Frontiers in pharmacology · 2026
Development and pharmacokinetic evaluation of granisetron hydrochloride buccal tablets for optimized chemotherapy-induced nausea and vomiting (CINV) relief.
СтатьяНазвание и аннотация: Перевод в очереди
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Thalluri Chandrashekar, Naik Bukke Sarad Pawar, Vasam Malliukarjun, Medhi Jharna, Chettupalli Ananda Kumar, Mamilla Mugaiahgari Bharath Kumar, Narapureddy Bayapa Reddy, Yata Vinod Kumar, Chander Thatipelli Ravi
Аннотация
INTRODUCTION: Chemotherapy-induced nausea and vomiting (CINV) limits treatment adherence; this study aimed to develop optimized Granisetron hydrochloride buccal tablets to improve therapeutic performance and bioavailability.
METHODS: Tablets were prepared by direct compression and optimized using response surface methodology with HPMC K4M (X1) and carbomer 934P (X2). Compatibility was assessed by FT-IR and DSC, while mucoadhesion, t50, drug release, kinetics, and pharmacokinetics were evaluated.
RESULTS: No drug-excipient interactions were observed. The optimized formulation (F3; 50 mg HPMC K4M and 15 mg carbomer 934P) showed adequate mucoadhesion (8.25 ± 0.12 g), prolonged release (t50 ≈ 323 ± 0.35 min), and 70.23% ± 2.14% release at 8 h. Release followed the korsmeyer-peppas model, indicating anomalous transport. Pharmacokinetic studies showed significantly higher Cmax and AUC than oral tablets (p < 0.04).
DISCUSSION: The optimized buccal system provides controlled release and enhanced pharmacokinetic performance, suggesting a promising alternative approach for effective CINV management.
METHODS: Tablets were prepared by direct compression and optimized using response surface methodology with HPMC K4M (X1) and carbomer 934P (X2). Compatibility was assessed by FT-IR and DSC, while mucoadhesion, t50, drug release, kinetics, and pharmacokinetics were evaluated.
RESULTS: No drug-excipient interactions were observed. The optimized formulation (F3; 50 mg HPMC K4M and 15 mg carbomer 934P) showed adequate mucoadhesion (8.25 ± 0.12 g), prolonged release (t50 ≈ 323 ± 0.35 min), and 70.23% ± 2.14% release at 8 h. Release followed the korsmeyer-peppas model, indicating anomalous transport. Pharmacokinetic studies showed significantly higher Cmax and AUC than oral tablets (p < 0.04).
DISCUSSION: The optimized buccal system provides controlled release and enhanced pharmacokinetic performance, suggesting a promising alternative approach for effective CINV management.