Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19
Investigating bicelles as an oral drug delivery system and exploiting their structural benefits can pave the way to formulate hydrophobic drugs and potentiate their activity. Herein, the ability of non-ionic surfactants (labrasol ® , tween 80, cremophore EL and pluronic F127) to form curcumin loaded...
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creator | Mahmoud, Dina B. Bakr, Mohamed Mofreh Al-karmalawy, Ahmed A. Moatasim, Yassmin El Taweel, Ahmed Mostafa, Ahmed |
description | Investigating bicelles as an oral drug delivery system and exploiting their structural benefits can pave the way to formulate hydrophobic drugs and potentiate their activity. Herein, the ability of non-ionic surfactants (labrasol
®
, tween 80, cremophore EL and pluronic F127) to form curcumin loaded bicelles with phosphatidylcholine, utilizing a simple method, was investigated. Molecular docking was used to understand the mechanism of bicelles formation. The % transmittance and TEM exhibited bicelles formation with labrasol
®
and tween 80, while cremophor EL and pluronic F127 tended to form mixed micelles. The surfactant-based nanostructures significantly improved curcumin dissolution (99.2 ± 2.6% within 10 min in case of tween 80-based bicelles) compared to liposomes and curcumin suspension in non-sink conditions. The prepared formulations improved curcumin
ex vivo
permeation over liposomes and drug suspension. Further, the therapeutic antiviral activity of the formulated curcumin against SARS-CoV-2 was potentiated over drug suspension. Although both Labrasol
®
and tween 80 bicelles could form bicelles and enhance the oral delivery of curcumin when compared to liposomes and drug suspension, the mixed micelles formulations depicted superiority than bicelles formulations. Our findings provide promising formulations that can be utilized for further preclinical and clinical studies of curcumin as an antiviral therapy for COVID-19 patients.
Graphical Abstract |
doi_str_mv | 10.1208/s12249-021-02197-2 |
format | Article |
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®
, tween 80, cremophore EL and pluronic F127) to form curcumin loaded bicelles with phosphatidylcholine, utilizing a simple method, was investigated. Molecular docking was used to understand the mechanism of bicelles formation. The % transmittance and TEM exhibited bicelles formation with labrasol
®
and tween 80, while cremophor EL and pluronic F127 tended to form mixed micelles. The surfactant-based nanostructures significantly improved curcumin dissolution (99.2 ± 2.6% within 10 min in case of tween 80-based bicelles) compared to liposomes and curcumin suspension in non-sink conditions. The prepared formulations improved curcumin
ex vivo
permeation over liposomes and drug suspension. Further, the therapeutic antiviral activity of the formulated curcumin against SARS-CoV-2 was potentiated over drug suspension. Although both Labrasol
®
and tween 80 bicelles could form bicelles and enhance the oral delivery of curcumin when compared to liposomes and drug suspension, the mixed micelles formulations depicted superiority than bicelles formulations. Our findings provide promising formulations that can be utilized for further preclinical and clinical studies of curcumin as an antiviral therapy for COVID-19 patients.
Graphical Abstract</description><identifier>ISSN: 1530-9932</identifier><identifier>EISSN: 1530-9932</identifier><identifier>DOI: 10.1208/s12249-021-02197-2</identifier><identifier>PMID: 34966978</identifier><language>eng</language><publisher>Cham: Springer International Publishing</publisher><subject>Antiviral Agents ; Biochemistry ; Biomedical and Life Sciences ; Biomedicine ; Biotechnology ; COVID-19 ; Curcumin ; Feasibility Studies ; Humans ; Micelles ; Molecular Docking Simulation ; Pharmacology/Toxicology ; Pharmacy ; Research Article ; SARS-CoV-2 ; Surface-Active Agents</subject><ispartof>AAPS PharmSciTech, 2021-12, Vol.23 (1), p.44, Article 44</ispartof><rights>The Author(s) 2021</rights><rights>2021. The Author(s).</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c512t-897f7db1a0ffc2d96ec6d7707f8369ebfafd2e7e54eb63e7ffed7f9a918346093</citedby><cites>FETCH-LOGICAL-c512t-897f7db1a0ffc2d96ec6d7707f8369ebfafd2e7e54eb63e7ffed7f9a918346093</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1208/s12249-021-02197-2$$EPDF$$P50$$Gspringer$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1208/s12249-021-02197-2$$EHTML$$P50$$Gspringer$$Hfree_for_read</linktohtml><link.rule.ids>230,314,780,784,885,27924,27925,41488,42557,51319</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/34966978$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Mahmoud, Dina B.</creatorcontrib><creatorcontrib>Bakr, Mohamed Mofreh</creatorcontrib><creatorcontrib>Al-karmalawy, Ahmed A.</creatorcontrib><creatorcontrib>Moatasim, Yassmin</creatorcontrib><creatorcontrib>El Taweel, Ahmed</creatorcontrib><creatorcontrib>Mostafa, Ahmed</creatorcontrib><title>Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19</title><title>AAPS PharmSciTech</title><addtitle>AAPS PharmSciTech</addtitle><addtitle>AAPS PharmSciTech</addtitle><description>Investigating bicelles as an oral drug delivery system and exploiting their structural benefits can pave the way to formulate hydrophobic drugs and potentiate their activity. Herein, the ability of non-ionic surfactants (labrasol
®
, tween 80, cremophore EL and pluronic F127) to form curcumin loaded bicelles with phosphatidylcholine, utilizing a simple method, was investigated. Molecular docking was used to understand the mechanism of bicelles formation. The % transmittance and TEM exhibited bicelles formation with labrasol
®
and tween 80, while cremophor EL and pluronic F127 tended to form mixed micelles. The surfactant-based nanostructures significantly improved curcumin dissolution (99.2 ± 2.6% within 10 min in case of tween 80-based bicelles) compared to liposomes and curcumin suspension in non-sink conditions. The prepared formulations improved curcumin
ex vivo
permeation over liposomes and drug suspension. Further, the therapeutic antiviral activity of the formulated curcumin against SARS-CoV-2 was potentiated over drug suspension. Although both Labrasol
®
and tween 80 bicelles could form bicelles and enhance the oral delivery of curcumin when compared to liposomes and drug suspension, the mixed micelles formulations depicted superiority than bicelles formulations. Our findings provide promising formulations that can be utilized for further preclinical and clinical studies of curcumin as an antiviral therapy for COVID-19 patients.
Graphical Abstract</description><subject>Antiviral Agents</subject><subject>Biochemistry</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotechnology</subject><subject>COVID-19</subject><subject>Curcumin</subject><subject>Feasibility Studies</subject><subject>Humans</subject><subject>Micelles</subject><subject>Molecular Docking Simulation</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Research Article</subject><subject>SARS-CoV-2</subject><subject>Surface-Active Agents</subject><issn>1530-9932</issn><issn>1530-9932</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><sourceid>C6C</sourceid><sourceid>EIF</sourceid><recordid>eNp9UU1v1DAQtRCIlsIf4IB85BLwRxLHHJCWwJaVKopU4Go5znjrKrEX26lU_gP_uV62VOWCZGtGmvfePM1D6CUlbygj3dtEGatlRRjdfykq9ggd04aTSkrOHj_oj9CzlK4IYZxK_hQd8Vq2rRTdMfp9YeKSnXe_nN_ifAl4DTq5wU0u3-Bg8ZfgXXkGXyzRapO1zwnngNchzniTQo5hV6YfnIFpgrSn9Es0y-z8O6zx15DBZ6cnvCrl2sXS9dqPbtQZ8GqrnU8Z9-c_Nh8rKp-jJ1ZPCV7c1RP0ff3pW_-5Ojs_3fSrs8o0lOWqk8KKcaCaWGvYKFsw7SgEEbbjrYTBajsyENDUMLQchLUwCiu1pB2vWyL5CXp_0N0twwyjKRaLMbWLbtbxRgXt1L8T7y7VNlyrTtCWdE0ReH0nEMPPBVJWs0v7C2gPYUmKtbSphegoLVB2gJoYUopg79dQovY5qkOOqmSo_uSoWCG9emjwnvI3uALgB0AqI7-FqK7CEn052v9kbwEsjayL</recordid><startdate>20211229</startdate><enddate>20211229</enddate><creator>Mahmoud, Dina B.</creator><creator>Bakr, Mohamed Mofreh</creator><creator>Al-karmalawy, Ahmed A.</creator><creator>Moatasim, Yassmin</creator><creator>El Taweel, Ahmed</creator><creator>Mostafa, Ahmed</creator><general>Springer International Publishing</general><scope>C6C</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>20211229</creationdate><title>Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19</title><author>Mahmoud, Dina B. ; Bakr, Mohamed Mofreh ; Al-karmalawy, Ahmed A. ; Moatasim, Yassmin ; El Taweel, Ahmed ; Mostafa, Ahmed</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c512t-897f7db1a0ffc2d96ec6d7707f8369ebfafd2e7e54eb63e7ffed7f9a918346093</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>Antiviral Agents</topic><topic>Biochemistry</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Biotechnology</topic><topic>COVID-19</topic><topic>Curcumin</topic><topic>Feasibility Studies</topic><topic>Humans</topic><topic>Micelles</topic><topic>Molecular Docking Simulation</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Research Article</topic><topic>SARS-CoV-2</topic><topic>Surface-Active Agents</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Mahmoud, Dina B.</creatorcontrib><creatorcontrib>Bakr, Mohamed Mofreh</creatorcontrib><creatorcontrib>Al-karmalawy, Ahmed A.</creatorcontrib><creatorcontrib>Moatasim, Yassmin</creatorcontrib><creatorcontrib>El Taweel, Ahmed</creatorcontrib><creatorcontrib>Mostafa, Ahmed</creatorcontrib><collection>Springer Nature OA Free Journals</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>AAPS PharmSciTech</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Mahmoud, Dina B.</au><au>Bakr, Mohamed Mofreh</au><au>Al-karmalawy, Ahmed A.</au><au>Moatasim, Yassmin</au><au>El Taweel, Ahmed</au><au>Mostafa, Ahmed</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19</atitle><jtitle>AAPS PharmSciTech</jtitle><stitle>AAPS PharmSciTech</stitle><addtitle>AAPS PharmSciTech</addtitle><date>2021-12-29</date><risdate>2021</risdate><volume>23</volume><issue>1</issue><spage>44</spage><pages>44-</pages><artnum>44</artnum><issn>1530-9932</issn><eissn>1530-9932</eissn><abstract>Investigating bicelles as an oral drug delivery system and exploiting their structural benefits can pave the way to formulate hydrophobic drugs and potentiate their activity. Herein, the ability of non-ionic surfactants (labrasol
®
, tween 80, cremophore EL and pluronic F127) to form curcumin loaded bicelles with phosphatidylcholine, utilizing a simple method, was investigated. Molecular docking was used to understand the mechanism of bicelles formation. The % transmittance and TEM exhibited bicelles formation with labrasol
®
and tween 80, while cremophor EL and pluronic F127 tended to form mixed micelles. The surfactant-based nanostructures significantly improved curcumin dissolution (99.2 ± 2.6% within 10 min in case of tween 80-based bicelles) compared to liposomes and curcumin suspension in non-sink conditions. The prepared formulations improved curcumin
ex vivo
permeation over liposomes and drug suspension. Further, the therapeutic antiviral activity of the formulated curcumin against SARS-CoV-2 was potentiated over drug suspension. Although both Labrasol
®
and tween 80 bicelles could form bicelles and enhance the oral delivery of curcumin when compared to liposomes and drug suspension, the mixed micelles formulations depicted superiority than bicelles formulations. Our findings provide promising formulations that can be utilized for further preclinical and clinical studies of curcumin as an antiviral therapy for COVID-19 patients.
Graphical Abstract</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><pmid>34966978</pmid><doi>10.1208/s12249-021-02197-2</doi><oa>free_for_read</oa></addata></record> |
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subjects | Antiviral Agents Biochemistry Biomedical and Life Sciences Biomedicine Biotechnology COVID-19 Curcumin Feasibility Studies Humans Micelles Molecular Docking Simulation Pharmacology/Toxicology Pharmacy Research Article SARS-CoV-2 Surface-Active Agents |
title | Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19 |
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