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Liposomes and liposome-like nanoparticles:From anti-fungal infection to the COVID-19 pandemic treatment 被引量:1
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作者 Yonglong He Wanting Zhang +4 位作者 Qingqing Xiao Lifang Fan dechun huang Wei Chen Wei He 《Asian Journal of Pharmaceutical Sciences》 SCIE CAS 2022年第6期817-837,共21页
The liposome is the first nanomedicine transformed into the market and applied to human patients.Since then,such phospholipid bilayer vesicles have undergone technological advancements in delivering small molecular-we... The liposome is the first nanomedicine transformed into the market and applied to human patients.Since then,such phospholipid bilayer vesicles have undergone technological advancements in delivering small molecular-weight compounds and biological drugs.Numerous investigations about liposome uses were conducted in different treatment fields,including anti-tumor,anti-fungal,anti-bacterial,and clinical analgesia,owing to liposome's ability to reduce drug cytotoxicity and improve the therapeutic efficacy and combinatorial delivery.In particular,two liposomal vaccines were approved in 2021 to combat COVID-19.Herein,the clinically used liposomes are reviewed by introducing various liposomal preparations in detail that are currently proceeding in the clinic or on the market.Finally,we discuss the challenges of developing liposomes and cutting-edge liposomal delivery for biological drugs and combination therapy. 展开更多
关键词 Liposomes Drug delivery Clinical application COVID-19 pandemic
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Preparing anti-SARS-CoV-2 agent EIDD-2801by a practical and scalable approach,and quick evaluation via machine learning
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作者 Zhen Qin Bin Dong +5 位作者 Renbing Wang dechun huang Jubo Wang Xi Feng Jinlei Bian Zhiyu Li 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2021年第11期3678-3682,共5页
EIDD-2801 is an orally bioavailable prodrug,which will be applied for emergency use authorization from the U.S.Food and Drug Administration for the treatment of COVID-19.To investigate the optimal parameters,EIDD-2801... EIDD-2801 is an orally bioavailable prodrug,which will be applied for emergency use authorization from the U.S.Food and Drug Administration for the treatment of COVID-19.To investigate the optimal parameters,EIDD-2801 was optimized via a four-step synthesis with high purity of 99.9%.The hydroxylamination procedure was telescoped in a one-pot and the final step was precisely controlled on reagents,temperature and reaction time.Compared to the original route,the yield of the new route was enhanced from 17% to 58% without column chromatography.The optimized synthesis has been successfully determinated on a decagram scale:the first step at 200 g and the final step at 20 g.Besides,the relationship between yield and temperature,time,and reagents in the deprotection step was investigated via Shapley value explanation and machine learning approach-decision tree method.The results revealed that reagents have the greatest impact on yield estimation,followed by the temperature. 展开更多
关键词 EIDD-2801 SARS-CoV-2 Antiviral drug Decision tree Shapley value
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