Stability of sulforaphane for topical formulation
Abstract Context: Sulforaphane (SFN) is a natural compound that has been investigated as a chemopreventive agent. SFN has been shown to inhibit the activator-protein-1 (AP-1) transcription factor and may be effective for inhibition of ultraviolet (UV) induced skin carcinogenesis. This study was desi...
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| Veröffentlicht in: | Drug development and industrial pharmacy 2014-04, Vol.40 (4), p.494-502 |
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| creator | Franklin, Stephen J. Dickinson, Sally E. Karlage, Kelly L. Bowden, G. T. Myrdal, Paul B. |
| description | Abstract
Context: Sulforaphane (SFN) is a natural compound that has been investigated as a chemopreventive agent. SFN has been shown to inhibit the activator-protein-1 (AP-1) transcription factor and may be effective for inhibition of ultraviolet (UV) induced skin carcinogenesis. This study was designed to investigate the stability of SFN as a function of pH, temperature and in various solvents and formulations.
Materials and methods: Stability was analyzed using high-performance liquid chromatography. A potential lead formulation was identified and evaluated in vivo.
Results: SFN was determined to undergo apparent first-order degradation kinetics for the conditions explored. It was observed that SFN undergoes base catalyzed degradation. Buffer species and solvent type impacts stability as well. SFN was found to be very sensitive to temperature with degradation rate changing by a factor of nearly 3.1 for every 10 °C change in temperature (at pH 4.0). SFN completely degraded after 30 days in a conventional pharmaceutical cream formulation. Improved stability was observed in organic formulation components. Stability studies were conducted on two nonaqueous topical formulations: a polyethylene glycol (PEG) ointment base and an organic oleaginous base.
Conclusion: Topically applied SFN in the PEG base formulation significantly reduced AP-1 activation after UV stimulation in the skin of a transgenic mouse model, indicating that SFN in this formulation retains efficacy in vivo. |
| doi_str_mv | 10.3109/03639045.2013.768634 |
| format | Article |
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Context: Sulforaphane (SFN) is a natural compound that has been investigated as a chemopreventive agent. SFN has been shown to inhibit the activator-protein-1 (AP-1) transcription factor and may be effective for inhibition of ultraviolet (UV) induced skin carcinogenesis. This study was designed to investigate the stability of SFN as a function of pH, temperature and in various solvents and formulations.
Materials and methods: Stability was analyzed using high-performance liquid chromatography. A potential lead formulation was identified and evaluated in vivo.
Results: SFN was determined to undergo apparent first-order degradation kinetics for the conditions explored. It was observed that SFN undergoes base catalyzed degradation. Buffer species and solvent type impacts stability as well. SFN was found to be very sensitive to temperature with degradation rate changing by a factor of nearly 3.1 for every 10 °C change in temperature (at pH 4.0). SFN completely degraded after 30 days in a conventional pharmaceutical cream formulation. Improved stability was observed in organic formulation components. Stability studies were conducted on two nonaqueous topical formulations: a polyethylene glycol (PEG) ointment base and an organic oleaginous base.
Conclusion: Topically applied SFN in the PEG base formulation significantly reduced AP-1 activation after UV stimulation in the skin of a transgenic mouse model, indicating that SFN in this formulation retains efficacy in vivo.</description><identifier>ISSN: 0363-9045</identifier><identifier>EISSN: 1520-5762</identifier><identifier>DOI: 10.3109/03639045.2013.768634</identifier><identifier>PMID: 23611476</identifier><language>eng</language><publisher>England: Informa Healthcare USA, Inc</publisher><subject>Activator-protein-1 ; Administration, Cutaneous ; Animals ; Anticarcinogenic Agents - administration & dosage ; Anticarcinogenic Agents - chemistry ; Anticarcinogenic Agents - pharmacology ; base catalysis ; Chromatography, High Pressure Liquid ; degradation ; Drug Stability ; Drug Storage ; Female ; Hydrogen-Ion Concentration ; hydrolysis ; in vivo ; isothiocyanate ; Isothiocyanates - administration & dosage ; Isothiocyanates - chemistry ; Isothiocyanates - pharmacology ; Kinetics ; Mice ; Mice, Transgenic ; Polyethylene Glycols - chemistry ; Skin - drug effects ; Skin - radiation effects ; Solvents - chemistry ; Temperature ; Time Factors ; Transcription Factor AP-1 - antagonists & inhibitors ; Ultraviolet Rays - adverse effects ; UVB</subject><ispartof>Drug development and industrial pharmacy, 2014-04, Vol.40 (4), p.494-502</ispartof><rights>2014 Informa Healthcare USA, Inc. All rights reserved: reproduction in whole or part not permitted 2014</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c519t-8b34fd9a1786b04d4c402504eb43e6d89f28a73f8fcfc04686b8109c2b8418223</citedby><cites>FETCH-LOGICAL-c519t-8b34fd9a1786b04d4c402504eb43e6d89f28a73f8fcfc04686b8109c2b8418223</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,315,781,785,886,27929,27930</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23611476$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Franklin, Stephen J.</creatorcontrib><creatorcontrib>Dickinson, Sally E.</creatorcontrib><creatorcontrib>Karlage, Kelly L.</creatorcontrib><creatorcontrib>Bowden, G. T.</creatorcontrib><creatorcontrib>Myrdal, Paul B.</creatorcontrib><title>Stability of sulforaphane for topical formulation</title><title>Drug development and industrial pharmacy</title><addtitle>Drug Dev Ind Pharm</addtitle><description>Abstract
Context: Sulforaphane (SFN) is a natural compound that has been investigated as a chemopreventive agent. SFN has been shown to inhibit the activator-protein-1 (AP-1) transcription factor and may be effective for inhibition of ultraviolet (UV) induced skin carcinogenesis. This study was designed to investigate the stability of SFN as a function of pH, temperature and in various solvents and formulations.
Materials and methods: Stability was analyzed using high-performance liquid chromatography. A potential lead formulation was identified and evaluated in vivo.
Results: SFN was determined to undergo apparent first-order degradation kinetics for the conditions explored. It was observed that SFN undergoes base catalyzed degradation. Buffer species and solvent type impacts stability as well. SFN was found to be very sensitive to temperature with degradation rate changing by a factor of nearly 3.1 for every 10 °C change in temperature (at pH 4.0). SFN completely degraded after 30 days in a conventional pharmaceutical cream formulation. Improved stability was observed in organic formulation components. Stability studies were conducted on two nonaqueous topical formulations: a polyethylene glycol (PEG) ointment base and an organic oleaginous base.
Conclusion: Topically applied SFN in the PEG base formulation significantly reduced AP-1 activation after UV stimulation in the skin of a transgenic mouse model, indicating that SFN in this formulation retains efficacy in vivo.</description><subject>Activator-protein-1</subject><subject>Administration, Cutaneous</subject><subject>Animals</subject><subject>Anticarcinogenic Agents - administration & dosage</subject><subject>Anticarcinogenic Agents - chemistry</subject><subject>Anticarcinogenic Agents - pharmacology</subject><subject>base catalysis</subject><subject>Chromatography, High Pressure Liquid</subject><subject>degradation</subject><subject>Drug Stability</subject><subject>Drug Storage</subject><subject>Female</subject><subject>Hydrogen-Ion Concentration</subject><subject>hydrolysis</subject><subject>in vivo</subject><subject>isothiocyanate</subject><subject>Isothiocyanates - administration & dosage</subject><subject>Isothiocyanates - chemistry</subject><subject>Isothiocyanates - pharmacology</subject><subject>Kinetics</subject><subject>Mice</subject><subject>Mice, Transgenic</subject><subject>Polyethylene Glycols - chemistry</subject><subject>Skin - drug effects</subject><subject>Skin - radiation effects</subject><subject>Solvents - chemistry</subject><subject>Temperature</subject><subject>Time Factors</subject><subject>Transcription Factor AP-1 - antagonists & inhibitors</subject><subject>Ultraviolet Rays - adverse effects</subject><subject>UVB</subject><issn>0363-9045</issn><issn>1520-5762</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMtOwzAQRS0EoqXwBwjlB1L8iuNsilDFS6rEAlhbjmMTV24cOS6of0-iUEQ3Xc1Ic--dmQPANYJzgmBxCwkjBaTZHENE5jnjjNATMEUZhmmWM3wKpoMkHTQTcNF1awgRLrLsHEwwYQjRnE0BeouytM7GXeJN0m2d8UG2tWx00ndJ9K1V0g39ZutktL65BGdGuk5f_dYZ-Hh8eF8-p6vXp5fl_SpVGSpiyktCTVVIlHNWQlpRRSHOINUlJZpVvDCYy5wYbpRRkPbnl7x_S-GSU8QxJjOwGHPbbbnRldJNDNKJNtiNDDvhpRWHk8bW4tN_CcI5hSzrA-gYoILvuqDNnxdBMSAUe4RiQChGhL3t5v_eP9OeWS-4GwW2GbDIbx9cJaLcOR9MkI2y3RB_dMXiIKHW0sVayaDF2m9D02M9fuMPnmyUYw</recordid><startdate>20140401</startdate><enddate>20140401</enddate><creator>Franklin, Stephen J.</creator><creator>Dickinson, Sally E.</creator><creator>Karlage, Kelly L.</creator><creator>Bowden, G. T.</creator><creator>Myrdal, Paul B.</creator><general>Informa Healthcare USA, Inc</general><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>5PM</scope></search><sort><creationdate>20140401</creationdate><title>Stability of sulforaphane for topical formulation</title><author>Franklin, Stephen J. ; Dickinson, Sally E. ; Karlage, Kelly L. ; Bowden, G. T. ; Myrdal, Paul B.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c519t-8b34fd9a1786b04d4c402504eb43e6d89f28a73f8fcfc04686b8109c2b8418223</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Activator-protein-1</topic><topic>Administration, Cutaneous</topic><topic>Animals</topic><topic>Anticarcinogenic Agents - administration & dosage</topic><topic>Anticarcinogenic Agents - chemistry</topic><topic>Anticarcinogenic Agents - pharmacology</topic><topic>base catalysis</topic><topic>Chromatography, High Pressure Liquid</topic><topic>degradation</topic><topic>Drug Stability</topic><topic>Drug Storage</topic><topic>Female</topic><topic>Hydrogen-Ion Concentration</topic><topic>hydrolysis</topic><topic>in vivo</topic><topic>isothiocyanate</topic><topic>Isothiocyanates - administration & dosage</topic><topic>Isothiocyanates - chemistry</topic><topic>Isothiocyanates - pharmacology</topic><topic>Kinetics</topic><topic>Mice</topic><topic>Mice, Transgenic</topic><topic>Polyethylene Glycols - chemistry</topic><topic>Skin - drug effects</topic><topic>Skin - radiation effects</topic><topic>Solvents - chemistry</topic><topic>Temperature</topic><topic>Time Factors</topic><topic>Transcription Factor AP-1 - antagonists & inhibitors</topic><topic>Ultraviolet Rays - adverse effects</topic><topic>UVB</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Franklin, Stephen J.</creatorcontrib><creatorcontrib>Dickinson, Sally E.</creatorcontrib><creatorcontrib>Karlage, Kelly L.</creatorcontrib><creatorcontrib>Bowden, G. T.</creatorcontrib><creatorcontrib>Myrdal, Paul 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>PubMed Central (Full Participant titles)</collection><jtitle>Drug development and industrial pharmacy</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Franklin, Stephen J.</au><au>Dickinson, Sally E.</au><au>Karlage, Kelly L.</au><au>Bowden, G. T.</au><au>Myrdal, Paul B.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Stability of sulforaphane for topical formulation</atitle><jtitle>Drug development and industrial pharmacy</jtitle><addtitle>Drug Dev Ind Pharm</addtitle><date>2014-04-01</date><risdate>2014</risdate><volume>40</volume><issue>4</issue><spage>494</spage><epage>502</epage><pages>494-502</pages><issn>0363-9045</issn><eissn>1520-5762</eissn><abstract>Abstract
Context: Sulforaphane (SFN) is a natural compound that has been investigated as a chemopreventive agent. SFN has been shown to inhibit the activator-protein-1 (AP-1) transcription factor and may be effective for inhibition of ultraviolet (UV) induced skin carcinogenesis. This study was designed to investigate the stability of SFN as a function of pH, temperature and in various solvents and formulations.
Materials and methods: Stability was analyzed using high-performance liquid chromatography. A potential lead formulation was identified and evaluated in vivo.
Results: SFN was determined to undergo apparent first-order degradation kinetics for the conditions explored. It was observed that SFN undergoes base catalyzed degradation. Buffer species and solvent type impacts stability as well. SFN was found to be very sensitive to temperature with degradation rate changing by a factor of nearly 3.1 for every 10 °C change in temperature (at pH 4.0). SFN completely degraded after 30 days in a conventional pharmaceutical cream formulation. Improved stability was observed in organic formulation components. Stability studies were conducted on two nonaqueous topical formulations: a polyethylene glycol (PEG) ointment base and an organic oleaginous base.
Conclusion: Topically applied SFN in the PEG base formulation significantly reduced AP-1 activation after UV stimulation in the skin of a transgenic mouse model, indicating that SFN in this formulation retains efficacy in vivo.</abstract><cop>England</cop><pub>Informa Healthcare USA, Inc</pub><pmid>23611476</pmid><doi>10.3109/03639045.2013.768634</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
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| source | MEDLINE; EBSCOhost Business Source Complete |
| subjects | Activator-protein-1 Administration, Cutaneous Animals Anticarcinogenic Agents - administration & dosage Anticarcinogenic Agents - chemistry Anticarcinogenic Agents - pharmacology base catalysis Chromatography, High Pressure Liquid degradation Drug Stability Drug Storage Female Hydrogen-Ion Concentration hydrolysis in vivo isothiocyanate Isothiocyanates - administration & dosage Isothiocyanates - chemistry Isothiocyanates - pharmacology Kinetics Mice Mice, Transgenic Polyethylene Glycols - chemistry Skin - drug effects Skin - radiation effects Solvents - chemistry Temperature Time Factors Transcription Factor AP-1 - antagonists & inhibitors Ultraviolet Rays - adverse effects UVB |
| title | Stability of sulforaphane for topical formulation |
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