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• W3208562227 endingPage "783" @default.
• W3208562227 startingPage "772" @default.
• W3208562227 abstract "Strong infectivity enables coronavirus disease 2019 (COVID-19) to rage throughout the world. Moreover, the lack of drugs with definite therapeutic effects further aggravates the spread of the pandemic. Remdesivir is one of the most promising anti-severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) drugs. However, the limited clinical effects make its therapeutic effect controversial, which may result from the poor accumulation and activation of remdesivir in the lung. Therefore, we developed lyophilized remdesivir liposomes (Rdv-lips) which can be reconstituted as liposomal aerosol for pulmonary delivery to improve the in vivo behavior of existing remdesivir cyclodextrin conclusion compound (Rdv-cyc) injections. Liposome encapsulation endowed remdesivir with much higher solubility and better biocompatibility. The in vitro liposomal aerosol characterization demonstrated that Rdv-lips possessed a mass median aerodynamic diameter of 4.118 µm and fine particle fraction (<5 µm) higher than 50%, indicating good pulmonary delivery properties. Compared to the Rdv-cyc intravenous injection group, the Rdv-lips inhalation group displayed a nearly 100-fold increase in the remdesivir-active metabolite nucleotide triphosphate (NTP) concentration and better NTP accumulation in the lung than the Rdv-cyc inhalation group. A faster transition from remdesivir to NTP of Rdv-lips (inhalation) could also be observed due to better cell uptake. Compared to other preparations, the superiority of Rdv-lips was further evidenced by the results of an in vivo safety study, with little possibility of inducing inflammation. In conclusion, Rdv-lips for pulmonary delivery will be a potent formulation to improve the in vivo behavior of remdesivir and exert better therapeutic effects in COVID-19 treatment." @default.
• W3208562227 created "2021-11-08" @default.
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• W3208562227 date "2021-11-01" @default.
• W3208562227 modified "2023-10-15" @default.
• W3208562227 title "Liposomal remdesivir inhalation solution for targeted lung delivery as a novel therapeutic approach for COVID-19" @default.
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• W3208562227 doi "https://doi.org/10.1016/j.ajps.2021.09.002" @default.
• W3208562227 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8529908" @default.
• W3208562227 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34703490" @default.
• W3208562227 hasPublicationYear "2021" @default.
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