Keck Cornelia M, Abdelkader Ayat, Pelikh Olga, Wiemann Sabrina, Kaushik Vasudha, Specht David, Eckert Ralph W, Alnemari Reem M, Dietrich Henriette, Brüßler Jana
Department of Pharmaceutics and Biopharmaceutics, Philipps-University of Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany.
Pharmaceutics. 2022 Mar 19;14(3):678. doi: 10.3390/pharmaceutics14030678.
(1) Background: The ex vivo porcine ear model is often used for the determination of the dermal penetration efficacy of chemical compounds. This study investigated the influence of the post-slaughter storage time of porcine ears on the dermal penetration efficacy of chemical compounds. (2) Methods: Six different formulations (curcumin and different fluorescent dyes in different vehicles and/or nanocarriers) were tested on ears that were (i) freshly obtained, (ii) stored for 24 or 48 h at 4 °C after slaughter before use and (iii) freshly frozen and defrosted 12 h before use. (3) Results: Results showed that porcine ears undergo post-mortem changes. The changes can be linked to rigor mortis and all other well-described phenomena that occur with carcasses after slaughter. The post-mortem changes modify the skin properties of the ears and affect the penetration efficacy. The onset of rigor mortis causes a decrease in the water-holding capacity of the ears, which leads to reduced penetration of chemical compounds. The water-holding capacity increases once the rigor is released and results in an increased penetration efficacy for chemical compounds. Despite different absolute penetration values, no differences in the ranking of penetration efficacies between the different formulations were observed between the differently aged ears. (4) Conclusions: All different types of ears can be regarded to be suitable for dermal penetration testing of chemical compounds. The transepidermal water loss (TEWL) and/or skin hydration of the ears were not correlated with the ex vivo penetration efficacy because both an impaired skin barrier and rigor mortis cause elevated skin hydration and TEWL values but an opposite penetration efficacy. Other additional values (for example, pH and/or autofluorescence of the skin) should, therefore, be used to select suitable and non-suitable skin areas for ex vivo penetration testing. Finally, data from this study confirmed that smartFilms and nanostructured lipid carriers (NLC) represent superior formulation strategies for efficient dermal and transdermal delivery of curcumin.
(1) 背景：离体猪耳模型常用于测定化合物的皮肤渗透效果。本研究调查了猪耳屠宰后储存时间对化合物皮肤渗透效果的影响。(2) 方法：在以下几种猪耳上测试了六种不同配方（姜黄素以及不同载体和/或纳米载体中的不同荧光染料）：(i) 刚获取的；(ii) 屠宰后在4℃储存24或48小时后使用的；(iii) 刚冷冻并在使用前12小时解冻的。(3) 结果：结果表明猪耳会发生死后变化。这些变化与尸僵以及屠宰后胴体出现的所有其他已充分描述的现象有关。死后变化改变了耳朵的皮肤特性并影响渗透效果。尸僵的出现导致耳朵持水能力下降，进而使化合物的渗透减少。尸僵解除后持水能力增加，导致化合物的渗透效果增强。尽管绝对渗透值不同，但在不同老化程度的耳朵之间，不同配方的渗透效果排名没有差异。(4) 结论：所有不同类型的耳朵都可被视为适合进行化合物的皮肤渗透测试。耳朵的经表皮水分流失（TEWL）和/或皮肤水合作用与离体渗透效果无关，因为皮肤屏障受损和尸僵都会导致皮肤水合作用和TEWL值升高，但渗透效果相反。因此，应使用其他附加值（例如皮肤的pH值和/或自发荧光）来选择适合和不适合进行离体渗透测试的皮肤区域。最后，本研究的数据证实，智能薄膜和纳米结构脂质载体（NLC）代表了用于姜黄素高效皮肤和透皮递送的优越配方策略。
