PDF(Pubmed)
Abstract：
Frequent and variant infections are caused by the virtue of opportunistic fungi pathogens. Candidiasis, aspergillosis, and mucormycosis are pathogenic microorganisms that give rise to vast fungal diseases that alternate between moderate to fatal in severity. The use of fluconazole as an antifungal drug was limited due to the acquired resistance in some types of Candida and other fungal species. This study aims to consolidate fluconazole\'s biological effectiveness against several pathogenic fungi. Six active monoterpenes (MTs) of carvacrol, linalool, geraniol, α-terpinene, citronellal, and nerolidol were selected and encapsulated in nanostructure lipid carrier (NLC) with (NLC-Flu-MTs) and/without (NLC-MTs) fluconazole in one nanoformulation to determine if they will act synergistically or not? The synthesized nanoformulation NLC-Flu-MTs and NLC-MTs exhibited very good particle size of 144.5 nm and 138.6 nm for size and zeta potential values of (- 23.5 mV) and (- 20.3 mV), respectively. Transmission electron microscope investigation confirmed that the synthesized NLCs have regular and spherical shape. The abundance and concentration of the six released monoterpenes were determined, as a novel approach, using GC-MS with very good results and validity. In-vitro antifungal screening was done before and after nano co-delivery against seven pathogenic, and aggressive fungi of Candida tropicalis, Candida krusei, Candida glabrata, Geotrichum Candidum, Candidaalbicans, Aspergillus Niger, and mucor circinelloides. Inhibition Zone diameter (IZD) and the minimum inhibitory concentration (MIC) were measured. Nanoformulations NLC-Flu-MTs and NLC-MTs manifested potential and unique biological susceptibility against all the tested microorganisms with reduced (MIC) values, especially against Candida Tropicalis (MIC = 0.97 µg/ml) which represents 16-fold of the value shown by NLC-MTs (MIC = 15.6 µg/ml) and 64-fold of fluconazole free before nanoformulation (MIC = 62.5 µg/ml). The efficiency of nanomaterials, particularly NLC-Flu-MTs, has become evident in the diminishing value of MIC which affirmed the synergism between fluconazole and the other six monoterpenes.
摘要：
频繁和变异感染是由机会性真菌病原体引起的。念珠菌病,曲霉病,和毛霉菌病是致病微生物，引起广泛的真菌疾病，严重程度在中度到致命之间交替。由于某些类型的念珠菌和其他真菌物种的获得性耐药性，氟康唑作为抗真菌药物的使用受到限制。本研究旨在巩固氟康唑对几种病原真菌的生物学效应。香芹酚的六种活性单萜（MT），芳樟醇,香叶醇,α-萜品烯,香茅醛,选择并在一个纳米制剂中与（NLC-Flu-MTs）和/或不与（NLC-MTs）氟康唑一起封装在纳米结构脂质载体（NLC）中，以确定它们是否会协同作用？合成的纳米制剂NLC-Flu-MTs和NLC-MTs表现出非常好的粒径，分别为144.5nm和138.6nm，尺寸和zeta电位值为（-23.5-分别。透射电子显微镜研究证实，合成的NLC具有规则和球形。确定了六种释放的单萜的丰度和浓度，作为一种新颖的方法，使用GC-MS具有很好的结果和有效性。在纳米共给药前后进行了体外抗真菌筛选，以及热带念珠菌的侵袭性真菌,克鲁斯念珠菌,光滑念珠菌,念珠菌，白色念珠菌,黑曲霉,和circinelloides粘液。测量抑制区直径(IZD)和最小抑制浓度(MIC)。纳米制剂NLC-Flu-MTs和NLC-MTs表现出对所有测试微生物的潜在和独特的生物敏感性，降低了（MIC）值，特别是针对热带假丝酵母（MIC=0.97µg/ml），这是NLC-MTs显示的值的16倍（MIC=15.6µg/ml）和纳米制剂前不含氟康唑的64倍（MIC=62.5µg/ml）。纳米材料的效率，特别是NLC-Flu-MTs，MIC的递减值已变得明显，这证实了氟康唑与其他六种单萜之间的协同作用。
