ABSTRACT
AIM: Doxepin is a traditional tricyclic antidepressant with analgesic and anesthetic properties when applied topically to the mucosa. Doxepin is one approach in treating insomnia and depression in Parkinson's disease. Patients with Parkinson's disease suffer difficulties in swallowing. Therefore, it was the aim of this study to develop a buccal-adhesive delivery system. METHODS: Pectin was modified with cysteine. Stability assays in form of disintegration assay according to the Ph.Eur were performed. Furthermore, bioadhesiveness on buccal mucosa was investigated incorporating the drug doxepin. RESULTS: The adhesiveness was improved 1.4-fold and revealed a sustained release over 3 h. CONCLUSION: Taking these findings into account, the modifications render this designed excipient fruitful for buccal delivery.
Subject(s)
Cysteine/chemistry , Doxepin/administration & dosage , Drug Carriers/administration & dosage , Drug Carriers/chemistry , Pectins/chemistry , Adhesiveness , Administration, Buccal , Cell Survival/drug effects , Cells, Cultured , Doxepin/adverse effects , Doxepin/pharmacokinetics , Drug Liberation , Drug Stability , Humans , Mouth Mucosa/drug effectsABSTRACT
AIM: It was the aim of this study to synthesize pectin (PEC) with sulfhydryl groups and evaluate its suitability in buccal application. MATERIALS & METHODS: Native PEC was chemically modified by covalent attachment of sulfhydryl-bearing cysteine (CYS). Stability assays in form of water uptake behavior and erosion study were performed. Additionally, mucoadhesive study on buccal mucosa was performed. RESULTS: Pectin-cysteine (PECCYS) was successfully synthesized as proved by IR and Ellman's assay exhibiting 436.59 ± 127.87 µmol thiol groups per gram polymer. Stability assay showed that PECCYS revealed a 2.27-fold improved water uptake and mucoadhesiveness augmented 3.75-fold in comparison to unmodified PEC. CONCLUSION: PECCYS might be a future suitable excipient for buccal adhesive application.
