Stability, Permeability and Cytotoxicity of Buccal Films in Allergy Treatment

Abstract

Oral mucoadhesive systems, such as polymer films, are among innovative pharmaceutical products. These systems can be applied in swallowing problems and can also be used in geriatrics and paediatrics. In our earlier work, we successfully formulated buccal mucoadhesive polymer films, which contained cetirizine-hydrochloride (CTZ) as the API. The present study focused on investigating the stability and permeability of the prepared films. The stability of the films was studied with an accelerated stability test. During the stability test, thickness, breaking hardness and in vitro mucoadhesivity were analysed. Furthermore, the interactions were studied with FT-IR spectroscopy, and the changes in the amount of the API were also monitored. Cytotoxicity and cell line permeability studies were carried out on TR 146 buccal cells. Compositions that can preserve more than 85% of the API after 6 months were found. Most of the compositions had a high cell viability of more than 50%. Citric acid (CA) decreased the stability and reduced every physical parameter of the films. However, cell line studies showed that the permeability of the films was enhanced. In our work, we successfully formulated CTZ-containing buccal films with adequate stability, high cell viability and appropriate absorption properties.

Keywords: alginate; antihistamine; buccal films; cetirizine; cytotoxicity; drug delivery; mucoadhesive; permeability; stability.

Figure 1

Breaking hardness of the prepared films (Samples 2, 4, 6, 8, 10, 12 contain CA) (* p < 0.05; n = 6). The samples were compared to the freshly prepared sample (0 months).

Figure 2

Mucoadhesivity of the prepared films (Samples 2, 4, 6, 8, 10, 12 contain CA) (* p < 0.05; n = 6). The samples were compared to the freshly prepared sample (0 months).

Figure 3

API content for different films during accelerated stability study (Samples 2, 4, 6, 8, 10, 12 contain CA) (n = 6).

Figure 4

Results of the FT-IR spectra of the prepared films (Part “A” Sample 1, Part “B” Sample 8).

Figure 5

Permeation curves of polymer films on artificial membrane (n = 6).

Figure 6

Apparent permeability values of buccal films calculated from the permeability rate of CTZ between 60 and 90 min. Each film was investigated in three separate, parallel cell culture inserts (n = 3). * Significant difference was found only between Sample 2 and Sample 12.

Figure 7

Transported CTZ–time curves of buccal films on the TR-146 cell line. Each film was investigated in three separate, parallel cell culture inserts (Samples 2, 8, 12 contain CA) (n = 3).