Horablaga Adina, Şibu Ciobanu Alina, Megyesi Corina Iuliana, Gligor Pane Dina, Bujancă Gabriel Stelian, Velciov Ariana Bianca, Morariu Florica Emilia, Hădărugă Daniel Ioan, Mişcă Corina Dana, Hădărugă Nicoleta Gabriela
Department of Sustainable Development and Environmental Engineering, University of Life Sciences "King Mihai I" from Timişoara, Calea Aradului 119, 300645 Timişoara, Romania.
Doctoral School "Engineering of Vegetable and Animal Resources", University of Life Sciences "King Mihai I" from Timişoara, Calea Aradului 119, 300645 Timişoara, Romania.
Plants (Basel). 2023 Jun 17;12(12):2352. doi: 10.3390/plants12122352.
This is the first study on the modeling of the controlled release of the estimated antioxidants (flavonoids or flavonolignans) from β-cyclodextrin (β-CD)/hydrophilic vegetable extract complexes and the modeling of transdermal pharmaceutical formulations based on these complexes using an overall estimation by the spectrophotometric method. The Korsmeyer-Peppas model was chosen for evaluating the release mechanisms. β-CD/chamomile ( L., Asteraceae) ethanolic extract and β-CD/milk thistle ( L., Asteraceae) ethanolic extract complexes were obtained by the co-crystallization method with good recovering yields of 55-76%, slightly lower than for β-CD/silibinin or silymarin complexes (~87%). According to differential scanning calorimetry (DSC) and Karl Fischer water titration (KFT), the thermal stability of complexes is similar to β-CD hydrate while the hydration water content is lower, revealing the formation of molecular inclusion complexes. In the Korsmeyer-Peppas model, β-CD/ flower extract complexes reveal Case II transport mechanisms, while the corresponding complexes with leaf extracts indicate non-Fickian diffusion for the controlled release of antioxidants in ethanol 60 and 96%. The same non-Fickian diffusion was revealed by β-CD/ extract and β-CD/silibinin complexes. On the contrary, almost all model transdermal pharmaceutical formulations based on β-CD/ extract complexes and all those based on β-CD/ extract complexes revealed non-Fickian diffusion for the antioxidant release. These results indicate that -bonding is mainly involved in the diffusion of antioxidants into a β-CD based matrix, while the controlled release of antioxidants in model formulations is mainly due to hydrophobic interactions. Results obtained in this study can be further used for studying the particular antioxidants (namely rutin or silibinin, quantified, for example, by liquid chromatographic techniques) for their transdermal transport and biological effects in innovatively designed pharmaceutical formulations that can be obtained using "green" methods and materials.
这是第一项关于从β-环糊精（β-CD）/亲水性植物提取物复合物中可控释放预估抗氧化剂（类黄酮或黄酮木脂素）的建模研究，以及基于这些复合物的透皮药物制剂建模研究，采用分光光度法进行整体评估。选择Korsmeyer-Peppas模型来评估释放机制。β-CD/洋甘菊（菊科，L.）乙醇提取物和β-CD/水飞蓟（菊科，L.）乙醇提取物复合物通过共结晶法获得，回收率良好，为55 - 76%，略低于β-CD/水飞蓟宾或水飞蓟素复合物（约87%）。根据差示扫描量热法（DSC）和卡尔费休水分滴定法（KFT），复合物的热稳定性与β-CD水合物相似，而水合水含量较低，表明形成了分子包合物。在Korsmeyer-Peppas模型中，β-CD/花提取物复合物显示出Case II转运机制，而相应的叶提取物复合物在60%和96%乙醇中抗氧化剂的控释表明为非菲克扩散。β-CD/提取物和β-CD/水飞蓟宾复合物也显示出相同的非菲克扩散。相反，几乎所有基于β-CD/提取物复合物的模型透皮药物制剂以及所有基于β-CD/提取物复合物的制剂在抗氧化剂释放方面均显示出非菲克扩散。这些结果表明，氢键主要参与抗氧化剂向基于β-CD的基质中的扩散，而模型制剂中抗氧化剂的控释主要归因于疏水相互作用。本研究中获得的结果可进一步用于研究特定的抗氧化剂（即芦丁或水飞蓟宾，例如通过液相色谱技术定量）在创新设计的药物制剂中的透皮转运和生物学效应，这些制剂可使用“绿色”方法和材料获得。
