National Nanotechnology Center, National Science and Technology Development Agency, Thailand Science Park, Pathumthani, Thailand.
Department of Chemical Engineering, Faculty of Engineering, Chulalongkorn University, Bangkok, Thailand.
Int J Pharm. 2018 Mar 1;538(1-2):21-29. doi: 10.1016/j.ijpharm.2017.12.016. Epub 2017 Dec 8.
In this study, the inclusion complex formation between α-mangostin and water-soluble quaternized β-CD grafted-chitosan (QCD-g-CS) was investigated. Inclusion complex formation with encapsulation efficiency (%EE) of 5, 15 and 75% can be varied using high speed homogenizer. Tuning %EE plays a role on physicochemical and biological properties of α-mangostin/QCD-g-CS complex. Molecular dynamics simulations indicate that α-mangostin is included within the hydrophobic β-CD cavity and being absorbed on the QCD-g-CS surface, with these results being confirmed by Fourier transform infrared (FTIR) spectroscopy. Probing the release characteristics of the inclusion complex at various %EE (5%, 15% and 75%) in simulated saliva (pH 6.8) demonstrated that α-mangostin release rates were dependent on % EE (order 5% > 15% > 75%). Additionally, higher antimicrobial and anti-inflammation activities were observed for the inclusion complex than those of free α-mangostin due to enhance the solubility of α-mangostin through the inclusion complex with QCD-g-CS.
在这项研究中，研究了α-倒捻子素与水溶性季铵化β-环糊精接枝壳聚糖（QCD-g-CS）之间的包合复合物的形成。使用高速匀浆机可以改变包合复合物的包封效率（% EE）为 5、15 和 75%。调整% EE 对 α-倒捻子素/QCD-g-CS 复合物的物理化学和生物学性质起着重要作用。分子动力学模拟表明，α-倒捻子素被包含在疏水性β-CD 空腔内，并被吸收在 QCD-g-CS 表面上，傅里叶变换红外（FTIR）光谱证实了这一结果。在模拟唾液（pH 6.8）中，研究了不同% EE（5%、15%和 75%）下包合复合物的释放特性，结果表明α-倒捻子素的释放速率取决于% EE（顺序为 5%>15%>75%）。此外，由于通过与 QCD-g-CS 的包合复合物提高了α-倒捻子素的溶解度，因此包含复合物的抗菌和抗炎活性比游离α-倒捻子素更高。
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