Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin
The main purpose of this study was to prepare binary lipids-based nanostructured lipid carriers to improve the oral bioavailability of silymarin, a poorly water-soluble liver protectant. Silymarin-loaded nanostructured lipid carriers were prepared by the method of high-pressure homogenization with g...
Gespeichert in:
Veröffentlicht in: | Journal of biomaterials applications 2014-02, Vol.28 (6), p.887-896 |
---|---|
Hauptverfasser: | , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
container_end_page | 896 |
---|---|
container_issue | 6 |
container_start_page | 887 |
container_title | Journal of biomaterials applications |
container_volume | 28 |
creator | Shangguan, Mingzhu Lu, Yi Qi, Jianping Han, Jin Tian, Zhiqiang Xie, Yunchang Hu, Fuqiang Yuan, Hailong Wu, Wei |
description | The main purpose of this study was to prepare binary lipids-based nanostructured lipid carriers to improve the oral bioavailability of silymarin, a poorly water-soluble liver protectant. Silymarin-loaded nanostructured lipid carriers were prepared by the method of high-pressure homogenization with glycerol distearates (Precirol ATO-5) and oleic acid as the solid and liquid lipids, respectively, and lecithin (Lipoid E 100) and Tween-80 as the emulsifiers. The silymarin-nanostructured lipid carrier prepared under optimum conditions was spherical in shape with mean particle size of ∼78.87 nm, entrapment efficiency of 87.55%, loading capacity of 8.32%, and zeta potential of −65.3 mV, respectively. In vitro release of silymarin-nanostructured lipid carriers was very limited even after 12 h, while in vitro lipolysis showed fast digestion of nanostructured lipid carriers within 1 h. Relative oral bioavailability of silymarin-nanostructured lipid carriers in Beagle dogs was 2.54- and 3.10-fold that of marketed Legalon® and silymarin solid dispersion pellets, respectively. It was concluded that nanostructured lipid carriers were potential drug delivery systems to improve the bioavailability of silymarin. Other than improved dissolution, alternative mechanisms such as facilitated absorption as well as lymphatic transport may contribute to bioavailability enhancement. |
doi_str_mv | 10.1177/0885328213485141 |
format | Article |
fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_1685827504</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sage_id>10.1177_0885328213485141</sage_id><sourcerecordid>1492621248</sourcerecordid><originalsourceid>FETCH-LOGICAL-c440t-db1339cc43c249582d49973700eb4815fe6871e0d07e9996c16013949e709b543</originalsourceid><addsrcrecordid>eNqNkc1LxDAQxYMoun7cPUmPXqozSdokR138ggUveq5pmkqk26xJu9D_3qyrHgTB0zC83zyG9wg5RbhAFOISpCwYlRQZlwVy3CEzLBjkEijdJbONnG_0A3IY4xsAFIqX--SAcgBZUjUjL9eu12HKOrdyTcxrHW2T9br3cQijGcaQ1k8tMzoEZ0PMWh8yt1wFv06aD7rLauf1WrtO165zw5T5Nouum5Y6uP6Y7LW6i_bkax6R59ubp_l9vni8e5hfLXLDOQx5UyNjyhjODOWqkLThSgkmAGzNJRatLaVACw0Iq5QqDZaATHFlBai64OyInG9902Pvo41DtXTR2K7TvfVjrLCUyVUU8A-UK1pSpFz-BwUhKUNMKGxRE3yMwbbVKrgUwVQhVJu2qt9tpZOzL_exXtrm5-C7ngTkWyDqV1u9-TH0KcO_DT8A58mbFQ</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>1490782311</pqid></control><display><type>article</type><title>Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin</title><source>MEDLINE</source><source>SAGE Complete A-Z List</source><creator>Shangguan, Mingzhu ; Lu, Yi ; Qi, Jianping ; Han, Jin ; Tian, Zhiqiang ; Xie, Yunchang ; Hu, Fuqiang ; Yuan, Hailong ; Wu, Wei</creator><creatorcontrib>Shangguan, Mingzhu ; Lu, Yi ; Qi, Jianping ; Han, Jin ; Tian, Zhiqiang ; Xie, Yunchang ; Hu, Fuqiang ; Yuan, Hailong ; Wu, Wei</creatorcontrib><description>The main purpose of this study was to prepare binary lipids-based nanostructured lipid carriers to improve the oral bioavailability of silymarin, a poorly water-soluble liver protectant. Silymarin-loaded nanostructured lipid carriers were prepared by the method of high-pressure homogenization with glycerol distearates (Precirol ATO-5) and oleic acid as the solid and liquid lipids, respectively, and lecithin (Lipoid E 100) and Tween-80 as the emulsifiers. The silymarin-nanostructured lipid carrier prepared under optimum conditions was spherical in shape with mean particle size of ∼78.87 nm, entrapment efficiency of 87.55%, loading capacity of 8.32%, and zeta potential of −65.3 mV, respectively. In vitro release of silymarin-nanostructured lipid carriers was very limited even after 12 h, while in vitro lipolysis showed fast digestion of nanostructured lipid carriers within 1 h. Relative oral bioavailability of silymarin-nanostructured lipid carriers in Beagle dogs was 2.54- and 3.10-fold that of marketed Legalon® and silymarin solid dispersion pellets, respectively. It was concluded that nanostructured lipid carriers were potential drug delivery systems to improve the bioavailability of silymarin. Other than improved dissolution, alternative mechanisms such as facilitated absorption as well as lymphatic transport may contribute to bioavailability enhancement.</description><identifier>ISSN: 0885-3282</identifier><identifier>EISSN: 1530-8022</identifier><identifier>DOI: 10.1177/0885328213485141</identifier><identifier>PMID: 24008629</identifier><language>eng</language><publisher>London, England: SAGE Publications</publisher><subject>Administration, Oral ; Animals ; Bioavailability ; Biological Availability ; Carriers ; Dogs ; Drug delivery systems ; Homogenizing ; In vitro testing ; Lecithin ; Lipids ; Lipids - chemistry ; Lipolysis ; Microscopy, Electron, Transmission ; Nanostructure ; Nanostructures ; Particle Size ; Silymarin - administration & dosage ; Silymarin - blood ; Silymarin - pharmacokinetics</subject><ispartof>Journal of biomaterials applications, 2014-02, Vol.28 (6), p.887-896</ispartof><rights>The Author(s) 2013 Reprints and permissions: sagepub.co.uk/journalsPermissions.nav</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c440t-db1339cc43c249582d49973700eb4815fe6871e0d07e9996c16013949e709b543</citedby><cites>FETCH-LOGICAL-c440t-db1339cc43c249582d49973700eb4815fe6871e0d07e9996c16013949e709b543</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://journals.sagepub.com/doi/pdf/10.1177/0885328213485141$$EPDF$$P50$$Gsage$$H</linktopdf><linktohtml>$$Uhttps://journals.sagepub.com/doi/10.1177/0885328213485141$$EHTML$$P50$$Gsage$$H</linktohtml><link.rule.ids>314,780,784,21819,27924,27925,43621,43622</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/24008629$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Shangguan, Mingzhu</creatorcontrib><creatorcontrib>Lu, Yi</creatorcontrib><creatorcontrib>Qi, Jianping</creatorcontrib><creatorcontrib>Han, Jin</creatorcontrib><creatorcontrib>Tian, Zhiqiang</creatorcontrib><creatorcontrib>Xie, Yunchang</creatorcontrib><creatorcontrib>Hu, Fuqiang</creatorcontrib><creatorcontrib>Yuan, Hailong</creatorcontrib><creatorcontrib>Wu, Wei</creatorcontrib><title>Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin</title><title>Journal of biomaterials applications</title><addtitle>J Biomater Appl</addtitle><description>The main purpose of this study was to prepare binary lipids-based nanostructured lipid carriers to improve the oral bioavailability of silymarin, a poorly water-soluble liver protectant. Silymarin-loaded nanostructured lipid carriers were prepared by the method of high-pressure homogenization with glycerol distearates (Precirol ATO-5) and oleic acid as the solid and liquid lipids, respectively, and lecithin (Lipoid E 100) and Tween-80 as the emulsifiers. The silymarin-nanostructured lipid carrier prepared under optimum conditions was spherical in shape with mean particle size of ∼78.87 nm, entrapment efficiency of 87.55%, loading capacity of 8.32%, and zeta potential of −65.3 mV, respectively. In vitro release of silymarin-nanostructured lipid carriers was very limited even after 12 h, while in vitro lipolysis showed fast digestion of nanostructured lipid carriers within 1 h. Relative oral bioavailability of silymarin-nanostructured lipid carriers in Beagle dogs was 2.54- and 3.10-fold that of marketed Legalon® and silymarin solid dispersion pellets, respectively. It was concluded that nanostructured lipid carriers were potential drug delivery systems to improve the bioavailability of silymarin. Other than improved dissolution, alternative mechanisms such as facilitated absorption as well as lymphatic transport may contribute to bioavailability enhancement.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Bioavailability</subject><subject>Biological Availability</subject><subject>Carriers</subject><subject>Dogs</subject><subject>Drug delivery systems</subject><subject>Homogenizing</subject><subject>In vitro testing</subject><subject>Lecithin</subject><subject>Lipids</subject><subject>Lipids - chemistry</subject><subject>Lipolysis</subject><subject>Microscopy, Electron, Transmission</subject><subject>Nanostructure</subject><subject>Nanostructures</subject><subject>Particle Size</subject><subject>Silymarin - administration & dosage</subject><subject>Silymarin - blood</subject><subject>Silymarin - pharmacokinetics</subject><issn>0885-3282</issn><issn>1530-8022</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkc1LxDAQxYMoun7cPUmPXqozSdokR138ggUveq5pmkqk26xJu9D_3qyrHgTB0zC83zyG9wg5RbhAFOISpCwYlRQZlwVy3CEzLBjkEijdJbONnG_0A3IY4xsAFIqX--SAcgBZUjUjL9eu12HKOrdyTcxrHW2T9br3cQijGcaQ1k8tMzoEZ0PMWh8yt1wFv06aD7rLauf1WrtO165zw5T5Nouum5Y6uP6Y7LW6i_bkax6R59ubp_l9vni8e5hfLXLDOQx5UyNjyhjODOWqkLThSgkmAGzNJRatLaVACw0Iq5QqDZaATHFlBai64OyInG9902Pvo41DtXTR2K7TvfVjrLCUyVUU8A-UK1pSpFz-BwUhKUNMKGxRE3yMwbbVKrgUwVQhVJu2qt9tpZOzL_exXtrm5-C7ngTkWyDqV1u9-TH0KcO_DT8A58mbFQ</recordid><startdate>20140201</startdate><enddate>20140201</enddate><creator>Shangguan, Mingzhu</creator><creator>Lu, Yi</creator><creator>Qi, Jianping</creator><creator>Han, Jin</creator><creator>Tian, Zhiqiang</creator><creator>Xie, Yunchang</creator><creator>Hu, Fuqiang</creator><creator>Yuan, Hailong</creator><creator>Wu, Wei</creator><general>SAGE Publications</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><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7SR</scope><scope>7TB</scope><scope>7U5</scope><scope>8BQ</scope><scope>F28</scope><scope>JG9</scope><scope>L7M</scope></search><sort><creationdate>20140201</creationdate><title>Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin</title><author>Shangguan, Mingzhu ; Lu, Yi ; Qi, Jianping ; Han, Jin ; Tian, Zhiqiang ; Xie, Yunchang ; Hu, Fuqiang ; Yuan, Hailong ; Wu, Wei</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c440t-db1339cc43c249582d49973700eb4815fe6871e0d07e9996c16013949e709b543</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Bioavailability</topic><topic>Biological Availability</topic><topic>Carriers</topic><topic>Dogs</topic><topic>Drug delivery systems</topic><topic>Homogenizing</topic><topic>In vitro testing</topic><topic>Lecithin</topic><topic>Lipids</topic><topic>Lipids - chemistry</topic><topic>Lipolysis</topic><topic>Microscopy, Electron, Transmission</topic><topic>Nanostructure</topic><topic>Nanostructures</topic><topic>Particle Size</topic><topic>Silymarin - administration & dosage</topic><topic>Silymarin - blood</topic><topic>Silymarin - pharmacokinetics</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shangguan, Mingzhu</creatorcontrib><creatorcontrib>Lu, Yi</creatorcontrib><creatorcontrib>Qi, Jianping</creatorcontrib><creatorcontrib>Han, Jin</creatorcontrib><creatorcontrib>Tian, Zhiqiang</creatorcontrib><creatorcontrib>Xie, Yunchang</creatorcontrib><creatorcontrib>Hu, Fuqiang</creatorcontrib><creatorcontrib>Yuan, Hailong</creatorcontrib><creatorcontrib>Wu, Wei</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><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Engineered Materials Abstracts</collection><collection>Mechanical & Transportation Engineering Abstracts</collection><collection>Solid State and Superconductivity Abstracts</collection><collection>METADEX</collection><collection>ANTE: Abstracts in New Technology & Engineering</collection><collection>Materials Research Database</collection><collection>Advanced Technologies Database with Aerospace</collection><jtitle>Journal of biomaterials applications</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Shangguan, Mingzhu</au><au>Lu, Yi</au><au>Qi, Jianping</au><au>Han, Jin</au><au>Tian, Zhiqiang</au><au>Xie, Yunchang</au><au>Hu, Fuqiang</au><au>Yuan, Hailong</au><au>Wu, Wei</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin</atitle><jtitle>Journal of biomaterials applications</jtitle><addtitle>J Biomater Appl</addtitle><date>2014-02-01</date><risdate>2014</risdate><volume>28</volume><issue>6</issue><spage>887</spage><epage>896</epage><pages>887-896</pages><issn>0885-3282</issn><eissn>1530-8022</eissn><abstract>The main purpose of this study was to prepare binary lipids-based nanostructured lipid carriers to improve the oral bioavailability of silymarin, a poorly water-soluble liver protectant. Silymarin-loaded nanostructured lipid carriers were prepared by the method of high-pressure homogenization with glycerol distearates (Precirol ATO-5) and oleic acid as the solid and liquid lipids, respectively, and lecithin (Lipoid E 100) and Tween-80 as the emulsifiers. The silymarin-nanostructured lipid carrier prepared under optimum conditions was spherical in shape with mean particle size of ∼78.87 nm, entrapment efficiency of 87.55%, loading capacity of 8.32%, and zeta potential of −65.3 mV, respectively. In vitro release of silymarin-nanostructured lipid carriers was very limited even after 12 h, while in vitro lipolysis showed fast digestion of nanostructured lipid carriers within 1 h. Relative oral bioavailability of silymarin-nanostructured lipid carriers in Beagle dogs was 2.54- and 3.10-fold that of marketed Legalon® and silymarin solid dispersion pellets, respectively. It was concluded that nanostructured lipid carriers were potential drug delivery systems to improve the bioavailability of silymarin. Other than improved dissolution, alternative mechanisms such as facilitated absorption as well as lymphatic transport may contribute to bioavailability enhancement.</abstract><cop>London, England</cop><pub>SAGE Publications</pub><pmid>24008629</pmid><doi>10.1177/0885328213485141</doi><tpages>10</tpages></addata></record> |
fulltext | fulltext |
identifier | ISSN: 0885-3282 |
ispartof | Journal of biomaterials applications, 2014-02, Vol.28 (6), p.887-896 |
issn | 0885-3282 1530-8022 |
language | eng |
recordid | cdi_proquest_miscellaneous_1685827504 |
source | MEDLINE; SAGE Complete A-Z List |
subjects | Administration, Oral Animals Bioavailability Biological Availability Carriers Dogs Drug delivery systems Homogenizing In vitro testing Lecithin Lipids Lipids - chemistry Lipolysis Microscopy, Electron, Transmission Nanostructure Nanostructures Particle Size Silymarin - administration & dosage Silymarin - blood Silymarin - pharmacokinetics |
title | Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin |
url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-04T17%3A29%3A48IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Binary%20lipids-based%20nanostructured%20lipid%20carriers%20for%20improved%20oral%20bioavailability%20of%20silymarin&rft.jtitle=Journal%20of%20biomaterials%20applications&rft.au=Shangguan,%20Mingzhu&rft.date=2014-02-01&rft.volume=28&rft.issue=6&rft.spage=887&rft.epage=896&rft.pages=887-896&rft.issn=0885-3282&rft.eissn=1530-8022&rft_id=info:doi/10.1177/0885328213485141&rft_dat=%3Cproquest_cross%3E1492621248%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=1490782311&rft_id=info:pmid/24008629&rft_sage_id=10.1177_0885328213485141&rfr_iscdi=true |