S-protected gellan gum: Decisive approach towards mucoadhesive antimicrobial vaginal films.

Abstract

The aim of this study was to synthesize novel polymeric excipients forming mucoadhesive films for treatment of vaginal microbial infections. 2-(2-Amino ethyldisulfanyl) nicotinic acid was conjugated with gellan gum via amide bond formation. The structure of the resulting S-protected gellan gum was confirmed by 1H NMR. S-protected gellan gum variants were characterized for thiol content, cytotoxicity, rheological behaviour and film forming capability. Depending on the added amount of AMENA degree of thiolation was 81 ± 13 (S-GG 81) and 174 ± 16 (S-GG 174) μmol/g, respectively. Vaginal films were casted from S-protected gellan gum variants and studied for adherence to vaginal mucosa, drug release and antimicrobial activity. S-protected gellan gum remained biocompatible showing >87% cell viability. S-GG 81 and S-GG 174 exhibited 1.84- and 4.3-fold increased dynamic viscosity in porcine mucus in comparison to unmodified gellan gum, respectively. Compared to gellan gum films, thiol functionalized gellan gum films showed 3-fold improved adhesion on mucosal surface over a period of 3 h along with significant antimicrobial activity. Moreover, S-protected gellan gum provided a sustained release of metronidazole. According to these results, S-protected gellan gum proved to be a promising novel excipient for casting vaginal films, exhibiting strongly improved mucoadhesive and antimicrobial properties.

• Authors: Aamir Jalil, Mulazim Hussain Asim, Nguyet-Minh Nguyen Le, Flavia Laffleur, Barbara Matuszczak, Martina Tribus, Andreas Bernkop-Schnürch
• Journal: International journal of biological macromolecules (Int J Biol Macromol) Vol. 130 Pg. 148-157 (Jun 01 2019) ISSN: 1879-0003 [Electronic] Netherlands
• PMID: 30779984 (Publication Type: Journal Article)
• Copyright: Copyright © 2019 Elsevier B.V. All rights reserved.

Chemical References

• Anti-Bacterial Agents
• Drug Carriers
• Polysaccharides, Bacterial
• Metronidazole
• Sulfur
• gellan gum

Topics

• Adhesiveness
• Animals
• Anti-Bacterial Agents (chemistry, pharmacology)
• Caco-2 Cells
• Drug Carriers (chemistry)
• Drug Liberation
• Escherichia coli (drug effects)
• Female
• Humans
• Materials Testing
• Metronidazole (chemistry, pharmacology)
• Mucous Membrane (chemistry)
• Polysaccharides, Bacterial (chemistry)
• Rheology
• Sulfur (chemistry)
• Swine
• Vagina (chemistry)