Binsuwaidan Reem, Sultan Amal A, Negm Walaa A, Attallah Nashwah G M, Alqahtani Moneerah J, Hussein Ismail A, Shaldam Moataz A, El-Sherbeni Suzy A, Elekhnawy Engy
Department of Pharmaceutical Science, College of Pharmacy, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi Arabia.
Department of Pharmaceutical Technology, College of Pharmacy, Tanta University, Tanta 31527, Egypt.
Pharmaceuticals (Basel). 2022 Aug 24;15(9):1043. doi: 10.3390/ph15091043.
Owing to the disseminating resistance among pathogenic bacteria, especially , there is a high need for alternate compounds with antibacterial activity. Herein, lycopene was isolated from L. Molecular docking approach was employed to explore lycopene binding affinity to selected vital proteins of with the binding mechanisms being investigated. This proposed a promising antibacterial activity of lycopene. However, the pharmacological use of lycopene is hampered by its poor solubility and limited oral bioavailability. Accordingly, bilosomes were fabricated for oral lycopene delivery. The computed entrapment efficiency, mean vesicular size, and zeta potential values for the optimized formulation were 93.2 ± 0.6%, 485.8 ± 35.3 nm, and -38.3 ± 4, respectively. In vitro drug release studies revealed controlled lycopene release from constructed bilosomes, with the drug liberation being based on the Higuchi kinetics model. Transmission electron microscopic evaluation of bilosomes revealed spherical nanovesicles free from aggregates. Moreover, the in vitro and in vivo antibacterial activity of lycopene and its constructed formulations against multidrug-resistant isolates were explored. The optimized bilosomes exhibited the lowest minimum inhibitory concentrations ranging from 8 to 32 µg/mL. In addition, scanning electron microscopy revealed remarkable deformation and lysis of the bilosomes-treated bacterial cells. Regarding in vivo investigation, a lung infection model in mice was employed. The tested bilosomes reduced the inflammation and congestion in the treated mice's lung tissues, resulting in normal-sized bronchioles and alveoli with very few congested vessels. In addition, it resulted in a significant reduction in pulmonary fibrosis. In conclusion, this study investigated the potential activity of the naturally isolated lycopene in controlling infections triggered by multidrug-resistant isolates. Furthermore, it introduced bilosomes as a promising biocompatible nanocarrier for modulation of oral lycopene delivery and in vivo antimicrobial activity.
由于致病细菌中耐药性的传播，特别是……，因此迫切需要具有抗菌活性的替代化合物。在此，从……中分离出番茄红素。采用分子对接方法探索番茄红素与……选定关键蛋白的结合亲和力，并研究其结合机制。这表明番茄红素具有良好的抗菌活性。然而，番茄红素的药理应用受到其溶解度差和口服生物利用度有限的阻碍。因此，制备了双分子层脂质体用于口服递送番茄红素。优化制剂的计算包封率、平均囊泡大小和zeta电位值分别为93.2±0.6%、485.8±35.3 nm和-38.3±4。体外药物释放研究表明，构建的双分子层脂质体可控制番茄红素的释放，药物释放符合Higuchi动力学模型。双分子层脂质体的透射电子显微镜评估显示为无聚集的球形纳米囊泡。此外，还研究了番茄红素及其构建制剂对多重耐药……分离株的体外和体内抗菌活性。优化后的双分子层脂质体表现出最低的最低抑菌浓度，范围为8至32μg/mL。此外，扫描电子显微镜显示双分子层脂质体处理的细菌细胞出现明显变形和裂解。关于体内研究，采用了小鼠肺部感染模型。测试的双分子层脂质体减轻了治疗小鼠肺组织的炎症和充血，导致细支气管和肺泡大小正常，充血血管极少。此外，它还显著减少了肺纤维化。总之，本研究调查了天然分离的番茄红素在控制多重耐药……分离株引发的感染方面的潜在活性。此外，它还引入了双分子层脂质体作为一种有前景的生物相容性纳米载体，用于调节口服番茄红素递送和体内抗菌活性。
