Optimasi Pektin dan Hydroxypropyl Methylcellulose dalam Sediaan Fast Dissolving Sublingual Film (FDSF) Granisetron Hidroklorida

Abstract

Chemotherapy-induced nausea and vomiting (CINV) is a common adverse effect of chemotherapy that may reduce cancer treatment success in up to 40% of patients. Granisetron hydrochloride, a selective 5-HT₃ receptor antagonist, is widely used as an antiemetic for CINV management; however, conventional oral administration is limited by dysphagia, delayed onset of action, and low oral bioavailability of approximately 60%. Fast Dissolving Sublingual Film (FDSF) is a drug delivery system that rapidly disintegrates in the oral cavity, provides rapid onset of action, and bypasses first-pass metabolism. This study employed a combination of pectin and Hydroxypropyl Methylcellulose to obtain films with rapid disintegration and adequate mechanical properties. Formulation optimization was conducted using a two-factor, two-level factorial design with pectin (0.20 g and 0.30 g) and HPMC K100 (0.020 g and 0.030 g). The films were prepared by the solvent casting method and evaluated for disintegration time, folding endurance, and drug content. All formulations met the evaluation criteria. Increasing polymer concentrations prolonged disintegration time and enhanced folding endurance, with pectin identified as the dominant factor influencing both responses. Optimization using Design Expert version 13.0.5 produced an optimum formulation containing 0.30 g pectin and 0.03 g HPMC K100, with a disintegration time of 31.26 seconds and folding endurance of 682 folds. Verification using a one-sample t-test in SPSS version 22.0 showed no significant difference between predicted and experimental results. In vitro release testing demonstrated 100.86% drug release within 7 minutes, while FTIR analysis confirmed bo changes were observed in the active functional groups of granisetron hydrochloride.