Enhanced In Situ Availability of Aphanizomenon Flos-Aquae Constituents Entrapped in Buccal Films for the Treatment of Oxidative Stress-Related Oral Diseases: Biomechanical Characterization and In Vitro/Ex Vivo Evaluation
Enhanced In Situ Availability of Aphanizomenon Flos-Aquae Constituents Entrapped in Buccal Films for the Treatment of Oxidative Stress-Related Oral Diseases: Biomechanical Characterization and In Vitro/Ex Vivo Evaluation
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DOI：
10.3390/pharmaceutics11010035
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发表时间：
2019-01-01
期刊：
影响因子：
5.4
通讯作者：
Campisi, Giuseppina
中科院分区：
文献类型：
--
作者：
De Caro, Viviana;Murgia, Denise;Campisi, Giuseppina
近年来，氧化应激在口腔疾病发病中的关键作用越来越受到重视，抗氧化剂的应用也越来越受到重视。Aphanizomenonflos-aquae （AFA）是一种具有抗氧化和抗炎特性的单细胞蓝绿藻。本研究的目的是制备和表征负载AFA的黏附薄层膜，最终用于氧化应激（OS）相关口腔疾病的治疗。首先，为了提高AFA成分的生物利用度，通过能够破坏细胞壁的高频均质处理适当的食品级原料。因此，采用溶剂铸造法制备了Eudragit (R) e100基口腔膜，其中AFA含量分别为7%和18%。膜的厚度、重量和药物含量均匀，溶胀程度低，黏附性好，药物释放控制。力学测试表明，薄膜的弹性模量接近5 MPa，非常适合人类口腔应用而没有不适，此外双轴测试突出了明显的材料各向同性。通过猪粘膜的渗透研究表明，薄膜能够促进AFA在组织中的渗透，当舌下给药时，它们产生的药物通量比AFA溶液高6倍。新的配方代表了一个有趣的替代化妆品和营养保健品的发展，具有功能性的吸引力，含有植物提取物。
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. Aphanizomenonflos-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 (R) 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.