Department of Food and Drug, Parco Area delle Scienze 27/A, Università di Parma, 43124 Parma, Italy.
Department of Food and Drug, Parco Area delle Scienze 27/A, Università di Parma, 43124 Parma, Italy.
Eur J Pharm Sci. 2018 Mar 30;115:233-239. doi: 10.1016/j.ejps.2018.01.031.
The aim of the present work was to investigate the potential of microemulsions for the buccal administration of triamcinolone acetonide. Microemulsions were developed by the construction of pseudoternary phase diagrams, using the aqueous titration method. Among all microemulsions prepared and tested for stability, three were selected and submitted to characterization and in vitro permeation/retention experiments, using pig esophageal epithelium, an accepted model of the buccal mucosa. Furthermore, one microemulsion was added of excipients (stearylamine, CTAB and chitosan) able to alter the charge of droplets. The results obtained show that the permeation of triamcinolone acetonide across pig esophageal epithelium was not influenced by the droplet size nor by the composition, but only by the presence of chitosan, polysaccharide able to increase the transport across mono and stratified epithelia. The determination of the permeation parameters allowed us to show that chitosan acts on the diffusion parameter across the tissue and not on the partitioning parameter; for the same reason the tissue retention of triamcinolone acetonide was not modified. Triamcinolone flux (2.6 μg cm h) was too low to make systemic administration feasible (dose required 2.5 to 60 mg/day). The amount of triamcinolone acetonide recovered in the mucosa after only 10 min. of microemulsion application was much higher than after overnight application of the commercial paste Omicilon® A. This suggests that triamcinolone acetonide microemulsions can be an interesting alternative to the commercial formulation to treat diseases of the buccal mucosa. Owing to the fast uptake by the tissue, the formulation can be used as a mouthwash.
本工作旨在研究微乳在曲安奈德经口腔给药中的应用潜力。采用水相滴定法构建伪三元相图，开发微乳。在所有制备并测试稳定性的微乳中，选择了三种进行特征描述和体外渗透/保留实验，使用猪食管上皮，这是口腔黏膜的公认模型。此外，还向一种微乳中添加了能够改变液滴电荷的赋形剂（硬脂胺、CTAB 和壳聚糖）。结果表明，曲安奈德在猪食管上皮中的渗透不受液滴大小或组成的影响，而仅受壳聚糖的影响，壳聚糖是一种能够增加单和分层上皮跨膜转运的多糖。渗透参数的测定表明壳聚糖作用于组织中的扩散参数，而不是分配参数；出于同样的原因，曲安奈德在组织中的保留没有改变。曲安奈德通量（2.6μg cm h）太低，无法进行全身给药（所需剂量为 2.5 至 60mg/天）。微乳应用 10 分钟后在粘膜中回收的曲安奈德量远高于 Omicilon® A 商业糊剂的 overnight 应用量。这表明曲安奈德微乳可以作为治疗口腔黏膜疾病的商业制剂的一种替代制剂。由于组织的快速吸收，该制剂可用作漱口剂。
