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Abstract
In recent years, the key role of oxidative stress in pathogenesis of oral diseases has been emphasized and the use of antioxidant agents has been encouraged. Aphanizomenon flos-aquae (AFA) is a unicellular blue-green alga with antioxidant and anti-inflammatory properties. The aim of this study was the formulation and characterization of mucoadhesive thin layer films loaded with AFA, finalized to the treatment of oxidative stress (OS)-related oral diseases. First, to enhance the bioavailability of AFA constituents, the raw food grade material was appropriately treated by a high frequency homogenization able to disrupt cell walls. Thus, Eudragit® E100-based buccal films were produced by the solvent casting method, containing 7% and 18% of AFA. The films, characterized by uniformity in thickness, weight, and drug content, showed low swelling degree, good muco-adhesiveness and controlled drug release. The mechanical tests showed elastic moduli of films of almost 5 MPa that is well-suitable for human buccal applications without discomfort, besides biaxial tests highlighted a marked material isotropy. Permeation studies through porcine mucosae demonstrated the ability of films to promote AFA penetration in the tissues, and when sublingually administered, they produced a drug flux up to six-fold higher than an AFA solution. The new formulations represent an interesting alternative for the development of cosmetics and nutraceuticals with a functional appeal containing plant extracts.
Highlights
During recent years, there is a rise of oral diseases related to oxidative stress [1]
This source could represent an obstacle to bioavailability of antioxidant components because, to be absorbed, they must be released from the cells in which they are entrapped in the dry state
The first objective was the use of raw food grade material, appropriately treated by a homogenization process able to disrupt the cellular matrix to enhance the bioavailability of its constituents
Summary
There is a rise of oral diseases related to oxidative stress [1]. Periodontal disease, oral lichen planus (OLP), and oral cancer are the mostly related to oxidative stress. It is shown that OS is involved in the, not yet understood, pathogenesis of OLP [4]; higher levels of salivary ROS, lipid peroxidation, nitric oxide, and nitrite levels are found in OLP patients [5]. The antioxidant activity is decreased in OLP patients, compared to healthy subjects [6]. OS is related with oral cancer: increase in lipid peroxidation and a reduced antioxidant activity are reported [7]
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