Aljihani Shokran A, Alehaideb Zeyad, Alarfaj Reem E, Alghoribi Majed F, Akiel Maaged A, Alenazi Thamer H, Al-Fahad Ahmed J, Al Tamimi Saad M, Albakr Turki M, Alshehri Abdulrahman, Alyahya Saad M, Yassin Alaa Eldeen B, Halwani Majed A
Nanomedicine Department, King Abdullah International Medical Research Center, King Saud bin Abdulaziz University for Health Sciences, Riyadh, Saudi Arabia.
Department of Medical Genomics, King Abdullah International Medical Research Center, King Saud bin Abdulaziz University for Health Sciences, Riyadh, Saudi Arabia.
Saudi J Biol Sci. 2020 Nov;27(11):3065-3071. doi: 10.1016/j.sjbs.2020.09.012. Epub 2020 Sep 12.
is an that could develop resistance to various antibiotics and become a multi-drug resistant (MDR) bacterium. Options for treating MDR are limited and the pipeline is somewhat dry when it comes to antibiotics for MDR bacteria, so we aimed to explore more options to help in treating MDR . The purpose of this study is to examine the synergistic effect of a liposomal formulations of co-encapsulated azithromycin and N-acetylcysteine against Liposomal azithromycin (LA) and liposomal azithromycin/N-acetylcysteine (LAN) were compared to free azithromycin. A broth dilution was used to measure the MIC and MBC of both formulations. The biofilm reduction activity, thermal stability measurements, stability studies, and cell toxicity analysis were performed. LA and LAN effectively reduced the MIC of SA10 strain, to 3 μg/ml and 2.5 μg/ml respectively. LAN at 1 × MIC recorded a 93.22% effectiveness in reducing an SA10 biofilm. The LA and LAN formulations were also structurally stable to 212 ± 2 °C and 198 ± 3 °C, respectively. In biological conditions, the formulations were largely stable in PBS conditions; however, they illustrated limited stability in sputum and plasma. We conclude that the formulation presented could be a promising therapy for resistance circumstances providing the stability conditions have been enhanced.
是一种可能对多种抗生素产生耐药性并成为多重耐药（MDR）细菌的细菌。治疗MDR的选择有限，而且在针对MDR细菌的抗生素方面，研发进展有些停滞，所以我们旨在探索更多有助于治疗MDR的选择。本研究的目的是检验共包封阿奇霉素和N - 乙酰半胱氨酸的脂质体制剂对的协同作用。将脂质体阿奇霉素（LA）和脂质体阿奇霉素/N - 乙酰半胱氨酸（LAN）与游离阿奇霉素进行比较。采用肉汤稀释法测量两种制剂的最低抑菌浓度（MIC）和最低杀菌浓度（MBC）。进行了生物膜减少活性、热稳定性测量、稳定性研究和细胞毒性分析。LA和LAN分别有效降低了金黄色葡萄球菌SA10菌株的MIC至3μg/ml和2.5μg/ml。1×MIC的LAN在减少金黄色葡萄球菌SA10生物膜方面记录了93.22%的有效性。LA和LAN制剂在结构上分别对212±2°C和198±3°C稳定。在生物学条件下，制剂在磷酸盐缓冲盐水（PBS）条件下基本稳定；然而，它们在痰液和血浆中显示出有限的稳定性。我们得出结论，所呈现的制剂在增强稳定性条件后可能是治疗耐药情况的一种有前景的疗法。
