Enhanced Nasal Deposition and Anti-Coronavirus Effect of Favipiravir-Loaded Mucoadhesive Chitosan–Alginate Nanoparticles
Favipiravir (FVR) is a repurposed antiviral drug for treating mild to moderate cases of the novel coronavirus disease 2019 (COVID-19). However, its poor solubility and permeability limit its clinical efficacy. To overcome its physicochemical and pharmacokinetic limitations, we statistically designed...
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MDPI AG
2022-12-01
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Series: | Pharmaceutics |
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Online Access: | https://www.mdpi.com/1999-4923/14/12/2680 |
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author | Khent Primo Alcantara Nonthaneth Nalinratana Nopporn Chutiwitoonchai Agnes L. Castillo Wijit Banlunara Opa Vajragupta Pornchai Rojsitthisak Pranee Rojsitthisak |
author_facet | Khent Primo Alcantara Nonthaneth Nalinratana Nopporn Chutiwitoonchai Agnes L. Castillo Wijit Banlunara Opa Vajragupta Pornchai Rojsitthisak Pranee Rojsitthisak |
author_sort | Khent Primo Alcantara |
collection | DOAJ |
description | Favipiravir (FVR) is a repurposed antiviral drug for treating mild to moderate cases of the novel coronavirus disease 2019 (COVID-19). However, its poor solubility and permeability limit its clinical efficacy. To overcome its physicochemical and pharmacokinetic limitations, we statistically designed a mucoadhesive chitosan–alginate nanoparticles (MCS-ALG-NPs) as a new carrier for FVR using response surface methodology, which provided suitable characteristics for transmucosal delivery. The use of mucoadhesive polymers for intranasal administration promotes the residence time and contact of FVR in the mucus membrane. The optimized FVR-MCS-ALG-NPs demonstrated superior mucoadhesion, higher permeation and deposition in the nasal mucosa, and a significant increase in the inhibition of viral replication over 35-fold compared with free FVR. The overall results suggest that MCS-ALG-NPs could be used as an effective mucoadhesive carrier to enhance the activity of FVR against COVID-19. |
first_indexed | 2024-03-09T15:58:33Z |
format | Article |
id | doaj.art-9a43ec0a7799480bb6ff83374d9f55be |
institution | Directory Open Access Journal |
issn | 1999-4923 |
language | English |
last_indexed | 2024-03-09T15:58:33Z |
publishDate | 2022-12-01 |
publisher | MDPI AG |
record_format | Article |
series | Pharmaceutics |
spelling | doaj.art-9a43ec0a7799480bb6ff83374d9f55be2023-11-24T17:20:08ZengMDPI AGPharmaceutics1999-49232022-12-011412268010.3390/pharmaceutics14122680Enhanced Nasal Deposition and Anti-Coronavirus Effect of Favipiravir-Loaded Mucoadhesive Chitosan–Alginate NanoparticlesKhent Primo Alcantara0Nonthaneth Nalinratana1Nopporn Chutiwitoonchai2Agnes L. Castillo3Wijit Banlunara4Opa Vajragupta5Pornchai Rojsitthisak6Pranee Rojsitthisak7Center of Excellence in Natural Products for Ageing and Chronic Diseases, Chulalongkorn University, Bangkok 10330, ThailandCenter of Excellence in Natural Products for Ageing and Chronic Diseases, Chulalongkorn University, Bangkok 10330, ThailandNational Center for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency, Pathum Thani 12120, ThailandFaculty of Pharmacy, The Graduate School, Research Center for the Natural and Applied Sciences (RCNAS), University of Santo Tomas, Manila 1008, PhilippinesDepartment of Pathology, Faculty of Veterinary Science, Chulalongkorn University, Bangkok 10330, ThailandCenter of Excellence in Natural Products for Ageing and Chronic Diseases, Chulalongkorn University, Bangkok 10330, ThailandCenter of Excellence in Natural Products for Ageing and Chronic Diseases, Chulalongkorn University, Bangkok 10330, ThailandCenter of Excellence in Natural Products for Ageing and Chronic Diseases, Chulalongkorn University, Bangkok 10330, ThailandFavipiravir (FVR) is a repurposed antiviral drug for treating mild to moderate cases of the novel coronavirus disease 2019 (COVID-19). However, its poor solubility and permeability limit its clinical efficacy. To overcome its physicochemical and pharmacokinetic limitations, we statistically designed a mucoadhesive chitosan–alginate nanoparticles (MCS-ALG-NPs) as a new carrier for FVR using response surface methodology, which provided suitable characteristics for transmucosal delivery. The use of mucoadhesive polymers for intranasal administration promotes the residence time and contact of FVR in the mucus membrane. The optimized FVR-MCS-ALG-NPs demonstrated superior mucoadhesion, higher permeation and deposition in the nasal mucosa, and a significant increase in the inhibition of viral replication over 35-fold compared with free FVR. The overall results suggest that MCS-ALG-NPs could be used as an effective mucoadhesive carrier to enhance the activity of FVR against COVID-19.https://www.mdpi.com/1999-4923/14/12/2680response surface methodologyBox–Behnken designchitosanalginateSARS-CoV-2antiviral |
spellingShingle | Khent Primo Alcantara Nonthaneth Nalinratana Nopporn Chutiwitoonchai Agnes L. Castillo Wijit Banlunara Opa Vajragupta Pornchai Rojsitthisak Pranee Rojsitthisak Enhanced Nasal Deposition and Anti-Coronavirus Effect of Favipiravir-Loaded Mucoadhesive Chitosan–Alginate Nanoparticles Pharmaceutics response surface methodology Box–Behnken design chitosan alginate SARS-CoV-2 antiviral |
title | Enhanced Nasal Deposition and Anti-Coronavirus Effect of Favipiravir-Loaded Mucoadhesive Chitosan–Alginate Nanoparticles |
title_full | Enhanced Nasal Deposition and Anti-Coronavirus Effect of Favipiravir-Loaded Mucoadhesive Chitosan–Alginate Nanoparticles |
title_fullStr | Enhanced Nasal Deposition and Anti-Coronavirus Effect of Favipiravir-Loaded Mucoadhesive Chitosan–Alginate Nanoparticles |
title_full_unstemmed | Enhanced Nasal Deposition and Anti-Coronavirus Effect of Favipiravir-Loaded Mucoadhesive Chitosan–Alginate Nanoparticles |
title_short | Enhanced Nasal Deposition and Anti-Coronavirus Effect of Favipiravir-Loaded Mucoadhesive Chitosan–Alginate Nanoparticles |
title_sort | enhanced nasal deposition and anti coronavirus effect of favipiravir loaded mucoadhesive chitosan alginate nanoparticles |
topic | response surface methodology Box–Behnken design chitosan alginate SARS-CoV-2 antiviral |
url | https://www.mdpi.com/1999-4923/14/12/2680 |
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