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Telmisartan loaded lipid nanocarrier as a potential repurposing approach to treat glioma: characterization, apoptosis evaluation in U87MG cells, pharmacokinetic and molecular simulation study
The study explores anticancer potential of telmisartan (TS) loaded lipid nanocarriers (TLNs) in glioma cells as a potential repurposing nanomodality along with estimation of drug availability at rat brain. Experimental TLNs were produced by previously reported method and characterized. anticancer ef...
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| Published in: | Nanotechnology 2024-10, Vol.35 (42), p.425101 |
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| Language: | English |
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| container_issue | 42 |
| container_start_page | 425101 |
| container_title | Nanotechnology |
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| creator | Rout, Sagar Satapathy, Bhabani Sankar Sahoo, Rudra Narayan Pattnaik, Snigdha |
| description | The study explores anticancer potential of telmisartan (TS) loaded lipid nanocarriers (TLNs) in glioma cells as a potential repurposing nanomodality along with estimation of drug availability at rat brain. Experimental TLNs were produced by previously reported method and characterized.
anticancer efficacy of experimental TLNs was estimated by MTT, confocal microscopy, and FACs analysis in glioma cells. Plasma and brain pharmacokinetic (PK) parameters were also analysed by LCMS/MS. Spherical, nanosized, homogenous, unilamellar, TLNs were reported having desirable drug loading (9.5% ± 0.6%), negative zeta potential and sustained TS release tendency. FITC-TLNs were sufficiently internalized into U87MG cells line within 0.5 h incubation period. IC
for TLNs was considerably higher than free TS in the tested glioma cell lines. Further, TLNs induced superior apoptotic effect in U87MG cells than TS. PK (plasma/brain) data depicted higher AUC,
, MRT with lower Cl
for TLNs suggesting improved bioavailability,
residence and sustained drug availability than free TS administration. Docking studies rationalized
results as preferably higher binding affinity (docking score:12.4) was detected for TS with glioma proteins. Further,
studies in glioma bearing xenograft model is underway for futuristic clinical validation of TLNs. |
| doi_str_mv | 10.1088/1361-6528/ad64e0 |
| format | article |
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anticancer efficacy of experimental TLNs was estimated by MTT, confocal microscopy, and FACs analysis in glioma cells. Plasma and brain pharmacokinetic (PK) parameters were also analysed by LCMS/MS. Spherical, nanosized, homogenous, unilamellar, TLNs were reported having desirable drug loading (9.5% ± 0.6%), negative zeta potential and sustained TS release tendency. FITC-TLNs were sufficiently internalized into U87MG cells line within 0.5 h incubation period. IC
for TLNs was considerably higher than free TS in the tested glioma cell lines. Further, TLNs induced superior apoptotic effect in U87MG cells than TS. PK (plasma/brain) data depicted higher AUC,
, MRT with lower Cl
for TLNs suggesting improved bioavailability,
residence and sustained drug availability than free TS administration. Docking studies rationalized
results as preferably higher binding affinity (docking score:12.4) was detected for TS with glioma proteins. Further,
studies in glioma bearing xenograft model is underway for futuristic clinical validation of TLNs.</description><identifier>ISSN: 0957-4484</identifier><identifier>ISSN: 1361-6528</identifier><identifier>EISSN: 1361-6528</identifier><identifier>DOI: 10.1088/1361-6528/ad64e0</identifier><identifier>PMID: 39025086</identifier><identifier>CODEN: NNOTER</identifier><language>eng</language><publisher>England: IOP Publishing</publisher><subject>Animals ; Antineoplastic Agents - administration & dosage ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacokinetics ; Antineoplastic Agents - pharmacology ; apoptosis ; Apoptosis - drug effects ; Brain Neoplasms - drug therapy ; Brain Neoplasms - metabolism ; Brain Neoplasms - pathology ; Cell Line, Tumor ; Drug Carriers - chemistry ; Drug Carriers - pharmacokinetics ; Drug Liberation ; Drug Repositioning ; Glioma - drug therapy ; Glioma - metabolism ; Glioma - pathology ; Humans ; lipid nanocarriers ; Lipids - chemistry ; Male ; Molecular Docking Simulation ; Nanoparticles - chemistry ; pharmacokinetics ; Rats ; telmisartan ; Telmisartan - administration & dosage ; Telmisartan - chemistry ; Telmisartan - pharmacokinetics ; Telmisartan - pharmacology ; U87MG cells</subject><ispartof>Nanotechnology, 2024-10, Vol.35 (42), p.425101</ispartof><rights>2024 IOP Publishing Ltd</rights><rights>2024 IOP Publishing Ltd.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c253t-310ed112d6d55e8f4d20dfcc0f0d88173fc9800d364a9e55d38181e7f0db7b943</cites><orcidid>0000-0002-9175-8356</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/39025086$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Rout, Sagar</creatorcontrib><creatorcontrib>Satapathy, Bhabani Sankar</creatorcontrib><creatorcontrib>Sahoo, Rudra Narayan</creatorcontrib><creatorcontrib>Pattnaik, Snigdha</creatorcontrib><title>Telmisartan loaded lipid nanocarrier as a potential repurposing approach to treat glioma: characterization, apoptosis evaluation in U87MG cells, pharmacokinetic and molecular simulation study</title><title>Nanotechnology</title><addtitle>Nano</addtitle><addtitle>Nanotechnology</addtitle><description>The study explores anticancer potential of telmisartan (TS) loaded lipid nanocarriers (TLNs) in glioma cells as a potential repurposing nanomodality along with estimation of drug availability at rat brain. Experimental TLNs were produced by previously reported method and characterized.
anticancer efficacy of experimental TLNs was estimated by MTT, confocal microscopy, and FACs analysis in glioma cells. Plasma and brain pharmacokinetic (PK) parameters were also analysed by LCMS/MS. Spherical, nanosized, homogenous, unilamellar, TLNs were reported having desirable drug loading (9.5% ± 0.6%), negative zeta potential and sustained TS release tendency. FITC-TLNs were sufficiently internalized into U87MG cells line within 0.5 h incubation period. IC
for TLNs was considerably higher than free TS in the tested glioma cell lines. Further, TLNs induced superior apoptotic effect in U87MG cells than TS. PK (plasma/brain) data depicted higher AUC,
, MRT with lower Cl
for TLNs suggesting improved bioavailability,
residence and sustained drug availability than free TS administration. Docking studies rationalized
results as preferably higher binding affinity (docking score:12.4) was detected for TS with glioma proteins. Further,
studies in glioma bearing xenograft model is underway for futuristic clinical validation of TLNs.</description><subject>Animals</subject><subject>Antineoplastic Agents - administration & dosage</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacokinetics</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>apoptosis</subject><subject>Apoptosis - drug effects</subject><subject>Brain Neoplasms - drug therapy</subject><subject>Brain Neoplasms - metabolism</subject><subject>Brain Neoplasms - pathology</subject><subject>Cell Line, Tumor</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Carriers - pharmacokinetics</subject><subject>Drug Liberation</subject><subject>Drug Repositioning</subject><subject>Glioma - drug therapy</subject><subject>Glioma - metabolism</subject><subject>Glioma - pathology</subject><subject>Humans</subject><subject>lipid nanocarriers</subject><subject>Lipids - chemistry</subject><subject>Male</subject><subject>Molecular Docking Simulation</subject><subject>Nanoparticles - chemistry</subject><subject>pharmacokinetics</subject><subject>Rats</subject><subject>telmisartan</subject><subject>Telmisartan - administration & dosage</subject><subject>Telmisartan - chemistry</subject><subject>Telmisartan - pharmacokinetics</subject><subject>Telmisartan - pharmacology</subject><subject>U87MG cells</subject><issn>0957-4484</issn><issn>1361-6528</issn><issn>1361-6528</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><recordid>eNp9kUFrFTEQxxdR7LN69yQ5Kry1yWazm-etFK1CxUt7DvOS2TY1m8QkK9Qv51cz21d7EiEwMPn9h0x-TfOa0feMSnnC-MDaQXTyBMzQI33SbB5bT5sN3Ymx7XvZHzUvcr6llDHZsefNEd_RTlA5bJrfl-hmmyEV8MQFMGiIs9Ea4sEHDSlZTAQyARJDQV8sOJIwLimGbP01gRhTAH1DSiAlIRRy7WyY4QPRN5BAF0z2FxQb_LayIZYaywR_glvuu8R6ciXHr-dEo3N5S2KNzaDDd-uxWE3AGzIHh3pxkEi2c633wVwWc_eyeTaBy_jqoR43V58-Xp59bi--nX85O71odSd4aTmjaBjrzGCEQDn1pqNm0ppO1EjJRj7pnaTU8KGHHQphuGSS4Viv9-N-1_Pj5u1hbt32x4K5qPpr64vBY1iy4lR2Qzf2gleUHlCdQs4JJxWTnSHdKUbVqk2tjtTqSB201cibh-nLfkbzGPjrqQLbA2BDVLdhSb4u-7957_6Br0YVF6rv6hGMMhXNxP8AYjO0TA</recordid><startdate>20241014</startdate><enddate>20241014</enddate><creator>Rout, Sagar</creator><creator>Satapathy, Bhabani Sankar</creator><creator>Sahoo, Rudra Narayan</creator><creator>Pattnaik, Snigdha</creator><general>IOP Publishing</general><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><orcidid>https://orcid.org/0000-0002-9175-8356</orcidid></search><sort><creationdate>20241014</creationdate><title>Telmisartan loaded lipid nanocarrier as a potential repurposing approach to treat glioma: characterization, apoptosis evaluation in U87MG cells, pharmacokinetic and molecular simulation study</title><author>Rout, Sagar ; Satapathy, Bhabani Sankar ; Sahoo, Rudra Narayan ; Pattnaik, Snigdha</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c253t-310ed112d6d55e8f4d20dfcc0f0d88173fc9800d364a9e55d38181e7f0db7b943</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Animals</topic><topic>Antineoplastic Agents - administration & dosage</topic><topic>Antineoplastic Agents - chemistry</topic><topic>Antineoplastic Agents - pharmacokinetics</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>apoptosis</topic><topic>Apoptosis - drug effects</topic><topic>Brain Neoplasms - drug therapy</topic><topic>Brain Neoplasms - metabolism</topic><topic>Brain Neoplasms - pathology</topic><topic>Cell Line, Tumor</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Carriers - pharmacokinetics</topic><topic>Drug Liberation</topic><topic>Drug Repositioning</topic><topic>Glioma - drug therapy</topic><topic>Glioma - metabolism</topic><topic>Glioma - pathology</topic><topic>Humans</topic><topic>lipid nanocarriers</topic><topic>Lipids - chemistry</topic><topic>Male</topic><topic>Molecular Docking Simulation</topic><topic>Nanoparticles - chemistry</topic><topic>pharmacokinetics</topic><topic>Rats</topic><topic>telmisartan</topic><topic>Telmisartan - administration & dosage</topic><topic>Telmisartan - chemistry</topic><topic>Telmisartan - pharmacokinetics</topic><topic>Telmisartan - pharmacology</topic><topic>U87MG cells</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Rout, Sagar</creatorcontrib><creatorcontrib>Satapathy, Bhabani Sankar</creatorcontrib><creatorcontrib>Sahoo, Rudra Narayan</creatorcontrib><creatorcontrib>Pattnaik, Snigdha</creatorcontrib><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><jtitle>Nanotechnology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Rout, Sagar</au><au>Satapathy, Bhabani Sankar</au><au>Sahoo, Rudra Narayan</au><au>Pattnaik, Snigdha</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Telmisartan loaded lipid nanocarrier as a potential repurposing approach to treat glioma: characterization, apoptosis evaluation in U87MG cells, pharmacokinetic and molecular simulation study</atitle><jtitle>Nanotechnology</jtitle><stitle>Nano</stitle><addtitle>Nanotechnology</addtitle><date>2024-10-14</date><risdate>2024</risdate><volume>35</volume><issue>42</issue><spage>425101</spage><pages>425101-</pages><issn>0957-4484</issn><issn>1361-6528</issn><eissn>1361-6528</eissn><coden>NNOTER</coden><abstract>The study explores anticancer potential of telmisartan (TS) loaded lipid nanocarriers (TLNs) in glioma cells as a potential repurposing nanomodality along with estimation of drug availability at rat brain. Experimental TLNs were produced by previously reported method and characterized.
anticancer efficacy of experimental TLNs was estimated by MTT, confocal microscopy, and FACs analysis in glioma cells. Plasma and brain pharmacokinetic (PK) parameters were also analysed by LCMS/MS. Spherical, nanosized, homogenous, unilamellar, TLNs were reported having desirable drug loading (9.5% ± 0.6%), negative zeta potential and sustained TS release tendency. FITC-TLNs were sufficiently internalized into U87MG cells line within 0.5 h incubation period. IC
for TLNs was considerably higher than free TS in the tested glioma cell lines. Further, TLNs induced superior apoptotic effect in U87MG cells than TS. PK (plasma/brain) data depicted higher AUC,
, MRT with lower Cl
for TLNs suggesting improved bioavailability,
residence and sustained drug availability than free TS administration. Docking studies rationalized
results as preferably higher binding affinity (docking score:12.4) was detected for TS with glioma proteins. Further,
studies in glioma bearing xenograft model is underway for futuristic clinical validation of TLNs.</abstract><cop>England</cop><pub>IOP Publishing</pub><pmid>39025086</pmid><doi>10.1088/1361-6528/ad64e0</doi><tpages>17</tpages><orcidid>https://orcid.org/0000-0002-9175-8356</orcidid></addata></record> |
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| ispartof | Nanotechnology, 2024-10, Vol.35 (42), p.425101 |
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| source | Institute of Physics:Jisc Collections:IOP Publishing Read and Publish 2024-2025 (Reading List) |
| subjects | Animals Antineoplastic Agents - administration & dosage Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - pharmacology apoptosis Apoptosis - drug effects Brain Neoplasms - drug therapy Brain Neoplasms - metabolism Brain Neoplasms - pathology Cell Line, Tumor Drug Carriers - chemistry Drug Carriers - pharmacokinetics Drug Liberation Drug Repositioning Glioma - drug therapy Glioma - metabolism Glioma - pathology Humans lipid nanocarriers Lipids - chemistry Male Molecular Docking Simulation Nanoparticles - chemistry pharmacokinetics Rats telmisartan Telmisartan - administration & dosage Telmisartan - chemistry Telmisartan - pharmacokinetics Telmisartan - pharmacology U87MG cells |
| title | Telmisartan loaded lipid nanocarrier as a potential repurposing approach to treat glioma: characterization, apoptosis evaluation in U87MG cells, pharmacokinetic and molecular simulation study |
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