1. Development of controlled drug release systems based on thiolated polymers
- Author
-
Sabine Scholler, Andreas Bernkop-Schnürch, and Regina G Biebel
- Subjects
Polymers ,Acrylic Resins ,Pharmaceutical Science ,Dosage form ,chemistry.chemical_compound ,Adhesives ,Polymer chemistry ,Pharmaceutic Aids ,Mucoadhesion ,Organic chemistry ,Cysteine ,Disulfides ,Sulfhydryl Compounds ,Carbodiimide ,chemistry.chemical_classification ,Drug Carriers ,Mucous Membrane ,Thiomer ,Water ,Polymer ,Hydrogen-Ion Concentration ,Controlled release ,Freeze Drying ,Solubility ,chemistry ,Carboxymethylcellulose Sodium ,Delayed-Action Preparations ,Drug delivery ,Adsorption ,Tablets, Enteric-Coated ,Rifampin ,Drug carrier - Abstract
The purpose of the present study was to generate mucoadhesive matrix-tablets based on thiolated polymers. Mediated by a carbodiimide, l -cysteine was thereby covalently linked to polycarbophil (PCP) and sodium carboxymethylcellulose (CMC). The resulting thiolated polymers displayed 100±8 and 1280±84 μmol thiol groups per gram, respectively (means±S.D.; n=6–8). In aqueous solutions these modified polymers were capable of forming inter- and/or intramolecular disulfide bonds. The velocity of this process augmented with increase of the polymer- and decrease of the proton-concentration. The oxidation proceeded more rapidly within thiolated PCP than within thiolated CMC. Due to the formation of disulfide bonds within thiol-containing polymers, the stability of matrix-tablets based on such polymers could be strongly improved. Whereas tablets based on the corresponding unmodified polymer disintegrated within 2 h, the swollen carrier matrix of thiolated CMC and PCP remained stable for 6.2 h (mean, n=4) and more than 48 h, respectively. Release studies of the model drug rifampicin demonstrated that a controlled release can be provided by thiolated polymer tablets. The combination of high stability, controlled drug release and mucoadhesive properties renders matrix-tablets based on thiolated polymers useful as novel drug delivery systems.
- Published
- 2000
- Full Text
- View/download PDF