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首页> 外文期刊>Materials science & engineering >Synergy between surfactants and mucoadhesive polymers enhances the transbuccal permeation of local anesthetics from freeze-dried tablets
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Synergy between surfactants and mucoadhesive polymers enhances the transbuccal permeation of local anesthetics from freeze-dried tablets

机译：表面活性剂和粘膜粘附聚合物之间的协同作用增强了冻干片剂中局部麻醉药的透颊渗透性

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摘要

We report on the advance of freeze-dried mucoadhesive orodispersible tablets (ODTs) loaded with prilocaine (PRC) and lidocaine (LDC) hydrochlorides, aiming to promote noninvasive buccal anesthesia. The influences of combining biocompatible polymers (pullulan and HPMC K100 LV) and a blend of surfactants (oleic acid, polysorbate 80 and propylene glycol) acting as chemical enhancers on the permeation of such drugs through the esophageal porcine epithelium and in vitro mucoadhesion were investigated. The ODTs were also characterized in terms of average weight, thickness, pH, drug content, in vitro release, thermal behavior and scanning electronic microscopy. A dissolution test showed fast drug release within one hour. The drug release data for all ODTs fitted first order. No significant influence of the type of mucoadhesive polymer on release was observed, while the drug release from ODTs decreased in the presence of chemical enhancers. For the ODT containing pullulan the drug release mechanism was anomalous transport, whist for all others it was case-II transport. A remarkable synergic effect between pullulan and chemical enhancers on the permeation flux, lag time, and permeability coefficient of both drugs, but mainly for PRC was observed. Pullulan together with permeation enhancers also substantially improved the work of mucoadhesion as compared to HPMC. In contrast, HPMC improved drug retention in the epithelium. The novel drug delivery platform achieved by combining a freezedrying technique, mucoadhesive biocompatible polymers, and chemical permeation enhancers displayed an effective strategy for the transbuccal delivery of PRC and LDC that can be used to improve needle-free buccal anesthesia.
机译：我们报告载有丙胺卡因（PRC）和利多卡因（LDC）盐酸盐的冻干粘膜黏膜口腔分散片（ODT）的进展，旨在促进无创颊麻醉。研究了将生物相容性聚合物（普鲁兰酶和HPMC K100 LV）与作为化学增强剂的表面活性剂（油酸，聚山梨酯80和丙二醇）的混合物对此类药物通过食道猪上皮的渗透和体外粘膜黏附的影响。还用平均重量，厚度，pH，药物含量，体外释放，热行为和扫描电子显微镜表征了ODT。溶出度测试显示一小时内药物快速释放。所有ODT的药物释放数据符合一阶。没有观察到粘膜粘附聚合物类型对释放的显着影响，而在化学增强剂的存在下，ODTs的药物释放减少。对于含有支链淀粉的ODT，药物释放机制是异常运输，而对于其他所有药物，则是病例二运输。支链淀粉和化学增强剂之间对两种药物的渗透通量，滞后时间和渗透系数具有显着的协同作用，但主要针对PRC。与HPMC相比，支链淀粉与渗透促进剂还大大改善了粘膜粘附的作用。相反，HPMC改善了药物在上皮细胞中的滞留性。通过结合冻干技术，粘膜粘附性生物相容性聚合物和化学渗透促进剂实现的新型药物递送平台显示了PRC和LDC经颊递送的有效策略，可用于改善无针颊麻醉。

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