BACKGROUND Nordihydroguaiaretic acid (NDGA) is a plant lignan obtained from creosote bush, known to possess anti-oxidant, anti-cancer and anti-viral activities and is being used in traditional medicine. However, toxicity studies indicated liver and kidney damage despite its immense medicinal properties. There has been a recent increase of curiosity in the chemical synthesis of NDGA derivatives for therapeutic applications. NDGA derivatives have been developed as better alternatives to NDGA and for targeted delivery to the site of tissue by chemical derivatives. In this regard, an analog of NDGA, Acetyl NDGA (Ac-NDGA), has been synthesized based on a previous procedure and formulated as a nanostructured complex with Polycaprolactone/Polyethylene glycol polymer matrices, by o/w solvent evaporation method. RESULTS The drug-incorporated polymeric nanospheres exhibited a drug load of 10.0 ± 0.5 µg drug per mg of nanospheres in acetonitrile solvent with 49.95 ± 10% encapsulation efficiency and 33-41% drug loading capacity with different batches of nanospheres preparation. The in vitro drug release characteristics indicated 82 ± 0.25% drug release at 6 h in methanol. Further, the nanospheres have been characterized extensively to evaluate their suitability for therapeutic delivery. CONCLUSIONS The present studies indicate a new and efficient formulation of the nanostructured AcNDGA with good therapeutic potential.

中文翻译：

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纳米结构去甲二氢愈创木酸类似物的简便合成和纳米级特征，可用于治疗应用。

背景技术北二氢愈创木酸（NDGA）是从杂酚丛中获得的植物木脂素，已知具有抗氧化，抗癌和抗病毒活性，并且被用于传统医学中。然而，毒性研究表明，尽管其巨大的药用特性，但仍会损害肝脏和肾脏。最近，用于治疗用途的NDGA衍生物的化学合成中的好奇心有所增加。NDGA衍生物已被开发为NDGA的更好替代品，并通过化学衍生物定向递送至组织部位。在这方面，已经基于先前的步骤合成了NDGA的类似物乙酰基NDGA（Ac-NDGA），并通过o / w溶剂蒸发法将其配制成与聚己内酯/聚乙二醇聚合物基质的纳米结构复合物。结果掺入药物的聚合物纳米球在乙腈溶剂中的载药量为每毫克纳米球10.0±0.5 µg药物，包封效率为49.95±10％，不同批次的纳米球制剂载药量为33-41％。体外药物释放特征表明在甲醇中6 h时药物释放为82±0.25％。此外，已对纳米球进行了广泛表征，以评估其在治疗性治疗中的适用性。结论本研究表明具有良好治疗潜力的纳米结构AcNDGA的新型有效配方。体外药物释放特征表明在甲醇中6 h时药物释放为82±0.25％。此外，已对纳米球进行了广泛表征，以评估其在治疗性治疗中的适用性。结论本研究表明具有良好治疗潜力的纳米结构AcNDGA的新型有效配方。体外药物释放特征表明在甲醇中6 h时药物释放为82±0.25％。此外，已对纳米球进行了广泛表征，以评估其在治疗性治疗中的适用性。结论本研究表明具有良好治疗潜力的新型纳米结构AcNDGA的有效配方。