Solid lipid nanoparticles (SLN) for controlled drug delivery – Drug release and release mechanism
Solid lipid nanoparticles (SLN) are particulate systems for parenteral drug administration with mean particle diameters ranging from 50 up to 1000 nm. The model drugs tetracaine, etomidate and prednisolone were incorporated (1, 5 and 10%) to study the drug load, effect of drug incorporation on the s...
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| Veröffentlicht in: | European journal of pharmaceutics and biopharmaceutics 1998-03, Vol.45 (2), p.149-155 |
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| container_title | European journal of pharmaceutics and biopharmaceutics |
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| creator | zur Mühlen, Annette Schwarz, Cora Mehnert, Wolfgang |
| description | Solid lipid nanoparticles (SLN) are particulate systems for parenteral drug administration with mean particle diameters ranging from 50 up to 1000 nm. The model drugs tetracaine, etomidate and prednisolone were incorporated (1, 5 and 10%) to study the drug load, effect of drug incorporation on the structure of the lipid matrix and the release profiles and mechanism. SLN were produced by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state (500/1500 bar, 3/10 cycles). In case of tetracaine and etomidate, high drug loadings up to 10% could be achieved when using Compritol 888 ATO and Dynasan 112 as matrix material. The melting behavior of the drug loaded particles revealed that little or no interactions between drug and lipid occured. A burst drug release (100% release |
| doi_str_mv | 10.1016/S0939-6411(97)00150-1 |
| format | Article |
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The model drugs tetracaine, etomidate and prednisolone were incorporated (1, 5 and 10%) to study the drug load, effect of drug incorporation on the structure of the lipid matrix and the release profiles and mechanism. SLN were produced by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state (500/1500 bar, 3/10 cycles). In case of tetracaine and etomidate, high drug loadings up to 10% could be achieved when using Compritol 888 ATO and Dynasan 112 as matrix material. The melting behavior of the drug loaded particles revealed that little or no interactions between drug and lipid occured. A burst drug release (100% release<1 min) was observed with tetracaine and etomidate SLN, which was attributed to the large surface area of the nanoparticles and drug enrichment in the outer shell of the particles. In contrast, prednisolone loaded SLN showed a distinctly prolonged release over a monitored period of 5 weeks. Depending on the chemical nature of the lipid matrix, 83.8 and 37.1% drug were released (cholesterol and compritol, respectively). These results demonstrate the principle suitability of SLN as a prolonged release formulation for lipophilic drugs.</description><identifier>ISSN: 0939-6411</identifier><identifier>EISSN: 1873-3441</identifier><identifier>DOI: 10.1016/S0939-6411(97)00150-1</identifier><identifier>PMID: 9704911</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Biological and medical sciences ; Chemistry, Pharmaceutical ; Crystallization ; Drug Carriers - chemistry ; Drug Delivery Systems ; Drug incorporation ; Etomidate - chemistry ; General pharmacology ; Intravenous drug delivery ; Lipids - chemistry ; Medical sciences ; Microspheres ; Pharmaceutical Preparations - administration & dosage ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Prednisolone - chemistry ; Solid lipid nanoparticles ; Tetracaine - chemistry</subject><ispartof>European journal of pharmaceutics and biopharmaceutics, 1998-03, Vol.45 (2), p.149-155</ispartof><rights>1998 Elsevier Science B.V.</rights><rights>1998 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c455t-df24b968642959c54bb4087105ca5e304c1bcb096766e264efcab5e103b1a3f3</citedby><cites>FETCH-LOGICAL-c455t-df24b968642959c54bb4087105ca5e304c1bcb096766e264efcab5e103b1a3f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0939641197001501$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2216543$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9704911$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>zur Mühlen, Annette</creatorcontrib><creatorcontrib>Schwarz, Cora</creatorcontrib><creatorcontrib>Mehnert, Wolfgang</creatorcontrib><title>Solid lipid nanoparticles (SLN) for controlled drug delivery – Drug release and release mechanism</title><title>European journal of pharmaceutics and biopharmaceutics</title><addtitle>Eur J Pharm Biopharm</addtitle><description>Solid lipid nanoparticles (SLN) are particulate systems for parenteral drug administration with mean particle diameters ranging from 50 up to 1000 nm. The model drugs tetracaine, etomidate and prednisolone were incorporated (1, 5 and 10%) to study the drug load, effect of drug incorporation on the structure of the lipid matrix and the release profiles and mechanism. SLN were produced by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state (500/1500 bar, 3/10 cycles). In case of tetracaine and etomidate, high drug loadings up to 10% could be achieved when using Compritol 888 ATO and Dynasan 112 as matrix material. The melting behavior of the drug loaded particles revealed that little or no interactions between drug and lipid occured. A burst drug release (100% release<1 min) was observed with tetracaine and etomidate SLN, which was attributed to the large surface area of the nanoparticles and drug enrichment in the outer shell of the particles. In contrast, prednisolone loaded SLN showed a distinctly prolonged release over a monitored period of 5 weeks. Depending on the chemical nature of the lipid matrix, 83.8 and 37.1% drug were released (cholesterol and compritol, respectively). These results demonstrate the principle suitability of SLN as a prolonged release formulation for lipophilic drugs.</description><subject>Biological and medical sciences</subject><subject>Chemistry, Pharmaceutical</subject><subject>Crystallization</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Delivery Systems</subject><subject>Drug incorporation</subject><subject>Etomidate - chemistry</subject><subject>General pharmacology</subject><subject>Intravenous drug delivery</subject><subject>Lipids - chemistry</subject><subject>Medical sciences</subject><subject>Microspheres</subject><subject>Pharmaceutical Preparations - administration & dosage</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Prednisolone - chemistry</subject><subject>Solid lipid nanoparticles</subject><subject>Tetracaine - chemistry</subject><issn>0939-6411</issn><issn>1873-3441</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkM1u1DAQxy1EVbYfj1DJB4TaQ6gn_kh8qlChgLRqD9u75dgTMHLirZ2t1BvvwBvyJGS7q71y8Vj-_2Y8-hFyAewjMFDXK6a5rpQAuNTNFWMgWQVvyALahldcCHhLFgfkHTkp5RdjTDSyPSbHumFCAyyIW6UYPI1hPZ-jHdPa5im4iIVerpb3V7RPmbo0TjnFiJ76vPlBPcbwjPmF_v39h37evmSMaAtSO_rDfUD3046hDGfkqLex4Pm-npLHuy-Pt9-q5cPX77eflpUTUk6V72vRadUqUWupnRRdJ1jbAJPOSuRMOOhcx7RqlMJaCeyd7SQC4x1Y3vNT8mE3dp3T0wbLZIZQHMZoR0ybYhreSi60mkG5A11OpWTszTqHweYXA8xs3ZpXt2YrzujGvLo1MPdd7D_YdAP6Q9de5py_3-e2OBv7bEcXygGra1BS8Bm72WE4u3gOmE1xAUeHPmR0k_Ep_GeRfyJllko</recordid><startdate>19980301</startdate><enddate>19980301</enddate><creator>zur Mühlen, Annette</creator><creator>Schwarz, Cora</creator><creator>Mehnert, Wolfgang</creator><general>Elsevier B.V</general><general>Elsevier Science</general><scope>IQODW</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>7X8</scope></search><sort><creationdate>19980301</creationdate><title>Solid lipid nanoparticles (SLN) for controlled drug delivery – Drug release and release mechanism</title><author>zur Mühlen, Annette ; Schwarz, Cora ; Mehnert, Wolfgang</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c455t-df24b968642959c54bb4087105ca5e304c1bcb096766e264efcab5e103b1a3f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Biological and medical sciences</topic><topic>Chemistry, Pharmaceutical</topic><topic>Crystallization</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Delivery Systems</topic><topic>Drug incorporation</topic><topic>Etomidate - chemistry</topic><topic>General pharmacology</topic><topic>Intravenous drug delivery</topic><topic>Lipids - chemistry</topic><topic>Medical sciences</topic><topic>Microspheres</topic><topic>Pharmaceutical Preparations - administration & dosage</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Prednisolone - chemistry</topic><topic>Solid lipid nanoparticles</topic><topic>Tetracaine - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>zur Mühlen, Annette</creatorcontrib><creatorcontrib>Schwarz, Cora</creatorcontrib><creatorcontrib>Mehnert, Wolfgang</creatorcontrib><collection>Pascal-Francis</collection><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>European journal of pharmaceutics and biopharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>zur Mühlen, Annette</au><au>Schwarz, Cora</au><au>Mehnert, Wolfgang</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Solid lipid nanoparticles (SLN) for controlled drug delivery – Drug release and release mechanism</atitle><jtitle>European journal of pharmaceutics and biopharmaceutics</jtitle><addtitle>Eur J Pharm Biopharm</addtitle><date>1998-03-01</date><risdate>1998</risdate><volume>45</volume><issue>2</issue><spage>149</spage><epage>155</epage><pages>149-155</pages><issn>0939-6411</issn><eissn>1873-3441</eissn><abstract>Solid lipid nanoparticles (SLN) are particulate systems for parenteral drug administration with mean particle diameters ranging from 50 up to 1000 nm. The model drugs tetracaine, etomidate and prednisolone were incorporated (1, 5 and 10%) to study the drug load, effect of drug incorporation on the structure of the lipid matrix and the release profiles and mechanism. SLN were produced by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state (500/1500 bar, 3/10 cycles). In case of tetracaine and etomidate, high drug loadings up to 10% could be achieved when using Compritol 888 ATO and Dynasan 112 as matrix material. The melting behavior of the drug loaded particles revealed that little or no interactions between drug and lipid occured. A burst drug release (100% release<1 min) was observed with tetracaine and etomidate SLN, which was attributed to the large surface area of the nanoparticles and drug enrichment in the outer shell of the particles. In contrast, prednisolone loaded SLN showed a distinctly prolonged release over a monitored period of 5 weeks. Depending on the chemical nature of the lipid matrix, 83.8 and 37.1% drug were released (cholesterol and compritol, respectively). These results demonstrate the principle suitability of SLN as a prolonged release formulation for lipophilic drugs.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>9704911</pmid><doi>10.1016/S0939-6411(97)00150-1</doi><tpages>7</tpages></addata></record> |
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| identifier | ISSN: 0939-6411 |
| ispartof | European journal of pharmaceutics and biopharmaceutics, 1998-03, Vol.45 (2), p.149-155 |
| issn | 0939-6411 1873-3441 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Biological and medical sciences Chemistry, Pharmaceutical Crystallization Drug Carriers - chemistry Drug Delivery Systems Drug incorporation Etomidate - chemistry General pharmacology Intravenous drug delivery Lipids - chemistry Medical sciences Microspheres Pharmaceutical Preparations - administration & dosage Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Prednisolone - chemistry Solid lipid nanoparticles Tetracaine - chemistry |
| title | Solid lipid nanoparticles (SLN) for controlled drug delivery – Drug release and release mechanism |
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