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Polymers 2015, 7(11), 2223-2244; doi:10.3390/polym7111510

The Effect of β-Glycerophosphate Crosslinking on Chitosan Cytotoxicity and Properties of Hydrogels for Vaginal Application

1
Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2c, Białystok 15-222, Poland
2
Department of Pharmaceutical Analysis, Medical University of Białystok, Mickiewicza 2d, Białystok 15-222, Poland
3
Department of Haematological Diagnostics, Medical University of Białystok,Waszyngtona 15a, Białystok 15-269, Poland
4
Institute of Chemistry, University of Białystok, Hurtowa 1, Białystok 15-399, Poland
*
Authors to whom correspondence should be addressed.
Academic Editor: Jianxun Ding
Received: 24 September 2015 / Revised: 21 October 2015 / Accepted: 28 October 2015 / Published: 4 November 2015
(This article belongs to the Special Issue Functional Polymers for Medical Applications)
View Full-Text   |   Download PDF [4477 KB, uploaded 4 November 2015]   |  

Abstract

Mucoadhesive gelling systems based on chitosan and chitosan/β-glycerophosphate (β-GP) were developed in order to increase clotrimazole residence time in the vaginal cavity. Ex vivo mucoadhesiveness using porcine vaginal mucosa followed with mechanical, viscoelastic, and swelling properties of prepared hydrogels were evaluated. Drug-free, sterile, unmodified, and β-GP crosslinked chitosan were investigated for the in vitro cytotoxicity in CRL 2616 human vaginal mucosa cells using MTT assay, fluorescent microscopy, and flow cytometry analysis. Chitosan/β-GP hydrogels exhibited pseudoplastic and thixotropic properties. Ionic interaction between β-GP and chitosan improved mechanical properties of hydrogels in terms of hardness, cohesiveness, and compressibility. The hydrogels’ ability to interact with porcine vaginal mucosa (measured as force of detachment and work of adhesion) was comparable to those obtained with reference mucoadhesive gel Replens™. Surprisingly, greater mucoadhesive properties were noticed for chitosan/β-GP hydrogels. The cytotoxic effect of unmodified and β-GP crosslinked chitosan was hardly affected by chitosan molecular weight, exhibited mainly through inducing apoptosis, and was found to be significantly lower in the presence of chitosan/β-GP. Furthermore, the higher amount of β-GP was used to crosslink chitosan, the lower cytotoxic effect was observed. View Full-Text
Keywords: hitosan; β-glycerophosphate; ion crosslinking; mucoadhesion; cytotoxicity; CRL 2616 cell line hitosan; β-glycerophosphate; ion crosslinking; mucoadhesion; cytotoxicity; CRL 2616 cell line
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Szymaǹska, E.; Sosnowska, K.; Miltyk, W.; Rusak, M.; Basa, A.; Winnicka, K. The Effect of β-Glycerophosphate Crosslinking on Chitosan Cytotoxicity and Properties of Hydrogels for Vaginal Application. Polymers 2015, 7, 2223-2244.

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