Abstract
Objective: This study was undertaken to determine the bioavailability of ondansetron gel in experimental animals and humans applying UPLC as an analytical tool and evaluation of the antiemetic effect of ondansetron gel in cisplatin-induced emesis in rats.
 Methods: Ondansetron gel (F13: sodium alginate 7% w/w) was used, marketed I. V. ondansetron (Zofran) ® was chosen as reference. The bioavailability study in rabbits was selected as a parallel design using nine healthy rabbits divided into three groups whereas, bioavailability study in humans was an open-label, wherein 6 healthy subjects administered ondansetron gel. The potential effect of ondansetron gel was evaluated for the prevention of different phases of emesis motivated by exposure to antineoplastic drugs (cisplatin) by determination of body weight loss, water and food intake applying kaolin-pica model in rats using seventy-two rats divided into six groups.
 Results: Ondansetron gel (0.5%) showed detectable plasma concentration 22.833±2.17 ng/m1 after ¼ h and 419.55±2.17 ng/ml after 1-h post-treatment in rabbits and human respectively and concentration was maintained above-reported minimum effective concentration for more than 2.5 h for rabbits and 7 h for humans compared to 1.75 h after I. V. administration.
 The ondansetron gel significantly reduces all phases of cisplatin-induced emesis and a decrease in body weight, water, and food consumption was significantly attenuated.
 Conclusion: Based on the high efficacy of gel on emesis induced by cisplatin, and its high bioavailability, transdermal ondansetron gel could be a promising convenient system to prevent nausea and vomiting following administration of antineoplastic drugs.
Highlights
Ondansetron is a selective 5-HT3 (5-hydroxytryptamine, or serotonin) antagonist receptor [1,2,3,4,5]
Based on the high efficacy of gel on emesis induced by cisplatin, and its high bioavailability, transdermal ondansetron gel could be a promising convenient system to prevent nausea and vomiting following administration of antineoplastic drugs
It is a primary drug utilized to treat, prohibit and stop chemotherapy-induced nausea and vomiting (CINV), it is efficient in prevailing postoperative nausea and vomiting (PONV) and after radiation therapy-induced nausea and vomiting [6,7,8]
Summary
Ondansetron is a selective 5-HT3 (5-hydroxytryptamine, or serotonin) antagonist receptor [1,2,3,4,5]. Intravenous (IV) route has quick effects, but it confers a local pain and for its short half-life, ondansetron requires recurrent administrations. Oral administration has many disadvantages as it not desirable in nausea and vomiting, difficulties occurred in the gastrointestinal tract during absorption due to enzymes, food-drug interactions, etc. Ondansetron transdermal gel was formulated and evaluated from previous in vitro and ex vivo studies [9]. Whereas it is especially suitable for cancer patients who suffer from frequent episodes of vomiting and nausea and they cannot keep the oral dosage form and intravenous chemotherapy formerly worn out their veins
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