DEVELOPMENT OF CONTROLLED RELEASE FORMULATION OF PALONOSETRON HYDROCHLORIDE USING NOVEL PARENTERAL DRUG DELIVERY SYSTEM

Abstract

The purpose of this study was to formulate and evaluate Parenteral Controlled Release Formulation of an antiemetic drug using the technology of in situ forming gel, based on temperature change mechanism in order to reduce the frequency of dosing and increase patient compliance in the long term treatment of Chemotherapy induced nausea and vomiting. Formulation was optimized, prepared, filled aseptically, sterilized and evaluated for prerequisites of Parenterals and other parameters like gelation temperature, gel strength, viscosity, drug content, in vitro and in vivo studies and stability studies. It was prepared using cold method and optimized by 3³ factorial design, comprising of drug, Pluronic F127, HPMC K 100M ,PEG 400,was found to be clear, colorless, isotonic, sterile, pH as 6.2-6.5, viscosity of 1400cps, syringeable through 21 gauze needle, forming a stable in-situ gel at body temperature having gel strength of 16.47gm/cm showing a controlled release of 96.0 % in Simulated Body fluid at 120hrs following Korsmeyer

–peppas model .The in vivo pharmacokinetics showed increase in tmax and AUC. Histopathological analysis showed no signs of inflammation or necrosis or any other cellular changes. The sterile formulation packed in amber colored ampoule was found to stable with most suitable storage condition at the refrigerator temperature. Thus, a biocompatible, stable parenteral formulation was developed which can be an alternative and convenient approach to the patients that require frequent parenteral administration, reducing the frequency of dosing and ultimately increasing patient compliance and comfort.