Department of Pharmacy, University of Salerno, via Giovanni Paolo II, 132, 84084 Fisciano, SA, Italy.
Department of Pharmacy, University of Salerno, via Giovanni Paolo II, 132, 84084 Fisciano, SA, Italy.
Carbohydr Polym. 2017 Jun 1;165:22-29. doi: 10.1016/j.carbpol.2017.02.025. Epub 2017 Feb 8.
In this study, hypromellose acetate succinate (HPMCAS) stable submicronic particles loaded with a soy isoflavones extract have been obtained by nano spray drying technology. HPMCAS has been used as excipient able to increase both stability and supersaturation levels of the active ingredients hence able to enhance skin penetration performance of genistein and daidzein. The influence of polymer/extract ratio as other process variables, on particle size, morphology and permeation performance, have been investigated. Particles in submicronic range (mean size around 550nm) and narrow size distribution with high encapsulation efficiency (up to 86%) were obtained. HPMCAS was able to improve amorphization of genistein during the atomization process and avoid recrystallization during storage, even in harsh environmental condition. Moreover, the enhanced affinity of the optimized formulations with aqueous media, strongly increased isoflavones penetration through membrane with diffusive properties well-correlated to human skin, up to 10-fold higher than pure soy isoflavones extract raw material.
本研究采用纳米喷雾干燥技术,制备了醋酸琥珀酸羟丙甲纤维素酯(HPMCAS)稳定的载有大豆异黄酮提取物的亚微米级颗粒。HPMCAS 可用作赋形剂,可提高活性成分的稳定性和过饱和度水平,从而增强染料木素和大豆苷元的皮肤渗透性能。研究了聚合物/提取物比例等其他工艺变量对粒径、形态和渗透性能的影响。获得了亚微米级范围(平均粒径约为 550nm)的窄粒径分布和高包封效率(高达 86%)的颗粒。HPMCAS 能够在雾化过程中提高染料木素的非晶化程度,并在储存过程中避免重结晶,即使在恶劣的环境条件下也是如此。此外,优化配方与水相的亲和力增强,大大增加了异黄酮通过具有与人皮肤相关的扩散特性的膜的渗透,比纯大豆异黄酮提取物原料高 10 倍。