Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy.
Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy.
Int J Pharm. 2021 Jun 1;602:120606. doi: 10.1016/j.ijpharm.2021.120606. Epub 2021 Apr 20.
18β-glycyrrhetinic acid (Gly), a natural compound obtained from licorice, is known both for the anti-inflammatory and antioxidant activities and for this reason useful for wound treatment. Due to its poor solubility, Gly is not suitable for formulations used in conventional topical products such as gels, foams and creams. Polymeric bioadhesive microparticles (MP), loaded with Gly, were developed to be introduced in the wound bed and swell, once in contact with the exudate, to form a hydrogel in situ able to close the wound. The MP were prepared by spray drying method from the polymeric solution of polysaccharide sodium carboxymethyl cellulose (CMC) and copolymer Soluplus® (SL). Soluplus® introduction in MP composition, using a 3:1 ratio (CMC/SL wt./wt.), allowed to stabilize Gly in non-crystalline form, favoring the improvement of water solubility, and to obtain a spherical with rugged surface MP morphology. Ex vivo studies showed these MP maintain high swelling capability and are able to form in situ a hydrogel for wound repair. The controlled release of Gly from the hydrogel stimulates keratinocyte growth, potentially supporting the physiological healing processes.
18β-甘草次酸（Gly）是一种从甘草中提取的天然化合物，具有抗炎和抗氧化活性，因此可用于伤口治疗。由于其溶解度差，Gly 不适合用于传统局部产品（如凝胶、泡沫和乳膏）的配方。载有 Gly 的聚合物生物粘附性微球（MP）被开发出来，用于引入伤口床，一旦与渗出物接触，就会在原位形成水凝胶，从而封闭伤口。MP 是通过喷雾干燥法从多糖羧甲基纤维素钠（CMC）和共聚物 Soluplus®（SL）的聚合物溶液中制备的。在 MP 组成中引入 Soluplus®（CMC/SL 的重量比为 3:1），可以将 Gly 稳定在非晶态，有利于提高水溶性，并获得具有粗糙表面的球形 MP 形态。离体研究表明，这些 MP 保持高的溶胀能力，并能够原位形成水凝胶用于伤口修复。Gly 从水凝胶中的控制释放刺激角质细胞生长，可能支持生理愈合过程。
