Kravanja Katja Andrina, Finšgar Matjaž, Knez Željko, Knez Marevci Maša
Faculty of Chemistry and Chemical Engineering, University of Maribor, Smetanova 17, 2000 Maribor, Slovenia.
Pharmaceutics. 2022 Aug 11;14(8):1670. doi: 10.3390/pharmaceutics14081670.
Various active compounds isolated from natural sources exhibit remarkable benefits, making them attractive for pharmaceutical and biomedical applications, such as antioxidant, antimicrobial, and anti-inflammatory activities, which contribute to the treatment of cardiovascular diseases, neurodegenerative disorders, various types of cancer, diabetes, and obesity. However, their major drawbacks are their reactivity, instability, relatively poor water solubility, and consequently low bioavailability. Synthetic drugs often face similar challenges associated with inadequate solubility or burst release in gastrointestinal media, despite being otherwise a safe and effective option for the treatment of numerous diseases. Therefore, drug-eluting pharmaceutical formulations have been of great importance over the years in efforts to improve the bioavailability of active compounds by increasing their solubility and achieving their controlled release in body media. This review highlights the success of the fabrication of micro- and nanoformulations using environmentally friendly supercritical fluid technologies for the processing and incorporation of active compounds. Several novel approaches, namely micronization to produce micro- and nano-sized particles, supercritical drying to produce aerogels, supercritical foaming, and supercritical solvent impregnation, are described in detail, along with the currently available drug delivery data for these formulations.
从天然来源分离出的各种活性化合物具有显著的益处,使其在制药和生物医学应用中具有吸引力,例如抗氧化、抗菌和抗炎活性,这些有助于治疗心血管疾病、神经退行性疾病、各种类型的癌症、糖尿病和肥胖症。然而,它们的主要缺点是其反应性、不稳定性、相对较差的水溶性以及因此导致的低生物利用度。合成药物尽管在治疗多种疾病方面是一种安全有效的选择,但通常也面临与胃肠道介质中溶解度不足或突释相关的类似挑战。因此,多年来药物洗脱制剂在通过提高活性化合物的溶解度并在体内介质中实现其控释来提高其生物利用度的努力中一直非常重要。本综述强调了使用环境友好的超临界流体技术制备用于加工和掺入活性化合物的微制剂和纳米制剂的成功。详细描述了几种新颖的方法,即微粉化以生产微米和纳米尺寸的颗粒、超临界干燥以生产气凝胶、超临界发泡和超临界溶剂浸渍,以及这些制剂目前可用的药物递送数据。