S-protected gellan gum: Decisive approach towards mucoadhesive antimicrobial vaginal films
Autor: | Barbara Matuszczak, Flavia Laffleur, Andreas Bernkop-Schnürch, Martina Tribus, Aamir Jalil, Nguyet-Minh Nguyen Le, Mulazim Hussain Asim |
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Rok vydání: | 2019 |
Předmět: |
Swine
Excipient 02 engineering and technology Biochemistry 03 medical and health sciences chemistry.chemical_compound Structural Biology Metronidazole Materials Testing Escherichia coli Mucoadhesion medicine Animals Humans Molecular Biology Thiol functionalized 030304 developmental biology Drug Carriers 0303 health sciences Mucous Membrane Chemistry Vaginal mucosa Polysaccharides Bacterial Adhesiveness General Medicine Adhesion 021001 nanoscience & nanotechnology Biocompatible material Antimicrobial Gellan gum Anti-Bacterial Agents Drug Liberation Vagina Female Caco-2 Cells Rheology 0210 nano-technology Sulfur medicine.drug Nuclear chemistry |
Zdroj: | International Journal of Biological Macromolecules. 130:148-157 |
ISSN: | 0141-8130 |
DOI: | 10.1016/j.ijbiomac.2019.02.092 |
Popis: | 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. |
Databáze: | OpenAIRE |
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