Department of Pharmacy, Laboratório Escola de Farmácia Industrial, Federal University of Rio Grande do Norte, Natal, RN 59012-570, Brazil.
Department of Pharmacy, Laboratório de Química Farmacêutica Computacional, Federal University of Rio Grande do Norte, Natal, RN 59012-570, Brazil.
Int J Mol Sci. 2020 Jan 31;21(3):942. doi: 10.3390/ijms21030942.
The development of inclusion complexes is used to encapsulate nonpolar compounds and improve their physicochemical characteristics. This study aims to develop complexes made up of Mart oil (EOO) and β-cyclodextrin (β-CD) or hydroxypropyl-β-cyclodextrin (HP-β-CD) by either kneading (KND) or slurry (SL). Complexes were analyzed by molecular modeling, Fourier-transform infrared spectroscopy, scanning electron microscopy, powder X-ray diffraction, thermogravimetry analysis and differential scanning calorimetry. The antibacterial activity was expressed as Minimum Inhibitory Concentration (MIC), and the antibiotic resistance modulatory activity as subinhibitory concentration (MIC/8) against , , and . Inclusion complexes with β-CD and HP-β-CD were confirmed, and efficiency was proven by an interaction energy between oleic acid and β-CD of -41.28 ± 0.57 kJ/mol. MIC values revealed higher antibacterial activity of complexes compared to the isolated oil. The modulatory response of EOO and EOO-β-CD prepared by KND as well as of EOO-β-CD and EOO-HP-β-CD prepared by SL showed a synergistic effect with ampicillin against , whereas it was not significant with the other drugs tested, maintaining the biological response of antibiotics. The antimicrobial response exhibited by the complexes is of great significance because it subsidizes studies for the development of new pharmaceutical forms.
包合复合物的开发用于包裹非极性化合物并改善它们的物理化学性质。本研究旨在通过 kneading（KND）或 slurry（SL）制备由 Mart 油（EOO）和 β-环糊精（β-CD）或羟丙基-β-环糊精（HP-β-CD）组成的复合物。通过分子建模、傅里叶变换红外光谱、扫描电子显微镜、粉末 X 射线衍射、热重分析和差示扫描量热法对复合物进行分析。抗菌活性表示为最小抑菌浓度（MIC），抗生素耐药调节活性表示为亚抑菌浓度（MIC/8），针对 、 、 和 。证实了与 β-CD 和 HP-β-CD 的包合物，油酸与 β-CD 之间的相互作用能证明其效率为 -41.28 ± 0.57 kJ/mol。MIC 值表明复合物的抗菌活性高于分离油。通过 KND 制备的 EOO 和 EOO-β-CD 以及通过 SL 制备的 EOO-β-CD 和 EOO-HP-β-CD 的调制响应显示与氨苄西林对 有协同作用，而与其他测试药物则不显著，保持抗生素的生物学反应。复合物表现出的抗菌反应具有重要意义，因为它支持了开发新药物形式的研究。
