Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra- 835215 Ranchi, Jharkhand, India.
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Curr Drug Deliv. 2020;17(10):845-860. doi: 10.2174/1567201817666200415112657.
Quercetin (QT, 3,3',4',5,7-pentahydroxyflavone), is a natural flavonoid with nutritional value and acts as a potential free-radical scavenger (antioxidant). QT has also been explored for its anti-cancer as well as anti-proliferative activities against numerous cancerous cells. Moreover, QT exhibits significant pro-apoptotic activity against tumor cells and is well established to control the growth of different carcinoma cells at various phases of the cell cycle. Hence, it can reduce the burden of human solid cancer and metastasis. Both these activities have been established in a diverse class of human cell lines in-vitro as well as in animal models (in-vivo). Apart from the promising therapeutic activities of QT molecule, their applications have been limited due to some major concerns, including low oral bioavailability and poor aqueous solubility. Also, rapid gastrointestinal digestion of QT seems to be a key barrier for its clinical translations for oral drug delivery in conventional dosage form. Henceforth, to overcome these drawbacks, QT is loaded with liposomal systems, which exhibit promising outcomes in the upregulation of QT by the epithelial system and also improved its targeting at the site of action. Furthermore, Liposomes based Drug Delivery Systems (LDDS) have showed significant therapeutic activity with conjugated drug moiety and exhibit safety, biocompatibility, biodegradability, and mitigated toxicity despite having certain limitations associated with physiological and biological barriers. Herein, in this review, we have focused on the mechanism related with the chemotherapeutic activity of QT and also discussed the promising activity of QT-loaded LDDS as a potent chemotherapeutic agent for cancer therapy.
槲皮素(QT,3,3',4',5,7-五羟基黄酮)是一种具有营养价值的天然类黄酮,可作为潜在的自由基清除剂(抗氧化剂)。QT 还因其抗癌和抗增殖活性而被广泛探索,对许多癌细胞均有抑制作用。此外,QT 对肿瘤细胞具有显著的促凋亡活性,已被证实可控制不同癌细胞在细胞周期的各个阶段的生长。因此,它可以减轻人类实体瘤和转移的负担。这些活性已在体外多种人类细胞系和动物模型(体内)中得到证实。除了 QT 分子具有有前途的治疗活性外,由于一些主要问题,包括口服生物利用度低和水溶性差,其应用受到限制。此外,QT 在胃肠道中的快速消化似乎是其临床转化为常规剂型口服药物的关键障碍。因此,为了克服这些缺点,QT 被加载到脂质体系统中,这些系统在通过上皮系统上调 QT 方面表现出有希望的结果,并改善了其在作用部位的靶向性。此外,基于脂质体的药物传递系统(LDDS)与共轭药物部分结合显示出显著的治疗活性,并表现出安全性、生物相容性、生物降解性和减轻的毒性,尽管存在与生理和生物屏障相关的某些限制。在此,在这篇综述中,我们重点介绍了 QT 的化学治疗活性相关的机制,并讨论了负载 QT 的 LDDS 作为癌症治疗的有效化学治疗药物的有前途的活性。