Bhargav E, Mohammed Nawaz, Singh Udit Narayan, Ramalingam P, Challa Ranadheer Reddy, Vallamkonda Bhaskar, Ahmad Sheikh F, Dsnbk Prasanth, Pasala Praveen Kumar, Rudrapal Mithun
Raghavendra Institute of Pharmaceutical Education and Research, Anantapur, Andhra Pradesh, India.
Department of Pharmaceutical Analysis, National Institute of Pharmaceutical Education and Research (NIPER), Hajipur, Bihar, India.
Heliyon. 2024 Sep 4;10(17):e37430. doi: 10.1016/j.heliyon.2024.e37430. eCollection 2024 Sep 15.
This study aimed to enhance the efficacy of quercetin (QT) by formulating it into a liposomal drug delivery system utilizing the concept of central composite design. The drug:lipid ratio, cholesterol concentration, and sonication time were selected as independent variables in the study. The vesicle and percentage entrapment efficiency were selected as the dependent variables. Quercetin nanoliposomes (QT-NLs) were prepared via a combination of ethanol injection and thin film hydration. The vesicle size and entrapment efficiency of all formulations were within the ranges of 100 nm and >80 %, respectively. The zeta potential value indicated the stability of the optimized formulation. The contour plots were used to select the desired batch range. SEM studies revealed an imperfect crystalline morphology without any unwanted agglomeration. MTT assays on VERO cell lines indicated the safety of the developed formulation. MTT assays of MCF-7 cells revealed IC values of 5.8 μM and 7.9 μM for QT-NLs and QT, respectively. In our study, the optimized formulation exhibited late and early apoptosis and necrosis when used to treat MCF-7 cells. S and G2/M cell cycle phases of MCF-7 cell arrest were confirmed by the cell cycle report. At sub-G0/G1 phase, 2.10 ± 1.1 %; G0/G1 phase, 34.13 ± 1.9 %; S phase, 34.55 ± 0.98 %; and G2/M phase, 26.24 ± 1.7 % of cell arrest were observed. The results demonstrated the effectiveness of the proposed design for the development of corn starch-coated QT-NLs and their activity in breast cancer cell lines.
本研究旨在利用中心复合设计理念,将槲皮素(QT)制成脂质体药物递送系统,以提高其疗效。研究中选取药物与脂质比例、胆固醇浓度和超声处理时间作为自变量,将囊泡和包封率作为因变量。通过乙醇注入法和薄膜水化法相结合制备槲皮素纳米脂质体(QT-NLs)。所有制剂的囊泡大小和包封率分别在100 nm范围内和>80%。ζ电位值表明了优化制剂的稳定性。等高线图用于选择所需的批次范围。扫描电子显微镜研究显示晶体形态不完美,但无任何不必要的团聚。对VERO细胞系进行的MTT试验表明所开发制剂的安全性。对MCF-7细胞进行的MTT试验显示,QT-NLs和QT的IC值分别为5.8 μM和7.9 μM。在我们的研究中,优化制剂用于治疗MCF-7细胞时表现出晚期和早期凋亡及坏死。细胞周期报告证实了MCF-7细胞停滞在S期和G2/M期。在亚G0/G1期,观察到2.10±1.1%的细胞停滞;在G0/G1期,为34.13±1.9%;在S期,为34.55±0.98%;在G2/M期,为26.24±1.7%。结果证明了所提出的设计用于开发玉米淀粉包衣的QT-NLs及其在乳腺癌细胞系中的活性的有效性。