Effect of PEG6000 on the In Vitro and In Vivo Transdermal Permeation of Ondansetron Hydrochloride from EVA1802 Membranes

Abstract

The objective was to evaluate ethylene vinyl acetate (EVA) copolymer membranes with vinyl acetate content of 18% w/w (EVA1802) for transdermal delivery of ondansetron hydrochloride. The EVA1802 membranes containing selected concentrations (0, 5, 10 and 15% w/w) of PEG6000 were prepared, and subjected to in vitro permeation studies from a nerodilol-based drug reservoir. Flux of ondansetron from EVA1802 membranes without PEG6000 was 64.1 +/- 0.6 microg/cm(2.)h, and with 10%w/w of PEG6000 (EVA1802-PEG6000-10) it increased to 194.9 +/- 4.6 microg/cm(2.)h. However, with 15%w/w of PEG6000, EVA1802 membranes produced a burst release of drug which in turn decreased drug flux. The EVA1802-PEG6000-10 membrane was coated with an adhesive emulsion, applied to rat epidermis and subjected to in vitro permeation studies against controls. Flux of ondansetron from transdermal patch across rat epidermis was 111.7 +/- 1.3 microg/cm(2.)h, which is about 1.3 times the required flux. A TTS was fabricated using adhesive-coated EVA1802-PEG6000-10 membrane and other TTS components, and subjected to in vivo delivery in human volunteers against a control. It was concluded from the comparative pharmacokinetic study that TTS of ondansetron, prepared with EVA1802-PEG6000-10 membrane, provided average steady-state plasma concentration on par with multiple-dosed oral tablets, but with a low percent of peak-to-trough fluctuation.

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

“…It has a molecular weight of 293 Da, a logP value of 2.07 and its pKa is about 7.4 [ 18 , 19 ]. The effects of various vehicles, delivery systems and enhancers on transdermal OND delivery have been reported in the literature [ 19 , 20 , 21 , 22 ], but there are a few reports indicating the possibility of developing transdermal film formulations of OND [ 22 , 23 , 24 , 25 ].…”

Pharmacokinetic parameters of ondansetron in rats after oral solution and transdermal invasomes gel: A comparison study

“…At all times, the mobile phase was filtered through a 0.22 µm microfilter and degassed with a sonicator before being pumped in isocratic mode at a flow rate of 1 ml/min while the eluent was monitored at 216 nm. Using several dilutions of stock solutions by mobile phase, working standard solutions of ONDS were created with a concentration range of 5-100 ng/ml to construct a calibration curve [17]. All of the measurements were done in triplicate.…”

Preparation, Evaluation, and Histopathological Studies of Ondansetron-Loaded Invasomes Transdermal Gel

“…Equation 1 estimated the area of application for human skin required to obtain (Css) and provide a maximum therapeutic effect [26].…”