Soto Ernesto R, Rus Florentina, Ostroff Gary R
Program in Molecular Medicine, University of Massachusetts Medical School, Worcester, MA 01605, USA.
J Funct Biomater. 2024 Jul 23;15(8):203. doi: 10.3390/jfb15080203.
Addressing the growing problem of antifungal resistance in medicine and agriculture requires the development of new drugs and strategies to preserve the efficacy of existing fungicides. One approach is to utilize delivery technologies. Yeast particles (YPs) are 3-5 µm porous, hollow microspheres, a byproduct of food-grade yeast extract manufacturing processes and an efficient and flexible drug delivery platform. Here, we report the use of YPs for encapsulation of tetraconazole (TET) and prothioconazole (PRO) with high payload capacity and stability. The YP PRO samples were active against both sensitive and azole-resistant strains of . The higher efficacy of YP PRO versus free PRO is due to interactions between PRO and saponifiable lipids in the YPs. Encapsulation of PRO in glucan lipid particles (GLPs), a highly purified form of YPs that do not contain saponifiable lipids, did not result in enhanced PRO activity. We evaluated the co-encapsulation of PRO with a mixture of the terpenes: geraniol, eugenol, and thymol. Samples co-encapsulating PRO and terpenes in YPs or GLPs were active on both sensitive and azole-resistant . These approaches could lead to the development of more effective drug combinations co-encapsulated in YPs for agricultural or GLPs for pharmaceutical applications.
应对医学和农业领域日益严重的抗真菌耐药性问题,需要开发新药物和策略以保持现有杀菌剂的功效。一种方法是利用递送技术。酵母颗粒(YPs)是3 - 5微米的多孔中空微球,是食品级酵母提取物制造过程的副产物,也是一种高效且灵活的药物递送平台。在此,我们报告了利用YPs对戊唑醇(TET)和丙硫菌唑(PRO)进行包封,具有高载药量和稳定性。YP PRO样品对敏感和耐唑菌株均有活性。YP PRO比游离PRO具有更高的功效,这是由于PRO与YPs中可皂化脂质之间的相互作用。将PRO包封在葡聚糖脂质颗粒(GLPs)中,GLPs是不含可皂化脂质的高度纯化形式的YPs,并未导致PRO活性增强。我们评估了PRO与萜类混合物香叶醇、丁香酚和百里酚的共包封。在YPs或GLPs中共包封PRO和萜类的样品对敏感和耐唑菌株均有活性。这些方法可能会促成开发出更有效的药物组合,在农业中以YPs共包封,在制药应用中以GLPs共包封。