Polymeric nanoparticles and nanomicelles of hydroxychloroquine co-loaded with azithromycin potentiate anti-SARS-CoV-2 effect

Abstract

The outbreak of coronavirus (COVID-19) has put the world in an unprecedented scenario. To reestablish the world routine as promote the effective treatment of this disease, the world is looking for new (and old) drug that can efficiently kill the virus. In this study, we have developed two nanosystems: polymeric nanoparticles and nanomicelles-based on hydroxychloroquine and azithromycin. The nanosystem was fully characterized by AFM and DLS techniques. Also, the nanosystems were radiolabeled with 99m Tc and pulmonary applied (installation) in vivo to evaluate the biological behavior. The toxicity of both nanosystem were evaluated in primary cells (FGH). Finally, both nanosystems were evaluated in vitro against the SARS-CoV-2. The results demonstrated that the methodology used to produce the nanomicelles and the nanoparticle was efficient, the characterization showed a nanoparticle with a spherical shape and a medium size of 390 nm and a nanomicelle also with a spherical shape and a medium size of 602 nm. The nanomicelles were more efficient (~ 70%) against SARS-CoV-2 than the nanoparticles. The radiolabeling process with 99m Tc was efficient (> 95%) in both nanosystems and the pulmonary application demonstrated to be a viable route for both nanosystems with a local retention time of approximately, 24 h. None of the nanosystems showed cytotoxic effect on FGH cells, even in high doses, corroborating the safety of both nanosystems. Thus, claiming the benefits of the nanotechnology, especially with regard the reduced adverse we believe that the use of nanosystems for COVID-19 treatment can be an optimized choice. Graphical abstract Supplementary Information The online version contains supplementary material available at 10.1007/s40097-022-00476-3.

Macrophage Cell Membrane‐Cloaked Nanoplatforms for Biomedical Applications

“…The ongoing pandemic crisis caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) remains a serious global health problem, in which the absence of specific therapeutic regimens greatly contributes to the high mortality and morbidity associated with coronavirus disease 2019 (COVID-19). [26,159] Alveolar macrophages are a crucial primary line of defense against invaders, which express specific membrane receptors involved in cytokine uptake and binding of the spike protein on the coronavirus surface, thus suppressing virus infection by diverting them from target cells and blocking viral cellular entry, while mitigating the excessive inflammatory and immune responses. In a recent effort to develop a multifunctional biomimetic nanosystem against COVID-19 infection, polymeric PLGA NP cores containing 2TPE-2NDTA, an efficient photothermal agent, were wrapped with alveolar macrophage-derived membranes (Figure 17A).…”

Novel polymer-based hydrogels of recent research in drug delivery for disease treatment related to SARS-CoV-2 virus

“…systems for disease treatment related to SARS-CoV-2 virus Polymeric nanoparticles are another type of carrier widely used in drug delivery systems to treat diseases related to the SARS-CoV-2 virus. These nanoparticles are composed of biocompatible and biodegradable polymers [104,105], such as poly(lactic-co-glycolic acid) (PLGA) [77], polyethylene glycol (PEG) [106], or chitosan [107]. Polymeric nanoparticles can encapsulate a wide range of drugs, including antiviral agents [104], antibodies [108], or nucleic acids [109], protecting them from degradation and improving their stability [77,106].…”

Methods for Radiolabelling Nanoparticles: SPECT Use (Part 1)

“…The radiolabelling of the NPs with a direct method can also be performed with a short incubation between SnCl 2 and the NPs, followed by the addition of 99m Tc in the solution. This method was used to radiolabel several types of NPs: octreotide NPs, cerium oxide NPs (CeO 2 -NPs), mesoporous silica NPs, poly-γ-glutamic acid NPs conjugated with folic acid, carbon-based mesoporous NPs, zirconium NPs, serum albumin nanoparticles, polymeric NPs, and dendrimer glycoconjugate [ 26 , 27 , 28 , 29 , 30 , 31 , 32 , 33 , 34 ]. All the studies showed a high final LE, but the formation of radiocolloids often requires further purification of the solution.…”