Pharmacy Department, Federal University of Sergipe, Sergipe, Brazil.
Department of Biological Chemistry, Regional University of Cariri, Crato, Ceará, Brazil.
Biomed Pharmacother. 2017 May;89:201-207. doi: 10.1016/j.biopha.2017.01.158. Epub 2017 Feb 20.
Cyclodextrins (CDs) have been used as important pharmaceutical excipients for improve the physicochemical properties of the drugs of low solubility as the essential oil of Hyptis martiusii. This oil is important therapeutically, but the low solubility and bioavailability compromises your use. Therein, the aim of this study was to obtain and to characterize physico-chemically the samples obtained by physical mixture (PM), paste complexation (PC) and slurry complexation (SC) of the essential oil Hyptis martiusii (EOHM) in β-CD, and to compare the antibacterial and modulatory-antibiotic activity of products obtained and oil free. The physicochemical characterization was performed by differential scanning calorimetry (DSC), thermogravimetry/derivative thermogravimetry (TG/DTG), scanning electron microscopy (SEM), X-ray diffraction (XRD) and Karl Fischer titration. Additionally, the antibacterial tests were performed by microdilution technique. Thus, it was observed that the PM method showed low complexing capacity, unlike PC and SC in which it was observed the formation of inclusion complexes. In addition, the second stage of the TG/DTG curves showed that SC was the best method inclusion with mass loss of 6.9% over the PC that was 6.0%. The XRD results corroborate with the results above suggesting the formation of new solid phase and the SEM photomicrographs showed the porous surface of the samples PC and SC. The essential oil alone demonstrated an antibacterial and modulatory effect against the S. aureus and the Gram negative strain, respectively. However, the β-CD and the inclusion complex did not demonstrate any biological activity in the performed antibacterial assays.
环糊精（CDs）已被用作改善低溶解度药物理化性质的重要药用辅料，如 Hyptis martiusii 的精油。这种油在治疗上很重要，但低溶解度和生物利用度影响了它的应用。因此，本研究的目的是获得并表征通过物理混合物（PM）、糊剂络合（PC）和浆液络合（SC）获得的 Hyptis martiusii 精油（EOHM）与β-CD 样品的物理化学性质，并比较所得产物和无油的抗菌和调节抗生素活性。物理化学表征通过差示扫描量热法（DSC）、热重/导数热重（TG/DTG）、扫描电子显微镜（SEM）、X 射线衍射（XRD）和卡尔费休滴定法进行。此外，通过微量稀释技术进行了抗菌试验。因此，观察到 PM 方法表现出低的包合能力，而 PC 和 SC 方法则观察到形成了包合物。此外，TG/DTG 曲线的第二阶段表明，SC 是最佳的包合方法，质量损失为 6.9%，而 PC 为 6.0%。XRD 结果与上述结果一致，表明形成了新的固相，SEM 照片显示了 PC 和 SC 样品的多孔表面。单独的精油对金黄色葡萄球菌和革兰氏阴性菌均表现出抗菌和调节作用。然而，β-CD 和包合物在进行的抗菌试验中均没有表现出任何生物活性。
