Microemulsion containing triamcinolone acetonide for buccal administration
Microemulsion containing triamcinolone acetonide for buccal administration
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DOI：
10.1016/j.ejps.2018.01.031
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发表时间：
2018-03-30
影响因子：
4.6
通讯作者：
Santi, P.
中科院分区：
文献类型：
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作者：
Padula, C.;Telo, I.;Santi, P.
本工作的目的是调查的潜在微乳的颊部给药的曲安奈德。用水滴定法建立了微乳液的拟三元相图。在所有制备和稳定性测试的微乳液中，选择了三种，并使用猪食管上皮（一种公认的颊粘膜模型）进行表征和体外渗透/保留实验。此外，一个微乳液中添加的赋形剂（硬脂胺，CTAB和壳聚糖）能够改变液滴的电荷，得到的结果表明，曲安奈德穿过猪食管上皮的渗透是不受液滴的大小，也不是由组合物，但只有壳聚糖，多糖的存在下，能够增加跨单层和复层上皮的运输。渗透参数的测定使我们能够表明，壳聚糖作用于整个组织的扩散参数，而不是分配参数;出于同样的原因，曲安奈德的组织保留没有修改。曲安西龙的流量（2.6 μ g cm（-2）h（-1））太低，不能进行全身给药（需要的剂量为2.5 ~ 60 mg/天）。微乳应用仅10分钟后，粘膜中回收的曲安西龙丙酮化物的量远高于市售糊剂Omicilon（R）A过夜应用后的量。这表明，曲安奈德微乳可以是一个有趣的替代商业制剂治疗颊粘膜疾病。由于组织的快速吸收，该制剂可用作漱口水。
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 mu g cm(-2) h(-1)) 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 (R) 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.