Dental Physical Science Unit, Faculty of Medicine and Dentistry, Queen Mary University of London, Mile End Road, London E1 4NS, UK.
Dental Physical Science Unit, Faculty of Medicine and Dentistry, Queen Mary University of London, Mile End Road, London E1 4NS, UK.
Dent Mater. 2023 Jun;39(6):595-602. doi: 10.1016/j.dental.2023.04.005. Epub 2023 May 5.
Recurrent aphthous stomatitis (RAS) is a painful disorder that commonly appears as ulcers on the oral mucosa, lasting ∼two weeks (minor) to months (major and herpetiform). Current treatment often necessitates the use of topical steroids in the form of pastes, mouthwashes, or gels, but these forms are often ineffective due to inadequate drug contact time with the ulcers. In this study, the performance of novel bilayer mucoadhesive buccal films loaded with triamcinolone acetonide (TA) has been evaluated for targeted drug delivery.
Experimental mucoadhesive films of hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), and polyvinyl pyrrolidone (PVP) were prepared by the solvent casting method, and ethyl cellulose (EC) was applied as the backing layer. The films were characterized for their physical properties, including swelling index (SI), folding endurance, adhesion force with porcine buccal mucosa, residence time and in-vitro drug release.
The data showed that the films were flexible with folding endurance> 300 times. With porcine buccal mucosa i) suitable adhesion forces were obtained (between 2.72 and 4.03 N), ii) residence times of> 24 h, and iii) surface pH between 6.8 and 7.1 indicating they would be non-irritant. All films released 100% TA over 6 h, but with varying profiles. The release of TA (over 6 h) from PVP-free films followed Fickian diffusion kinetics (diffusion-controlled release of drug), whereas the mechanism of release from PVP-containing films was found to be a superposition of diffusion-controlled and erosion-controlled release (anomalous).
The developed films hold great promise for potentially treating RAS and other oral conditions.
复发性阿弗他口炎（RAS）是一种常见的口腔黏膜疼痛性疾病，表现为溃疡，持续时间约为两周（轻度）至数月（重度和疱疹样）。目前的治疗方法通常需要使用局部类固醇，如糊剂、漱口水或凝胶，但由于与溃疡接触时间不足，这些形式往往效果不佳。在这项研究中，评估了载有曲安奈德（TA）的新型双层黏膜粘附颊膜用于靶向药物递送的性能。
通过溶剂浇铸法制备羟丙基甲基纤维素（HPMC）、聚乙烯醇（PVA）和聚乙烯吡咯烷酮（PVP）的实验性黏膜粘附膜，并将乙基纤维素（EC）用作背衬层。对膜的物理性质进行了表征，包括溶胀指数（SI）、耐折性、与猪口腔黏膜的粘附力、停留时间和体外药物释放。
数据显示，膜具有柔韧性，耐折性>300 次。与猪口腔黏膜：i）获得了合适的粘附力（在 2.72 和 4.03 N 之间），ii）停留时间>24 h，以及 iii）表面 pH 值在 6.8 和 7.1 之间，表明它们不会有刺激性。所有膜在 6 h 内释放了 100%的 TA，但释放曲线不同。无 PVP 膜的 TA 释放（6 h 内）遵循菲克扩散动力学（药物扩散控制释放），而 PVP 含膜的释放机制则发现是扩散控制和侵蚀控制释放的叠加（异常）。
开发的膜在治疗 RAS 和其他口腔疾病方面具有很大的潜力。
