Alves Michele C, de Almeida Priscila A, Polonini Hudson C, Bhering Carla A P, de O Ferreira Anderson, Brandao Marcos A F, Raposo Nadia R B
Nucleo de Pesquisa e Inovacao em Ciencias da Saúde (NUPICS), Federal University of Juiz de Fora, Juiz de Fora, Brazil.
Suprema - Faculdade de Ciencias Medicas e da Saude de Juiz de Fora, Juiz de Fora, Brazil.
Curr Drug Deliv. 2018;15(8):1123-1134. doi: 10.2174/1567201815666180116090258.
Taxifolin (TAX) is a flavonoid that has numerous pharmacological properties, including an antioxidant ability superior to that of other flavonoids due to its particular structure. Nevertheless, it has low oral bioavailability, which limits its therapeutic application. In this context, potentially important approaches for systemic drug delivery could be by alternative routes such as skin and vaginal mucosa, once both routes have a variety of advantages compared with the oral route, including the ability to bypass both first-pass hepatic metabolism and the consequent degradation in the gastrointestinal tract. Vaginal delivery could also account for a local effect, or an effect on circumvent microregion.
The major objective of this study was to develop and validate a high-performance liquid chromatography (HPLC) method for the determination of TAX in a semisolid dosage forms and then to evaluate ex vivo permeations across porcine vaginal mucosa and human skin.
TAX was incorporated into an oil-in-water emulsion developed previously by our group. Method for quantification was developed and validated using HPLC. Permeation through human skin and vaginal porcine mucosa were conducted in Franz-type cells.
The method was precise (CV < 5%), accurate (recovery between 98% and 102%), linear (R2> 0.99), specific, and robust. Permeation experiments through porcine vaginal mucosa and human skin presented permeated percentages equal to 87.43% and 48.09% (per dose), respectively.
The results suggest that, in the matrixes studied, TAX may be able to exert its biological activities systemically when applied by these routes. Furthermore, it exhibits greater permeability potential when administered by intravaginal route.
紫杉叶素（TAX）是一种黄酮类化合物，具有多种药理特性，因其特殊结构，其抗氧化能力优于其他黄酮类化合物。然而，它的口服生物利用度较低，这限制了其治疗应用。在这种情况下，全身给药的潜在重要途径可能是通过皮肤和阴道黏膜等替代途径，因为这两种途径与口服途径相比具有多种优势，包括能够绕过肝脏首过代谢以及随之而来的胃肠道降解。阴道给药还可能产生局部作用，或对周围微区域产生作用。
本研究的主要目的是开发并验证一种高效液相色谱（HPLC）法，用于测定半固体剂型中的TAX，然后评估其在猪阴道黏膜和人体皮肤上的离体渗透情况。
将TAX掺入我们小组之前开发的水包油乳液中。使用HPLC开发并验证定量方法。在Franz型扩散池进行人体皮肤和猪阴道黏膜的渗透实验。
该方法精密度高（CV<5%）、准确度高（回收率在98%至102%之间）、线性良好（R2>0.99）、专属性强且稳健。通过猪阴道黏膜和人体皮肤的渗透实验显示，渗透百分比分别为87.43%和48.09%（每剂量）。
结果表明，在所研究的基质中，TAX通过这些途径给药时可能能够在全身发挥其生物活性。此外，经阴道给药时，它表现出更大的渗透潜力。
