Honokiol-loaded nanoparticles (HK-loaded NPs) exhibit potential antitumor activity; however, the factors affecting their antitumor efficacy are still unclear and need to be explored. This research was aimed to systematically estimate the influence of feed weight ratio (FWR) and nanocarrier structure on antitumor activity. Accordingly, three types of ethylene glycol derivatives, including linear poly(ethylene glycol) with molar mass of 2000 (PEG₄₅), first and second generation oligo(ethylene glycol) dendrons (G1 and G2) were used as nanocarriers, and a series of HK-loaded NPs with different FWR were prepared successfully using the evaporation-ultrasonication method. These NPs showed similar stability but demonstrated differences with respect to particle size, morphology, cumulative profile, and antitumor efficacy. The influence of the FWR was studied using G1 dendrons as nanocarriers; the results indicated that the particle size and morphology of G1 NPs were significantly affected, and G1 NPs (8/1), with the FWR of 8/1 for HK versus G1 dendron, exhibited the highest antitumor activity among all G1 NPs. Furthermore, the influence of nanocarrier structure was investigated at the FWR of 4/1; the findings revealed reduction in the particle diameter from 280 nm to 109 nm and change in morphology from sphere to flower-like structure with an increase in the branch degree from linear to dendron. Moreover, G2 NPs (4/1), with the FWR of 4/1 for HK versus G2 dendron, carrying the highest branch degree exhibited the greatest antitumor efficacy among all. These results are suggestive of influence of particle size and morphology on antitumor efficacy of HK-loaded NPs. Conclusively, this study demonstrated nanocarrier structure and the FWR significantly affect the antitumor efficacy of NPs, which should be optimized for designing nanoscale delivery systems.

中文翻译：

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用乙二醇衍生物修饰的基于和厚朴酚的纳米药物可促进抗肿瘤功效。

负载和厚朴酚的纳米颗粒（负载 HK 的 NPs）表现出潜在的抗肿瘤活性；然而，影响其抗肿瘤疗效的因素尚不清楚，需要进一步探索。本研究旨在系统地评估饲料重量比 (FWR) 和纳米载体结构对抗肿瘤活性的影响。因此，三种类型的乙二醇衍生物，包括摩尔质量为 2000 的线性聚（乙二醇）（PEG ₄₅)、第一代和第二代低聚(乙二醇)树枝状结构(G1和G2)作为纳米载体，采用蒸发-超声法成功制备了一系列不同FWR的HK负载纳米颗粒。这些 NPs 表现出相似的稳定性，但在粒径、形态、累积特征和抗肿瘤功效方面表现出差异。使用G1树突作为纳米载体研究了FWR的影响；结果表明，G1 NPs 的粒径和形态受到显着影响，G1 NPs (8/1)，HK 与 G1 树突的 FWR 为 8/1，在所有 G1 NPs 中表现出最高的抗肿瘤活性。此外，在4/1的FWR下研究了纳米载体结构的影响；研究结果表明，粒径从 280 nm 减小到 109 nm，形态从球形变为花状结构，分支度从线性增加到树枝状。此外，具有最高分支度的 G2 NPs (4/1)，HK 与 G2 树突的 FWR 为 4/1，具有最高的抗肿瘤功效。这些结果表明粒径和形态对载有 HK 的 NPs 的抗肿瘤功效的影响。总之，这项研究表明纳米载体结构和 FWR 显着影响 NPs 的抗肿瘤功效，应优化设计纳米级递送系统。具有最高分支度的表现出最大的抗肿瘤功效。这些结果表明粒径和形态对载有 HK 的 NPs 的抗肿瘤功效的影响。总之，这项研究表明纳米载体结构和 FWR 显着影响 NPs 的抗肿瘤功效，应优化设计纳米级递送系统。具有最高分支度的表现出最大的抗肿瘤功效。这些结果表明粒径和形态对载有 HK 的 NPs 的抗肿瘤功效的影响。总之，这项研究表明纳米载体结构和 FWR 显着影响 NPs 的抗肿瘤功效，应优化设计纳米级递送系统。