Meenatchi Venkatasamy, Narayanan Kannan Badri, Sood Ankur, Han Sung Soo
School of Chemical Engineering, Yeungnam University, Gyeongsan-si, Gyeongsangbuk-do 38541, Republic of Korea; Department of Physiology, Saveetha Dental College and Hospitals, Saveetha Institute of Medical and Technical Science (SIMATS), Saveetha University, Chennai, 600077, India.
School of Chemical Engineering, Yeungnam University, Gyeongsan-si, Gyeongsangbuk-do 38541, Republic of Korea.
Int J Pharm. 2024 Sep 5;662:124293. doi: 10.1016/j.ijpharm.2024.124293. Epub 2024 May 31.
Nanoencapsulation has gained considerable attention because of its unique features and advantages in anticancer drug delivery. Amygdalin (AMY) is an anticancer compound, showing limitations in its applications by low stability. Herein, the inclusion complexes (ICs) of AMY with β-cyclodextrin (βCD), and its derivatives such as 2-hydroxypropyl-βCD (HPβCD) and methyl-βCD (MβCD) were fabricated. The fabricated AMY/CD-ICs were thoroughly evaluated using Fourier-transform infrared spectroscopy, powder X-ray diffraction, thermogravimetric/differential thermal analysis, proton nuclear magnetic resonance, ultraviolet-visible diffuse reflectance spectroscopy, and photoluminescence techniques. Double reciprocal profile study of the absorption and fluorescence spectra revealed that the AMY formed the ICs with βCD derivatives at a guest/host stoichiometric ratio of 1/1. The thermal stability of AMY was enhanced as the IC formation aid observed by the shift of thermal degradation temperature of AMY from the range of ∼ 220-250 °C to > 295 °C. Theoretical analyses of the energetic, electronic, and global reactivity parameters of the AMY/CD-ICs were evaluated using the PM3 method. Further assessment of the dissolution diagrams of AMY/CD-ICs revealed a burst release profile. In addition, cell toxicity was evaluated using the MTT assay, and the results showed that AMY/CD-ICs had significantly more efficacious in inhibiting HeLa cancer cells than AMY. These results proved that the IC formations with CDs significantly enhanced the anticancer activity of AMY.
纳米包封因其在抗癌药物递送方面的独特特性和优势而备受关注。苦杏仁苷(AMY)是一种抗癌化合物,但由于稳定性低,其应用受到限制。在此,制备了AMY与β-环糊精(βCD)及其衍生物如2-羟丙基-βCD(HPβCD)和甲基-βCD(MβCD)的包合物(ICs)。使用傅里叶变换红外光谱、粉末X射线衍射、热重/差示热分析、质子核磁共振、紫外可见漫反射光谱和光致发光技术对制备的AMY/CD-ICs进行了全面评估。吸收光谱和荧光光谱的双倒数曲线研究表明,AMY与βCD衍生物以客体/主体化学计量比1/1形成ICs。通过观察AMY的热降解温度从约220-250°C范围转移到>295°C,发现随着IC的形成,AMY的热稳定性得到增强。使用PM3方法对AMY/CD-ICs的能量、电子和全局反应性参数进行了理论分析。对AMY/CD-ICs溶解曲线的进一步评估显示出突释曲线。此外,使用MTT法评估细胞毒性,结果表明AMY/CD-ICs在抑制HeLa癌细胞方面比AMY更有效。这些结果证明,与CD形成ICs显著增强了AMY的抗癌活性。