Key Laboratory of Modern Preparation of TCM of Ministry of Education, Institute for Advanced Study, Jiangxi University of Chinese Medicine, Nanchang 330004, China.
Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Molecules. 2024 Feb 4;29(3):715. doi: 10.3390/molecules29030715.
Porous materials are widely used as an effective strategy for the solubilization of insoluble drugs. In order to improve the solubility and bioavailability of low water-solubility drugs, it is necessary to prepare porous materials. Mannitol is one of the most popular excipients in food and drug formulations. In this study, porous mannitol was investigated as a drug carrier for low water solubility drugs. Its fabrication, drug loading, and drug release mechanisms were investigated. Porous mannitol was fabricated using the co-spray-antisolvent process and utilizing polyvinylpyrrolidone K30 (PVP K30) as the template agent. Porous mannitol particles were prepared by changing the proportion of the template agent, spraying the particles with mannitol, and eluting with ethanol in order to regulate their pore structure. In subsequent studies, porous mannitol morphology and characteristics were determined systematically. Furthermore, curcumin and ibuprofen, two poorly water-soluble drugs, were loaded into porous mannitol, and their release profiles were analyzed. The results of the study indicated that porous mannitol can be prepared using PVP K30 as a template and that the amount of template agent can be adjusted in order to control the structure of the porous mannitol. When the template agent was added in amounts of 1%, 3%, and 5%, the mannitol pore size increased by 167.80%, 95.16%, and 163.98%, respectively, compared to raw mannitol. Molecular docking revealed that mannitol and drugs are adsorbents and adhere to each other by force interaction. The cumulative dissolution of curcumin and ibuprofen-loaded porous mannitol reached 69% and 70%, respectively. The release mechanism of curcumin and ibuprofen from drug-loaded mannitol was suitable for the Korsmeyer-Peppas kinetic model. In summary, the co-spray-antisolvent method proved effective in fabricating porous materials rapidly, and porous mannitol had a remarkable effect on drug solubilization. The results obtained are conducive to the development of porous materials.
多孔材料被广泛用作增溶难溶性药物的有效策略。为了提高低水溶性药物的溶解度和生物利用度，需要制备多孔材料。甘露醇是食品和药物配方中最常用的赋形剂之一。在这项研究中，研究了多孔甘露醇作为低水溶性药物的载体。研究了其制备、载药和药物释放机制。通过共喷雾-抗溶剂法制备多孔甘露醇，并利用聚乙烯吡咯烷酮 K30（PVP K30）作为模板剂。通过改变模板剂的比例、喷雾甘露醇并以乙醇洗脱来制备多孔甘露醇颗粒，以调节其孔结构。在后续研究中，系统地确定了多孔甘露醇的形态和特性。此外，将两种难溶性药物姜黄素和布洛芬载入多孔甘露醇中，并分析其释放曲线。研究结果表明，可以使用 PVP K30 作为模板制备多孔甘露醇，并且可以调节模板剂的用量来控制多孔甘露醇的结构。当模板剂添加量分别为 1%、3%和 5%时，甘露醇的孔径分别比原甘露醇增加了 167.80%、95.16%和 163.98%。分子对接表明，甘露醇和药物是吸附剂，通过力相互作用吸附在一起。载有姜黄素和布洛芬的多孔甘露醇的累积溶解率分别达到 69%和 70%。载药甘露醇中姜黄素和布洛芬的释放机制符合 Korsmeyer-Peppas 动力学模型。总之，共喷雾-抗溶剂法被证明是一种快速制备多孔材料的有效方法，多孔甘露醇对药物增溶效果显著。研究结果有利于多孔材料的开发。
