Ali Hala R, Ali Moustafa R K, Wu Yue, Selim Salah A, Abdelaal Hazem F M, Nasr Essam A, El-Sayed Mostafa A
School of Chemistry and Biochemistry, Georgia Institute of Technology , Atlanta, Georgia 30332-0400, United States.
Animal Health Research Institute (AHRI) , Department of Bacteriology and Immunology, Dokki, Giza, Egypt.
Bioconjug Chem. 2016 Oct 19;27(10):2486-2492. doi: 10.1021/acs.bioconjchem.6b00430. Epub 2016 Sep 22.
TB remains a challenging disease to control worldwide. Nanoparticles have been used as drug carriers to deliver high concentrations of antibiotics directly to the site of infection, reducing the duration of treatment along with any side effects of off-target toxicities after systemic exposure to the antibiotics. Herein we have developed a drug delivery platform where gold nanorods (AuNRs) are conjugated to rifampicin (RF), which is released after uptake into macrophage cells (RAW264.7). Due to the nature of the macrophage cells, the nanoparticles are actively internalized into macrophages and release RF after uptake, under the safety frame of the host cells (macrophage). AuNRs without RF conjugation exhibit obvious antimicrobial activity. Therefore, AuNRs could be a promising antimycobacterial agent and an effective delivery vehicle for the antituberculosis drug Rifampicin for use in tuberculosis therapy.
在全球范围内,结核病仍然是一种难以控制的疾病。纳米颗粒已被用作药物载体,将高浓度抗生素直接输送到感染部位,从而缩短治疗时间,并减少全身暴露于抗生素后产生的脱靶毒性等副作用。在此,我们开发了一种药物递送平台,其中金纳米棒(AuNRs)与利福平(RF)偶联,利福平在被巨噬细胞(RAW264.7)摄取后释放。由于巨噬细胞的特性,纳米颗粒在宿主细胞(巨噬细胞)的安全框架下被巨噬细胞主动内化并在摄取后释放RF。未偶联RF的AuNRs表现出明显的抗菌活性。因此,AuNRs可能是一种有前景的抗分枝杆菌剂,也是用于结核病治疗的抗结核药物利福平的有效递送载体。