Department of Pharmaceutical Technology, Faculty of Pharmacy of the University of Coimbra, University of Coimbra, Coimbra, Portugal; REQUIMTE/LAQV, Group of Pharmaceutical Technology, Faculty of Pharmacy of the University of Coimbra, University of Coimbra, Coimbra, Portugal.
Department of Pharmaceutical Technology, Faculty of Pharmacy of the University of Coimbra, University of Coimbra, Coimbra, Portugal; REQUIMTE/LAQV, Group of Pharmaceutical Technology, Faculty of Pharmacy of the University of Coimbra, University of Coimbra, Coimbra, Portugal.
Colloids Surf B Biointerfaces. 2022 Oct;218:112758. doi: 10.1016/j.colsurfb.2022.112758. Epub 2022 Aug 5.
The use of essential oils has gained importance due to their wide range of biological properties. Essential oils comprise a complex mixture of volatile organic compounds (VOCs), so the study of VOCs as active pharmaceutical ingredients is often more precise and fruitful. VOCs are natural origin molecules that constitute a sustainable alternative to synthetic drugs due to their important therapeutic value. However, VOCs possess poor solubility in aqueous solutions, high volatility, and, consequently, low stability and bioavailability, limiting VOC handling in industry and their potential use in therapeutics, despite their promising biological properties. Thereby, cyclodextrins (CDs) have emerged as suitable carriers of VOCs, giving rise to so-called VOC/CD inclusion complexes. CDs constitute an inexpensive viable solution for encapsulating VOCs to improve their properties, namely their apparent solubility and stability toward pH, light, and temperature. This review provides a conceptual framework of several VOC/CD inclusion complexes developed. In addition, the most exploited preparation techniques and their influence on the values of encapsulation efficiency and formation constant (K) are highlighted. The most recent in vitro or in vivo biological experiments regarding VOC/CD inclusion complexes in the development of pharmaceutical products are also presented. Finally, the toxicological, and regulatory aspects are discussed.
由于其广泛的生物学特性,精油的使用变得越来越重要。精油是一种复杂的挥发性有机化合物(VOC)混合物,因此,将 VOC 作为活性药物成分进行研究通常更为精确和有成效。VOC 是天然来源的分子,由于其重要的治疗价值,构成了合成药物的可持续替代品。然而,VOC 在水中的溶解度差、挥发性高,因此稳定性和生物利用度低,限制了其在工业中的处理和在治疗中的潜在用途,尽管它们具有有前景的生物学特性。因此,环糊精(CD)已成为 VOC 的合适载体,从而产生了所谓的 VOC/CD 包合物。CD 是一种廉价可行的解决方案,可用于封装 VOC,以改善其性质,即提高其表观溶解度和对 pH 值、光和温度的稳定性。本文综述了几种已开发的 VOC/CD 包合物。此外,还强调了最常用的制备技术及其对包封效率和形成常数(K)值的影响。还介绍了关于在药物产品开发中使用 VOC/CD 包合物的最新的体外或体内生物学实验。最后,讨论了毒理学和监管方面的问题。