Del Gaudio Pasquale, Sansone Francesca, Mencherini Teresa, De Cicco Felicetta, Russo Paola, Aquino Rita Patrizia
Department of Pharmacy, University of Salerno, Fisciano, SA, Italy.
Planta Med. 2017 Mar;83(5):426-433. doi: 10.1055/s-0042-110179. Epub 2016 Jun 24.
Pharmacological evidences have correlated a low incidence of osteoporosis, breast cancer, cardiovascular disease, and colon cancer in Asian populations, high consumers of soya, to the properties of soy isoflavones, more specifically to daidzein and genistein. However, in spite of the potent biological activity, their poor water solubility has a strong negative effect on bioavailability. In this study, an innovative technique, nano spray drying, was used to obtain nanoparticles loaded with a soybean dry extract while carboxymethyl cellulose was used as the excipient. The optimization of the process conditions allowed for the manufacturing of stable nanoparticles with a mean size of around 650 nm, a narrow size distribution, and a high encapsulation efficiency (between 78 % and 89 %). The presence of carboxymethyl cellulose was able to stabilize the isoflavone extract and enhance its affinity with aqueous media, strongly increasing its permeation through biological membranes up to 4.5-fold higher than pure soy isoflavone extract raw material and twice its homologous minispray-dried formulation. These results are very useful for the administration of the extract, either topically or orally, suggesting that the isoflanones extract nanoparticulate powder obtained by nano spray drying has great potential to enhance extract bioavailability and could be used as an ingredient to be enclosed in dietary supplements and nutraceutical and cosmeceutical products.
药理学证据表明,在大豆高消费人群的亚洲人口中,骨质疏松症、乳腺癌、心血管疾病和结肠癌的发病率较低,这与大豆异黄酮的特性有关,更具体地说是与大豆苷元和染料木黄酮有关。然而,尽管它们具有强大的生物活性,但其较差的水溶性对生物利用度有很大的负面影响。在本研究中,采用了一种创新技术——纳米喷雾干燥法,以获得负载大豆干提取物的纳米颗粒,同时使用羧甲基纤维素作为赋形剂。工艺条件的优化使得能够制备出稳定的纳米颗粒,其平均尺寸约为650nm,粒径分布窄,包封率高(78%至89%)。羧甲基纤维素的存在能够稳定异黄酮提取物,并增强其与水性介质的亲和力,使其透过生物膜的渗透率大幅提高,比纯大豆异黄酮提取物原料高出4.5倍,是其同源微喷雾干燥制剂的两倍。这些结果对于提取物的局部或口服给药非常有用,表明通过纳米喷雾干燥获得的异黄酮提取物纳米颗粒粉末具有提高提取物生物利用度的巨大潜力,可作为一种成分用于膳食补充剂、营养保健品和化妆品中。