白血病，特别是急性髓性白血病（AML）被认为是一种严重的健康状况，在成人中患病率很高。因此，迫切需要寻找新的 AML 治疗方式。本研究旨在开发一种生物相容性纳米制剂，用于有效口服植物药；黄芩苷 (BAC) 用于 AML 治疗。基于生物活性天然成分的脂质纳米胶囊（LNC）；使用简单的相转化方法制备了作为生物表面活性剂的鼠李糖脂（RL）和精油芳樟醇（LIN）。精心设计的 BAC-LNC 直径为 61.1 nm，PDI 为 0.2。包封率超过98%，药物释放缓慢，储存稳定性高，可保存3个月以上。此外，与 BAC 悬浮液相比，BAC-LNC 在大鼠体内的口服生物利用度提高了 2.3 倍，且半衰期和平均停留时间更长。体外抗癌研究证实了 BAC-LNC 对人白血病单核细胞 (THP-1) 具有显着的细胞毒性。 BAC-LNC 具有更高的细胞摄取、细胞凋亡能力和抗增殖活性，并可抑制 DNA 合成阶段。最后，通过评估各种肿瘤生物标志物进行的机制研究表明，BAC-LNC 下调血管生成标志物、血管内皮生长因子 (VEGF) 和抗凋亡标志物 (BCl-2)，并上调细胞凋亡标志物 (Caspase-3)。和BAX）。 BAC 生物活性 LNC 的疗效提高，充分证明了其作为 AML 治疗有前景的纳米平台的药物治疗潜力。版权所有 © 2024 Elsevier B.V. 保留所有权利。

Leukemia, particularly acute myeloid leukemia (AML) is considered a serious health condition with high prevalence among adults. Accordingly, finding new therapeutic modalities for AML is urgently needed. This study aimed to develop a biocompatible nanoformulation for effective oral delivery of the phytomedicine; baicalin (BAC) for AML treatment. Lipid nanocapsules (LNCs) based on bioactive natural components; rhamnolipids (RL) as a biosurfactant and the essential oil linalool (LIN), were prepared using a simple phase-inversion method. The elaborated BAC-LNCs displayed 61.1 nm diameter and 0.2 PDI. Entrapment efficiency exceeded 98 % with slow drug release and high storage-stability over 3-months. Moreover, BAC-LNCs enhanced BAC oral bioavailability by 2.3-fold compared to BAC suspension in rats with higher half-life and mean residence-time. In vitro anticancer studies confirmed the prominent cytotoxicity of BAC-LNCs on the human leukemia monocytes (THP-1). BAC-LNCs exerted higher cellular uptake, apoptotic capability and antiproliferative activity with DNA synthesis-phase arrest. Finally, a mechanistic study performed through evaluation of various tumor biomarkers revealed that BAC-LNCs downregulated the angiogenic marker, vascular endothelial growth-factor (VEGF) and the anti-apoptotic marker (BCl-2) and upregulated the apoptotic markers (Caspase-3 and BAX). The improved efficacy of BAC bioactive-LNCs substantially recommends their pharmacotherapeutic potential as a promising nanoplatform for AML treatment.Copyright © 2024 Elsevier B.V. All rights reserved.