Program in Molecular Medicine, University of Massachusetts Medical School, Worcester, MA 01605, USA.
Molecules. 2022 Jun 2;27(11):3580. doi: 10.3390/molecules27113580.
Yeast particles (YPs) are 3−5 µm hollow and porous microspheres, a byproduct of some food grade yeast (Saccharomyces cerevisiae) extract manufacturing processes. Terpenes can be efficiently encapsulated inside YPs by passive diffusion through the porous cell walls. As previously published, this YP terpene encapsulation approach has been successfully implemented (1) to develop and commercialize fungicide and nematicide products for agricultural applications, (2) to co-load high potency agrochemical actives dissolved in terpenes or suitable solvents, and (3) to identify YP terpenes with broad-acting anthelmintic activity for potential pharmaceutical applications. These first-generation YP terpene materials were developed with a <2:1 terpene: YP weight ratio. Here we report methods to increase the terpene loading capacity in YPs up to 5:1 terpene: YP weight ratio. Hyper-loaded YP terpenes extend the kinetics of payload release up to three-fold compared to the commercialized YP terpene formulations. Hyper-loaded YP-terpene compositions were further optimized to achieve high terpene storage encapsulation stability from −20 °C to 54 °C. The development of hyper-loaded YP terpenes has a wide range of potential agricultural and pharmaceutical applications with terpenes and other compatible active substances that could benefit from a delivery system with a high payload loading capacity combined with increased payload stability and sustained release properties.
酵母颗粒(Yeast Particles,YPs)是 3-5μm 的中空多孔微球,是某些食品级酵母(酿酒酵母)提取物制造工艺的副产品。萜类化合物可以通过多孔细胞壁的被动扩散有效地封装在 YPs 中。如前所述,这种 YP 萜类化合物包封方法已成功实施(1)开发和商业化用于农业应用的杀真菌剂和杀线虫剂产品,(2)共负载溶解在萜类化合物或合适溶剂中的高功效农用化学品活性剂,以及(3)鉴定具有广泛驱虫活性的 YP 萜类化合物,用于潜在的药物应用。第一代 YP 萜类材料的开发采用了 <2:1 的萜类化合物:YPs 重量比。在这里,我们报告了将萜类化合物在 YPs 中的负载能力提高到 5:1 萜类化合物:YPs 重量比的方法。与商业化的 YP 萜类化合物制剂相比,超负载 YP 萜类化合物将有效载荷释放的动力学延长了三倍。进一步优化了超负载 YP-萜类化合物组合物,以实现从-20°C 到 54°C 的高萜类化合物储存封装稳定性。超负载 YP 萜类化合物的开发具有广泛的农业和制药应用潜力,可将萜类化合物和其他相容的活性物质应用于具有高有效载荷负载能力、增加有效载荷稳定性和持续释放特性的输送系统。