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Lipid nanoconstructs for superior hepatoprotection: In vitro assessments as predictive tool for in vivo translation
[Display omitted] To investigate comparative in vitro and in vivo performance of lipid vesicular and particulate systems in escalating oral bioavailability for superior hepatoprotection. Systems were fabricated using easy to scale up process and novel excipients to deliver Silibinin. In vitro charac...
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| Published in: | International journal of pharmaceutics 2020-04, Vol.579, p.119176, Article 119176 |
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| Main Authors: | , , , , , , , |
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| cited_by | cdi_FETCH-LOGICAL-c365t-35089b1b4de2250f9bd3aa80216ea6bab623c06df628345935d21fbea2ae1f783 |
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| cites | cdi_FETCH-LOGICAL-c365t-35089b1b4de2250f9bd3aa80216ea6bab623c06df628345935d21fbea2ae1f783 |
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| container_start_page | 119176 |
| container_title | International journal of pharmaceutics |
| container_volume | 579 |
| creator | Dhawan, V. Sutariya, B. Lokras, A. Thamm, J. Saraf, M. Warawdekar, U. Fahr, A. Nagarsenker, M. |
| description | [Display omitted]
To investigate comparative in vitro and in vivo performance of lipid vesicular and particulate systems in escalating oral bioavailability for superior hepatoprotection.
Systems were fabricated using easy to scale up process and novel excipients to deliver Silibinin. In vitro characterization followed by pharmacokinetic and pharmacodynamic evaluation in rats was conducted to establish a correlation.
Nanoformulations resulted in 20 fold increase in solubilisation and significant increase in permeation. 2.5 fold increase in bioavailability was evident in vivo. Vesicles demonstrated greatest hepatoprotective potential in efficacy study.
The findings establish a link between in vitro and in vivo performance to rank order lipid nanoartchitects. Concurrently, a significant potential in therapeutic intervention of hepatotoxicity is envisaged as elucidated. |
| doi_str_mv | 10.1016/j.ijpharm.2020.119176 |
| format | article |
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To investigate comparative in vitro and in vivo performance of lipid vesicular and particulate systems in escalating oral bioavailability for superior hepatoprotection.
Systems were fabricated using easy to scale up process and novel excipients to deliver Silibinin. In vitro characterization followed by pharmacokinetic and pharmacodynamic evaluation in rats was conducted to establish a correlation.
Nanoformulations resulted in 20 fold increase in solubilisation and significant increase in permeation. 2.5 fold increase in bioavailability was evident in vivo. Vesicles demonstrated greatest hepatoprotective potential in efficacy study.
The findings establish a link between in vitro and in vivo performance to rank order lipid nanoartchitects. Concurrently, a significant potential in therapeutic intervention of hepatotoxicity is envisaged as elucidated.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2020.119176</identifier><identifier>PMID: 32119898</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Administration, Oral ; Animals ; Biological Availability ; Carbon Tetrachloride ; Chemical and Drug Induced Liver Injury - prevention & control ; Drug Liberation ; Drug Stability ; Excipients - chemistry ; Female ; GeluPearl ; Hepatoprotection ; In Vitro Techniques ; LeciPlex ; Lipid nanosystems ; Lipids - chemistry ; Liver ; Liver - enzymology ; Nanotechnology - methods ; Oral bioavailability ; Particle Size ; Permeability ; Rats ; Silibinin ; Silybin - blood ; Silybin - chemistry ; Silybin - pharmacokinetics ; Silybin - pharmacology ; Solubility ; Surface Properties</subject><ispartof>International journal of pharmaceutics, 2020-04, Vol.579, p.119176, Article 119176</ispartof><rights>2020 Elsevier B.V.</rights><rights>Copyright © 2020 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c365t-35089b1b4de2250f9bd3aa80216ea6bab623c06df628345935d21fbea2ae1f783</citedby><cites>FETCH-LOGICAL-c365t-35089b1b4de2250f9bd3aa80216ea6bab623c06df628345935d21fbea2ae1f783</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27923,27924</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/32119898$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Dhawan, V.</creatorcontrib><creatorcontrib>Sutariya, B.</creatorcontrib><creatorcontrib>Lokras, A.</creatorcontrib><creatorcontrib>Thamm, J.</creatorcontrib><creatorcontrib>Saraf, M.</creatorcontrib><creatorcontrib>Warawdekar, U.</creatorcontrib><creatorcontrib>Fahr, A.</creatorcontrib><creatorcontrib>Nagarsenker, M.</creatorcontrib><title>Lipid nanoconstructs for superior hepatoprotection: In vitro assessments as predictive tool for in vivo translation</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>[Display omitted]
To investigate comparative in vitro and in vivo performance of lipid vesicular and particulate systems in escalating oral bioavailability for superior hepatoprotection.
Systems were fabricated using easy to scale up process and novel excipients to deliver Silibinin. In vitro characterization followed by pharmacokinetic and pharmacodynamic evaluation in rats was conducted to establish a correlation.
Nanoformulations resulted in 20 fold increase in solubilisation and significant increase in permeation. 2.5 fold increase in bioavailability was evident in vivo. Vesicles demonstrated greatest hepatoprotective potential in efficacy study.
The findings establish a link between in vitro and in vivo performance to rank order lipid nanoartchitects. Concurrently, a significant potential in therapeutic intervention of hepatotoxicity is envisaged as elucidated.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Biological Availability</subject><subject>Carbon Tetrachloride</subject><subject>Chemical and Drug Induced Liver Injury - prevention & control</subject><subject>Drug Liberation</subject><subject>Drug Stability</subject><subject>Excipients - chemistry</subject><subject>Female</subject><subject>GeluPearl</subject><subject>Hepatoprotection</subject><subject>In Vitro Techniques</subject><subject>LeciPlex</subject><subject>Lipid nanosystems</subject><subject>Lipids - chemistry</subject><subject>Liver</subject><subject>Liver - enzymology</subject><subject>Nanotechnology - methods</subject><subject>Oral bioavailability</subject><subject>Particle Size</subject><subject>Permeability</subject><subject>Rats</subject><subject>Silibinin</subject><subject>Silybin - blood</subject><subject>Silybin - chemistry</subject><subject>Silybin - pharmacokinetics</subject><subject>Silybin - pharmacology</subject><subject>Solubility</subject><subject>Surface Properties</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><recordid>eNqFkF1LwzAUhoMobk5_gpI_0JmPNW29ERl-DAbe6HVIk1OWsjYlyQr-e1M3vfUqh_C870kehG4pWVJCxX27tO2wU75bMsLSHa1oIc7QnJYFz_iqEOdoTnhRZjkt-AxdhdASQgSj_BLNOEt8WZVzFLZ2sAb3qnfa9SH6g44BN87jcBjA2zTsYFDRDd5F0NG6_gFvejza6B1WIUAIHfQpowIePBibmBFwdG7_U2MndnQ4etWHvZoKrtFFo_YBbk7nAn2-PH-s37Lt--tm_bTNNBd5zHhOyqqm9coAYzlpqtpwpUrCqAAlalULxjURphGs5Ku84rlhtKlBMQW0KUq-QPmxV3sXgodGDt52yn9JSuQkUbbyJFFOEuVRYsrdHXPDoe7A_KV-rSXg8QhAev1owcugLfQ6_d4nR9I4-8-Kb7oQiUE</recordid><startdate>20200415</startdate><enddate>20200415</enddate><creator>Dhawan, V.</creator><creator>Sutariya, B.</creator><creator>Lokras, A.</creator><creator>Thamm, J.</creator><creator>Saraf, M.</creator><creator>Warawdekar, U.</creator><creator>Fahr, A.</creator><creator>Nagarsenker, M.</creator><general>Elsevier B.V</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></search><sort><creationdate>20200415</creationdate><title>Lipid nanoconstructs for superior hepatoprotection: In vitro assessments as predictive tool for in vivo translation</title><author>Dhawan, V. ; 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To investigate comparative in vitro and in vivo performance of lipid vesicular and particulate systems in escalating oral bioavailability for superior hepatoprotection.
Systems were fabricated using easy to scale up process and novel excipients to deliver Silibinin. In vitro characterization followed by pharmacokinetic and pharmacodynamic evaluation in rats was conducted to establish a correlation.
Nanoformulations resulted in 20 fold increase in solubilisation and significant increase in permeation. 2.5 fold increase in bioavailability was evident in vivo. Vesicles demonstrated greatest hepatoprotective potential in efficacy study.
The findings establish a link between in vitro and in vivo performance to rank order lipid nanoartchitects. Concurrently, a significant potential in therapeutic intervention of hepatotoxicity is envisaged as elucidated.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>32119898</pmid><doi>10.1016/j.ijpharm.2020.119176</doi></addata></record> |
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| ispartof | International journal of pharmaceutics, 2020-04, Vol.579, p.119176, Article 119176 |
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| source | ScienceDirect Freedom Collection |
| subjects | Administration, Oral Animals Biological Availability Carbon Tetrachloride Chemical and Drug Induced Liver Injury - prevention & control Drug Liberation Drug Stability Excipients - chemistry Female GeluPearl Hepatoprotection In Vitro Techniques LeciPlex Lipid nanosystems Lipids - chemistry Liver Liver - enzymology Nanotechnology - methods Oral bioavailability Particle Size Permeability Rats Silibinin Silybin - blood Silybin - chemistry Silybin - pharmacokinetics Silybin - pharmacology Solubility Surface Properties |
| title | Lipid nanoconstructs for superior hepatoprotection: In vitro assessments as predictive tool for in vivo translation |
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