Qiao Zifan, Chen Lihua, Bello Mubarak G, Huang Shiyu
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Chinese Medicine, No. 1688, Meiling Road, Nanchang 330004, China.
Department of Pharmaceutics and Industrial Pharmacy, Kaduna State University, Kaduna 800244, Nigeria.
Pharmaceutics. 2025 Apr 9;17(4):497. doi: 10.3390/pharmaceutics17040497.
Muscone (MUS), a primary active component of musk, is known for its significant pharmacological properties. However, its clinical application is limited due to poor water solubility and moderate stability. This study aims to address these limitations by encapsulating MUS within biodegradable γ-cyclodextrin metal-organic frameworks (γ-CD-MOFs) using a solvent-free method to enable oral MUS delivery by improving solubility and stability, pending in vivo validation. MUS was encapsulated into γ-CD-MOFs using a solvent-free method, achieving an optimal loading rate of 10.6 ± 0.7%. Comprehensive characterization was performed using scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), and thermogravimetric analysis (TGA). Biocompatibility was assessed using RAW264.7 cells, and molecular dynamics simulations were conducted to study the interactions between MUS and γ-CD-MOFs. Characterization techniques confirmed the successful encapsulation of MUS into γ-CD-MOFs. Biocompatibility studies revealed no cytotoxicity, indicating that the system is safe for drug delivery. Molecular dynamics simulations showed that MUS preferentially occupies the large spherical cages of γ-CD-MOFs, driven by non-covalent interactions. Solubility tests and in vitro release studies demonstrated that the solubility of MUS was improved after encapsulation within γ-CD-MOFs. Stability assessments indicated that γ-CD-MOFs significantly enhanced the thermal and photostability of MUS, with high residual amounts remaining under various storage conditions. This study demonstrates the potential of γ-CD-MOFs to solidify MUS, enhance its solubility, and improve its storage stability, providing a foundation for its future use in pharmaceutical applications.
麝香酮（MUS）是麝香的主要活性成分，以其显著的药理特性而闻名。然而，由于其水溶性差和稳定性一般，其临床应用受到限制。本研究旨在通过使用无溶剂方法将MUS包裹在可生物降解的γ-环糊精金属有机框架（γ-CD-MOFs）中来解决这些限制，以便通过提高溶解度和稳定性实现MUS的口服给药，尚待体内验证。采用无溶剂方法将MUS包裹到γ-CD-MOFs中，实现了10.6±0.7%的最佳负载率。使用扫描电子显微镜（SEM）、X射线衍射（XRD）、傅里叶变换红外光谱（FTIR）和热重分析（TGA）进行了全面表征。使用RAW264.7细胞评估了生物相容性，并进行了分子动力学模拟以研究MUS与γ-CD-MOFs之间的相互作用。表征技术证实了MUS成功包裹到γ-CD-MOFs中。生物相容性研究表明没有细胞毒性，表明该系统用于药物递送是安全的。分子动力学模拟表明，在非共价相互作用的驱动下，MUS优先占据γ-CD-MOFs的大球形笼。溶解度测试和体外释放研究表明，MUS包裹在γ-CD-MOFs中后溶解度得到提高。稳定性评估表明，γ-CD-MOFs显著提高了MUS的热稳定性和光稳定性，在各种储存条件下都有高残留量。本研究证明了γ-CD-MOFs固化MUS、提高其溶解度和改善其储存稳定性的潜力，为其未来在药物应用中的使用奠定了基础。
