Biocolloid & Fluid Physics Group, Department of Applied Physics, Faculty of Sciences, University of Granada, 18071, Spain.
Nanomedicine (Lond). 2014 Dec;9(18):2761-72. doi: 10.2217/nnm.14.35.
N-oleoylethanolamine (OEA) is a lipid mediator that acts as a satiety factor. The main limiting factor for its administration is its poor water solubility. We designed and characterized new nanoemulsions as delivery system for hydrophobic compounds such as OEA.
MATERIALS & METHODS: The nanoemulsion components and preparation methods were selected in order to achieve the desired final properties. Then, we evaluated the in vivo properties of the nanoemulsions as drug-delivery systems testing the anorectic effects of OEA in rats after both intragastric and intraperitoneal administration. The in vivo toxicity of the nanoemulsions was evaluated after a 3-week treatment.
Nanoemulsions proved to be stable, nontoxic and had no effect on feeding behavior when administered without OEA. The effects of OEA were observable after its oral and parenteral administration with the nanoemulsions to 24-h fasted rats, finding a better efficacy compared with a vehicle containing Tween(®) 20 (Sigma-Aldrich, MO, USA) after oral administration.
These results support the efficacy of these nanoemulsions to deliver highly hydrophobic bioactive drugs.
N-油酰乙醇胺（OEA）是一种作为饱腹感因子的脂类介质。其给药的主要限制因素是其较差的水溶性。我们设计并表征了新的纳米乳剂作为疏水性化合物如 OEA 的递送系统。
选择纳米乳剂的成分和制备方法，以达到所需的最终性质。然后，我们评估了纳米乳剂作为药物递送系统的体内性质，测试了 OEA 在经口和腹腔内给药后对禁食大鼠的厌食作用。在 3 周的治疗后，评估了纳米乳剂的体内毒性。
纳米乳剂被证明是稳定的、无毒的，并且在没有 OEA 时给药不会影响摄食行为。当用纳米乳剂给 24 小时禁食的大鼠经口和腹腔内给药时，OEA 的作用是可观察到的，与含有吐温 20（Sigma-Aldrich，MO，美国）的载体相比，口服给药具有更好的疗效。
这些结果支持这些纳米乳剂能够输送高度疏水性生物活性药物的功效。
