Pakistan journal of pharmaceutical sciences · 2026
Design, in vitro and in vivo evaluation of buccal patches for mucosal delivery of analgesics and antiseptics for the treatment of oral mucositis.
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Perveen Farzana, Mudassir Jahanzeb, Hussain Ikhlaq, Majeed Abdul
Аннотация
BACKGROUND: Oral mucositis is an inflammatory condition of the oral mucosa and causes pain associated with oral mucositis, leading to impaired quality of life. Localized drug delivery systems may provide effective treatment while avoiding the drawbacks of systemic administration.
OBJECTIVE: The purpose of this study was to formulate a buccal patch of lidocaine, fentanyl, and cetylpyridinium chloride using chitosan (CS), glycerol (G) and propylene glycol (PPG) to treat oral mucositis as a safe alternative to systemic administration.
METHODS: Solvent casting was used to create mucoadhesive buccal patches. Several characteristics were evaluated to optimize the buccal patch, including folding endurance, thickness measurement, mucoadhesion study, drug release, cell viability, permeation study and pharmacokinetic study. In addition, physicochemical interaction between CS, G and PPG was examined using FTIR, DSC and TGA.
RESULTS: The optimized buccal patch BP4 showed a swelling index of 70%. All of the bioadhesive patches showed surface pH ranging from 6.2 ± 0.18 to 7.2 ± 0.18. Further, the BP4 had an adhesion force of 69 ± 3.06 × 10-3 N. The in vitro release of cetylpyridinium chloride, fentanyl and lidocaine from BP4 was 85%, 65% and 75%, respectively, for 12 hours. Ex vivo penetration study revealed 70%, 58%, and 78% penetration from three drugs, lidocaine, fentanyl, and cetylpyridinium chloride, respectively, from optimized buccal patches (BP4). When compared to suspension, the buccal administration of fentanyl and lidocaine in rabbits verified a notable increase in the bioavailability of the drugs.
CONCLUSION: The developed mucoadhesive buccal patch represents a promising and safe localized delivery system for analgesic and antiseptic agents in the treatment of oral mucositis, offering sustained drug release and improved bioavailability.
OBJECTIVE: The purpose of this study was to formulate a buccal patch of lidocaine, fentanyl, and cetylpyridinium chloride using chitosan (CS), glycerol (G) and propylene glycol (PPG) to treat oral mucositis as a safe alternative to systemic administration.
METHODS: Solvent casting was used to create mucoadhesive buccal patches. Several characteristics were evaluated to optimize the buccal patch, including folding endurance, thickness measurement, mucoadhesion study, drug release, cell viability, permeation study and pharmacokinetic study. In addition, physicochemical interaction between CS, G and PPG was examined using FTIR, DSC and TGA.
RESULTS: The optimized buccal patch BP4 showed a swelling index of 70%. All of the bioadhesive patches showed surface pH ranging from 6.2 ± 0.18 to 7.2 ± 0.18. Further, the BP4 had an adhesion force of 69 ± 3.06 × 10-3 N. The in vitro release of cetylpyridinium chloride, fentanyl and lidocaine from BP4 was 85%, 65% and 75%, respectively, for 12 hours. Ex vivo penetration study revealed 70%, 58%, and 78% penetration from three drugs, lidocaine, fentanyl, and cetylpyridinium chloride, respectively, from optimized buccal patches (BP4). When compared to suspension, the buccal administration of fentanyl and lidocaine in rabbits verified a notable increase in the bioavailability of the drugs.
CONCLUSION: The developed mucoadhesive buccal patch represents a promising and safe localized delivery system for analgesic and antiseptic agents in the treatment of oral mucositis, offering sustained drug release and improved bioavailability.