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Modulation of stability and mucoadhesive properties of chitosan microspheres for therapeutic gastric application.
Int J Pharm. 2013 Sep 15; 454(1):116-24.IJ

Abstract

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 ∼170 μm 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 10mM of genipin for 1h did not dissolve and doubled their size to approximately 345 μm. 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 2h in the stomach of C57BL/6 mice.

Authors+Show Affiliations

INEB - Instituto de Engenharia Biomédica, Rua do Campo Alegre, 823, 4150-180 Porto, Portugal.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23850814

Citation

Fernandes, Mariana, et al. "Modulation of Stability and Mucoadhesive Properties of Chitosan Microspheres for Therapeutic Gastric Application." International Journal of Pharmaceutics, vol. 454, no. 1, 2013, pp. 116-24.
Fernandes M, Gonçalves IC, Nardecchia S, et al. Modulation of stability and mucoadhesive properties of chitosan microspheres for therapeutic gastric application. Int J Pharm. 2013;454(1):116-24.
Fernandes, M., Gonçalves, I. C., Nardecchia, S., Amaral, I. F., Barbosa, M. A., & Martins, M. C. (2013). Modulation of stability and mucoadhesive properties of chitosan microspheres for therapeutic gastric application. International Journal of Pharmaceutics, 454(1), 116-24. https://doi.org/10.1016/j.ijpharm.2013.06.068
Fernandes M, et al. Modulation of Stability and Mucoadhesive Properties of Chitosan Microspheres for Therapeutic Gastric Application. Int J Pharm. 2013 Sep 15;454(1):116-24. PubMed PMID: 23850814.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Modulation of stability and mucoadhesive properties of chitosan microspheres for therapeutic gastric application. AU - Fernandes,Mariana, AU - Gonçalves,Inês C, AU - Nardecchia,Stefania, AU - Amaral,Isabel F, AU - Barbosa,Mário A, AU - Martins,M Cristina L, Y1 - 2013/07/11/ PY - 2013/05/22/received PY - 2013/06/21/revised PY - 2013/06/27/accepted PY - 2013/7/16/entrez PY - 2013/7/16/pubmed PY - 2014/2/28/medline KW - Biomaterials KW - Chitosan KW - Genipin KW - Helicobacter pylori KW - Microspheres KW - Mucoadhesion SP - 116 EP - 24 JF - International journal of pharmaceutics JO - Int J Pharm VL - 454 IS - 1 N2 - 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 ∼170 μm 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 10mM of genipin for 1h did not dissolve and doubled their size to approximately 345 μm. 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 2h in the stomach of C57BL/6 mice. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/23850814/Modulation_of_stability_and_mucoadhesive_properties_of_chitosan_microspheres_for_therapeutic_gastric_application_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(13)00588-7 DB - PRIME DP - Unbound Medicine ER -