TY - JOUR
T1 - Graphene oxide as a functional excipient in buccal films for delivery of clotrimazole
T2 - effect of molecular interactions on drug release and antifungal activity in vitro
AU - Huang, J
AU - Jacobsen, J
AU - Larsen, S W
AU - Genina, N
AU - van de Weert, M
AU - Müllertz, A
AU - Nielsen, H M
AU - Mu, H
N1 - Copyright © 2020. Published by Elsevier B.V.
PY - 2020
Y1 - 2020
N2 - 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.
AB - 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.
U2 - 10.1016/j.ijpharm.2020.119811
DO - 10.1016/j.ijpharm.2020.119811
M3 - Journal article
C2 - 32877734
VL - 589
SP - 1
EP - 9
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
M1 - 119811
ER -