Graphene oxide as a functional excipient in buccal films for delivery of clotrimazole: Effect of molecular interactions on drug release and antifungal activity in vitro.

Antifungal activity Clotrimazole Graphene oxide Molecular interaction Polyelectrolyte film

Journal

International journal of pharmaceutics
ISSN: 1873-3476
Titre abrégé: Int J Pharm
Pays: Netherlands
ID NLM: 7804127

Informations de publication

Date de publication:
15 Nov 2020
Historique:
received: 06 07 2020
revised: 17 08 2020
accepted: 20 08 2020
pubmed: 3 9 2020
medline: 22 6 2021
entrez: 3 9 2020
Statut: ppublish

Résumé

Graphene oxide (GO) is an amphiphilic, high surface area material with great potential as a functional excipient in drug delivery. The present study aimed at incorporating GO in buccal polyelectrolyte films for delivery of antifungal drugs and investigating the effect of GO on the film properties and drug release profiles, as well as antifungal activities. Mucoadhesive excipients chitosan and alginate were selected to form polyelectrolyte films with the antifungal drug clotrimazole. The buccal formulations were prepared by mixing the excipients and clotrimazole via probe sonication, followed by film casting and drying. Inclusion of GO in the formulations increased clotrimazole release from the films in vitro (pH 6.8), possibly due to GO altering the electrostatic interactions between chitosan and alginate. An increase of in vitro activity against Candida albicans was observed when 0.04 wt% GO was added in the formulation containing clotrimazole. However, when the GO amount increased to 0.09 wt%, the films had similar antifungal ability to the films with 0.04 wt% GO, suggesting that the electrostatic and hydrophobic interactions between GO and clotrimazole also affects the antifungal effect of clotrimazole. In summary, GO has a great potential as a functional excipient for delivery of antifungal drugs.

Identifiants

pubmed: 32877734
pii: S0378-5173(20)30796-1
doi: 10.1016/j.ijpharm.2020.119811
pii:
doi:

Substances chimiques

Antifungal Agents 0
Excipients 0
graphene oxide 0
Graphite 7782-42-5
Clotrimazole G07GZ97H65

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

119811

Informations de copyright

Copyright © 2020 Elsevier B.V. All rights reserved.

Auteurs

J Huang (J)

Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.

J Jacobsen (J)

Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.

S W Larsen (SW)

Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.

N Genina (N)

Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.

M van de Weert (M)

Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.

A Müllertz (A)

Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.

H M Nielsen (HM)

Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.

H Mu (H)

Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark. Electronic address: huiling.mu@sund.ku.dk.

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Classifications MeSH