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Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes
[Display omitted] The primary purpose of the present study was to design and optimize a liposomal formulation of the poorly water-soluble drug oleanolic acid (OA) to improve its oral bioavailability, and prolong the duration of therapeutic drug level. Liposomes containing a soybean lecithin and chol...
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Published in: | International journal of pharmaceutics 2017-01, Vol.517 (1-2), p.1-7 |
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The primary purpose of the present study was to design and optimize a liposomal formulation of the poorly water-soluble drug oleanolic acid (OA) to improve its oral bioavailability, and prolong the duration of therapeutic drug level. Liposomes containing a soybean lecithin and cholesterol lipid bilayer, a protective hydrophilic polyvinylpyrrolidone-K30 (PVP-K30) coating, and a protective bile salt, sodium deoxycholate, were prepared by a thin-film dispersion method coupled with sonication. Several properties of the PVP-modified OA liposomes (PVPOALs), including surface morphology, particle size, zeta potential and entrapment efficiency were extensively characterized. The pharmacokinetic parameters of PVPOALs in rats were determined by UPLC–MS/MS following oral administration. The results of the characterization studies demonstrated that PVPOALs were spherical particles with an average particle size of 179.4nm and a zeta potential of −28.8mV. The drug encapsulation efficiency was more than 90%. After freeze-drying, the prepared liposomes possessed high entrapment efficiency of more than 90%. The mean particle size was 194.8nm, and the zeta potential was about −30.9mV. Furthermore, as compared to the commercial tablets, the liposomal formulation enhanced the maximum plasma concentration (Cmax) of OA by 6.90-fold in rat plasma. The relative bioavailability of PVP-modified liposomes was 607.9%. The research work in the paper suggests that PVP-modified liposomes could serve as a practical oral preparation for OA in future cancer therapy. |
doi_str_mv | 10.1016/j.ijpharm.2016.11.056 |
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The primary purpose of the present study was to design and optimize a liposomal formulation of the poorly water-soluble drug oleanolic acid (OA) to improve its oral bioavailability, and prolong the duration of therapeutic drug level. Liposomes containing a soybean lecithin and cholesterol lipid bilayer, a protective hydrophilic polyvinylpyrrolidone-K30 (PVP-K30) coating, and a protective bile salt, sodium deoxycholate, were prepared by a thin-film dispersion method coupled with sonication. Several properties of the PVP-modified OA liposomes (PVPOALs), including surface morphology, particle size, zeta potential and entrapment efficiency were extensively characterized. The pharmacokinetic parameters of PVPOALs in rats were determined by UPLC–MS/MS following oral administration. The results of the characterization studies demonstrated that PVPOALs were spherical particles with an average particle size of 179.4nm and a zeta potential of −28.8mV. The drug encapsulation efficiency was more than 90%. After freeze-drying, the prepared liposomes possessed high entrapment efficiency of more than 90%. The mean particle size was 194.8nm, and the zeta potential was about −30.9mV. Furthermore, as compared to the commercial tablets, the liposomal formulation enhanced the maximum plasma concentration (Cmax) of OA by 6.90-fold in rat plasma. The relative bioavailability of PVP-modified liposomes was 607.9%. The research work in the paper suggests that PVP-modified liposomes could serve as a practical oral preparation for OA in future cancer therapy.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2016.11.056</identifier><identifier>PMID: 27899320</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Administration, Oral ; Animals ; Antineoplastic Agents, Phytogenic - administration & dosage ; Antineoplastic Agents, Phytogenic - blood ; Antineoplastic Agents, Phytogenic - pharmacokinetics ; Bioavailability ; Biological Availability ; Chromatography, High Pressure Liquid ; Drug Carriers - chemistry ; Drug Compounding ; Drug Design ; Drug Stability ; Liposomes ; Male ; Oleanolic acid ; Oleanolic Acid - administration & dosage ; Oleanolic Acid - blood ; Oleanolic Acid - pharmacokinetics ; Particle Size ; Polyvinylpyrrolidone ; Povidone - chemistry ; Rats, Sprague-Dawley ; Sodium deoxycholate ; Solubility ; Surface Properties</subject><ispartof>International journal of pharmaceutics, 2017-01, Vol.517 (1-2), p.1-7</ispartof><rights>2016 Elsevier B.V.</rights><rights>Copyright © 2016 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c431t-5915af7b2a520854ca6f50bea3deabfb89e64898fdecb3bb7ef72fbd8881b63</citedby><cites>FETCH-LOGICAL-c431t-5915af7b2a520854ca6f50bea3deabfb89e64898fdecb3bb7ef72fbd8881b63</cites></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/27899320$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Liu, Yan</creatorcontrib><creatorcontrib>Luo, Xiao</creatorcontrib><creatorcontrib>Xu, Xiaochao</creatorcontrib><creatorcontrib>Gao, Nannan</creatorcontrib><creatorcontrib>Liu, Xiaohong</creatorcontrib><title>Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>[Display omitted]
The primary purpose of the present study was to design and optimize a liposomal formulation of the poorly water-soluble drug oleanolic acid (OA) to improve its oral bioavailability, and prolong the duration of therapeutic drug level. Liposomes containing a soybean lecithin and cholesterol lipid bilayer, a protective hydrophilic polyvinylpyrrolidone-K30 (PVP-K30) coating, and a protective bile salt, sodium deoxycholate, were prepared by a thin-film dispersion method coupled with sonication. Several properties of the PVP-modified OA liposomes (PVPOALs), including surface morphology, particle size, zeta potential and entrapment efficiency were extensively characterized. The pharmacokinetic parameters of PVPOALs in rats were determined by UPLC–MS/MS following oral administration. The results of the characterization studies demonstrated that PVPOALs were spherical particles with an average particle size of 179.4nm and a zeta potential of −28.8mV. The drug encapsulation efficiency was more than 90%. After freeze-drying, the prepared liposomes possessed high entrapment efficiency of more than 90%. The mean particle size was 194.8nm, and the zeta potential was about −30.9mV. Furthermore, as compared to the commercial tablets, the liposomal formulation enhanced the maximum plasma concentration (Cmax) of OA by 6.90-fold in rat plasma. The relative bioavailability of PVP-modified liposomes was 607.9%. The research work in the paper suggests that PVP-modified liposomes could serve as a practical oral preparation for OA in future cancer therapy.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Antineoplastic Agents, Phytogenic - administration & dosage</subject><subject>Antineoplastic Agents, Phytogenic - blood</subject><subject>Antineoplastic Agents, Phytogenic - pharmacokinetics</subject><subject>Bioavailability</subject><subject>Biological Availability</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Compounding</subject><subject>Drug Design</subject><subject>Drug Stability</subject><subject>Liposomes</subject><subject>Male</subject><subject>Oleanolic acid</subject><subject>Oleanolic Acid - administration & dosage</subject><subject>Oleanolic Acid - blood</subject><subject>Oleanolic Acid - pharmacokinetics</subject><subject>Particle Size</subject><subject>Polyvinylpyrrolidone</subject><subject>Povidone - chemistry</subject><subject>Rats, Sprague-Dawley</subject><subject>Sodium deoxycholate</subject><subject>Solubility</subject><subject>Surface Properties</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><recordid>eNqFkE1r3DAQhkVpaDZJf0KLjj3UjmRZtnwqJTQfEOhCS65CHyMyW9tyJO9C8uvjZDe59jTMzPvOyzyEfOGs5Iw355sSN9O9SUNZLW3Jeclk84GsuGpFIeq2-UhWTLSqkLwVx-Qk5w1jrKm4-ESOq1Z1najYityvE0wmmRnj-J265aBxMyR8ep1QM3qKI93hLtLXNOPiPxxhRkfzvPWPNAa6vlsXQ_QYEDyNPZgx9sveOPS0xynmOEA-I0fB9Bk-H-op-XP56-_FdXH7--rm4udt4WrB50J2XJrQ2srIiilZO9MEySwY4cHYYFUHTa06FTw4K6xtIbRVsF4pxW0jTsm3_dUpxYct5FkPmB30vRkhbrPmqpaV5EyxRSr3UpdizgmCnhIOJj1qzvQLYr3RB8T6BbHmXC-IF9_XQ8TWDuDfXW9MF8GPvQCWN3cISWeHMDrwmMDN2kf8T8QzPu2Sug</recordid><startdate>20170130</startdate><enddate>20170130</enddate><creator>Liu, Yan</creator><creator>Luo, Xiao</creator><creator>Xu, Xiaochao</creator><creator>Gao, Nannan</creator><creator>Liu, Xiaohong</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><scope>7X8</scope></search><sort><creationdate>20170130</creationdate><title>Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes</title><author>Liu, Yan ; Luo, Xiao ; Xu, Xiaochao ; Gao, Nannan ; Liu, Xiaohong</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c431t-5915af7b2a520854ca6f50bea3deabfb89e64898fdecb3bb7ef72fbd8881b63</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Antineoplastic Agents, Phytogenic - administration & dosage</topic><topic>Antineoplastic Agents, Phytogenic - blood</topic><topic>Antineoplastic Agents, Phytogenic - pharmacokinetics</topic><topic>Bioavailability</topic><topic>Biological Availability</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Compounding</topic><topic>Drug Design</topic><topic>Drug Stability</topic><topic>Liposomes</topic><topic>Male</topic><topic>Oleanolic acid</topic><topic>Oleanolic Acid - administration & dosage</topic><topic>Oleanolic Acid - blood</topic><topic>Oleanolic Acid - pharmacokinetics</topic><topic>Particle Size</topic><topic>Polyvinylpyrrolidone</topic><topic>Povidone - chemistry</topic><topic>Rats, Sprague-Dawley</topic><topic>Sodium deoxycholate</topic><topic>Solubility</topic><topic>Surface Properties</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Liu, Yan</creatorcontrib><creatorcontrib>Luo, Xiao</creatorcontrib><creatorcontrib>Xu, Xiaochao</creatorcontrib><creatorcontrib>Gao, Nannan</creatorcontrib><creatorcontrib>Liu, Xiaohong</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>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Liu, Yan</au><au>Luo, Xiao</au><au>Xu, Xiaochao</au><au>Gao, Nannan</au><au>Liu, Xiaohong</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2017-01-30</date><risdate>2017</risdate><volume>517</volume><issue>1-2</issue><spage>1</spage><epage>7</epage><pages>1-7</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>[Display omitted]
The primary purpose of the present study was to design and optimize a liposomal formulation of the poorly water-soluble drug oleanolic acid (OA) to improve its oral bioavailability, and prolong the duration of therapeutic drug level. Liposomes containing a soybean lecithin and cholesterol lipid bilayer, a protective hydrophilic polyvinylpyrrolidone-K30 (PVP-K30) coating, and a protective bile salt, sodium deoxycholate, were prepared by a thin-film dispersion method coupled with sonication. Several properties of the PVP-modified OA liposomes (PVPOALs), including surface morphology, particle size, zeta potential and entrapment efficiency were extensively characterized. The pharmacokinetic parameters of PVPOALs in rats were determined by UPLC–MS/MS following oral administration. The results of the characterization studies demonstrated that PVPOALs were spherical particles with an average particle size of 179.4nm and a zeta potential of −28.8mV. The drug encapsulation efficiency was more than 90%. After freeze-drying, the prepared liposomes possessed high entrapment efficiency of more than 90%. The mean particle size was 194.8nm, and the zeta potential was about −30.9mV. Furthermore, as compared to the commercial tablets, the liposomal formulation enhanced the maximum plasma concentration (Cmax) of OA by 6.90-fold in rat plasma. The relative bioavailability of PVP-modified liposomes was 607.9%. The research work in the paper suggests that PVP-modified liposomes could serve as a practical oral preparation for OA in future cancer therapy.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>27899320</pmid><doi>10.1016/j.ijpharm.2016.11.056</doi><tpages>7</tpages></addata></record> |
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subjects | Administration, Oral Animals Antineoplastic Agents, Phytogenic - administration & dosage Antineoplastic Agents, Phytogenic - blood Antineoplastic Agents, Phytogenic - pharmacokinetics Bioavailability Biological Availability Chromatography, High Pressure Liquid Drug Carriers - chemistry Drug Compounding Drug Design Drug Stability Liposomes Male Oleanolic acid Oleanolic Acid - administration & dosage Oleanolic Acid - blood Oleanolic Acid - pharmacokinetics Particle Size Polyvinylpyrrolidone Povidone - chemistry Rats, Sprague-Dawley Sodium deoxycholate Solubility Surface Properties |
title | Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes |
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