Optimised formulation and characterisation of liposomes for enhanced stability and antiproliferative efficacy of <i>Orthosiphon aristatus</i> var. <i>aristatus</i> extract in lung cancer treatment

This study aimed to characterise and evaluate the antiproliferative potency of a standardised 50% ethanol extract of <i>Orthosiphon aristatus</i> var. <i>aristatus</i> leaves against human lung cancer cells <i>in vitro</i>. A liposomal drug delivery system was developed to enhance bioavailability and efficacy. Three formulations were designed with different extract-to-phospholipid ratios, phospholipid, and cholesterol content. NP2, formulated with a 1:1 extract-to-phosphatidylcholine ratio and 20% cholesterol, demonstrated optimal stability and efficacy. Liposomes were quantitatively and qualitatively characterised using light microscopy, TEM, SEM, zeta sizer, and zeta potential analysis. NP2 demonstrated better bioactive compounds release properties and better stability than the extract. The extract and liposomes inhibited the proliferation of human lung adenocarcinoma (A549) and normal endothelial cells (EA.hy926). The findings indicate that the extract possesses potent anti-lung cancer activity, with the NP2 liposomal formulation enhancing its therapeutic potential.

本研究旨在对标准化50%乙醇提取物——肾茶原变种（Orthosiphon aristatus var. aristatus叶片的抗增殖活性进行表征与评价，该提取物针对人肺癌细胞的体外（in vitro）活性。本研究开发了一种脂质体药物递送系统以提升其生物利用度与药效。研究设计了三种不同提取物与磷脂比例、磷脂用量及胆固醇含量的制剂。其中NP2采用1:1的提取物与磷脂酰胆碱比例，并添加20%胆固醇，展现出最优的稳定性与药效。通过光学显微镜、透射电子显微镜（TEM）、扫描电子显微镜（SEM）、粒度电位仪（zeta sizer）及Zeta电位分析，对所制备的脂质体进行定量与定性表征。NP2的生物活性成分释放特性与稳定性均优于原始提取物。该提取物及所制备的脂质体均可抑制人肺腺癌（A549）与正常内皮细胞（EA.hy926）的增殖。研究结果表明，该提取物具有强效的抗肺癌活性，而NP2脂质体制剂可进一步提升其治疗潜力。

搜集汇总

背景与挑战

背景概述

该数据集包含优化脂质体配方以增强Orthosiphon aristatus var. aristatus提取物在肺癌治疗中稳定性和抗增殖效果的研究数据，重点介绍了NP2配方的优异表现。