Sartaj Ali, Alam Meraj, Biswas Largee, Yar Mohammad Shahar, Mir Showkat Rasool, Verma Anita Kamra, Baboota Sanjula, Ali Javed
Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.
Nanobiotech Lab, Kirori Mal College, University of Delhi, Delhi, India.
J Drug Target. 2022 Dec;30(10):1113-1134. doi: 10.1080/1061186X.2022.2104292. Epub 2022 Aug 5.
The current research investigated the development and evaluation of dual drug-loaded nanostructure lipidic carriers (NLCs) of green tea extract and Ribociclib.
study were performed to determine the effectiveness of combinational approach. The prepared NLCs were subjected to drug release, lipolysis, haemolysis and cell line studies to assess their prospect.
study was done to get docking score of EGCG (-8.98) close to Ribociclib (-10.78) in CDK-4 receptors. The prepared NLCs exhibited particle size (175.80 ± 3.51 nm); PDI (0.571 ± 0.012); and %EE [RBO (80.91 ± 1.66%) and GTE 75.98 ± 2.35%)] respectively. MCF-7 cell lines were used to evaluate the MTT assay, cellular uptake and antioxidant (ROS and SOD) of prepared NLCs. drug release showed the controlled release up to 72 h. lipolysis and haemolysis studies showed the availability of drugs at absorption sites and the greater prospects of NLCs respectively. Pharmacokinetic study revealed a 3.63-fold and 1.53-fold increment in RBO and GTE bioavailability in female Wistar rats respectively.
The prominent potential of green tea extract and RBO-loaded NLCs in enhancing their therapeutic efficacy for better treatment of breast cancer.
当前研究调查了绿茶提取物和瑞博西尼双重载药纳米结构脂质载体(NLCs)的开发与评价。
进行研究以确定联合方法的有效性。对制备的NLCs进行药物释放、脂解、溶血和细胞系研究以评估其前景。
研究得出表没食子儿茶素没食子酸酯(EGCG)(-8.98)在CDK-4受体中的对接分数接近瑞博西尼(-10.78)。制备的NLCs分别表现出粒径(175.80±3.51nm);多分散指数(PDI)(0.571±0.012);以及包封率[瑞博西尼(RBO)(80.91±1.66%)和绿茶提取物(GTE)75.98±2.35%]。使用MCF-7细胞系评估制备的NLCs的MTT法、细胞摄取和抗氧化剂(活性氧和超氧化物歧化酶)。药物释放显示长达72小时的控释。脂解和溶血研究分别显示药物在吸收部位的可用性和NLCs的更大前景。药代动力学研究表明,在雌性Wistar大鼠中,瑞博西尼和绿茶提取物的生物利用度分别提高了3.63倍和1.53倍。
绿茶提取物和载有瑞博西尼的NLCs在增强其治疗乳腺癌的疗效方面具有显著潜力。