Key parameters affecting the initial release (burst) and encapsulation efficiency of peptide-containing poly(lactide- co-glycolide) microparticles
The objective of this study was to identify key variables affecting the initial release (burst) and the encapsulation of leuprolide acetate-containing poly(lactide- co-glycolide) (PLGA) microparticles, which were prepared by the cosolvent evaporation method. Adjusting parameters, which affected the...
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| Veröffentlicht in: | International journal of pharmaceutics 2006-11, Vol.324 (2), p.168-175 |
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| container_title | International journal of pharmaceutics |
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| creator | Luan, Xiaosong Skupin, Marc Siepmann, Jürgen Bodmeier, Roland |
| description | The objective of this study was to identify key variables affecting the initial release (burst) and the encapsulation of leuprolide acetate-containing poly(lactide-
co-glycolide) (PLGA) microparticles, which were prepared by the cosolvent evaporation method. Adjusting parameters, which affected the PLGA precipitation kinetics, provided efficient ways to increase the encapsulation efficiency and to control the initial release. Addition of 0.05
M NaCl to the external aqueous phase increased the encapsulation efficiency and the initial release; in contrast, NaCl at high concentration (0.5
M) delayed polymer precipitation and resulted in non-porous microparticles with a low initial release. The presence of ethanol in the external phase led to porous microparticles with an increased initial release but a decreased encapsulation efficiency. The initial release also decreased with decreasing volume of the external phase and homogenization speed, as well as with covering the preparation apparatus; however, these variations had no significant effect on the encapsulation efficiency. Scale-up of the laboratory size by a factor of 5 and 25 showed insignificant influence on the encapsulation efficiency, particle size, and drug release. |
| doi_str_mv | 10.1016/j.ijpharm.2006.06.004 |
| format | Article |
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co-glycolide) (PLGA) microparticles, which were prepared by the cosolvent evaporation method. Adjusting parameters, which affected the PLGA precipitation kinetics, provided efficient ways to increase the encapsulation efficiency and to control the initial release. Addition of 0.05
M NaCl to the external aqueous phase increased the encapsulation efficiency and the initial release; in contrast, NaCl at high concentration (0.5
M) delayed polymer precipitation and resulted in non-porous microparticles with a low initial release. The presence of ethanol in the external phase led to porous microparticles with an increased initial release but a decreased encapsulation efficiency. The initial release also decreased with decreasing volume of the external phase and homogenization speed, as well as with covering the preparation apparatus; however, these variations had no significant effect on the encapsulation efficiency. Scale-up of the laboratory size by a factor of 5 and 25 showed insignificant influence on the encapsulation efficiency, particle size, and drug release.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2006.06.004</identifier><identifier>PMID: 16854540</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Biological and medical sciences ; Burst ; Delayed-Action Preparations ; Encapsulation efficiency ; Ethanol - administration & dosage ; General pharmacology ; Initial release ; Lactic Acid ; Leuprolide - administration & dosage ; Leuprolide - chemistry ; Medical sciences ; Microencapsulation ; Particle Size ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Poly(lactide- co-glycolide) ; Polyglycolic Acid ; Polymers ; Scale-up ; Sodium Chloride - administration & dosage ; Solvent evaporation method ; Volatilization</subject><ispartof>International journal of pharmaceutics, 2006-11, Vol.324 (2), p.168-175</ispartof><rights>2006 Elsevier B.V.</rights><rights>2006 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c490t-aebfcb1a60491ac151b454acb84362214338050137faa4f63b0209430bd841a83</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0378517306004546$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18225310$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16854540$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Luan, Xiaosong</creatorcontrib><creatorcontrib>Skupin, Marc</creatorcontrib><creatorcontrib>Siepmann, Jürgen</creatorcontrib><creatorcontrib>Bodmeier, Roland</creatorcontrib><title>Key parameters affecting the initial release (burst) and encapsulation efficiency of peptide-containing poly(lactide- co-glycolide) microparticles</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The objective of this study was to identify key variables affecting the initial release (burst) and the encapsulation of leuprolide acetate-containing poly(lactide-
co-glycolide) (PLGA) microparticles, which were prepared by the cosolvent evaporation method. Adjusting parameters, which affected the PLGA precipitation kinetics, provided efficient ways to increase the encapsulation efficiency and to control the initial release. Addition of 0.05
M NaCl to the external aqueous phase increased the encapsulation efficiency and the initial release; in contrast, NaCl at high concentration (0.5
M) delayed polymer precipitation and resulted in non-porous microparticles with a low initial release. The presence of ethanol in the external phase led to porous microparticles with an increased initial release but a decreased encapsulation efficiency. The initial release also decreased with decreasing volume of the external phase and homogenization speed, as well as with covering the preparation apparatus; however, these variations had no significant effect on the encapsulation efficiency. Scale-up of the laboratory size by a factor of 5 and 25 showed insignificant influence on the encapsulation efficiency, particle size, and drug release.</description><subject>Biological and medical sciences</subject><subject>Burst</subject><subject>Delayed-Action Preparations</subject><subject>Encapsulation efficiency</subject><subject>Ethanol - administration & dosage</subject><subject>General pharmacology</subject><subject>Initial release</subject><subject>Lactic Acid</subject><subject>Leuprolide - administration & dosage</subject><subject>Leuprolide - chemistry</subject><subject>Medical sciences</subject><subject>Microencapsulation</subject><subject>Particle Size</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Poly(lactide- co-glycolide)</subject><subject>Polyglycolic Acid</subject><subject>Polymers</subject><subject>Scale-up</subject><subject>Sodium Chloride - administration & dosage</subject><subject>Solvent evaporation method</subject><subject>Volatilization</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkc1q3DAQgEVpaTZpH6FFl5bk4K1kyT97CiWkPzTQS3sWY3mUaJEtV5ILfo0-ceWsIcfAgNDwzWhGHyHvONtzxutPx709Tg8Qhn3JWL1fg8kXZMfbRhRCNvVLsmOiaYuKN-KMnMd4ZBksuXhNznjdVrKSbEf-_cCFThBgwIQhUjAGdbLjPU0PSO1okwVHAzqEiPSym0NMVxTGnuKoYYqzg2T9SNEYq23OLdQbOuGUbI-F9mOC3CS3m7xbLh3oxzzVvrh3i_Yu367oYHXweYhktcP4hrwy4CK-3c4L8vvL7a-bb8Xdz6_fbz7fFVoeWCoAO6M7DjWTBw6aV7zLK4HuWinqsuRSiJZVjIvGAEhTi46V7CAF6_pWcmjFBfl46jsF_2fGmNRgo0bnYEQ_R1W3h0ZI1jwL8oNsStFUGaxOYF4nxoBGTcEOEBbFmVqtqaParKnVmlqDyVz3fntg7gbsn6o2TRn4sAEQNTgTYNQ2PnFtWVaCr9z1icP8b38tBhUfpWBvQ9aqem-fGeU_T-G6dg</recordid><startdate>20061106</startdate><enddate>20061106</enddate><creator>Luan, Xiaosong</creator><creator>Skupin, Marc</creator><creator>Siepmann, Jürgen</creator><creator>Bodmeier, Roland</creator><general>Elsevier B.V</general><general>Elsevier</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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20061106</creationdate><title>Key parameters affecting the initial release (burst) and encapsulation efficiency of peptide-containing poly(lactide- co-glycolide) microparticles</title><author>Luan, Xiaosong ; Skupin, Marc ; Siepmann, Jürgen ; Bodmeier, Roland</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c490t-aebfcb1a60491ac151b454acb84362214338050137faa4f63b0209430bd841a83</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>Biological and medical sciences</topic><topic>Burst</topic><topic>Delayed-Action Preparations</topic><topic>Encapsulation efficiency</topic><topic>Ethanol - administration & dosage</topic><topic>General pharmacology</topic><topic>Initial release</topic><topic>Lactic Acid</topic><topic>Leuprolide - administration & dosage</topic><topic>Leuprolide - chemistry</topic><topic>Medical sciences</topic><topic>Microencapsulation</topic><topic>Particle Size</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Poly(lactide- co-glycolide)</topic><topic>Polyglycolic Acid</topic><topic>Polymers</topic><topic>Scale-up</topic><topic>Sodium Chloride - administration & dosage</topic><topic>Solvent evaporation method</topic><topic>Volatilization</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Luan, Xiaosong</creatorcontrib><creatorcontrib>Skupin, Marc</creatorcontrib><creatorcontrib>Siepmann, Jürgen</creatorcontrib><creatorcontrib>Bodmeier, Roland</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>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Luan, Xiaosong</au><au>Skupin, Marc</au><au>Siepmann, Jürgen</au><au>Bodmeier, Roland</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Key parameters affecting the initial release (burst) and encapsulation efficiency of peptide-containing poly(lactide- co-glycolide) microparticles</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2006-11-06</date><risdate>2006</risdate><volume>324</volume><issue>2</issue><spage>168</spage><epage>175</epage><pages>168-175</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The objective of this study was to identify key variables affecting the initial release (burst) and the encapsulation of leuprolide acetate-containing poly(lactide-
co-glycolide) (PLGA) microparticles, which were prepared by the cosolvent evaporation method. Adjusting parameters, which affected the PLGA precipitation kinetics, provided efficient ways to increase the encapsulation efficiency and to control the initial release. Addition of 0.05
M NaCl to the external aqueous phase increased the encapsulation efficiency and the initial release; in contrast, NaCl at high concentration (0.5
M) delayed polymer precipitation and resulted in non-porous microparticles with a low initial release. The presence of ethanol in the external phase led to porous microparticles with an increased initial release but a decreased encapsulation efficiency. The initial release also decreased with decreasing volume of the external phase and homogenization speed, as well as with covering the preparation apparatus; however, these variations had no significant effect on the encapsulation efficiency. Scale-up of the laboratory size by a factor of 5 and 25 showed insignificant influence on the encapsulation efficiency, particle size, and drug release.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>16854540</pmid><doi>10.1016/j.ijpharm.2006.06.004</doi><tpages>8</tpages></addata></record> |
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| issn | 0378-5173 1873-3476 |
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| subjects | Biological and medical sciences Burst Delayed-Action Preparations Encapsulation efficiency Ethanol - administration & dosage General pharmacology Initial release Lactic Acid Leuprolide - administration & dosage Leuprolide - chemistry Medical sciences Microencapsulation Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Poly(lactide- co-glycolide) Polyglycolic Acid Polymers Scale-up Sodium Chloride - administration & dosage Solvent evaporation method Volatilization |
| title | Key parameters affecting the initial release (burst) and encapsulation efficiency of peptide-containing poly(lactide- co-glycolide) microparticles |
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