School of Basic Medical Sciences, Shandong First Medical University & Shandong Academy of Medical Sciences, Taian, China.
Drug Deliv. 2021 Dec;28(1):2574-2581. doi: 10.1080/10717544.2021.2009938.
In the present study, the porous starch (PS) was used as an efficient carrier of honokiol (HK), and the HK-loaded PS (HPS) delivery system was prepared by melting method without using organic solvents. Its physical-chemical properties, solubility and oral bioavailability were also investigated. The obtained results proved that the HK in the HPS was mostly amorphous when it was loaded into the PSs with 87.54 ± 1.52% of encapsulation efficiency (EE) and 12.51 ± 0.22% of drug loading (DL) capacity. The water-solubility of the HPS was increased to 115.27 ± 2.92 μg/mL (pH = 1.2, artificial gastric juice (AGJ)), 161.58 ± 3.42 (pH = 6.8, artificial intestinal juice (AIJ)) and 148.5 ± 1.89 μg/mL (pH = 5.5, simulated tumor microenvironment), being 6.07, 4.38 and 4.87-folds higher than free HK. dissolution tests showed the HK was significantly higher from HPS than from free HK. Furthermore, compared with free HK, the release rate and the bioavailability was also substantially improved for HK from the HPS. Meanwhile, the HPS generated a higher inhibition to HepG2 cells than free HK.
在本研究中，多孔淀粉（PS）被用作厚朴酚（HK）的有效载体，通过熔融法制备了载有 HK 的 PS（HPS）递送系统，而不使用有机溶剂。还研究了其物理化学性质、溶解度和口服生物利用度。结果表明，当 HK 以 87.54±1.52%的包封效率（EE）和 12.51±0.22%的载药量（DL）能力负载到 PS 中时，HPS 中的 HK 主要为无定形。HPS 的水溶性提高到 115.27±2.92μg/mL（pH=1.2，人工胃液（AGJ））、161.58±3.42（pH=6.8，人工肠液（AIJ））和 148.5±1.89μg/mL（pH=5.5，模拟肿瘤微环境），分别是游离 HK 的 6.07、4.38 和 4.87 倍。溶解试验表明，HPS 中 HK 的释放量明显高于游离 HK。此外，与游离 HK 相比，HPS 中 HK 的释放率和生物利用度也得到了显著提高。同时，HPS 对 HepG2 细胞的抑制作用也高于游离 HK。
