Avocado (Persea americana Mill.; Lauraceae) seed-derived polyhydroxylated fatty alcohols (PFAs) or polyols (i.e., avocadene and avocadyne) are metabolic modulators that selectively induce apoptosis of leukemia stem cells and reverse pathologies associated with diet-induced obesity. Delivery systems containing avocado polyols have not been described. Herein, natural surface active properties of these polyols are characterized and incorporated into self-emulsifying drug delivery systems (SEDDS) that rely on molecular self-assembly to form fine, transparent, oil-in-water (O/W) microemulsions as small as 20 nanometers in diameter. Mechanistically, a 1:1 molar ratio of avocadene and avocadyne (i.e., avocatin B or AVO was shown to be a eutectic mixture which can be employed as a novel, bioactive, co-surfactant that significantly reduces droplet size of medium-chain triglyceride O/W emulsions stabilized with polysorbate 80. In vitro cytotoxicity of avocado polyol-SEDDS in acute myeloid leukemia cell lines indicated significant increases in potency and bioactivity compared to conventional cell culture delivery systems. A pilot pharmacokinetic evaluation of AVO SEDDS in C57BL/6J mice revealed appreciable accumulation in whole blood and biodistribution in key target tissues. Lastly, incorporation of AVO in SEDDS significantly improved encapsulation of the poorly water-soluble drugs naproxen and curcumin.

鳄梨（ Persea americana Mill.；樟科）种子衍生的多羟基脂肪醇 (PFA) 或多元醇（即鳄梨烯和鳄梨苷）是代谢调节剂，可选择性诱导白血病干细胞凋亡并逆转与饮食引起的肥胖相关的病理。尚未描述含有鳄梨多元醇的递送系统。本文对这些多元醇的天然表面活性特性进行了表征，并将其纳入自乳化药物输送系统 (SEDDS) 中，该系统依靠分子自组装形成精细、透明的水包油 (O/W) 微乳液，小至直径20纳米。从机理上讲，摩尔比为 1:1 的鳄梨烯和鳄梨炔（即鳄梨苷 B 或 AVO）被证明是一种低共熔混合物，可用作新型生物活性辅助表面活性剂，可显着减小中链甘油三酯 O 的液滴尺寸。 /W 乳液用聚山梨酯 80 稳定。鳄梨多元醇-SEDDS 在急性髓系白血病细胞系中的体外细胞毒性表明，与传统细胞培养递送系统相比，AVO SEDDS 在 C57BL/6J 小鼠中的药代动力学试验显示显着增加。最后，AVO 在 SEDDS 中的掺入显着改善了水溶性差的药物萘普生和姜黄素的封装。