Stimulatory Effects of Soluplus® on Flufenamic Acid β-Cyclodextrin Supramolecular Complex: Physicochemical Characterization and Pre-clinical Anti-inflammatory Assessment
The present study demonstrates the solubility and dissolution of flufenamic acid (FLF)/β-cyclodextrin (β-CD)/Soluplus® supramolecular ternary inclusion complex. The binary and ternary inclusion complexes were prepared using solvent evaporation and the microwave irradiation method. The prepared inclu...
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creator | Alshehri, Sultan Imam, Syed Sarim Altamimi, Mohammad A. Hussain, Afzal Shakeel, Faiyaz Alshehri, Abdulhakeem |
description | The present study demonstrates the solubility and dissolution of flufenamic acid (FLF)/β-cyclodextrin (β-CD)/Soluplus® supramolecular ternary inclusion complex. The binary and ternary inclusion complexes were prepared using solvent evaporation and the microwave irradiation method. The prepared inclusion complexes were evaluated for physicochemical characterization and anti-inflammatory activity using a murine paw edema mol. The phase solubility studies demonstrated 4.59-fold and 17.54-fold enhancements in FLF solubility with β-CD alone and β-CD:Soluplus® combination compared with pure FLF, respectively. The
in vitro
drug release results revealed a significant improvement (
P
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doi_str_mv | 10.1208/s12249-020-01684-2 |
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in vitro
drug release results revealed a significant improvement (
P
< 0.05) in the release pattern compared with pure FLF. Maximum release was found with flufenamic acid binary and ternary complexes prepared using the microwave irradiation method,
i.e.
, 75.23 ± 3.12% and 95.36 ± 3.23% in 60 min, respectively. The physicochemical characterization results showed complex formation and conversion of the crystalline form of FLF to an amorphous form. The SEM study revealed the presence of a more agglomerated and amorphous structure of the solid particles, which confirmed the formation of complexes. The anti-inflammatory effect of the complex was higher than pure FLF. Therefore, the FLF:β-CD:Soluplus® inclusion complex may be a very valuable formulation with improved solubility, dissolution, and anti-inflammatory effect.</description><identifier>ISSN: 1530-9932</identifier><identifier>EISSN: 1530-9932</identifier><identifier>DOI: 10.1208/s12249-020-01684-2</identifier><identifier>PMID: 32430787</identifier><language>eng</language><publisher>Cham: Springer International Publishing</publisher><subject>Biochemistry ; Biomedical and Life Sciences ; Biomedicine ; Biotechnology ; Pharmacology/Toxicology ; Pharmacy ; Research Article</subject><ispartof>AAPS PharmSciTech, 2020-05, Vol.21 (5), p.145-145, Article 145</ispartof><rights>American Association of Pharmaceutical Scientists 2020</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c347t-9a70f5982d8321495ad4404e7561974bb84ed83715c08a089b98230f072144ec3</citedby><cites>FETCH-LOGICAL-c347t-9a70f5982d8321495ad4404e7561974bb84ed83715c08a089b98230f072144ec3</cites><orcidid>0000-0002-0922-9819</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1208/s12249-020-01684-2$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1208/s12249-020-01684-2$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,776,780,27901,27902,41464,42533,51294</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/32430787$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Alshehri, Sultan</creatorcontrib><creatorcontrib>Imam, Syed Sarim</creatorcontrib><creatorcontrib>Altamimi, Mohammad A.</creatorcontrib><creatorcontrib>Hussain, Afzal</creatorcontrib><creatorcontrib>Shakeel, Faiyaz</creatorcontrib><creatorcontrib>Alshehri, Abdulhakeem</creatorcontrib><title>Stimulatory Effects of Soluplus® on Flufenamic Acid β-Cyclodextrin Supramolecular Complex: Physicochemical Characterization and Pre-clinical Anti-inflammatory Assessment</title><title>AAPS PharmSciTech</title><addtitle>AAPS PharmSciTech</addtitle><addtitle>AAPS PharmSciTech</addtitle><description>The present study demonstrates the solubility and dissolution of flufenamic acid (FLF)/β-cyclodextrin (β-CD)/Soluplus® supramolecular ternary inclusion complex. The binary and ternary inclusion complexes were prepared using solvent evaporation and the microwave irradiation method. The prepared inclusion complexes were evaluated for physicochemical characterization and anti-inflammatory activity using a murine paw edema mol. The phase solubility studies demonstrated 4.59-fold and 17.54-fold enhancements in FLF solubility with β-CD alone and β-CD:Soluplus® combination compared with pure FLF, respectively. The
in vitro
drug release results revealed a significant improvement (
P
< 0.05) in the release pattern compared with pure FLF. Maximum release was found with flufenamic acid binary and ternary complexes prepared using the microwave irradiation method,
i.e.
, 75.23 ± 3.12% and 95.36 ± 3.23% in 60 min, respectively. The physicochemical characterization results showed complex formation and conversion of the crystalline form of FLF to an amorphous form. The SEM study revealed the presence of a more agglomerated and amorphous structure of the solid particles, which confirmed the formation of complexes. The anti-inflammatory effect of the complex was higher than pure FLF. Therefore, the FLF:β-CD:Soluplus® inclusion complex may be a very valuable formulation with improved solubility, dissolution, and anti-inflammatory effect.</description><subject>Biochemistry</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotechnology</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Research Article</subject><issn>1530-9932</issn><issn>1530-9932</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><recordid>eNp9kc1qFTEYhgdRbK3egAvJ0k00f9OZuDsMrRUKFo6uQ07mG09KfsYkAz29JcGFl9AL8JqMnSquXCXwPe9DvrxN85KSN5SR_m2mjAmJCSOY0NNeYPaoOaYtJ1hKzh7_cz9qnuV8TQjjVPKnzRFngpOu746bb9ti_eJ0iemAzqYJTMkoTmgb3TK7Jd99RzGgc7dMELS3Bm2MHdHPH3g4GBdHuCnJBrRd5qR9dGCqKqEh-tnBzTt0tT9ka6LZQ41qh4a9TtoUSPZWF1vFOozoKgE2zoZ7YhOKxTZMTnu_PmqTM-TsIZTnzZNJuwwvHs6T5vP52afhAl9-fP9h2Fxiw0VXsNQdmVrZs7HnjArZ6lEIIqBrT6nsxG7XC6ijjraG9Jr0cldZTibSVVqA4SfN69U7p_h1gVyUt9mAczpAXLJigtSPFZKLirIVNSnmnGBSc7Jep4OiRP0uSa0lqVqSui9JsRp69eBfdh7Gv5E_rVSAr0Cuo_AFkrqOSwp15_9pfwGAZ6GA</recordid><startdate>20200519</startdate><enddate>20200519</enddate><creator>Alshehri, Sultan</creator><creator>Imam, Syed Sarim</creator><creator>Altamimi, Mohammad A.</creator><creator>Hussain, Afzal</creator><creator>Shakeel, Faiyaz</creator><creator>Alshehri, Abdulhakeem</creator><general>Springer International Publishing</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0002-0922-9819</orcidid></search><sort><creationdate>20200519</creationdate><title>Stimulatory Effects of Soluplus® on Flufenamic Acid β-Cyclodextrin Supramolecular Complex: Physicochemical Characterization and Pre-clinical Anti-inflammatory Assessment</title><author>Alshehri, Sultan ; Imam, Syed Sarim ; Altamimi, Mohammad A. ; Hussain, Afzal ; Shakeel, Faiyaz ; Alshehri, Abdulhakeem</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c347t-9a70f5982d8321495ad4404e7561974bb84ed83715c08a089b98230f072144ec3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>Biochemistry</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Biotechnology</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Research Article</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Alshehri, Sultan</creatorcontrib><creatorcontrib>Imam, Syed Sarim</creatorcontrib><creatorcontrib>Altamimi, Mohammad A.</creatorcontrib><creatorcontrib>Hussain, Afzal</creatorcontrib><creatorcontrib>Shakeel, Faiyaz</creatorcontrib><creatorcontrib>Alshehri, Abdulhakeem</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>AAPS PharmSciTech</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Alshehri, Sultan</au><au>Imam, Syed Sarim</au><au>Altamimi, Mohammad A.</au><au>Hussain, Afzal</au><au>Shakeel, Faiyaz</au><au>Alshehri, Abdulhakeem</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Stimulatory Effects of Soluplus® on Flufenamic Acid β-Cyclodextrin Supramolecular Complex: Physicochemical Characterization and Pre-clinical Anti-inflammatory Assessment</atitle><jtitle>AAPS PharmSciTech</jtitle><stitle>AAPS PharmSciTech</stitle><addtitle>AAPS PharmSciTech</addtitle><date>2020-05-19</date><risdate>2020</risdate><volume>21</volume><issue>5</issue><spage>145</spage><epage>145</epage><pages>145-145</pages><artnum>145</artnum><issn>1530-9932</issn><eissn>1530-9932</eissn><abstract>The present study demonstrates the solubility and dissolution of flufenamic acid (FLF)/β-cyclodextrin (β-CD)/Soluplus® supramolecular ternary inclusion complex. The binary and ternary inclusion complexes were prepared using solvent evaporation and the microwave irradiation method. The prepared inclusion complexes were evaluated for physicochemical characterization and anti-inflammatory activity using a murine paw edema mol. The phase solubility studies demonstrated 4.59-fold and 17.54-fold enhancements in FLF solubility with β-CD alone and β-CD:Soluplus® combination compared with pure FLF, respectively. The
in vitro
drug release results revealed a significant improvement (
P
< 0.05) in the release pattern compared with pure FLF. Maximum release was found with flufenamic acid binary and ternary complexes prepared using the microwave irradiation method,
i.e.
, 75.23 ± 3.12% and 95.36 ± 3.23% in 60 min, respectively. The physicochemical characterization results showed complex formation and conversion of the crystalline form of FLF to an amorphous form. The SEM study revealed the presence of a more agglomerated and amorphous structure of the solid particles, which confirmed the formation of complexes. The anti-inflammatory effect of the complex was higher than pure FLF. Therefore, the FLF:β-CD:Soluplus® inclusion complex may be a very valuable formulation with improved solubility, dissolution, and anti-inflammatory effect.</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><pmid>32430787</pmid><doi>10.1208/s12249-020-01684-2</doi><tpages>1</tpages><orcidid>https://orcid.org/0000-0002-0922-9819</orcidid></addata></record> |
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subjects | Biochemistry Biomedical and Life Sciences Biomedicine Biotechnology Pharmacology/Toxicology Pharmacy Research Article |
title | Stimulatory Effects of Soluplus® on Flufenamic Acid β-Cyclodextrin Supramolecular Complex: Physicochemical Characterization and Pre-clinical Anti-inflammatory Assessment |
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