α-倒捻子素/甘草酸纳米胶束的制备、表征及评价

Preparation, Characterization and Performance Evaluation of α-Mangostin/Glycyrrhizic Acid Nanomicelles

摘要:

制备α-倒捻子素/甘草酸纳米胶束（α-Mangostin/glycyrrhizic Acid Nanomicelles, α-MG/GA NMs），以提高α-倒捻子素（α-Mangostin, α-MG）的溶解度和抗氧化活性。以甘草酸（Glycyrrhizic Acid, GA）为载体制备α-MG/GA NMs，并进行工艺优化，表征和体外释放度、体外抗氧化活性评价。结果表明，在最佳工艺下制得的α-MG/GA NMs中α-MG溶解度为232.65 μg/mL，比水中溶解度大了近1 163倍；α-MG/GA NMs粒径为123.46 nm、PDI为0.24、Zeta电位为-20.94 mV；透射电镜（TEM）和扫描电镜（SEM）显示其为类球形；冻干后在光照、高温、高湿条件下稳定性良好；傅里叶红外光谱（FT-IR）显示α-MG与GA可能发生氢键相互作用；体外释放结果表明α-MG/GA NMs能促进α-MG释放，具有缓释效果，在pH值7.4、5.0的释放介质中24 h累积释放率分别为47.03%、40.56%；与游离α-MG相比，α-MG/GA NMs的抗氧化活性更强，且GA与α-MG具有协同抗氧化作用，对DPPH自由基、ABTS+自由基清除作用的协同指数（CI值）分别为0.62、0.58。该研究制备的α-MG/GA NMs提高了α-MG的溶解度与抗氧化活性，为α-MG在食品、药品、化妆品等领域的应用提供了理论基础。

Abstract:

α-Mangostin/glycyrrhizic acid nanomicelles (α-MG/GA NMs) were prepared to improve the solubility and antioxidant activity of α-mangostin (α-MG). Glycyrrhizic acid (GA) was used as the carrier to prepare α-MG/GA NMs, and single factor design and response surface methodology were adopted to optimize the preparation process. The characteristics, in vitro release, and in vitro antioxidant activity of α-MG/GA NMs were evaluated. The results show that the solubility of α-MG in α-MG/GA NMs prepared under the optimal conditions reached 232.65 μg/mL, which is nearly 1163 times higher than that in water. The particle size of α-MG/GA NMs was 123.46 nm, and their PDI and zeta potential were 0.24 and -20.94 mV, respectively. Transmission electron microscopy (TEM) and scanning electron microscopy (SEM) showed that the NMs are spherical. After freeze-drying, the α-MG/GA NMs prepared were stable under irradiation at high temperature and high humidity. Fourier transform infrared spectroscopy (FT-IR) showed that hydrogen bonding interactions between α-MG and GA may take place. The in vitro release analysis demonstrated that α-MG/GA NMs can promote the release of α-MG and have a sustained release effect. The cumulative release rates of α-MG/GA NMs were 47.03% and 40.56% in release media with pH values of 7.4 and 5.0, respectively, for 24 h. Compared with that of free α-MG, the antioxidant activity of α-MG/GA NMs was more substantial. Furthermore, GA and α-MG had a synergistic antioxidant effect. The synergistic indexes (CI values) of DPPH and ABTS+ radical scavenging were 0.62 and 0.58, respectively. The α-MG/GA NMs prepared in this study improved the solubility and antioxidant activity of α-MG, providing a theoretical basis for applying α-MG in food, medicine, cosmetics, and other fields.