The effect of PAMAM dendrimer concentration, generation size and surface functional group on the aqueous solubility of candesartan cilexetil
This article investigates the aqueous solubility of the poorly soluble drug candesartan cilexetil (CC) in the presence of poly(amidoamine) (PAMAM) dendrimers. The effect of variables such as concentration, generation size (G2-G4), and surface groups (NH 2 , COOH and TRIS) of PAMAMs on the aqueous so...
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| Veröffentlicht in: | Pharmaceutical development and technology 2017-02, Vol.22 (1), p.111-121 |
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| creator | Ertürk, Ali Serol Gürbüz, Mustafa Ulvi Tülü, Metin |
| description | This article investigates the aqueous solubility of the poorly soluble drug candesartan cilexetil (CC) in the presence of poly(amidoamine) (PAMAM) dendrimers. The effect of variables such as concentration, generation size (G2-G4), and surface groups (NH
2
, COOH and TRIS) of PAMAMs on the aqueous solubility of CC was studied. A two-factor factorial (3 × 3) ANOVA design was used to study the effect of generation size and surface functional group of the PAMAMs. The results showed that the aqueous solubility of CC in the presence of carboxyl and TRIS-terminated PAMAMs was higher than those of amine-terminated PAMAMs, and the effect of surface functional group of the PAMAMs on the aqueous solubility of CC was dependent on the generation size (p G3.COOH (3456)>G4.TRIS (2362)>G2.COOH (1013)>G3.TRIS (749)>G2.TRIS (293)>G4.NH
2
(91)>G3.NH
2
(50)>G2.NH
2
(37). The CC-PAMAM dendrimer inclusion complexes were characterized by UV-Vis, attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) and differential thermal analysis (DTA) techniques. Regarding the results of these techniques, improvement in the solubility of CC is expected primarily through the intermolecular hydrogen bonding between the drug and internal tertiary and surface functional groups of the studied PAMAMs. |
| doi_str_mv | 10.1080/10837450.2016.1219372 |
| format | Article |
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2
, COOH and TRIS) of PAMAMs on the aqueous solubility of CC was studied. A two-factor factorial (3 × 3) ANOVA design was used to study the effect of generation size and surface functional group of the PAMAMs. The results showed that the aqueous solubility of CC in the presence of carboxyl and TRIS-terminated PAMAMs was higher than those of amine-terminated PAMAMs, and the effect of surface functional group of the PAMAMs on the aqueous solubility of CC was dependent on the generation size (p < 0.05). The sequence of the observed solubility fold enhancement due to PAMAMs was G4.COOH (8378)>G3.COOH (3456)>G4.TRIS (2362)>G2.COOH (1013)>G3.TRIS (749)>G2.TRIS (293)>G4.NH
2
(91)>G3.NH
2
(50)>G2.NH
2
(37). The CC-PAMAM dendrimer inclusion complexes were characterized by UV-Vis, attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) and differential thermal analysis (DTA) techniques. Regarding the results of these techniques, improvement in the solubility of CC is expected primarily through the intermolecular hydrogen bonding between the drug and internal tertiary and surface functional groups of the studied PAMAMs.</description><identifier>ISSN: 1083-7450</identifier><identifier>EISSN: 1097-9867</identifier><identifier>DOI: 10.1080/10837450.2016.1219372</identifier><identifier>PMID: 27484586</identifier><language>eng</language><publisher>England: Taylor & Francis</publisher><subject>Analysis of Variance ; Angiotensin II Type 1 Receptor Blockers - chemistry ; Antihypertensive Agents - chemistry ; Benzimidazoles - chemistry ; Biphenyl Compounds - chemistry ; candesartan cilexetil ; Dendrimers - chemistry ; Drug Carriers - chemistry ; inclusion complex ; PAMAM dendrimers ; Solubility ; solubilization ; Tetrazoles - chemistry ; Water - chemistry</subject><ispartof>Pharmaceutical development and technology, 2017-02, Vol.22 (1), p.111-121</ispartof><rights>2016 Informa UK Limited, trading as Taylor & Francis Group 2016</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c413t-fb1fa6910d6b531c0c2b25f931d6caee42b895944936469cbde2adf976bd65983</citedby><cites>FETCH-LOGICAL-c413t-fb1fa6910d6b531c0c2b25f931d6caee42b895944936469cbde2adf976bd65983</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27903,27904</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27484586$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ertürk, Ali Serol</creatorcontrib><creatorcontrib>Gürbüz, Mustafa Ulvi</creatorcontrib><creatorcontrib>Tülü, Metin</creatorcontrib><title>The effect of PAMAM dendrimer concentration, generation size and surface functional group on the aqueous solubility of candesartan cilexetil</title><title>Pharmaceutical development and technology</title><addtitle>Pharm Dev Technol</addtitle><description>This article investigates the aqueous solubility of the poorly soluble drug candesartan cilexetil (CC) in the presence of poly(amidoamine) (PAMAM) dendrimers. The effect of variables such as concentration, generation size (G2-G4), and surface groups (NH
2
, COOH and TRIS) of PAMAMs on the aqueous solubility of CC was studied. A two-factor factorial (3 × 3) ANOVA design was used to study the effect of generation size and surface functional group of the PAMAMs. The results showed that the aqueous solubility of CC in the presence of carboxyl and TRIS-terminated PAMAMs was higher than those of amine-terminated PAMAMs, and the effect of surface functional group of the PAMAMs on the aqueous solubility of CC was dependent on the generation size (p < 0.05). The sequence of the observed solubility fold enhancement due to PAMAMs was G4.COOH (8378)>G3.COOH (3456)>G4.TRIS (2362)>G2.COOH (1013)>G3.TRIS (749)>G2.TRIS (293)>G4.NH
2
(91)>G3.NH
2
(50)>G2.NH
2
(37). The CC-PAMAM dendrimer inclusion complexes were characterized by UV-Vis, attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) and differential thermal analysis (DTA) techniques. Regarding the results of these techniques, improvement in the solubility of CC is expected primarily through the intermolecular hydrogen bonding between the drug and internal tertiary and surface functional groups of the studied PAMAMs.</description><subject>Analysis of Variance</subject><subject>Angiotensin II Type 1 Receptor Blockers - chemistry</subject><subject>Antihypertensive Agents - chemistry</subject><subject>Benzimidazoles - chemistry</subject><subject>Biphenyl Compounds - chemistry</subject><subject>candesartan cilexetil</subject><subject>Dendrimers - chemistry</subject><subject>Drug Carriers - chemistry</subject><subject>inclusion complex</subject><subject>PAMAM dendrimers</subject><subject>Solubility</subject><subject>solubilization</subject><subject>Tetrazoles - chemistry</subject><subject>Water - chemistry</subject><issn>1083-7450</issn><issn>1097-9867</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kc2OFCEUhStG4_zoI2hYurBafqoo2NmZ6GgyE12Ma0LBZcTQ0AKVsX0GH1oq3ePSDdzkfueem3u67hXBG4IFftceNg0j3lBM-IZQItlEn3TnBMupl4JPT9dasH6FzrqLUn5gTITE4_PujE6DGEbBz7s_d98BgXNgKkoOfd3ebm-RhWiz30FGJkUDsWZdfYpv0T1EONao-N-AdLSoLNlpA8gt0awdHdB9TsseNai24frnAmkpqKSwzD74eliNTJNC0bnqiIwP8AuqDy-6Z06HAi9P_2X37eOHu6tP_c2X689X25veDITV3s3EaS4JtnweGTHY0JmOTjJiudEAA52FHOUwSMYHLs1sgWrr5MRny0cp2GX35jh3n1PbrlS188VACDquqyoiKJ8GLAVt6HhETU6lZHBq3y6j80ERrNYg1GMQag1CnYJoutcni2Xegf2nerx8A94fAR9dyjv9kHKwqupDSNllHY0viv3f4y_L6ppF</recordid><startdate>20170201</startdate><enddate>20170201</enddate><creator>Ertürk, Ali Serol</creator><creator>Gürbüz, Mustafa Ulvi</creator><creator>Tülü, Metin</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>20170201</creationdate><title>The effect of PAMAM dendrimer concentration, generation size and surface functional group on the aqueous solubility of candesartan cilexetil</title><author>Ertürk, Ali Serol ; Gürbüz, Mustafa Ulvi ; Tülü, Metin</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c413t-fb1fa6910d6b531c0c2b25f931d6caee42b895944936469cbde2adf976bd65983</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Analysis of Variance</topic><topic>Angiotensin II Type 1 Receptor Blockers - chemistry</topic><topic>Antihypertensive Agents - chemistry</topic><topic>Benzimidazoles - chemistry</topic><topic>Biphenyl Compounds - chemistry</topic><topic>candesartan cilexetil</topic><topic>Dendrimers - chemistry</topic><topic>Drug Carriers - chemistry</topic><topic>inclusion complex</topic><topic>PAMAM dendrimers</topic><topic>Solubility</topic><topic>solubilization</topic><topic>Tetrazoles - chemistry</topic><topic>Water - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ertürk, Ali Serol</creatorcontrib><creatorcontrib>Gürbüz, Mustafa Ulvi</creatorcontrib><creatorcontrib>Tülü, Metin</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>Pharmaceutical development and technology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ertürk, Ali Serol</au><au>Gürbüz, Mustafa Ulvi</au><au>Tülü, Metin</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The effect of PAMAM dendrimer concentration, generation size and surface functional group on the aqueous solubility of candesartan cilexetil</atitle><jtitle>Pharmaceutical development and technology</jtitle><addtitle>Pharm Dev Technol</addtitle><date>2017-02-01</date><risdate>2017</risdate><volume>22</volume><issue>1</issue><spage>111</spage><epage>121</epage><pages>111-121</pages><issn>1083-7450</issn><eissn>1097-9867</eissn><abstract>This article investigates the aqueous solubility of the poorly soluble drug candesartan cilexetil (CC) in the presence of poly(amidoamine) (PAMAM) dendrimers. The effect of variables such as concentration, generation size (G2-G4), and surface groups (NH
2
, COOH and TRIS) of PAMAMs on the aqueous solubility of CC was studied. A two-factor factorial (3 × 3) ANOVA design was used to study the effect of generation size and surface functional group of the PAMAMs. The results showed that the aqueous solubility of CC in the presence of carboxyl and TRIS-terminated PAMAMs was higher than those of amine-terminated PAMAMs, and the effect of surface functional group of the PAMAMs on the aqueous solubility of CC was dependent on the generation size (p < 0.05). The sequence of the observed solubility fold enhancement due to PAMAMs was G4.COOH (8378)>G3.COOH (3456)>G4.TRIS (2362)>G2.COOH (1013)>G3.TRIS (749)>G2.TRIS (293)>G4.NH
2
(91)>G3.NH
2
(50)>G2.NH
2
(37). The CC-PAMAM dendrimer inclusion complexes were characterized by UV-Vis, attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) and differential thermal analysis (DTA) techniques. Regarding the results of these techniques, improvement in the solubility of CC is expected primarily through the intermolecular hydrogen bonding between the drug and internal tertiary and surface functional groups of the studied PAMAMs.</abstract><cop>England</cop><pub>Taylor & Francis</pub><pmid>27484586</pmid><doi>10.1080/10837450.2016.1219372</doi><tpages>11</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Analysis of Variance Angiotensin II Type 1 Receptor Blockers - chemistry Antihypertensive Agents - chemistry Benzimidazoles - chemistry Biphenyl Compounds - chemistry candesartan cilexetil Dendrimers - chemistry Drug Carriers - chemistry inclusion complex PAMAM dendrimers Solubility solubilization Tetrazoles - chemistry Water - chemistry |
| title | The effect of PAMAM dendrimer concentration, generation size and surface functional group on the aqueous solubility of candesartan cilexetil |
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