Microemulsion-Based Vaginal Gel of Clotrimazole: Formulation, In Vitro Evaluation, and Stability Studies
The objective of the present investigation was to develop and evaluate microemulsion-based gel for the vaginal delivery of clotrimazole (CMZ). The solubility of CMZ in oils and surfactants was evaluated to identify components of the microemulsion. The ternary diagram was plotted to identify the area...
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| Veröffentlicht in: | AAPS PharmSciTech 2009-06, Vol.10 (2), p.476-481, Article 476 |
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| creator | Bachhav, Yogeshwar G. Patravale, Vandana B. |
| description | The objective of the present investigation was to develop and evaluate microemulsion-based gel for the vaginal delivery of clotrimazole (CMZ). The solubility of CMZ in oils and surfactants was evaluated to identify components of the microemulsion. The ternary diagram was plotted to identify the area of microemulsion existence. Various gelling agents were evaluated for their potential to gel the CMZ microemulsion without affecting its structure. The bioadhesive potential and antifungal activity of the CMZ microemulsion-based gel (CMZ-MBG) was determined in comparison to the marketed clotrimazole gel (Candid-V® gel) by
in vitro
methods. The chemical stability of CMZ in CMZ-MBG was determined as per the International Conference on Harmonization guidelines. The CMZ microemulsion exhibited globule size of 48.4 nm and polydispersity index of 0.75. Carbopol® ETD 2020 could successfully gel the CMZ microemulsion without disturbing the structure. The CMZ-MBG showed significantly higher (
P
|
| doi_str_mv | 10.1208/s12249-009-9233-2 |
| format | Article |
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in vitro
methods. The chemical stability of CMZ in CMZ-MBG was determined as per the International Conference on Harmonization guidelines. The CMZ microemulsion exhibited globule size of 48.4 nm and polydispersity index of 0.75. Carbopol® ETD 2020 could successfully gel the CMZ microemulsion without disturbing the structure. The CMZ-MBG showed significantly higher (
P
< 0.05)
in vitro
bioadhesion and antifungal activity as compared to that of Candid-V® gel. The stability studies indicated that CMZ undergoes acidic pH-catalyzed degradation at all the storage conditions at the end of 3 months.</description><identifier>ISSN: 1530-9932</identifier><identifier>EISSN: 1530-9932</identifier><identifier>DOI: 10.1208/s12249-009-9233-2</identifier><identifier>PMID: 19381825</identifier><language>eng</language><publisher>Boston: Springer US</publisher><subject>Acrylic Resins ; Antifungal Agents - administration & dosage ; Biochemistry ; Biomedical and Life Sciences ; Biomedicine ; Biotechnology ; Chemistry, Pharmaceutical ; Clotrimazole - administration & dosage ; Clotrimazole - chemistry ; Clotrimazole - pharmacology ; Drug Stability ; Emulsions ; Microbial Sensitivity Tests ; Pharmacology/Toxicology ; Pharmacy ; Polyvinyls - administration & dosage ; Research Article ; Solubility ; Vaginal Creams, Foams, and Jellies</subject><ispartof>AAPS PharmSciTech, 2009-06, Vol.10 (2), p.476-481, Article 476</ispartof><rights>American Association of Pharmaceutical Scientists 2009</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c537t-61357b9091d8dd90fcf2c762f0a9995ca9a8bd26f1c1720110f72423ab60e6033</citedby><cites>FETCH-LOGICAL-c537t-61357b9091d8dd90fcf2c762f0a9995ca9a8bd26f1c1720110f72423ab60e6033</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC2690796/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC2690796/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,27923,27924,41487,42556,51318,53790,53792</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19381825$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bachhav, Yogeshwar G.</creatorcontrib><creatorcontrib>Patravale, Vandana B.</creatorcontrib><title>Microemulsion-Based Vaginal Gel of Clotrimazole: Formulation, In Vitro Evaluation, and Stability Studies</title><title>AAPS PharmSciTech</title><addtitle>AAPS PharmSciTech</addtitle><addtitle>AAPS PharmSciTech</addtitle><description>The objective of the present investigation was to develop and evaluate microemulsion-based gel for the vaginal delivery of clotrimazole (CMZ). The solubility of CMZ in oils and surfactants was evaluated to identify components of the microemulsion. The ternary diagram was plotted to identify the area of microemulsion existence. Various gelling agents were evaluated for their potential to gel the CMZ microemulsion without affecting its structure. The bioadhesive potential and antifungal activity of the CMZ microemulsion-based gel (CMZ-MBG) was determined in comparison to the marketed clotrimazole gel (Candid-V® gel) by
in vitro
methods. The chemical stability of CMZ in CMZ-MBG was determined as per the International Conference on Harmonization guidelines. The CMZ microemulsion exhibited globule size of 48.4 nm and polydispersity index of 0.75. Carbopol® ETD 2020 could successfully gel the CMZ microemulsion without disturbing the structure. The CMZ-MBG showed significantly higher (
P
< 0.05)
in vitro
bioadhesion and antifungal activity as compared to that of Candid-V® gel. The stability studies indicated that CMZ undergoes acidic pH-catalyzed degradation at all the storage conditions at the end of 3 months.</description><subject>Acrylic Resins</subject><subject>Antifungal Agents - administration & dosage</subject><subject>Biochemistry</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotechnology</subject><subject>Chemistry, Pharmaceutical</subject><subject>Clotrimazole - administration & dosage</subject><subject>Clotrimazole - chemistry</subject><subject>Clotrimazole - pharmacology</subject><subject>Drug Stability</subject><subject>Emulsions</subject><subject>Microbial Sensitivity Tests</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Polyvinyls - administration & dosage</subject><subject>Research Article</subject><subject>Solubility</subject><subject>Vaginal Creams, Foams, and Jellies</subject><issn>1530-9932</issn><issn>1530-9932</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkUtLxDAQx4Movj-AF8nJk9XJZJs2HgRdfIHiwcc1pG26RrKNJq2gn94su_i4KIHJkPnNn8z8CdlhcMAQysPIEEcyA5CZRM4zXCLrLOeQSclx-Ue-RjZifAZAziRfJWsplqzEfJ083dg6eDMdXLS-y051NA191BPbaUcvjKO-pWPn-2Cn-sM7c0TPfUi07hO-T686-mj74OnZm3bD4lF3Db3rdWWd7d9TNjTWxC2y0moXzfbi3iQP52f348vs-vbianxyndU5L_pMMJ4XlQTJmrJpJLR1i3UhsAUtpcxrLXVZNShaVrMCgTFoCxwh15UAI4DzTXI8130ZqqlpatP1QTv1MhsgvCuvrfpd6eyTmvg3hUJCIUUS2FsIBP86mNirqY21cU53xg9RiYIjCM7-BZGlg2KUQDYH06ZjDKb9-g0DNTNSzY1UyUg1M1Jh6tn9OcZ3x8K5BOAciKnUTUxQz34IybX4h-onY0ap7g</recordid><startdate>20090601</startdate><enddate>20090601</enddate><creator>Bachhav, Yogeshwar G.</creator><creator>Patravale, Vandana B.</creator><general>Springer US</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>7QO</scope><scope>7T7</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>M7N</scope><scope>P64</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>20090601</creationdate><title>Microemulsion-Based Vaginal Gel of Clotrimazole: Formulation, In Vitro Evaluation, and Stability Studies</title><author>Bachhav, Yogeshwar G. ; Patravale, Vandana B.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c537t-61357b9091d8dd90fcf2c762f0a9995ca9a8bd26f1c1720110f72423ab60e6033</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Acrylic Resins</topic><topic>Antifungal Agents - administration & dosage</topic><topic>Biochemistry</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Biotechnology</topic><topic>Chemistry, Pharmaceutical</topic><topic>Clotrimazole - administration & dosage</topic><topic>Clotrimazole - chemistry</topic><topic>Clotrimazole - pharmacology</topic><topic>Drug Stability</topic><topic>Emulsions</topic><topic>Microbial Sensitivity Tests</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Polyvinyls - administration & dosage</topic><topic>Research Article</topic><topic>Solubility</topic><topic>Vaginal Creams, Foams, and Jellies</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bachhav, Yogeshwar G.</creatorcontrib><creatorcontrib>Patravale, Vandana B.</creatorcontrib><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>Industrial and Applied Microbiology Abstracts (Microbiology A)</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>AAPS PharmSciTech</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bachhav, Yogeshwar G.</au><au>Patravale, Vandana B.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Microemulsion-Based Vaginal Gel of Clotrimazole: Formulation, In Vitro Evaluation, and Stability Studies</atitle><jtitle>AAPS PharmSciTech</jtitle><stitle>AAPS PharmSciTech</stitle><addtitle>AAPS PharmSciTech</addtitle><date>2009-06-01</date><risdate>2009</risdate><volume>10</volume><issue>2</issue><spage>476</spage><epage>481</epage><pages>476-481</pages><artnum>476</artnum><issn>1530-9932</issn><eissn>1530-9932</eissn><abstract>The objective of the present investigation was to develop and evaluate microemulsion-based gel for the vaginal delivery of clotrimazole (CMZ). The solubility of CMZ in oils and surfactants was evaluated to identify components of the microemulsion. The ternary diagram was plotted to identify the area of microemulsion existence. Various gelling agents were evaluated for their potential to gel the CMZ microemulsion without affecting its structure. The bioadhesive potential and antifungal activity of the CMZ microemulsion-based gel (CMZ-MBG) was determined in comparison to the marketed clotrimazole gel (Candid-V® gel) by
in vitro
methods. The chemical stability of CMZ in CMZ-MBG was determined as per the International Conference on Harmonization guidelines. The CMZ microemulsion exhibited globule size of 48.4 nm and polydispersity index of 0.75. Carbopol® ETD 2020 could successfully gel the CMZ microemulsion without disturbing the structure. The CMZ-MBG showed significantly higher (
P
< 0.05)
in vitro
bioadhesion and antifungal activity as compared to that of Candid-V® gel. The stability studies indicated that CMZ undergoes acidic pH-catalyzed degradation at all the storage conditions at the end of 3 months.</abstract><cop>Boston</cop><pub>Springer US</pub><pmid>19381825</pmid><doi>10.1208/s12249-009-9233-2</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| source | MEDLINE; EZB-FREE-00999 freely available EZB journals; PubMed Central; Free Full-Text Journals in Chemistry; SpringerLink Journals - AutoHoldings |
| subjects | Acrylic Resins Antifungal Agents - administration & dosage Biochemistry Biomedical and Life Sciences Biomedicine Biotechnology Chemistry, Pharmaceutical Clotrimazole - administration & dosage Clotrimazole - chemistry Clotrimazole - pharmacology Drug Stability Emulsions Microbial Sensitivity Tests Pharmacology/Toxicology Pharmacy Polyvinyls - administration & dosage Research Article Solubility Vaginal Creams, Foams, and Jellies |
| title | Microemulsion-Based Vaginal Gel of Clotrimazole: Formulation, In Vitro Evaluation, and Stability Studies |
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