Abstract

Nowadays, the buccal administration of mucoadhesive films is very promising. Our aim was to prepare ascorbic acid-containing chitosan films to study the properties and structures important for applicability and optimize the composition. During the formulation of mucoadhesive films, chitosan as the polymer basis of the film was used. Ascorbic acid, which provided the acidic pH, was used in different concentrations (2–5%). The films were formulated by the solvent casting method. The properties of films important for applicability were investigated, such as physical parameters, mucoadhesive force, surface free energy, and breaking strength. The fine structure of the films was analyzed by atomic force microscopy, and the free volume was analyzed by PALS, which can be important for drug release kinetics and the location of the drug in the film. The applicability of the optimized composition was also tested with two different types of active ingredients. The structure of the films was also analyzed by XRPD and FTIR. Ascorbic acid can be used well in chitosan films, where it can function as a permeation enhancer when reacting to chitosan, it is biodegradable, and can be applied in 2% of our studies.

Highlights

  • The advantage of buccal films is that they do not have to be swallowed, so they can be used by patients who have difficulty swallowing, and the first-pass effect of the liver can be avoided, which means that a smaller amount of active ingredient is sufficient to reduce side effects

  • It can be seen that the highest value was found for the film made with acetic acid (Ref), 39.18 MPa, which can be explained by the fact that during the formation of chitosan acetate, the excess acetic acid evaporates from the system and does not affect the breaking strength (Figure 2)

  • It can be seen that in the case of a film containing 2% ascorbic acid (Film 2), the breaking strength is significantly lower, which is explained by the formation of chitosan ascorbate, which resulted in a different chemical structure and has different properties

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Summary

Introduction

Introduction published maps and institutional affilNowadays, bioadhesive formulations are increasingly becoming a very important class of dosage in the forms of films [1–3], tablets [4], nanoparticles [5,6], etc. Buccal mucoadhesive films are one of the most innovative and promising groups of dosage forms. The advantage of mucoadhesive forms is that the active ingredient can continuously absorb the biological barrier by adhering to the mucosa. The advantage of buccal films is that they do not have to be swallowed, so they can be used by patients who have difficulty swallowing, and the first-pass effect of the liver can be avoided, which means that a smaller amount of active ingredient is sufficient to reduce side effects. Mucoadhesive films that can adhere to the buccal mucosa can be produced with simple pharmaceutical technology solutions. A number of polymers that are suitable for this purpose have been used in the literature, such as cellulose derivatives [7], sodium alginate [8], or chitosan.

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