Department of Food Science, Rutgers, The State University of New Jersey , 65 Dudley Road, New Brunswick, New Jersey 08901, United States.
J Agric Food Chem. 2015 Jan 21;63(2):652-9. doi: 10.1021/jf504465a. Epub 2015 Jan 8.
Polymethoxyflavones (PMFs) are groups of compounds isolated from citrus peels that have been documented with wide arrays of health-promoting bioactivities. Because of their hydrophobic structure and high melting point, crystallized PMFs usually have poor systemic bioavailability when consumed orally. To improve the oral efficiency of PMFs, a viscoelastic emulsion system was formulated. Because of the crystalline nature, the inclusion of PMFs into the emulsion system faces great challenges in having sufficient loading capacity and stabilities. In this study, the process of optimizing the quality of emulsion-based formulation intended for PMF oral delivery was systematically studied. With alteration of the PMF loading concentration, processing temperature, and pressure, the emulsion with the desired droplet and crystal size can be effectively fabricated. Moreover, storage temperatures significantly influenced the stability of the crystal-containing emulsion system. The results from this study are a good illustration of system optimization and serve as a great reference for future formulation design of other hydrophobic crystalline compounds.
多甲氧基黄酮(PMFs)是从柑橘皮中分离得到的一组化合物,具有广泛的促进健康的生物活性。由于其疏水性结构和高熔点,结晶态的 PMFs 口服时通常系统生物利用度较差。为了提高 PMFs 的口服效率,我们设计了一种黏弹性乳液体系。由于结晶态的存在,PMFs 被包含在乳液体系中面临着巨大的挑战,包括足够的载药量和稳定性。在本研究中,我们系统地研究了优化基于乳液的 PMF 口服传递制剂质量的过程。通过改变 PMF 的载药量浓度、加工温度和压力,可以有效地制备出所需粒径的乳液。此外,储存温度对含晶体乳液体系的稳定性有显著影响。本研究的结果很好地说明了系统优化,并为其他疏水性结晶化合物的未来制剂设计提供了很好的参考。