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Isoliquiritigenin Nanoemulsion Preparation by Combined Sonication and Phase-Inversion Composition Method: In Vitro Anticancer Activities
Bioengineering Pub Date : 2022-08-10 , DOI: 10.3390/bioengineering9080382
Jianman Wang 1 , Hongjin Chen 2, 3, 4 , Tao Guo 1, 5 , Ping Yue 1, 5 , Tianbao Qian 1, 5 , Xiangyu Zeng 1, 5 , Yali Luo 1, 5 , Jiangmin Li 1, 5 , Lijing Teng 1, 5 , Qingyu Liu 1, 5 , Liang Hong 1, 5 , Zijiang Yu 1 , Zuquan Hu 1, 5
Affiliation  

Isoliquiritigenin (ILQ) has a number of biological activities such as antitumor and anti-inflammatory effects. However, biomedical applications of ILQ are impeded by its poor aqueous solubility. Therefore, in this research, we prepared a novel ILQ-loaded nanoemulsion, i.e., ILQ-NE, which consisted of Labrafil® M 1944 CS (oil), Cremophor® EL (surfactant), ILQ, and phosphate-buffered saline, by employing a combined sonication (high-energy) and phase-inversion composition (low-energy) method (denoted as the SPIC method). The ILQ-NE increased the ILQ solubility ~1000 times more than its intrinsic solubility. It contained spherical droplets with a mean diameter of 44.10 ± 0.28 nm and a narrow size distribution. The ILQ loading capacity was 4%. The droplet size of ILQ-NE remained unchanged during storage at 4 °C for 56 days. Nanoemulsion encapsulation effectively prevented ILQ from degradation under ultraviolet light irradiation, and enhanced the ILQ in vitro release rate. In addition, ILQ-NE showed higher cellular uptake and superior cytotoxicity to 4T1 cancer cells compared with free ILQ formulations. In conclusion, ILQ-NE may facilitate the biomedical application of ILQ, and the SPIC method presents an attractive avenue for bridging the merits and eliminating the shortcomings of traditional high-energy methods and low-energy methods.

中文翻译:

联合超声和相转化组合法制备异甘草素纳米乳:体外抗癌活性

异甘草素 (ILQ) 具有许多生物活性,例如抗肿瘤和抗炎作用。然而,ILQ 的生物医学应用因其水溶性差而受到阻碍。因此,在本研究中,我们制备了一种新型负载 ILQ 的纳米乳液,即 ILQ-NE,它由 Labrafil ® M 1944 CS(油)、Cremophor ®组成。EL(表面活性剂)、ILQ 和磷酸盐缓冲盐水,采用组合的超声处理(高能)和相转化组合物(低能)方法(表示为 SPIC 方法)。ILQ-NE 将 ILQ 溶解度提高到其固有溶解度的 1000 倍以上。它包含平均直径为 44.10 ± 0.28 nm 和窄尺寸分布的球形液滴。ILQ 负载能力为 4%。ILQ-NE 的液滴大小在 4 °C 储存 56 天期间保持不变。纳米乳液的包封有效地防止了ILQ在紫外光照射下的降解,提高了ILQ的体外释放率。此外,与游离 ILQ 制剂相比,ILQ-NE 对 4T1 癌细胞具有更高的细胞摄取和更高的细胞毒性。总之,ILQ-NE 可以促进 ILQ 的生物医学应用,
更新日期:2022-08-10
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