PDF(Pubmed)
Abstract：
Pentacyclic triterpenoids (TTs) represent a unique family of phytochemicals with interesting properties and pharmacological effects, with some representatives, such as betulinic acid (BA) and betulin (B), being mainly investigated as potential anticancer molecules. Considering the recent scientific and preclinical investigations, a review of their anticancer mechanisms, structure-related activity, and efficiency improved by their insertion in nanolipid vehicles for targeted delivery is presented. A systematic literature study about their effects on tumor cells in vitro and in vivo, as free molecules or encapsulated in liposomes or nanolipids, is discussed. A special approach is given to liposome-TTs and nanolipid-TTs complexes to be linked to microbubbles, known as contrast agents in ultrasonography. The production of such supramolecular conjugates to deliver the drugs to target cells via sonoporation represents a new scientific and applicative direction to improve TT efficiency, considering that they have limited availability as lipophilic molecules. Relevant and recent examples of in vitro and in vivo studies, as well as the challenges for the next steps towards the application of these complex delivery systems to tumor cells, are discussed, as are the challenges for the next steps towards the application of targeted delivery to tumor cells, opening new directions for innovative nanotechnological solutions.
摘要：
五环三萜类（TT）代表了一个独特的植物化学物质家族，具有有趣的特性和药理作用。一些代表,如桦木酸（BA）和桦木醇（B），主要作为潜在的抗癌分子进行研究。考虑到最近的科学和临床前调查，回顾了它们的抗癌机制，与结构相关的活动，提出了通过将它们插入纳米脂质载体中用于靶向递送而提高效率。关于它们在体外和体内对肿瘤细胞的影响的系统文献研究，作为游离分子或包封在脂质体或纳米脂质中，正在讨论。一种特殊的方法是将脂质体-TTs和纳米脂质-TTs复合物连接到微泡上，在超声检查中被称为造影剂。这种超分子偶联物的生产通过超声穿孔将药物递送到靶细胞代表了提高TT效率的新的科学和应用方向。考虑到它们作为亲脂性分子的可用性有限。体外和体内研究的相关和最近的例子，以及将这些复杂的递送系统应用于肿瘤细胞的下一步的挑战，讨论，以及将靶向递送应用于肿瘤细胞的下一步的挑战，为创新的纳米技术解决方案开辟新的方向。
