Investigating the effect of graphene oxide in chitosan/alginate-based foams on the release and antifungal activity of clotrimazole in vitro

J. Huang, J. Jacobsen, N. Genina, S. W. Larsen, H. M. Nielsen, A. Müllertz, H. Mu*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

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Abstract

Polyelectrolyte complexes (PECs) have been used as the matrix of solid foams for drug delivery. This study aimed at investigating the effect of graphene oxide (GO) and the composition of excipients in chitosan/alginate-based buccal foams on the clotrimazole release and antifungal activities. The investigation has been focused on the interactions of the drug with excipients in the foams, and the changes of ionization degree upon exposure to various media are discussed. The solid foams were prepared by mixing the excipients and clotrimazole via probe sonication, followed by a freeze-drying method. The pH values of the formulations were measured during the foam preparation process to estimate the ionization degree of clotrimazole and the other excipients. The foam matrix was the PECs between the cationic chitosan and anionic alginate. The mechanical strength of clotrimazole-loaded foams was lower than that of drug-free foams due to the positively charged clotrimazole interacting with the anionic alginate and interfering the PECs between chitosan and alginate. Addition of GO in the clotrimazole-loaded matrix made the foams mechanically stronger and contributed to a faster release of clotrimazole from the buccal foams by disrupting the electrostatic interactions between alginate and clotrimazole. However, addition of 1 wt% GO in the formulations didn't affect the antifungal activity of clotrimazole-loaded foams significantly. A lower amount GO in the formulation may be required for enhancing the antifungal effect, which should be further investigated in future.

Original languageEnglish
Article number106204
JournalEuropean Journal of Pharmaceutical Sciences
Volume174
Number of pages9
ISSN0928-0987
DOIs
Publication statusPublished - 2022

Bibliographical note

Funding Information:
The financial support by the University of Copenhagen, Denmark and Oversea Study Program of Guangzhou Elite Project for Jianfei Huang (JY201622) is appreciated. We would also like to thank Søren Michael Nielsen and Dr. Sylvia Natalie Kłodzińska for their technical assistance.

Funding Information:
The financial support by the University of Copenhagen , Denmark and Oversea Study Program of Guangzhou Elite Project for Jianfei Huang ( JY201622 ) is appreciated. We would also like to thank Søren Michael Nielsen and Dr. Sylvia Natalie Kłodzińska for their technical assistance.

Keywords

  • Alginate
  • Antifungal activity
  • Chitosan
  • Clotrimazole
  • Drug release
  • Polyelectrolyte foam

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