| Summary: | Woo-Jin Jeon,1,* Hong-Ki Lee,2,3,* Young-Guk Na,1 Minwoo Jung,1 Su-Cheol Han,2 Jeong Ho Hwang,2 Eunhye Jung,4 Dasom Hwang,4 Jin Soo Shin,4 Cheong-Weon Cho1 1College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon, 34134, Republic of Korea; 2Center for Companion Animal New Drug Development, Jeonbuk Branch, Korea Institute of Toxicology (KIT), Jeongeup, Jeollabuk-do, 53212, Republic of Korea; 3Human Health Risk Assessment Center, Jeonbuk Branch, Korea Institute of Toxicology (KIT), Jeongeup, Jeollabuk-do, 53212, Republic of Korea; 4Infectious Diseases Therapeutic Research Center, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea*These authors contributed equally to this workCorrespondence: Jin Soo Shin, Infectious Diseases Therapeutic Research Center, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea, Email jsshin@krict.re.kr Cheong-Weon Cho, College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon, 34134, Republic of Korea, Email chocw@cnu.ac.krIntroduction: The ongoing SARS-CoV-2 pandemic has affected public health, the economy, and society. This study reported a nanotechnology-based strategy to enhance the antiviral efficacy of the antiviral agent remdesivir (RDS).Results: We developed a nanosized spherical RDS-NLC in which the RDS was encapsulated in an amorphous form. The RDS-NLC significantly potentiated the antiviral efficacy of RDS against SARS-CoV-2 and its variants (alpha, beta, and delta). Our study revealed that NLC technology improved the antiviral effect of RDS against SARS-CoV-2 by enhancing the cellular uptake of RDS and reducing SARS-CoV-2 entry in cells. These improvements resulted in a 211% increase in the bioavailability of RDS.Conclusion: Thus, the application of NLC against SARS-CoV-2 may be a beneficial strategy to improve the antiviral effects of antiviral agents.Keywords: remdesivir, nanostructured lipid carrier, antiviral effect, SARS-CoV-2, virus entry
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