One-step production of darunavir solid dispersion nanoparticles coated with enteric polymers using electrospraying
Objectives The aim of this work was to investigate the feasibility of producing darunavir (DRV) solid dispersion nanoparticles coated with an enteric polymer in one single step using electrospraying. Methods The core‐shell nanoparticles were made using coaxial electrospraying. A solution of DRV with...
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Veröffentlicht in: | Journal of pharmacy and pharmacology 2016-05, Vol.68 (5), p.625-633 |
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container_title | Journal of pharmacy and pharmacology |
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creator | Nguyen, Duong Nhat Palangetic, Ljiljana Clasen, Christian Van den Mooter, Guy |
description | Objectives
The aim of this work was to investigate the feasibility of producing darunavir (DRV) solid dispersion nanoparticles coated with an enteric polymer in one single step using electrospraying.
Methods
The core‐shell nanoparticles were made using coaxial electrospraying. A solution of DRV with hydroxypropyl methylcellulose in a mixture of organic solvents formed the core, while the shell was produced from an enteric polymer (Eudragit L100) dissolved in an organic solvent. The final particles were evaluated in terms of morphology, physical state, encapsulation efficiency and in‐vitro dissolution.
Key findings
Nanoparticles of encapsulated DRV solid dispersions within Eudragit L100 were successfully prepared with high encapsulation efficiency (90%). The enteric coating layer reduced the percentage of DRV release in acidic medium in the in‐vitro dissolution test to less than 20%.
Conclusions
This study showed the potential of coaxial electrospraying for encapsulating solid dispersions within core‐shell structured nanoparticles. |
doi_str_mv | 10.1111/jphp.12459 |
format | Article |
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The aim of this work was to investigate the feasibility of producing darunavir (DRV) solid dispersion nanoparticles coated with an enteric polymer in one single step using electrospraying.
Methods
The core‐shell nanoparticles were made using coaxial electrospraying. A solution of DRV with hydroxypropyl methylcellulose in a mixture of organic solvents formed the core, while the shell was produced from an enteric polymer (Eudragit L100) dissolved in an organic solvent. The final particles were evaluated in terms of morphology, physical state, encapsulation efficiency and in‐vitro dissolution.
Key findings
Nanoparticles of encapsulated DRV solid dispersions within Eudragit L100 were successfully prepared with high encapsulation efficiency (90%). The enteric coating layer reduced the percentage of DRV release in acidic medium in the in‐vitro dissolution test to less than 20%.
Conclusions
This study showed the potential of coaxial electrospraying for encapsulating solid dispersions within core‐shell structured nanoparticles.</description><identifier>ISSN: 0022-3573</identifier><identifier>EISSN: 2042-7158</identifier><identifier>DOI: 10.1111/jphp.12459</identifier><identifier>PMID: 26272245</identifier><identifier>CODEN: JPPMAB</identifier><language>eng</language><publisher>England: Blackwell Publishing Ltd</publisher><subject>Aerosols ; Crystallography, X-Ray ; darunavir ; Darunavir - chemistry ; Drug Carriers ; Drug Compounding ; electrospraying ; enteric coating ; Feasibility Studies ; HIV Protease Inhibitors - chemistry ; Hydrogen-Ion Concentration ; Hypromellose Derivatives - chemistry ; Kinetics ; Nanoparticles ; Nanotechnology ; Particle Size ; Polymers ; Polymethacrylic Acids - chemistry ; Powder Diffraction ; solid dispersion ; Solubility ; Solvents - chemistry ; Spectrum Analysis ; Surface Properties ; Technology, Pharmaceutical - methods</subject><ispartof>Journal of pharmacy and pharmacology, 2016-05, Vol.68 (5), p.625-633</ispartof><rights>2015 Royal Pharmaceutical Society</rights><rights>2015 Royal Pharmaceutical Society.</rights><rights>Copyright © 2016 Royal Pharmaceutical Society</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4599-505b3aa70240e560cc6fa2b008b8beb92c96e4795dbefc50f3c70b50b545bd503</citedby><cites>FETCH-LOGICAL-c4599-505b3aa70240e560cc6fa2b008b8beb92c96e4795dbefc50f3c70b50b545bd503</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1111%2Fjphp.12459$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1111%2Fjphp.12459$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26272245$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Nguyen, Duong Nhat</creatorcontrib><creatorcontrib>Palangetic, Ljiljana</creatorcontrib><creatorcontrib>Clasen, Christian</creatorcontrib><creatorcontrib>Van den Mooter, Guy</creatorcontrib><title>One-step production of darunavir solid dispersion nanoparticles coated with enteric polymers using electrospraying</title><title>Journal of pharmacy and pharmacology</title><addtitle>J Pharm Pharmacol</addtitle><description>Objectives
The aim of this work was to investigate the feasibility of producing darunavir (DRV) solid dispersion nanoparticles coated with an enteric polymer in one single step using electrospraying.
Methods
The core‐shell nanoparticles were made using coaxial electrospraying. A solution of DRV with hydroxypropyl methylcellulose in a mixture of organic solvents formed the core, while the shell was produced from an enteric polymer (Eudragit L100) dissolved in an organic solvent. The final particles were evaluated in terms of morphology, physical state, encapsulation efficiency and in‐vitro dissolution.
Key findings
Nanoparticles of encapsulated DRV solid dispersions within Eudragit L100 were successfully prepared with high encapsulation efficiency (90%). The enteric coating layer reduced the percentage of DRV release in acidic medium in the in‐vitro dissolution test to less than 20%.
Conclusions
This study showed the potential of coaxial electrospraying for encapsulating solid dispersions within core‐shell structured nanoparticles.</description><subject>Aerosols</subject><subject>Crystallography, X-Ray</subject><subject>darunavir</subject><subject>Darunavir - chemistry</subject><subject>Drug Carriers</subject><subject>Drug Compounding</subject><subject>electrospraying</subject><subject>enteric coating</subject><subject>Feasibility Studies</subject><subject>HIV Protease Inhibitors - chemistry</subject><subject>Hydrogen-Ion Concentration</subject><subject>Hypromellose Derivatives - chemistry</subject><subject>Kinetics</subject><subject>Nanoparticles</subject><subject>Nanotechnology</subject><subject>Particle Size</subject><subject>Polymers</subject><subject>Polymethacrylic Acids - chemistry</subject><subject>Powder Diffraction</subject><subject>solid dispersion</subject><subject>Solubility</subject><subject>Solvents - chemistry</subject><subject>Spectrum Analysis</subject><subject>Surface Properties</subject><subject>Technology, Pharmaceutical - methods</subject><issn>0022-3573</issn><issn>2042-7158</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kcFvFCEYxYnR2LV68Q8wJF4ak2mBGWDnaBrtajZtD-oeCTDfWNZZQJhp3f9exm178FBCQgi_9_I9HkJvKTmlZZ1t4008pazh7TO0YKRhlaR8-RwtCGGsqrmsj9CrnLeEECmEeImOmGCSFcECpSsPVR4h4phCN9nRBY9DjzudJq9vXcI5DK7DncsRUp5fvfYh6jQ6O0DGNugROnznxhsMfoTkLI5h2O8Kjafs_E8MA9gxhRyT3pf7a_Si10OGN_fnMfr--dO381W1vrr4cv5xXdmSpK044abWWhLWEOCCWCt6zQwhS7M0YFpmWwGNbHlnoLec9LWVxPCyG246TupjdHLwLcl-T5BHtXPZwjBoD2HKisqW1ZJRRgv6_j90G6bky3QzVQjRipn6cKBsCZMT9Comt9NpryhRcxNqbkL9a6LA7-4tJ7OD7hF9-PoC0ANw5wbYP2Glvl6vrh9Mq4PGlcr-PGp0-qWErCVXm8sLtdysxI_1hqvL-i9wr6Up</recordid><startdate>201605</startdate><enddate>201605</enddate><creator>Nguyen, Duong Nhat</creator><creator>Palangetic, Ljiljana</creator><creator>Clasen, Christian</creator><creator>Van den Mooter, Guy</creator><general>Blackwell Publishing Ltd</general><general>Wiley Subscription Services, Inc</general><scope>BSCLL</scope><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>7QP</scope><scope>7TK</scope><scope>7U9</scope><scope>H94</scope><scope>K9.</scope><scope>M7N</scope><scope>7X8</scope></search><sort><creationdate>201605</creationdate><title>One-step production of darunavir solid dispersion nanoparticles coated with enteric polymers using electrospraying</title><author>Nguyen, Duong Nhat ; Palangetic, Ljiljana ; Clasen, Christian ; Van den Mooter, Guy</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4599-505b3aa70240e560cc6fa2b008b8beb92c96e4795dbefc50f3c70b50b545bd503</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Aerosols</topic><topic>Crystallography, X-Ray</topic><topic>darunavir</topic><topic>Darunavir - chemistry</topic><topic>Drug Carriers</topic><topic>Drug Compounding</topic><topic>electrospraying</topic><topic>enteric coating</topic><topic>Feasibility Studies</topic><topic>HIV Protease Inhibitors - chemistry</topic><topic>Hydrogen-Ion Concentration</topic><topic>Hypromellose Derivatives - chemistry</topic><topic>Kinetics</topic><topic>Nanoparticles</topic><topic>Nanotechnology</topic><topic>Particle Size</topic><topic>Polymers</topic><topic>Polymethacrylic Acids - chemistry</topic><topic>Powder Diffraction</topic><topic>solid dispersion</topic><topic>Solubility</topic><topic>Solvents - chemistry</topic><topic>Spectrum Analysis</topic><topic>Surface Properties</topic><topic>Technology, Pharmaceutical - methods</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Nguyen, Duong Nhat</creatorcontrib><creatorcontrib>Palangetic, Ljiljana</creatorcontrib><creatorcontrib>Clasen, Christian</creatorcontrib><creatorcontrib>Van den Mooter, Guy</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of pharmacy and pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Nguyen, Duong Nhat</au><au>Palangetic, Ljiljana</au><au>Clasen, Christian</au><au>Van den Mooter, Guy</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>One-step production of darunavir solid dispersion nanoparticles coated with enteric polymers using electrospraying</atitle><jtitle>Journal of pharmacy and pharmacology</jtitle><addtitle>J Pharm Pharmacol</addtitle><date>2016-05</date><risdate>2016</risdate><volume>68</volume><issue>5</issue><spage>625</spage><epage>633</epage><pages>625-633</pages><issn>0022-3573</issn><eissn>2042-7158</eissn><coden>JPPMAB</coden><abstract>Objectives
The aim of this work was to investigate the feasibility of producing darunavir (DRV) solid dispersion nanoparticles coated with an enteric polymer in one single step using electrospraying.
Methods
The core‐shell nanoparticles were made using coaxial electrospraying. A solution of DRV with hydroxypropyl methylcellulose in a mixture of organic solvents formed the core, while the shell was produced from an enteric polymer (Eudragit L100) dissolved in an organic solvent. The final particles were evaluated in terms of morphology, physical state, encapsulation efficiency and in‐vitro dissolution.
Key findings
Nanoparticles of encapsulated DRV solid dispersions within Eudragit L100 were successfully prepared with high encapsulation efficiency (90%). The enteric coating layer reduced the percentage of DRV release in acidic medium in the in‐vitro dissolution test to less than 20%.
Conclusions
This study showed the potential of coaxial electrospraying for encapsulating solid dispersions within core‐shell structured nanoparticles.</abstract><cop>England</cop><pub>Blackwell Publishing Ltd</pub><pmid>26272245</pmid><doi>10.1111/jphp.12459</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
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subjects | Aerosols Crystallography, X-Ray darunavir Darunavir - chemistry Drug Carriers Drug Compounding electrospraying enteric coating Feasibility Studies HIV Protease Inhibitors - chemistry Hydrogen-Ion Concentration Hypromellose Derivatives - chemistry Kinetics Nanoparticles Nanotechnology Particle Size Polymers Polymethacrylic Acids - chemistry Powder Diffraction solid dispersion Solubility Solvents - chemistry Spectrum Analysis Surface Properties Technology, Pharmaceutical - methods |
title | One-step production of darunavir solid dispersion nanoparticles coated with enteric polymers using electrospraying |
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