ANALYSIS OF TRANSDERMAL GEL FORMULATION OF APREPITANT

Abstract

Chemotherapy induced nausea and vomiting is a major problem that affects cancer patients’ quality of life and compliance to treatment regimen. One of the major causes of nausea and vomiting in the cancer patients is drug administration including cytotoxic and opioid analgesics. Its management is a huge burden on medical care and requires the use of rescue medication and emergency admission. Current guidelines propose 5-HT₃ receptor antagonists as a pharmacological intervention for acute and delayed chemotherapy induced nausea and vomiting^[1].  Aprepitant is a newer antiemetic drug that acts as neurokinin 1 receptor antagonist in the chemoreceptor trigger zone and prevents vomiting in patients undergoing chemotherapy. Combination of aprepitant, a 5-HT-3 receptor antagonist, and dexamethasone prevents acute emesis is administered by intra-venous route, which is invasive and possess less patient compliance. Thus, an alternative route for antiemetic therapy could be more advantageous. The Transdermal Drug Delivery System (TDDS) is a novel route for systemic drug delivery through intact skin. It also ensures that compounds are delivered, preferably at a specific rate to the circulation. Due to low solubility of aprepitant, a gel formulation can be developed. Among the various transdermal delivery systems, topical gel technology is preferred due to its superior efficiency, low irritation, longer duration of action (for once daily dosing) and higher patient satisfaction. Lecithin organogels show very promising results in transdermal drug delivery and they are known to be biocompatible. Optimization of the gel can be done by the addition of gelatin and further cross linking agents. They increase the drug permeation and provide for the slow and steady release of drugs.