Effect of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer on bioadhesion and release rate property of eplerenone pellets
The present study involved the design and development of oral bioadhesive pellets of eplerenone. A solid dispersion of eplerenone was developed with a hydrophilic carrier, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus ® ). Bioadhesive pellets were prepared fro...
Gespeichert in:
| Veröffentlicht in: | Drug development and industrial pharmacy 2017-05, Vol.43 (5), p.751-761 |
|---|---|
| Hauptverfasser: | , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 761 |
|---|---|
| container_issue | 5 |
| container_start_page | 751 |
| container_title | Drug development and industrial pharmacy |
| container_volume | 43 |
| creator | Kendre, Prakash Namdeo Chaudhari, Pravin Digambar |
| description | The present study involved the design and development of oral bioadhesive pellets of eplerenone. A solid dispersion of eplerenone was developed with a hydrophilic carrier, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus
®
). Bioadhesive pellets were prepared from this solid dispersion using a combination of HPMC K4M and Carbopol 934P. Both the solid dispersion and the pellets were evaluated for various physicochemical properties such as solubility, entrapment efficiency, drug content, surface morphology, mucoadhesion and swelling behavior. Analysis carried out using FT-IR, DSC and XRD found no interaction between the eplerenone and excipients. The solid dispersion had irregular-shaped smooth-surfaced particles of diameter 265 ± 105.5 μm. In TEM analysis, eplerenone particles of size 79-120 nm were found. The solubility and dissolution of eplerenone in the Soluplus
®
-based solid dispersion were 5.26 and 2.50 times greater, respectively. Investigation of the swelling behavior of the pellets showed that the thickness of the gel layer increased continuously over the duration of the study. Moreover, a correlation was observed between the thickness and strength of the gel layer and the percentage release. The mechanism of drug release was found to be non-Fickian (anomalous), with the release kinetics approaching first-order kinetics. The bioavailability of the eplerenone bioadhesive pellet formulation was studied using Wistar rats and was found to be improved. An in vivo mucoadhesion study showed that the pellets are retained for 24 h in rabbits. It was concluded that Soluplus
®
had a positive effect on the solubility and dissolution of pellets without affecting the bioadhesion. |
| doi_str_mv | 10.1080/03639045.2016.1220570 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_1859711324</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>1859711324</sourcerecordid><originalsourceid>FETCH-LOGICAL-c366t-a3bb54577f3bd0eabca06ddd9bb0dc7fffc890bf9f23f3377257ee0dd7982d1a3</originalsourceid><addsrcrecordid>eNp9kc9u1DAQxi0EokvhEUA-csniP3G8uYGqApUqcYGzNbHHbZATB9sLynvwwDjsFm49zWjmN9830kfIa872nB3YOyY72bNW7QXj3Z4LwZRmT8iOK8EapTvxlOw2ptmgC_Ii5--McdEr9ZxcCN32rWrljvy-9h5todHTJYb15zivgVpYUgxgC0zN_ylYLFDw7wTL_RpwRnoXVhsDvUvgC7Vx202YaJzpMEZw95jH2sPsaMKAkJGmqkGr_oKprJsvLgETzrGqLRgClvySPPMQMr4610vy7eP116vPze2XTzdXH24bK7uuNCCHQbVKay8HxxAGC6xzzvXDwJzV3nt76Nngey-kl1JroTQic073B-E4yEvy9qRb3_lxxFzMNGZbf4AZ4zEbflC95lyKtqLqhNoUc07ozZLGCdJqODNbIOYhELMFYs6B1Ls3Z4vjMKH7d_WQQAXen4Bx9jFN8Cum4EyBNcTkE8x2zEY-7vEHRlygBA</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>1859711324</pqid></control><display><type>article</type><title>Effect of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer on bioadhesion and release rate property of eplerenone pellets</title><source>MEDLINE</source><source>Business Source Complete</source><creator>Kendre, Prakash Namdeo ; Chaudhari, Pravin Digambar</creator><creatorcontrib>Kendre, Prakash Namdeo ; Chaudhari, Pravin Digambar</creatorcontrib><description>The present study involved the design and development of oral bioadhesive pellets of eplerenone. A solid dispersion of eplerenone was developed with a hydrophilic carrier, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus
®
). Bioadhesive pellets were prepared from this solid dispersion using a combination of HPMC K4M and Carbopol 934P. Both the solid dispersion and the pellets were evaluated for various physicochemical properties such as solubility, entrapment efficiency, drug content, surface morphology, mucoadhesion and swelling behavior. Analysis carried out using FT-IR, DSC and XRD found no interaction between the eplerenone and excipients. The solid dispersion had irregular-shaped smooth-surfaced particles of diameter 265 ± 105.5 μm. In TEM analysis, eplerenone particles of size 79-120 nm were found. The solubility and dissolution of eplerenone in the Soluplus
®
-based solid dispersion were 5.26 and 2.50 times greater, respectively. Investigation of the swelling behavior of the pellets showed that the thickness of the gel layer increased continuously over the duration of the study. Moreover, a correlation was observed between the thickness and strength of the gel layer and the percentage release. The mechanism of drug release was found to be non-Fickian (anomalous), with the release kinetics approaching first-order kinetics. The bioavailability of the eplerenone bioadhesive pellet formulation was studied using Wistar rats and was found to be improved. An in vivo mucoadhesion study showed that the pellets are retained for 24 h in rabbits. It was concluded that Soluplus
®
had a positive effect on the solubility and dissolution of pellets without affecting the bioadhesion.</description><identifier>ISSN: 0363-9045</identifier><identifier>EISSN: 1520-5762</identifier><identifier>DOI: 10.1080/03639045.2016.1220570</identifier><identifier>PMID: 27494543</identifier><language>eng</language><publisher>England: Taylor & Francis</publisher><subject>Adhesiveness - drug effects ; Administration, Oral ; Animals ; Bioadhesive pellets ; Biological Availability ; Chemistry, Pharmaceutical - methods ; Drug Implants - chemistry ; Drug Implants - metabolism ; Drug Liberation - drug effects ; eplerenone ; Excipients - chemistry ; gel strength ; Kinetics ; Particle Size ; Polyethylene Glycols - chemistry ; Polyvinyls - chemistry ; Rabbits ; Rats ; Rats, Wistar ; solid dispersion ; Solubility ; Soluplus ; Spectroscopy, Fourier Transform Infrared - methods ; Spironolactone - analogs & derivatives ; Spironolactone - chemistry ; Spironolactone - metabolism</subject><ispartof>Drug development and industrial pharmacy, 2017-05, Vol.43 (5), p.751-761</ispartof><rights>2016 Informa UK Limited, trading as Taylor & Francis Group 2016</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c366t-a3bb54577f3bd0eabca06ddd9bb0dc7fffc890bf9f23f3377257ee0dd7982d1a3</citedby><cites>FETCH-LOGICAL-c366t-a3bb54577f3bd0eabca06ddd9bb0dc7fffc890bf9f23f3377257ee0dd7982d1a3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27494543$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kendre, Prakash Namdeo</creatorcontrib><creatorcontrib>Chaudhari, Pravin Digambar</creatorcontrib><title>Effect of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer on bioadhesion and release rate property of eplerenone pellets</title><title>Drug development and industrial pharmacy</title><addtitle>Drug Dev Ind Pharm</addtitle><description>The present study involved the design and development of oral bioadhesive pellets of eplerenone. A solid dispersion of eplerenone was developed with a hydrophilic carrier, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus
®
). Bioadhesive pellets were prepared from this solid dispersion using a combination of HPMC K4M and Carbopol 934P. Both the solid dispersion and the pellets were evaluated for various physicochemical properties such as solubility, entrapment efficiency, drug content, surface morphology, mucoadhesion and swelling behavior. Analysis carried out using FT-IR, DSC and XRD found no interaction between the eplerenone and excipients. The solid dispersion had irregular-shaped smooth-surfaced particles of diameter 265 ± 105.5 μm. In TEM analysis, eplerenone particles of size 79-120 nm were found. The solubility and dissolution of eplerenone in the Soluplus
®
-based solid dispersion were 5.26 and 2.50 times greater, respectively. Investigation of the swelling behavior of the pellets showed that the thickness of the gel layer increased continuously over the duration of the study. Moreover, a correlation was observed between the thickness and strength of the gel layer and the percentage release. The mechanism of drug release was found to be non-Fickian (anomalous), with the release kinetics approaching first-order kinetics. The bioavailability of the eplerenone bioadhesive pellet formulation was studied using Wistar rats and was found to be improved. An in vivo mucoadhesion study showed that the pellets are retained for 24 h in rabbits. It was concluded that Soluplus
®
had a positive effect on the solubility and dissolution of pellets without affecting the bioadhesion.</description><subject>Adhesiveness - drug effects</subject><subject>Administration, Oral</subject><subject>Animals</subject><subject>Bioadhesive pellets</subject><subject>Biological Availability</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>Drug Implants - chemistry</subject><subject>Drug Implants - metabolism</subject><subject>Drug Liberation - drug effects</subject><subject>eplerenone</subject><subject>Excipients - chemistry</subject><subject>gel strength</subject><subject>Kinetics</subject><subject>Particle Size</subject><subject>Polyethylene Glycols - chemistry</subject><subject>Polyvinyls - chemistry</subject><subject>Rabbits</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>solid dispersion</subject><subject>Solubility</subject><subject>Soluplus</subject><subject>Spectroscopy, Fourier Transform Infrared - methods</subject><subject>Spironolactone - analogs & derivatives</subject><subject>Spironolactone - chemistry</subject><subject>Spironolactone - metabolism</subject><issn>0363-9045</issn><issn>1520-5762</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kc9u1DAQxi0EokvhEUA-csniP3G8uYGqApUqcYGzNbHHbZATB9sLynvwwDjsFm49zWjmN9830kfIa872nB3YOyY72bNW7QXj3Z4LwZRmT8iOK8EapTvxlOw2ptmgC_Ii5--McdEr9ZxcCN32rWrljvy-9h5todHTJYb15zivgVpYUgxgC0zN_ylYLFDw7wTL_RpwRnoXVhsDvUvgC7Vx202YaJzpMEZw95jH2sPsaMKAkJGmqkGr_oKprJsvLgETzrGqLRgClvySPPMQMr4610vy7eP116vPze2XTzdXH24bK7uuNCCHQbVKay8HxxAGC6xzzvXDwJzV3nt76Nngey-kl1JroTQic073B-E4yEvy9qRb3_lxxFzMNGZbf4AZ4zEbflC95lyKtqLqhNoUc07ozZLGCdJqODNbIOYhELMFYs6B1Ls3Z4vjMKH7d_WQQAXen4Bx9jFN8Cum4EyBNcTkE8x2zEY-7vEHRlygBA</recordid><startdate>20170504</startdate><enddate>20170504</enddate><creator>Kendre, Prakash Namdeo</creator><creator>Chaudhari, Pravin Digambar</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>20170504</creationdate><title>Effect of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer on bioadhesion and release rate property of eplerenone pellets</title><author>Kendre, Prakash Namdeo ; Chaudhari, Pravin Digambar</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c366t-a3bb54577f3bd0eabca06ddd9bb0dc7fffc890bf9f23f3377257ee0dd7982d1a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Adhesiveness - drug effects</topic><topic>Administration, Oral</topic><topic>Animals</topic><topic>Bioadhesive pellets</topic><topic>Biological Availability</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>Drug Implants - chemistry</topic><topic>Drug Implants - metabolism</topic><topic>Drug Liberation - drug effects</topic><topic>eplerenone</topic><topic>Excipients - chemistry</topic><topic>gel strength</topic><topic>Kinetics</topic><topic>Particle Size</topic><topic>Polyethylene Glycols - chemistry</topic><topic>Polyvinyls - chemistry</topic><topic>Rabbits</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>solid dispersion</topic><topic>Solubility</topic><topic>Soluplus</topic><topic>Spectroscopy, Fourier Transform Infrared - methods</topic><topic>Spironolactone - analogs & derivatives</topic><topic>Spironolactone - chemistry</topic><topic>Spironolactone - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kendre, Prakash Namdeo</creatorcontrib><creatorcontrib>Chaudhari, Pravin Digambar</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>Drug development and industrial pharmacy</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kendre, Prakash Namdeo</au><au>Chaudhari, Pravin Digambar</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer on bioadhesion and release rate property of eplerenone pellets</atitle><jtitle>Drug development and industrial pharmacy</jtitle><addtitle>Drug Dev Ind Pharm</addtitle><date>2017-05-04</date><risdate>2017</risdate><volume>43</volume><issue>5</issue><spage>751</spage><epage>761</epage><pages>751-761</pages><issn>0363-9045</issn><eissn>1520-5762</eissn><abstract>The present study involved the design and development of oral bioadhesive pellets of eplerenone. A solid dispersion of eplerenone was developed with a hydrophilic carrier, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus
®
). Bioadhesive pellets were prepared from this solid dispersion using a combination of HPMC K4M and Carbopol 934P. Both the solid dispersion and the pellets were evaluated for various physicochemical properties such as solubility, entrapment efficiency, drug content, surface morphology, mucoadhesion and swelling behavior. Analysis carried out using FT-IR, DSC and XRD found no interaction between the eplerenone and excipients. The solid dispersion had irregular-shaped smooth-surfaced particles of diameter 265 ± 105.5 μm. In TEM analysis, eplerenone particles of size 79-120 nm were found. The solubility and dissolution of eplerenone in the Soluplus
®
-based solid dispersion were 5.26 and 2.50 times greater, respectively. Investigation of the swelling behavior of the pellets showed that the thickness of the gel layer increased continuously over the duration of the study. Moreover, a correlation was observed between the thickness and strength of the gel layer and the percentage release. The mechanism of drug release was found to be non-Fickian (anomalous), with the release kinetics approaching first-order kinetics. The bioavailability of the eplerenone bioadhesive pellet formulation was studied using Wistar rats and was found to be improved. An in vivo mucoadhesion study showed that the pellets are retained for 24 h in rabbits. It was concluded that Soluplus
®
had a positive effect on the solubility and dissolution of pellets without affecting the bioadhesion.</abstract><cop>England</cop><pub>Taylor & Francis</pub><pmid>27494543</pmid><doi>10.1080/03639045.2016.1220570</doi><tpages>11</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0363-9045 |
| ispartof | Drug development and industrial pharmacy, 2017-05, Vol.43 (5), p.751-761 |
| issn | 0363-9045 1520-5762 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_1859711324 |
| source | MEDLINE; Business Source Complete |
| subjects | Adhesiveness - drug effects Administration, Oral Animals Bioadhesive pellets Biological Availability Chemistry, Pharmaceutical - methods Drug Implants - chemistry Drug Implants - metabolism Drug Liberation - drug effects eplerenone Excipients - chemistry gel strength Kinetics Particle Size Polyethylene Glycols - chemistry Polyvinyls - chemistry Rabbits Rats Rats, Wistar solid dispersion Solubility Soluplus Spectroscopy, Fourier Transform Infrared - methods Spironolactone - analogs & derivatives Spironolactone - chemistry Spironolactone - metabolism |
| title | Effect of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer on bioadhesion and release rate property of eplerenone pellets |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-06T21%3A29%3A02IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Effect%20of%20polyvinyl%20caprolactam-polyvinyl%20acetate-polyethylene%20glycol%20graft%20copolymer%20on%20bioadhesion%20and%20release%20rate%20property%20of%20eplerenone%20pellets&rft.jtitle=Drug%20development%20and%20industrial%20pharmacy&rft.au=Kendre,%20Prakash%20Namdeo&rft.date=2017-05-04&rft.volume=43&rft.issue=5&rft.spage=751&rft.epage=761&rft.pages=751-761&rft.issn=0363-9045&rft.eissn=1520-5762&rft_id=info:doi/10.1080/03639045.2016.1220570&rft_dat=%3Cproquest_cross%3E1859711324%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=1859711324&rft_id=info:pmid/27494543&rfr_iscdi=true |