Department of Food Science, Rutgers, the State University of New Jersey, 65 Dudley Road, New Brunswick, New Jersey 08901, USA.
J Agric Food Chem. 2012 May 30;60(21):5373-9. doi: 10.1021/jf300609p. Epub 2012 May 16.
Curcumin is a natural bioactive compound with many health-promoting benefits. Its low oral bioavailability limits its application in functional foods. In the present study, novel organogel-based nanoemulsions have been developed for oral delivery of curcumin and improvement of its bioavailability. Recently developed curcumin organogel was used as the oil phase in the curcumin nanoemulsion formulation. Tween 20 was selected as the emulsifier on the basis of maximum in vitro bioaccessibility of curcumin in the nanoemulsion. In vitro lipolysis profile revealed that the digestion of nanoemulsion was significantly faster and more complete than the organogel. Permeation experiments on Caco-2 cell monolayers suggested that digestion-diffusion was the major absorption mechanism for curcumin in the nanoemulsion. Furthermore, in vivo pharmacokinetics analysis on mice confirmed that the oral bioavailability of curcumin in the nanoemulsion was increased by 9-fold compared with unformulated curcumin. This novel formulation approach may also be used for oral delivery of other poorly soluble nutraceuticals with high loading capacity, which has significant impact in functional foods, dietary supplements and pharmaceutical industries.
姜黄素是一种天然生物活性化合物，具有许多促进健康的益处。但其口服生物利用度低，限制了其在功能性食品中的应用。本研究开发了基于新型姜黄素有机凝胶的纳米乳液，用于姜黄素的口服递送和提高其生物利用度。最近开发的姜黄素有机凝胶被用作纳米乳液配方中的油相。根据纳米乳液中姜黄素体外生物利用度最高的原则，选择吐温 20 作为乳化剂。体外脂肪消化曲线显示，纳米乳液的消化速度明显快于有机凝胶，且更完全。Caco-2 细胞单层的渗透实验表明，纳米乳液中姜黄素的主要吸收机制是消化-扩散。此外，在小鼠体内药代动力学分析证实，与未形成纳米乳液的姜黄素相比，纳米乳液中姜黄素的口服生物利用度提高了 9 倍。这种新型制剂方法也可用于其他疏水性营养保健品的口服递送，具有高载药量，对功能性食品、膳食补充剂和制药行业有重大影响。
