Abstract

FORMULATION AND CHARACTERIZATION OF GRANISETRON SUBLINGUAL BUCCAL FILMS USING DIFFERENT POLYMERS AND PLASTICIZERS

Naman Jain*, Dr. Arun Kumar Gupta, Dr. Gaurav Jain, Dr. Pankaj Kushwah, Dr. Prerna Chaturvedi, Dr. Antim Prajapat

Abstract

Background: Granisetron hydrochloride (Granisetron HCl) is a potent 5-HT₃ receptor antagonist used for the prevention of chemotherapy-induced nausea and vomiting. However, its extensive hepatic first-pass metabolism and delayed onset from oral dosage forms limit therapeutic efficiency. Sublingual buccal films offer a promising alternative for rapid systemic absorption and improved patient compliance. Methods: Granisetron HCl films were prepared by the solvent-casting method using different film-forming polymers hydroxypropyl methylcellulose (HPMC K4M), polyvinyl alcohol (PVA), and gelatin in various ratios. Propylene glycol was employed as a plasticizer, and citric acid anhydrous as a saliva-stimulating agent. The prepared films (F1–F5) were evaluated for physicochemical parameters, drug content, mechanical properties, surface pH, in- vitro disintegration, and dissolution behavior. Drug–excipient compatibility was examined using FTIR and DSC analyses. Results: All formulations exhibited smooth surfaces, uniform weight (49.5–55.8 mg), and adequate flexibility (folding endurance > 230). The surface pH (6.3–6.7) was within the physiological range of the buccal cavity, indicating mucosal safety. The disintegration time ranged from 9 to 14 seconds, with formulation F5 showing the fastest disintegration and highest cumulative drug release (98.34 %) within 25 minutes in phosphate buffer (pH 6.8). FTIR and DSC studies confirmed the absence of drug–excipient interactions and the thermal stability of the optimized formulation. Conclusion: The study demonstrates that sublingual buccal films of Granisetron HCl can be effectively formulated using HPMC and PVA with propylene glycol as plasticizer to achieve rapid disintegration and enhanced dissolution. The optimized formulation (F5) offers a patient-friendly, non-invasive dosage form with potential for rapid onset of action in the management of chemotherapy-induced nausea and vomiting.

Keywords: Granisetron HCl; sublingual buccal film; solvent casting; HPMC; PVA; propylene glycol; antiemetic therapy.