Hydrophilic and hydrophobic amino acid copolymers for nano-comminution of poorly soluble drugs
Nano-comminution has successfully brought nanoparticle formulations of poorly soluble drugs to our daily life. The key for the successful nano-comminution of a drug is the choice of a proper polymeric steric stabilizer. To systematically elucidate the rationale of stabilizer selection, two types of...
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| Veröffentlicht in: | International journal of pharmaceutics 2010-01, Vol.384 (1), p.173-180 |
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| container_title | International journal of pharmaceutics |
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| creator | Lee, M.K. Kim, S. Ahn, C.-H. Lee, J. |
| description | Nano-comminution has successfully brought nanoparticle formulations of poorly soluble drugs to our daily life. The key for the successful nano-comminution of a drug is the choice of a proper polymeric steric stabilizer. To systematically elucidate the rationale of stabilizer selection, two types of helical amino acid copolymers, relatively hydrophilic and hydrophobic copolymers, were used in nano-comminution. The hydrophilic copolymers had lysine as their major component. The addition of relatively hydrophobic leucine and phenylalanine to them could not make significant changes in particle size. However, when a small amount of hydrophilic glutamic acid or lysine was added into elastin-like hydrophobic copolymers of valine, glycine, and proline, significant composition dependence was found. Therefore, specific interactions between the functional groups of polymers and drug surfaces seem to be important for successful nano-comminution. The stimuli responsive behavior of the hydrophobic copolymer induced the temperature dependence of particle size. |
| doi_str_mv | 10.1016/j.ijpharm.2009.09.041 |
| format | Article |
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The key for the successful nano-comminution of a drug is the choice of a proper polymeric steric stabilizer. To systematically elucidate the rationale of stabilizer selection, two types of helical amino acid copolymers, relatively hydrophilic and hydrophobic copolymers, were used in nano-comminution. The hydrophilic copolymers had lysine as their major component. The addition of relatively hydrophobic leucine and phenylalanine to them could not make significant changes in particle size. However, when a small amount of hydrophilic glutamic acid or lysine was added into elastin-like hydrophobic copolymers of valine, glycine, and proline, significant composition dependence was found. Therefore, specific interactions between the functional groups of polymers and drug surfaces seem to be important for successful nano-comminution. The stimuli responsive behavior of the hydrophobic copolymer induced the temperature dependence of particle size.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2009.09.041</identifier><identifier>PMID: 19788919</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Amino Acid Sequence ; Amino Acids - chemistry ; Amino Acids - genetics ; Biological and medical sciences ; Dispersion ; General pharmacology ; Hydrophobic and Hydrophilic Interactions ; Medical sciences ; Molecular Sequence Data ; Nanocrystals ; Nanoparticles ; Nanoparticles - chemistry ; Nanotechnology - methods ; Particle engineering ; Particle Size ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. 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The key for the successful nano-comminution of a drug is the choice of a proper polymeric steric stabilizer. To systematically elucidate the rationale of stabilizer selection, two types of helical amino acid copolymers, relatively hydrophilic and hydrophobic copolymers, were used in nano-comminution. The hydrophilic copolymers had lysine as their major component. The addition of relatively hydrophobic leucine and phenylalanine to them could not make significant changes in particle size. However, when a small amount of hydrophilic glutamic acid or lysine was added into elastin-like hydrophobic copolymers of valine, glycine, and proline, significant composition dependence was found. Therefore, specific interactions between the functional groups of polymers and drug surfaces seem to be important for successful nano-comminution. The stimuli responsive behavior of the hydrophobic copolymer induced the temperature dependence of particle size.</description><subject>Amino Acid Sequence</subject><subject>Amino Acids - chemistry</subject><subject>Amino Acids - genetics</subject><subject>Biological and medical sciences</subject><subject>Dispersion</subject><subject>General pharmacology</subject><subject>Hydrophobic and Hydrophilic Interactions</subject><subject>Medical sciences</subject><subject>Molecular Sequence Data</subject><subject>Nanocrystals</subject><subject>Nanoparticles</subject><subject>Nanoparticles - chemistry</subject><subject>Nanotechnology - methods</subject><subject>Particle engineering</subject><subject>Particle Size</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Polymers - chemistry</subject><subject>Poorly water-soluble drug</subject><subject>Solubility</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE2LFDEQhoO4uOPqT1ByEU89ppLupHMSWdQVFrzsXg35dDKkO20yvTD_fruZRo9CQVHwvFXFg9A7IHsgwD8d9_E4HXQZ9pQQuV-rhRdoB71gDWsFf4l2hIm-6UCwa_S61iMhhFNgr9A1SNH3EuQO_bo7u5KnQ0zRYj06fLjM2azzEMeMtY0O2zzldB58qTjkgkc95sbmYQHmU8wjzgFPOZd0xjWn2SSPXZl_1zfoKuhU_dut36DHb18fbu-a-5_ff9x-uW8sk-2paSUP4L2R2riWccco1aBBBkZlJzoTKPeOm0Aoh44Ry5gJ2mtrqIBgRc9u0MfL3qnkP7OvJzXEan1KevR5rkqwFnhHGCxkdyFtybUWH9RU4qDLWQFRq1l1VJtZtZpVa7Vr7v12YTaDd_9Sm8oF-LABulqdQtGjjfUvRynrgANbuM8Xzi8-nqIvqtroR-tdLN6elMvxP688A4ZHm8E</recordid><startdate>20100115</startdate><enddate>20100115</enddate><creator>Lee, M.K.</creator><creator>Kim, S.</creator><creator>Ahn, C.-H.</creator><creator>Lee, J.</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>7X8</scope></search><sort><creationdate>20100115</creationdate><title>Hydrophilic and hydrophobic amino acid copolymers for nano-comminution of poorly soluble drugs</title><author>Lee, M.K. ; Kim, S. ; Ahn, C.-H. ; Lee, J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c394t-496f1eeb9abd436d322a1a19f329575bf26ed6bf0261530c33bfaeacb271fc783</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Amino Acid Sequence</topic><topic>Amino Acids - chemistry</topic><topic>Amino Acids - genetics</topic><topic>Biological and medical sciences</topic><topic>Dispersion</topic><topic>General pharmacology</topic><topic>Hydrophobic and Hydrophilic Interactions</topic><topic>Medical sciences</topic><topic>Molecular Sequence Data</topic><topic>Nanocrystals</topic><topic>Nanoparticles</topic><topic>Nanoparticles - chemistry</topic><topic>Nanotechnology - methods</topic><topic>Particle engineering</topic><topic>Particle Size</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Polymers - chemistry</topic><topic>Poorly water-soluble drug</topic><topic>Solubility</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Lee, M.K.</creatorcontrib><creatorcontrib>Kim, S.</creatorcontrib><creatorcontrib>Ahn, C.-H.</creatorcontrib><creatorcontrib>Lee, J.</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>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Lee, M.K.</au><au>Kim, S.</au><au>Ahn, C.-H.</au><au>Lee, J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Hydrophilic and hydrophobic amino acid copolymers for nano-comminution of poorly soluble drugs</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2010-01-15</date><risdate>2010</risdate><volume>384</volume><issue>1</issue><spage>173</spage><epage>180</epage><pages>173-180</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>Nano-comminution has successfully brought nanoparticle formulations of poorly soluble drugs to our daily life. The key for the successful nano-comminution of a drug is the choice of a proper polymeric steric stabilizer. To systematically elucidate the rationale of stabilizer selection, two types of helical amino acid copolymers, relatively hydrophilic and hydrophobic copolymers, were used in nano-comminution. The hydrophilic copolymers had lysine as their major component. The addition of relatively hydrophobic leucine and phenylalanine to them could not make significant changes in particle size. However, when a small amount of hydrophilic glutamic acid or lysine was added into elastin-like hydrophobic copolymers of valine, glycine, and proline, significant composition dependence was found. Therefore, specific interactions between the functional groups of polymers and drug surfaces seem to be important for successful nano-comminution. The stimuli responsive behavior of the hydrophobic copolymer induced the temperature dependence of particle size.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>19788919</pmid><doi>10.1016/j.ijpharm.2009.09.041</doi><tpages>8</tpages></addata></record> |
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| ispartof | International journal of pharmaceutics, 2010-01, Vol.384 (1), p.173-180 |
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| subjects | Amino Acid Sequence Amino Acids - chemistry Amino Acids - genetics Biological and medical sciences Dispersion General pharmacology Hydrophobic and Hydrophilic Interactions Medical sciences Molecular Sequence Data Nanocrystals Nanoparticles Nanoparticles - chemistry Nanotechnology - methods Particle engineering Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Polymers - chemistry Poorly water-soluble drug Solubility |
| title | Hydrophilic and hydrophobic amino acid copolymers for nano-comminution of poorly soluble drugs |
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