Modulation of stability and mucoadhesive properties of chitosan microspheres for therapeutic gastric application

• Type: Article in International Scientific Journal
• Date: 2013

Authors

Mariana Fernandes (Author) Other; Ines C Goncalves (Author) FEUP; Stefania Nardecchia (Author) Other; Isabel F Amaral (Author) FEUP; Mario A Barbosa (Author) ICBAS; Cristina C L Martins (Author) Other

Journal

Title: International Journal of Pharmaceutics

Vol. 454

Pages: 116-124

ISSN: 0378-5173

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 17 Citations

Scopus - 14 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-006-7AA

DOI: 10.1016/j.ijpharm.2013.06.068

Abstract (EN): Chitosan microspheres have been explored for pharmaceutical applications, namely as a drug delivery systems for Helicobacter pylori gastric infection treatment, due to their mucoadhesive capacity. In this study, a different application of chitosan microspheres is proposed aiming the creation of an H. pylori-binding system where, after oral administration, microspheres will capture and remove these bacteria from infected patients, taking advantage of their muco/bacterial adhesive process. However, mucoadhesion is influenced by the degree of crosslinking necessary to avoid microspheres dissolution in the acidic gastric environment. During this work, the effect of genipin crosslinking on the stability, size, charge and mucoadhesive properties of chitosan microspheres under acidic pH was studied. Chitosan microspheres with similar to 170 mu m were produced by ionotropic gelation and subsequently covalently crosslinked with genipin in different degrees. The crosslinking reaction was followed by infrared spectroscopy and time-lapse fluorescence microscopy, since we have demonstrated that the fluorescence intensity of chitosan microspheres increases with genipin chemical bonding to chitosan. Results showed that both the zeta potential and the swelling capacity of chitosan microspheres decrease with increasing crosslinking. When immersed in simulated gastric fluid (SGF) with pepsin for 7 days, chitosan microspheres crosslinked with 10 mM of genipin for 1 h did not dissolve and doubled their size to approximately 345 mu m. Furthermore, they maintained their in vitro mucoadhesion to soluble gastric mucins at both pH tested (3.6 and 6.5) and presented an in vivo retention time of around 2 h in the stomach of C57BL/6 mice.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9