In situ evaluation of drug-loaded microspheres on a mucosal surface under dynamic test conditions

The ability of polymeric microspheres fabricated from Carbopol, polycarbophil, chitosan or Gantrez to retain a model hydrophilic drug (sodium fluorescein) was evaluated in situ, using a dynamic test system and image analysis. This technique used oesophageal tissues and simulated the physiological conditions within the oral cavity in terms of temperature, humidity and saliva flow. The point of sample application was observed over a 2 h period by means of a digital camera. No significant differences in fluorescein colour intensity was obtained for the Gantrez and chitosan particles over 100 min, indicate that these two polymers provide the possibility of prolonged action. Carbopol and polycarbophil particles became rapidly swollen and released the sodium fluorescein completely within 20 min. It was concluded that the test system allowed the evaluation of the in situ behaviour of test particles, in terms of their ability to retain a water-soluble, coloured marker in 'dynamic' test conditions, and that chitosan and Gantrez were promising candidates for the production of mucoadhesive, sustained-release microspheres for water-soluble materials. (C) 2004 Elsevier B.V. All rights reserved.