{"title":"具有生物相容性的控释雷米替韦脂质体可抑制非小细胞肺癌细胞的端粒酶活性:制备、表征、体外生物学评价和分子对接分析","authors":"","doi":"10.1016/j.crbiot.2024.100256","DOIUrl":null,"url":null,"abstract":"<div><div>Non-small cell lung cancer (NSCLC) is a global leading cause of cancer mortality. Herein, remdesivir (RDV) was loaded into biocompatible liposomes (RDV-Lips) composed of 1,2-dipalmitoyl-sn‑glycero-3-phosphocholine (DPPC), cholesterol, and polyethylene glycol hexadecyl ether (Brij-58) to enhance its solubility and anticancer efficiency. The study highlighted the possible RDV-induced underlying events, emphasizing its inhibitory potential of telomerase activity through in-silico docking and in vitro studies. RDV-Lips were developed using thin-film hydration and then subjected to physicochemical characterizations. The selected formulations were evaluated for their stability, in vitro release, and in vitro anticancer activity. The size range of RDV-Lips was 83.8–157.9 nm with a polydispersity index (PDI) lower than 0.23 and entrapment exceeded 93%. The cholesterol content of RDV-Lips offered a control point of RDV release, where high and low concentrations exerted slow and fast release patterns, respectively. RDV-Lips showed enhanced anticancer activity and selectivity. They inhibited colony formation, increased lipid peroxidation, induced apoptosis, and inhibited the telomerase activity in a dose-dependent manner. In conclusion, RDV-Lips overcame RDV solubility problems and enhanced its anticancer efficiency. RDV could be a potential therapy against NSCLC via induction of oxidative stress and inhibition of the telomerase activity, which, in turn, restricts unlimited cellular proliferation and apoptosis induction.</div></div>","PeriodicalId":52676,"journal":{"name":"Current Research in Biotechnology","volume":null,"pages":null},"PeriodicalIF":3.6000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Biocompatible, controlled-release remdesivir-loaded liposomes tackling the telomerase activity of Non-Small cell lung cancer cells: Preparation, characterization, in vitro biological evaluation, and molecular docking analysis\",\"authors\":\"\",\"doi\":\"10.1016/j.crbiot.2024.100256\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Non-small cell lung cancer (NSCLC) is a global leading cause of cancer mortality. Herein, remdesivir (RDV) was loaded into biocompatible liposomes (RDV-Lips) composed of 1,2-dipalmitoyl-sn‑glycero-3-phosphocholine (DPPC), cholesterol, and polyethylene glycol hexadecyl ether (Brij-58) to enhance its solubility and anticancer efficiency. The study highlighted the possible RDV-induced underlying events, emphasizing its inhibitory potential of telomerase activity through in-silico docking and in vitro studies. RDV-Lips were developed using thin-film hydration and then subjected to physicochemical characterizations. The selected formulations were evaluated for their stability, in vitro release, and in vitro anticancer activity. The size range of RDV-Lips was 83.8–157.9 nm with a polydispersity index (PDI) lower than 0.23 and entrapment exceeded 93%. The cholesterol content of RDV-Lips offered a control point of RDV release, where high and low concentrations exerted slow and fast release patterns, respectively. RDV-Lips showed enhanced anticancer activity and selectivity. They inhibited colony formation, increased lipid peroxidation, induced apoptosis, and inhibited the telomerase activity in a dose-dependent manner. In conclusion, RDV-Lips overcame RDV solubility problems and enhanced its anticancer efficiency. RDV could be a potential therapy against NSCLC via induction of oxidative stress and inhibition of the telomerase activity, which, in turn, restricts unlimited cellular proliferation and apoptosis induction.</div></div>\",\"PeriodicalId\":52676,\"journal\":{\"name\":\"Current Research in Biotechnology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":3.6000,\"publicationDate\":\"2024-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current Research in Biotechnology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2590262824000820\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOTECHNOLOGY & APPLIED MICROBIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Research in Biotechnology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2590262824000820","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOTECHNOLOGY & APPLIED MICROBIOLOGY","Score":null,"Total":0}
Biocompatible, controlled-release remdesivir-loaded liposomes tackling the telomerase activity of Non-Small cell lung cancer cells: Preparation, characterization, in vitro biological evaluation, and molecular docking analysis
Non-small cell lung cancer (NSCLC) is a global leading cause of cancer mortality. Herein, remdesivir (RDV) was loaded into biocompatible liposomes (RDV-Lips) composed of 1,2-dipalmitoyl-sn‑glycero-3-phosphocholine (DPPC), cholesterol, and polyethylene glycol hexadecyl ether (Brij-58) to enhance its solubility and anticancer efficiency. The study highlighted the possible RDV-induced underlying events, emphasizing its inhibitory potential of telomerase activity through in-silico docking and in vitro studies. RDV-Lips were developed using thin-film hydration and then subjected to physicochemical characterizations. The selected formulations were evaluated for their stability, in vitro release, and in vitro anticancer activity. The size range of RDV-Lips was 83.8–157.9 nm with a polydispersity index (PDI) lower than 0.23 and entrapment exceeded 93%. The cholesterol content of RDV-Lips offered a control point of RDV release, where high and low concentrations exerted slow and fast release patterns, respectively. RDV-Lips showed enhanced anticancer activity and selectivity. They inhibited colony formation, increased lipid peroxidation, induced apoptosis, and inhibited the telomerase activity in a dose-dependent manner. In conclusion, RDV-Lips overcame RDV solubility problems and enhanced its anticancer efficiency. RDV could be a potential therapy against NSCLC via induction of oxidative stress and inhibition of the telomerase activity, which, in turn, restricts unlimited cellular proliferation and apoptosis induction.
期刊介绍:
Current Research in Biotechnology (CRBIOT) is a new primary research, gold open access journal from Elsevier. CRBIOT publishes original papers, reviews, and short communications (including viewpoints and perspectives) resulting from research in biotechnology and biotech-associated disciplines.
Current Research in Biotechnology is a peer-reviewed gold open access (OA) journal and upon acceptance all articles are permanently and freely available. It is a companion to the highly regarded review journal Current Opinion in Biotechnology (2018 CiteScore 8.450) and is part of the Current Opinion and Research (CO+RE) suite of journals. All CO+RE journals leverage the Current Opinion legacy-of editorial excellence, high-impact, and global reach-to ensure they are a widely read resource that is integral to scientists' workflow.