Song Jizheng, Hu Yu, Yang Shiyu, Liu Dexue, Tseng Yiider, Li Lingjun
College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, China.
Innovative Institute of Chinese Medicine and Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, China.
Polymers (Basel). 2025 Jan 27;17(3):349. doi: 10.3390/polym17030349.
Hydrophobic modification alters the properties of Pluronic F127 to form micelles more efficiently and enhances its drug-loading capacity. However, selecting the appropriate hydrophobic group for modification is laborious. In this paper, we propose an efficient approach for predicting key parameters to select hydrophobic groups for F127 modification prior to synthesis, in order to improve the formability and stability of the micelles. The results of nuclear magnetic resonance and isothermal titration calorimetry were utilized to establish a function for predicting the hydrophile-lipophile balance, critical micelle concentration, and Gibbs free energy of the products based on the structure of raw material. These predicted values can assist us in selecting suitable hydrophobic groups for F127 modification. Subsequently, we successfully tested our method and validated our work using pharmaceutical evaluation methods, such as appearance observation, particle size measurement, drug loading determination, equilibrium binding rate assessment, storage stability testing, and the plotting of accumulation release curves. Therefore, we suggest that our work could provide a model linking the molecular structure to properties, with the purpose of pre-selecting modification products that have advantages in micelle preparation. This can facilitate the application of F127 in preparing nano-micelles.
疏水修饰改变了泊洛沙姆F127的性质，使其能更高效地形成胶束，并提高其载药能力。然而，选择合适的疏水基团进行修饰是一项艰巨的任务。在本文中，我们提出了一种有效的方法，用于在合成前预测选择用于F127修饰的疏水基团的关键参数，以提高胶束的可形成性和稳定性。利用核磁共振和等温滴定量热法的结果，基于原料结构建立了一个用于预测产物亲水亲油平衡、临界胶束浓度和吉布斯自由能的函数。这些预测值可以帮助我们选择适合F127修饰的疏水基团。随后，我们成功地测试了我们的方法，并使用外观观察、粒径测量、载药量测定、平衡结合率评估、储存稳定性测试和累积释放曲线绘制等药物评价方法验证了我们的工作。因此，我们认为我们的工作可以提供一个将分子结构与性质联系起来的模型，目的是预先选择在胶束制备中具有优势的修饰产物。这可以促进F127在制备纳米胶束中的应用。
