Influence of different chitosan salts on the release of sodium diclofenac in colon-specific delivery

• Published in: International journal of pharmaceutics 2002-05, Vol.238 (1), p.51-59
• Main Authors: Orienti, I., Cerchiara, T., Luppi, B., Bigucci, F., Zuccari, G., Zecchi, V.
• Format: Article
• Language: English
• Subjects: Algorithms; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; beta-Glucosidase - chemistry; Biological and medical sciences; Bones, joints and connective tissue. Antiinflammatory agents; Buffers; Chitin - analogs & derivatives; Chitin - chemistry; Chitosan; Chitosan salts; Colon - metabolism; Colon-drug delivery; Diclofenac - administration & dosage; Diclofenac sodium; Drug Delivery Systems; Excipients; Hydrogen-Ion Concentration; Medical sciences; Molecular Weight; Pharmacology. Drug treatments; Solubility; Spectroscopy, Fourier Transform Infrared; Spray-drying; Temperature; Water
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/S0378-5173(02)00060-1

Chitosan (CH) was dissolved in aqueous solutions containing aspartic, glutamic, hydrochloric, lactic and citric acids to obtain different chitosan salts. Chitosan salts were collected from the solutions by spray-drying and the powders obtained were mixed with Sodium Diclofenac (SD), taken as a model anti-inflammatory drug. This study evaluated in vitro the influence of acid type on the release behaviour of SD from the physical mixture during gastrointestinal transit. The physical mixture of the chitosan salts with SD provided slower drug release than the pure drug both in acidic and alkaline pHs. In addition, the interaction with β-glucosidase at pH 7.0 enhanced the release rate. Among the CH salts used, glutamic and aspartic salts provided the best control of release.