Design and evaluation of oral nanoemulsion drug delivery system of mebudipine
A nanoemulsion drug delivery system was developed to increase the oral bioavailability of mebudipine as a calcium channel blocker with very low bioavailability profile. The impact of nano-formulation on the pharmacokinetic parameters of mebudipine in rats was investigated. Nanoemulsion formulations...
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Veröffentlicht in: | Drug delivery 2016-07, Vol.23 (6), p.2035-2043 |
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creator | Khani, Samira Keyhanfar, Fariborz Amani, Amir |
description | A nanoemulsion drug delivery system was developed to increase the oral bioavailability of mebudipine as a calcium channel blocker with very low bioavailability profile. The impact of nano-formulation on the pharmacokinetic parameters of mebudipine in rats was investigated. Nanoemulsion formulations containing ethyl oleate, Tween 80, Span 80, polyethylene glycol 400, ethanol and deionized water were prepared using probe sonicator. The optimum formulation was evaluated for physicochemical properties, such as particle size, morphology and stability. The particle size of optimum formulation was 22.8 ± 4.0 nm. Based on the results of this study, the relative bioavailability of mebudipine nanoemulsion was enhanced by about 2.6-, 2.0- and 1.9-fold, respectively, compared with suspension, ethyl oleate solution and micellar solution. In conclusion, nanoemulsion is an interesting option for the delivery of poorly water soluble molecules, such as mebudipine. |
doi_str_mv | 10.3109/10717544.2015.1088597 |
format | Article |
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The impact of nano-formulation on the pharmacokinetic parameters of mebudipine in rats was investigated. Nanoemulsion formulations containing ethyl oleate, Tween 80, Span 80, polyethylene glycol 400, ethanol and deionized water were prepared using probe sonicator. The optimum formulation was evaluated for physicochemical properties, such as particle size, morphology and stability. The particle size of optimum formulation was 22.8 ± 4.0 nm. Based on the results of this study, the relative bioavailability of mebudipine nanoemulsion was enhanced by about 2.6-, 2.0- and 1.9-fold, respectively, compared with suspension, ethyl oleate solution and micellar solution. In conclusion, nanoemulsion is an interesting option for the delivery of poorly water soluble molecules, such as mebudipine.</description><identifier>ISSN: 1071-7544</identifier><identifier>EISSN: 1521-0464</identifier><identifier>DOI: 10.3109/10717544.2015.1088597</identifier><identifier>PMID: 26406153</identifier><language>eng</language><publisher>England: Taylor & Francis</publisher><subject>Administration, Oral ; Animals ; Bioavailability ; Biological Availability ; Calcium Channel Blockers - administration & dosage ; Calcium Channel Blockers - chemistry ; Calcium Channel Blockers - pharmacokinetics ; Chemistry, Pharmaceutical ; Drug Carriers - chemistry ; Drug Delivery Systems ; Drug Stability ; Emulsions - chemistry ; mebudipine ; nanoemulsion ; Nanoparticles - chemistry ; Nifedipine - administration & dosage ; Nifedipine - analogs & derivatives ; Nifedipine - chemistry ; Nifedipine - pharmacokinetics ; Polysorbates - chemistry ; Polysorbates - metabolism ; Rats ; Solubility ; Solutions</subject><ispartof>Drug delivery, 2016-07, Vol.23 (6), p.2035-2043</ispartof><rights>2015 Informa UK Limited, trading as Taylor & Francis Group. 2015</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c432t-80e4a7cbd1690beb91fe4c8e738e5124735e014cc5f3e20433aa01470df168f3</citedby><cites>FETCH-LOGICAL-c432t-80e4a7cbd1690beb91fe4c8e738e5124735e014cc5f3e20433aa01470df168f3</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/26406153$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Khani, Samira</creatorcontrib><creatorcontrib>Keyhanfar, Fariborz</creatorcontrib><creatorcontrib>Amani, Amir</creatorcontrib><title>Design and evaluation of oral nanoemulsion drug delivery system of mebudipine</title><title>Drug delivery</title><addtitle>Drug Deliv</addtitle><description>A nanoemulsion drug delivery system was developed to increase the oral bioavailability of mebudipine as a calcium channel blocker with very low bioavailability profile. The impact of nano-formulation on the pharmacokinetic parameters of mebudipine in rats was investigated. Nanoemulsion formulations containing ethyl oleate, Tween 80, Span 80, polyethylene glycol 400, ethanol and deionized water were prepared using probe sonicator. The optimum formulation was evaluated for physicochemical properties, such as particle size, morphology and stability. The particle size of optimum formulation was 22.8 ± 4.0 nm. Based on the results of this study, the relative bioavailability of mebudipine nanoemulsion was enhanced by about 2.6-, 2.0- and 1.9-fold, respectively, compared with suspension, ethyl oleate solution and micellar solution. In conclusion, nanoemulsion is an interesting option for the delivery of poorly water soluble molecules, such as mebudipine.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Bioavailability</subject><subject>Biological Availability</subject><subject>Calcium Channel Blockers - administration & dosage</subject><subject>Calcium Channel Blockers - chemistry</subject><subject>Calcium Channel Blockers - pharmacokinetics</subject><subject>Chemistry, Pharmaceutical</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Delivery Systems</subject><subject>Drug Stability</subject><subject>Emulsions - chemistry</subject><subject>mebudipine</subject><subject>nanoemulsion</subject><subject>Nanoparticles - chemistry</subject><subject>Nifedipine - administration & dosage</subject><subject>Nifedipine - analogs & derivatives</subject><subject>Nifedipine - chemistry</subject><subject>Nifedipine - pharmacokinetics</subject><subject>Polysorbates - chemistry</subject><subject>Polysorbates - metabolism</subject><subject>Rats</subject><subject>Solubility</subject><subject>Solutions</subject><issn>1071-7544</issn><issn>1521-0464</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1P3DAQhi1UBMvCT6DKsZdsZ2I7H7dWSwuVFnHhbjnJGBk59tZOqPbfk2gXjj3Nh56ZV3oYu0XYcITmO0KFlRRiUwDKDUJdy6Y6YyuUBeYgSvFl7mcmX6BLdpXSKwDUWMgLdlmUAkqUfMUe7yjZF59p32f0pt2kRxt8FkwWonaZ1z7QMLm0LPs4vWQ9OftG8ZClQxppWMiB2qm3e-vpmp0b7RLdnOqaPf_-9bx9yHdP93-2P3d5J3gx5jWQ0FXX9lg20FLboCHR1VTxmiQWouKSAEXXScOpAMG51vNcQW-wrA1fs2_Ht_sY_k6URjXY1JFz2lOYksKqASgQG5xReUS7GFKKZNQ-2kHHg0JQi0j1IVItItVJ5Hz39RQxtQP1n1cf5mbgxxGw3oQ46H8hul6N-uBCNFH7zqbl__8y3gHKe4Ip</recordid><startdate>20160723</startdate><enddate>20160723</enddate><creator>Khani, Samira</creator><creator>Keyhanfar, Fariborz</creator><creator>Amani, Amir</creator><general>Taylor & Francis</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>20160723</creationdate><title>Design and evaluation of oral nanoemulsion drug delivery system of mebudipine</title><author>Khani, Samira ; Keyhanfar, Fariborz ; Amani, Amir</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c432t-80e4a7cbd1690beb91fe4c8e738e5124735e014cc5f3e20433aa01470df168f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Bioavailability</topic><topic>Biological Availability</topic><topic>Calcium Channel Blockers - administration & dosage</topic><topic>Calcium Channel Blockers - chemistry</topic><topic>Calcium Channel Blockers - pharmacokinetics</topic><topic>Chemistry, Pharmaceutical</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Delivery Systems</topic><topic>Drug Stability</topic><topic>Emulsions - chemistry</topic><topic>mebudipine</topic><topic>nanoemulsion</topic><topic>Nanoparticles - chemistry</topic><topic>Nifedipine - administration & dosage</topic><topic>Nifedipine - analogs & derivatives</topic><topic>Nifedipine - chemistry</topic><topic>Nifedipine - pharmacokinetics</topic><topic>Polysorbates - chemistry</topic><topic>Polysorbates - metabolism</topic><topic>Rats</topic><topic>Solubility</topic><topic>Solutions</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Khani, Samira</creatorcontrib><creatorcontrib>Keyhanfar, Fariborz</creatorcontrib><creatorcontrib>Amani, Amir</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>Drug delivery</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Khani, Samira</au><au>Keyhanfar, Fariborz</au><au>Amani, Amir</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Design and evaluation of oral nanoemulsion drug delivery system of mebudipine</atitle><jtitle>Drug delivery</jtitle><addtitle>Drug Deliv</addtitle><date>2016-07-23</date><risdate>2016</risdate><volume>23</volume><issue>6</issue><spage>2035</spage><epage>2043</epage><pages>2035-2043</pages><issn>1071-7544</issn><eissn>1521-0464</eissn><abstract>A nanoemulsion drug delivery system was developed to increase the oral bioavailability of mebudipine as a calcium channel blocker with very low bioavailability profile. The impact of nano-formulation on the pharmacokinetic parameters of mebudipine in rats was investigated. Nanoemulsion formulations containing ethyl oleate, Tween 80, Span 80, polyethylene glycol 400, ethanol and deionized water were prepared using probe sonicator. The optimum formulation was evaluated for physicochemical properties, such as particle size, morphology and stability. The particle size of optimum formulation was 22.8 ± 4.0 nm. Based on the results of this study, the relative bioavailability of mebudipine nanoemulsion was enhanced by about 2.6-, 2.0- and 1.9-fold, respectively, compared with suspension, ethyl oleate solution and micellar solution. In conclusion, nanoemulsion is an interesting option for the delivery of poorly water soluble molecules, such as mebudipine.</abstract><cop>England</cop><pub>Taylor & Francis</pub><pmid>26406153</pmid><doi>10.3109/10717544.2015.1088597</doi><tpages>9</tpages></addata></record> |
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subjects | Administration, Oral Animals Bioavailability Biological Availability Calcium Channel Blockers - administration & dosage Calcium Channel Blockers - chemistry Calcium Channel Blockers - pharmacokinetics Chemistry, Pharmaceutical Drug Carriers - chemistry Drug Delivery Systems Drug Stability Emulsions - chemistry mebudipine nanoemulsion Nanoparticles - chemistry Nifedipine - administration & dosage Nifedipine - analogs & derivatives Nifedipine - chemistry Nifedipine - pharmacokinetics Polysorbates - chemistry Polysorbates - metabolism Rats Solubility Solutions |
title | Design and evaluation of oral nanoemulsion drug delivery system of mebudipine |
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