Laboratório de Virologia Aplicada, Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, Brazil.
AAPS PharmSciTech. 2011 Jun;12(2):587-92. doi: 10.1208/s12249-011-9621-2. Epub 2011 May 4.
The porcine esophageal mucosa has been proposed as a substitute for the buccal mucosa barrier on ex vivo permeability studies mainly due to its large surface area as well as its easier preparation. Therefore, this study compared the ex vivo permeability parameters of two drugs (carmabazepine (CBZ) and triamcinolone acetonide (TAC)) with different permeabilities and physicochemical properties through buccal and esophageal mucosae using a Franz diffusion cell system and HPLC as detection method. The freezing effects on drug permeability parameters were also evaluated by comparing them when fresh and frozen tissues were used. The barrier properties were not affected by the freezing process since the obtained parameters for both drugs were similar in frozen and fresh tissues (buccal and esophageal mucosae). However, an increase of CBZ retention was shown in frozen tissues. Fresh and frozen esophageal mucosae provided higher permeation of TAC than on buccal mucosae while the obtained permeability parameters for CBZ were similar on both mucosae. According to our results, porcine esophageal mucosa could be used as a substitute for buccal mucosa on ex vivo studies involving CBZ but not TAC. Frozen tissues could be used as substitute for fresh tissues in both cases. However, any substitution should be done with care and only if previous tests were performed, because the results could differ depending on the tested drug.
猪食管黏膜因其较大的表面积和较容易的制备而被提议作为颊黏膜屏障的替代物，主要用于体外渗透研究。因此，本研究使用 Franz 扩散池系统和 HPLC 作为检测方法，比较了两种具有不同渗透性和物理化学性质的药物（卡马西平（CBZ）和曲安奈德（TAC））通过颊黏膜和食管黏膜的体外渗透参数。还通过比较新鲜和冷冻组织时使用的冷冻对药物渗透参数的影响来评估冷冻效果。由于两种药物在冷冻和新鲜组织中获得的参数相似，因此屏障特性不受冷冻过程的影响（颊黏膜和食管黏膜）。然而，冷冻组织中 CBZ 的保留率增加。新鲜和冷冻的食管黏膜对 TAC 的渗透高于颊黏膜，而 CBZ 的渗透参数在两种黏膜上相似。根据我们的结果，猪食管黏膜可用于替代涉及 CBZ 的体外研究中的颊黏膜，但不能替代 TAC。在这两种情况下，冷冻组织都可以替代新鲜组织。但是，任何替代都应该谨慎进行，并且只有在之前进行了测试，因为结果可能因测试药物而异。
