Publications, Pharmaceutical

Cyclosporine – A Micellar Nasal Spray: A Promising Antiviral Solution Against SARS-CoV-2

The upper airways serve as the primary entry point for Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), the virus responsible for COVID-19. Once the virus enters through the nasal passages, it can quickly spread to the lungs, leading to severe respiratory complications. To combat this, researchers have developed an innovative nasal spray formulation designed to prevent or treat SARS-CoV-2 infection at its earliest stages.

Download Cyclosporine Nasal Spray Publication
Author(s): Fabiola Guareschi, ADDRes Lab, Department of Food and Drug, University of Parma Elena Del Favero, Department of Medical Biotechnology and Translational Medicine, University of Milan Caterina Ricci, Department of Medical Biotechnology and Translational Medicine, University of Milan Laura Cantù, Department of Medical Biotechnology and Translational Medicine, University of Milan Martina Brandolini, Unit of Microbiology, The Great Romagna Hub Laboratory Vittorio Sambri, Unit of Microbiology, The Great Romagna Hub Laboratory Sara Nicoli, ADDRes Lab, Department of Food and Drug, University of Parma Silvia Pescina, ADDRes Lab, Department of Food and Drug, University of Parma Davide d'Angelo, ADDRes Lab, Department of Food and Drug, University of Parma Irene Rossi, Nanopharm Ltd Francesca Buttini, ADDRes Lab, Department of Food and Drug, University of Parma Ruggero Bettini, ADDRes Lab, Department of Food and Drug, University of Parma Fabio Sonvico, ADDRes Lab, Department of Food and Drug, University of Parma
30 Sep 2024

Innovative Formulation: Cyclosporine A-Loaded Micelles
The core of this groundbreaking research revolves around the development of micelles loaded with Cyclosporine A, a potent immunosuppressant. These micelles are crafted using α-tocopheryl-polyethylene-glycol succinate, a compound known for its excellent biocompatibility and ability to enhance drug solubility. The micellar formulation is specifically designed for nasal administration, offering a targeted approach to combat the virus right at the entry point.

 

Stability and Muco-penetration
One of the critical aspects of this study was to evaluate the behavior of these micelles in the presence of simulated nasal mucus. The results were promising, showing that the micelles exhibit long-term stability and a rapid muco-penetration rate. This means that the micelles can swiftly diffuse through the glycoprotein matrix of the nasal mucus, ensuring that the active drug, Cyclosporine A, is effectively delivered to the target site.

 

Spray Characteristics and Deposition Profile
The effectiveness of a nasal spray largely depends on its ability to uniformly distribute the drug throughout the nasal cavity. In this study, the spray characteristics and deposition profile of the micellar formulation were tested using a silicon nasal model. Three different nasal spray systems were evaluated, and the BiVax nasal spray pump from Aptar Pharma emerged as the most effective. This nasal spray system provided the widest and most uniform deposition, ensuring that the micelles are evenly distributed across the nasal cavity.

 

Antiviral Activity Against SARS-CoV-2
The antiviral efficacy of the Cyclosporine A-loaded micelles was tested against the Omicron BA.1 variant of SARS-CoV-2 using Vero E6 cells. The study simulated various treatment scenarios, including pre-infection, during infection, and post-infection of the upper airways. Remarkably, the micellar formulation achieved complete viral inactivation, whereas the non-formulated drug showed very low activity. This suggests a synergistic effect between Cyclosporine A and the micellar formulation, significantly enhancing the antiviral action.

 

To summarize: A Potential Game-Changer in COVID-19 Treatment
In conclusion, the development of Cyclosporine A-loaded micellar nasal spray represents a significant advancement in the fight against COVID-19. The formulation’s stability, rapid muco-penetration, and effective distribution within the nasal cavity, combined with its potent antiviral activity, make it a promising candidate for clinical use. This innovative approach not only offers a potential treatment for SARS-CoV-2 but also holds promise against a wide spectrum of coronavirus variants.
By targeting the virus at its entry point, this nasal spray could play a crucial role in preventing the spread of infection and reducing the severity of the disease. As research progresses, we can look forward to more effective and accessible treatments that can help control the pandemic and protect public health.

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