Kumar Akshay, Kurmi Balak Das, Singh Amrinder, Singh Dilpreet
Department of Quality Assurance, ISF College of Pharmacy, GT Road, Moga 142001, Punjab, India.
Department of Pharmaceutics, ISF College of Pharmacy, GT Road, Moga 142001, Punjab, India.
Explor Target Antitumor Ther. 2022;3(5):643-658. doi: 10.37349/etat.2022.00105. Epub 2022 Oct 31.
The uncontrolled and metastatic nature of cancer makes it worse and more unpredictable. Hence, many therapy and medication are used to control and treat cancer. However, apart from this, many medications cause various side effects. In America, nearly 8% of patients admitted to the hospital are due to side effects. Cancer is more seen in people residing in developed countries related of their lifestyle. There are various phytoconstituents molecules in which resveratrol (RSV) is the best-fitted molecule for cancer due to its significantly less adverse effect on the body. RSV inhibits the initiation and progression of cell proliferation due to the modulation of various pathways like the phosphoinositol 3 kinase (PI3K)/protein kinase B (AKT)/mammalian target of rapamycin (mTOR) pathway. RSV downgraded cell cycle-regulated proteins like cyclin E, cyclin D1, and proliferating cell nuclear antigen (PCNA) and induced the release of cytochrome c from the mitochondria, causing apoptosis or programmed cell death (PCD). A great benefit comes with some challenges, hence, RSV does suffer from poor solubility in water i.e. 0.05 mg/mL. It suffers from poor bioavailability due to being highly metabolized by the liver and intestine. Surprisingly, RSV metabolites also induce the metabolism of RSV. Hence, significantly less amount of RSV presented in the urine in the unchanged form. Due to some challenges like poor bioavailability, less aqueous solubility, and retention time in the body, researchers concluded to make the nanocarriers for better delivery. Adopting the technique of nano-formulations, increased topical penetration by up to 21%, improved nano-encapsulation and consequently improved bioavailability and permeability by many folds. Hence, the present review describes the complete profile of RSV and its nano-formulations for improving anti-cancer activity along with a patent survey.
癌症不受控制的转移性使其病情恶化且更难以预测。因此,人们使用多种疗法和药物来控制和治疗癌症。然而,除此之外,许多药物会引发各种副作用。在美国,近8%的住院患者是由副作用导致的。由于生活方式的原因,癌症在发达国家的人群中更为常见。植物成分分子种类繁多,其中白藜芦醇(RSV)因其对身体的不良影响显著较小,是最适合抗癌的分子。RSV通过调节多种信号通路,如磷酸肌醇3激酶(PI3K)/蛋白激酶B(AKT)/雷帕霉素靶蛋白(mTOR)信号通路,抑制细胞增殖的起始和进展。RSV可下调细胞周期调节蛋白,如细胞周期蛋白E、细胞周期蛋白D1和增殖细胞核抗原(PCNA),并诱导线粒体释放细胞色素c,从而导致细胞凋亡或程序性细胞死亡(PCD)。有好处也伴随着一些挑战,因此,RSV确实存在水溶性差的问题,即0.05 mg/mL。由于其在肝脏和肠道中被高度代谢,其生物利用度较低。令人惊讶的是,RSV的代谢产物也会诱导RSV的代谢。因此,尿液中以未改变形式存在的RSV量显著减少。由于存在生物利用度低、水溶性差和在体内停留时间短等挑战,研究人员决定制备纳米载体以实现更好的递送。采用纳米制剂技术,局部渗透率提高了21%,改善了纳米包封,从而使生物利用度和渗透率提高了许多倍。因此,本综述描述了RSV及其纳米制剂的完整概况,以提高抗癌活性,并进行了专利调查。