Potential of mucoadhesive chitosan glutamate microparticles as microbicide carriers - antiherpes activity and penetration behavior across the human vaginal epithelium

Chitosan glutamate (gCS) spray-dried microparticles appear promising carriers to overcome challenges associated with vaginal microbicide delivery. This study aimed at elucidating the penetration and mucoadhesive behavior of developed gCS multiunit carriers with zidovudine (ZVD) as a model antiretroviral agent in contact with excised human vaginal epithelium followed with an examination of in vitro antiherpes activity in immortal human keratinocytes HaCaT and human vaginal epithelial cells VK2-E6/E7. Both ZVD dispersion and placebo microparticles served as controls. Microparticles displayed feasible (comparable to commercial vaginal product) mucoadhesive and mucoretention characteristics to isolated human vaginal tissue. Ex vivo penetration studies revealed that gCS increased the accumulation of active agent in the vaginal epithelium but surprisingly did not facilitate its penetration across human tissue. Finally, the obtained antiviral results demonstrated the potential of gCS as an antiherpes adjunctive, whose mode of action was related to blocking viral attachment.

Medienart:

E-Artikel

Erscheinungsjahr:

2021

Erschienen:

2021

Enthalten in:

Zur Gesamtaufnahme - volume:28

Enthalten in:

Drug delivery - 28(2021), 1 vom: 12. Dez., Seite 2278-2288

Sprache:

Englisch

Beteiligte Personen:

Szymańska, Emilia [VerfasserIn]
Krzyżowska, Małgorzata [VerfasserIn]
Cal, Krzysztof [VerfasserIn]
Mikolaszek, Barbara [VerfasserIn]
Tomaszewski, Jakub [VerfasserIn]
Wołczyński, Sławomir [VerfasserIn]
Winnicka, Katarzyna [VerfasserIn]

Links:

Volltext

Themen:

3KX376GY7L
4B9XT59T7S
9012-76-4
Antiviral Agents
Antiviral activity
Chitosan
Chitosan glutamate
Drug Carriers
Ex vivo penetration studies
Glutamic Acid
HSV-2
Human vaginal epithelium
Journal Article
Microbicide vaginal carrier
Microparticles
Mucoretention
Zidovudine

Anmerkungen:

Date Completed 20.01.2022

Date Revised 20.01.2022

published: Print

Citation Status MEDLINE

doi:

10.1080/10717544.2021.1992037

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM332090493