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15. December 2016
Abstract The aim of this study was the design and evaluation of an entirely S-protected thiomer as matrix for intraorally administered films. The highly bucco-adhesive gelatin thiomer was designed based on the ligand cysteamine which was connected via disulfide bond with the aromatic leaving group 2-mercaptopyrimidine-4,6-diol (2-MPD). The thiol ligand cysteamine 2-MPD (Cys-2-MPD) was synthesized via the coupling of dimerised 2-MPD to cysteamine (Cys) and then attached to gelatin scaffold via a...
20. June 2016
AIM It is the aim of this study to synthesize hyaluronic acid (HA) derivatives bearing mucoadhesive properties and showing prolonged stability at pH 7.4 and under oxidative condition as liquid dosage form. METHODS HA was modified by thiolation with L-cysteine (HA-SH) and by conjugation with 2-mercaptonicotinic acid-L-cysteine ligand to obtain an S-protected derivative (HA-MNA). The polymers were characterized by determination of thiol group content and mercaptonicotinic acid content....
09. June 2016
Aim The purpose of the present study was to generate a novel mucoadhesive thiolated pullulan with protected thiol moieties and to evaluate its suitability as mucosal drug delivery system. Methods Two different synthetic pathways: bromination-nucleophilic substitution and reductive amination including periodate cleavage were utilized to synthesize such thiolated pullulans. The thiomer (pullulan-cysteamine) with the highest amount of free thiol groups was further enrolled in a reaction with...
19. January 2016
The thiolation of polyallylamine (PAAm) for use in mucoadhesive drug delivery has been achieved. PAAm was reacted with different ratios of Traut's reagent, yielding products with thiol contents ranging from 134–487 μmol/g. Full mucoadhesive characterisation of the thiolated PAAm samples was conducted using swelling studies, mucoadhesive testing on porcine intestinal tissue and rheology. Both swelling and cohesive properties of the thiolated PAAm products were vastly improved in comparison to...