Usach Iris, Alaimo Alessandro, Fernández Juan, Ambrosini Alessandro, Mocini Sara, Ochiuz Lacramioara, Peris José-Esteban
Department of Pharmacy and Pharmaceutical Technology and Parasitology, University of Valencia, Burjassot, 46100 Valencia, Spain.
Department of Pharmaceutical Technology, "Grigore T. Popa" University of Medicine and Pharmacy, 700115 Iasi, Romania.
Pharmaceutics. 2021 Feb 6;13(2):224. doi: 10.3390/pharmaceutics13020224.
spp. extracts are known for their use in traditional Korean, Chinese, and Japanese medicine in the treatment of gastrointestinal disorders, anxiety, and allergies. Among their main components with pharmacological activity, the most relevant are magnolol and honokiol, which also show antitumoral activity. The objectives of this work were to study some physicochemical properties of both substances and their stability under different conditions of temperature, pH, and oxidation. Additionally, liposomes of honokiol (the least stable compound) were formulated and characterized. Both compounds showed pH-dependent solubility, with different solubility-pH profiles. Magnolol showed a lower solubility than honokiol at acidic pH values, but a higher solubility at alkaline pH values. The partition coefficients were similar and relatively high for both compounds (log P ≈ 4.5), indicating their lipophilic nature. Honokiol was less stable than magnolol, mainly at neutral and basic pH values. To improve the poor stability of honokiol, it was suitably loaded in liposomes. The obtained liposomes were small in size (175 nm), homogeneous (polydispersity index = 0.17), highly negatively charged (-11 mV), and able to incorporate high amounts of honokiol (entrapment efficiency = 93.4%). The encapsulation of honokiol in liposomes increased its stability only at alkaline pH values.
某些植物提取物在传统的韩国、中国和日本医学中用于治疗胃肠道疾病、焦虑症和过敏症，因而闻名。在其具有药理活性的主要成分中，最相关的是厚朴酚和和厚朴酚，它们也具有抗肿瘤活性。这项工作的目的是研究这两种物质的一些物理化学性质以及它们在不同温度、pH值和氧化条件下的稳定性。此外，还制备并表征了和厚朴酚（最不稳定的化合物）脂质体。两种化合物均表现出pH依赖性溶解度，具有不同的溶解度-pH曲线。在酸性pH值下，厚朴酚的溶解度低于和厚朴酚，但在碱性pH值下，其溶解度更高。两种化合物的分配系数相似且相对较高（log P≈4.5），表明它们具有亲脂性。和厚朴酚比厚朴酚更不稳定，主要在中性和碱性pH值条件下。为了改善和厚朴酚较差的稳定性，将其适当地负载于脂质体中。所制备的脂质体尺寸小（175nm）、均一（多分散指数=0.17）、带高度负电荷（-11mV），并且能够包封大量的和厚朴酚（包封率=93.4%）。将和厚朴酚包封于脂质体中仅在碱性pH值下提高了其稳定性。
