic / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D019540:Area Under Curve; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D004355:Drug Stability; D005260:Female; D005782:Gels; D006801:Humans; D007099:Imipramine / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D008610:Menthol / Q000737:chemistry; D019301:Oleic Acid / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000378:metabolism / Q000473:pathology; D012995:Solubility
D000929:Antidepressive Agents, Tricyclic; D005782:Gels; D008610:Menthol; D019301:Oleic Acid; D007099:Imipramine