Enhanced Percutaneous Delivery of Methotrexate Using Micelles Prepared with Novel Cationic Amphipathic Material
Background: Methotrexate (MTX) is an antiproliferative drug widely used to treat inflammatory diseases and autoimmune diseases. The application of percutaneous administration is hindered due to its poor transdermal penetration. To reduce side effects and enhanced percutaneous delivery of MTX, novel...
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| Veröffentlicht in: | International journal of nanomedicine 2020-01, Vol.15, p.3539-3550 |
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| creator | Zhao, Yun-Chun Zheng, Hai-Li Wang, Xiao-Rong Zheng, Xiao-Ling Chen, Yue Fei, Wei-Dong Zheng, Yong-Quan Wang, Wen-Xi Zheng, Cai-Hong |
| description | Background: Methotrexate (MTX) is an antiproliferative drug widely used to treat inflammatory diseases and autoimmune diseases. The application of percutaneous administration is hindered due to its poor transdermal penetration. To reduce side effects and enhanced percutaneous delivery of MTX, novel methotrexate (MTX)-loaded micelles prepared with a amphiphilic cationic material, N,N-dimethyl-(N',N'-di-stearoyl-1-ethyl)1,3-diaminopropane (DMSAP), was designed.
Materials and Methods: DMSAP was synthesized via three steps using simple chemical agents. H nuclear magnetic resonance and mass spectroscopy were used to confirm the successful synthesis of DMSAP. A safe and non-toxic phosphatidylcholine, soybean phosphatidylcholine (SPC), was added to DMSAP at different ratios to form P/D-micelles. Then, MTX-entrapped micelles (M/P/D-micelles) were prepared by electrostatic adsorption. The physicochemical properties and blood stability of micelles were examined thoroughly. In addition, the transdermal potential of the micelles was evaluated by permeation experiments.
Results: In aqueous environments, DMSAP conjugates could self-assemble spontaneously into micelles with a low critical micelle concentration (CMC) of 0.056 mg/mL. Stable, spherical MTX-entrapped micelles (M/P/D-micelles) with a size of 100-120 nm and high zeta potential of +36.26 mV were prepared. In vitro permeation studies showed that M/P/D-micelles exhibited superior skin permeability and deposition of MTX in the epidermis and dermis compared with that of free MTX.
Conclusion: These special novel cationic M/P/D-micelles can enhance the permeability of MTX and are expected to be a promising percutaneous delivery system for therapy skin diseases. |
| doi_str_mv | 10.2147/IJN.S251431 |
| format | Article |
| fullrecord | <record><control><sourceid>gale_proqu</sourceid><recordid>TN_cdi_proquest_journals_2414096404</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><galeid>A626928936</galeid><doaj_id>oai_doaj_org_article_ccf42e3550874637868436d78a5f713f</doaj_id><sourcerecordid>A626928936</sourcerecordid><originalsourceid>FETCH-LOGICAL-c542t-9bd83dd923857b4a63769b041ccc2c86a082eda1e9b5a4b180b3e393f29bcdb53</originalsourceid><addsrcrecordid>eNqNks1vEzEQxVcIREvhxB2txBEl-HPtvSBVoUBQUypBz5bXO5t1tLGD7U3pf49pQtpIHJAPHo1_73lsvaJ4jdGUYCbez79eTb8TjhnFT4pTjIWcEITp00f1SfEixhVCXMiqfl6cUMKZQJicFv7C9doZaMtrCGZM2oEfY_kRBruFcFf6rlxA6n0K8EsnKG-idctyYQ0MA8TyOsBGh6y-takvr_wWhnKmk_XOmvJ8ventRqc-14ssDlYPL4tnnR4ivNrvZ8XNp4sfsy-Ty2-f57Pzy4nhjKRJ3bSStm1NqOSiYbqioqobxLAxhhhZaSQJtBpD3XDNGixRQ4HWtCN1Y9qG07NivvNtvV6pTbBrHe6U11bdN3xYKh2SNQMoYzpGgHKOpGD5IllJRqtWSM07gWmXvT7svDZjs4bWgEtBD0emxyfO9mrpt0oQxhkX2eDt3iD4nyPEpFZ-DC6_XxGGGaorhtgDtdR5Kuu6_OnarG006rwiVU1kTatMTf9B5dXC2hrvoLO5fyR4txOY4GMM0B0Gx0j9CZDKAVL7AGX6zeO3Hti_icmA3AG30PguGgs5PQcM5YxRyiQWuUJ4ZtN9GGZ-dOlhkv-R0t_4g-D4</addsrcrecordid><sourcetype>Open Website</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2414096404</pqid></control><display><type>article</type><title>Enhanced Percutaneous Delivery of Methotrexate Using Micelles Prepared with Novel Cationic Amphipathic Material</title><source>MEDLINE</source><source>DOVE Medical Press Journals</source><source>DOAJ Directory of Open Access Journals</source><source>Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals</source><source>PubMed Central Open Access</source><source>Web of Science - Science Citation Index Expanded - 2020<img src="https://exlibris-pub.s3.amazonaws.com/fromwos-v2.jpg" /></source><source>Access via Taylor & Francis (Open Access Collection)</source><source>PubMed Central</source><creator>Zhao, Yun-Chun ; Zheng, Hai-Li ; Wang, Xiao-Rong ; Zheng, Xiao-Ling ; Chen, Yue ; Fei, Wei-Dong ; Zheng, Yong-Quan ; Wang, Wen-Xi ; Zheng, Cai-Hong</creator><creatorcontrib>Zhao, Yun-Chun ; Zheng, Hai-Li ; Wang, Xiao-Rong ; Zheng, Xiao-Ling ; Chen, Yue ; Fei, Wei-Dong ; Zheng, Yong-Quan ; Wang, Wen-Xi ; Zheng, Cai-Hong</creatorcontrib><description>Background: Methotrexate (MTX) is an antiproliferative drug widely used to treat inflammatory diseases and autoimmune diseases. The application of percutaneous administration is hindered due to its poor transdermal penetration. To reduce side effects and enhanced percutaneous delivery of MTX, novel methotrexate (MTX)-loaded micelles prepared with a amphiphilic cationic material, N,N-dimethyl-(N',N'-di-stearoyl-1-ethyl)1,3-diaminopropane (DMSAP), was designed.
Materials and Methods: DMSAP was synthesized via three steps using simple chemical agents. H nuclear magnetic resonance and mass spectroscopy were used to confirm the successful synthesis of DMSAP. A safe and non-toxic phosphatidylcholine, soybean phosphatidylcholine (SPC), was added to DMSAP at different ratios to form P/D-micelles. Then, MTX-entrapped micelles (M/P/D-micelles) were prepared by electrostatic adsorption. The physicochemical properties and blood stability of micelles were examined thoroughly. In addition, the transdermal potential of the micelles was evaluated by permeation experiments.
Results: In aqueous environments, DMSAP conjugates could self-assemble spontaneously into micelles with a low critical micelle concentration (CMC) of 0.056 mg/mL. Stable, spherical MTX-entrapped micelles (M/P/D-micelles) with a size of 100-120 nm and high zeta potential of +36.26 mV were prepared. In vitro permeation studies showed that M/P/D-micelles exhibited superior skin permeability and deposition of MTX in the epidermis and dermis compared with that of free MTX.
Conclusion: These special novel cationic M/P/D-micelles can enhance the permeability of MTX and are expected to be a promising percutaneous delivery system for therapy skin diseases.</description><identifier>ISSN: 1178-2013</identifier><identifier>ISSN: 1176-9114</identifier><identifier>EISSN: 1178-2013</identifier><identifier>DOI: 10.2147/IJN.S251431</identifier><identifier>PMID: 32547012</identifier><language>eng</language><publisher>ALBANY: Dove Medical Press Ltd</publisher><subject><![CDATA[3-diaminopropane ; Administration, Cutaneous ; Adsorption ; Animals ; Cations ; Cattle ; Chemical weapons ; Dermatologic agents ; Drug Carriers - chemistry ; Drug Delivery Systems ; Electrolytes ; Experiments ; Humans ; Life Sciences & Biomedicine ; Lipids ; Mass spectrometry ; Methotrexate ; Methotrexate - administration & dosage ; Methotrexate - chemistry ; Mice ; micelle ; Micelles ; Morphology ; n-dimethyl-(n ; Nanoscience & Nanotechnology ; NMR ; Nuclear magnetic resonance ; Nuclear magnetic resonance spectroscopy ; n′-di-stearoyl-1-ethyl)1 ; Original Research ; Osmolar Concentration ; Particle Size ; percutaneous delivery ; Permeability ; Pharmacology & Pharmacy ; Phosphatidylcholines - chemistry ; Proton Magnetic Resonance Spectroscopy ; Science & Technology ; Science & Technology - Other Topics ; Serum Albumin, Bovine - chemistry ; Skin ; Skin - drug effects ; Skin diseases ; Soybeans ; Spectrum analysis ; Static Electricity ; Transdermal drug delivery systems]]></subject><ispartof>International journal of nanomedicine, 2020-01, Vol.15, p.3539-3550</ispartof><rights>2020 Zhao et al.</rights><rights>COPYRIGHT 2020 Dove Medical Press Limited</rights><rights>2020. This work is licensed under https://creativecommons.org/licenses/by-nc/3.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2020 Zhao et al. 2020 Zhao et al.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>true</woscitedreferencessubscribed><woscitedreferencescount>15</woscitedreferencescount><woscitedreferencesoriginalsourcerecordid>wos000533481700001</woscitedreferencesoriginalsourcerecordid><citedby>FETCH-LOGICAL-c542t-9bd83dd923857b4a63769b041ccc2c86a082eda1e9b5a4b180b3e393f29bcdb53</citedby><cites>FETCH-LOGICAL-c542t-9bd83dd923857b4a63769b041ccc2c86a082eda1e9b5a4b180b3e393f29bcdb53</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/PMC7245457/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7245457/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,315,729,782,786,866,887,2104,2116,3864,27931,27932,28255,53798,53800</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/32547012$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Zhao, Yun-Chun</creatorcontrib><creatorcontrib>Zheng, Hai-Li</creatorcontrib><creatorcontrib>Wang, Xiao-Rong</creatorcontrib><creatorcontrib>Zheng, Xiao-Ling</creatorcontrib><creatorcontrib>Chen, Yue</creatorcontrib><creatorcontrib>Fei, Wei-Dong</creatorcontrib><creatorcontrib>Zheng, Yong-Quan</creatorcontrib><creatorcontrib>Wang, Wen-Xi</creatorcontrib><creatorcontrib>Zheng, Cai-Hong</creatorcontrib><title>Enhanced Percutaneous Delivery of Methotrexate Using Micelles Prepared with Novel Cationic Amphipathic Material</title><title>International journal of nanomedicine</title><addtitle>INT J NANOMED</addtitle><addtitle>Int J Nanomedicine</addtitle><description>Background: Methotrexate (MTX) is an antiproliferative drug widely used to treat inflammatory diseases and autoimmune diseases. The application of percutaneous administration is hindered due to its poor transdermal penetration. To reduce side effects and enhanced percutaneous delivery of MTX, novel methotrexate (MTX)-loaded micelles prepared with a amphiphilic cationic material, N,N-dimethyl-(N',N'-di-stearoyl-1-ethyl)1,3-diaminopropane (DMSAP), was designed.
Materials and Methods: DMSAP was synthesized via three steps using simple chemical agents. H nuclear magnetic resonance and mass spectroscopy were used to confirm the successful synthesis of DMSAP. A safe and non-toxic phosphatidylcholine, soybean phosphatidylcholine (SPC), was added to DMSAP at different ratios to form P/D-micelles. Then, MTX-entrapped micelles (M/P/D-micelles) were prepared by electrostatic adsorption. The physicochemical properties and blood stability of micelles were examined thoroughly. In addition, the transdermal potential of the micelles was evaluated by permeation experiments.
Results: In aqueous environments, DMSAP conjugates could self-assemble spontaneously into micelles with a low critical micelle concentration (CMC) of 0.056 mg/mL. Stable, spherical MTX-entrapped micelles (M/P/D-micelles) with a size of 100-120 nm and high zeta potential of +36.26 mV were prepared. In vitro permeation studies showed that M/P/D-micelles exhibited superior skin permeability and deposition of MTX in the epidermis and dermis compared with that of free MTX.
Conclusion: These special novel cationic M/P/D-micelles can enhance the permeability of MTX and are expected to be a promising percutaneous delivery system for therapy skin diseases.</description><subject>3-diaminopropane</subject><subject>Administration, Cutaneous</subject><subject>Adsorption</subject><subject>Animals</subject><subject>Cations</subject><subject>Cattle</subject><subject>Chemical weapons</subject><subject>Dermatologic agents</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Delivery Systems</subject><subject>Electrolytes</subject><subject>Experiments</subject><subject>Humans</subject><subject>Life Sciences & Biomedicine</subject><subject>Lipids</subject><subject>Mass spectrometry</subject><subject>Methotrexate</subject><subject>Methotrexate - administration & dosage</subject><subject>Methotrexate - chemistry</subject><subject>Mice</subject><subject>micelle</subject><subject>Micelles</subject><subject>Morphology</subject><subject>n-dimethyl-(n</subject><subject>Nanoscience & Nanotechnology</subject><subject>NMR</subject><subject>Nuclear magnetic resonance</subject><subject>Nuclear magnetic resonance spectroscopy</subject><subject>n′-di-stearoyl-1-ethyl)1</subject><subject>Original Research</subject><subject>Osmolar Concentration</subject><subject>Particle Size</subject><subject>percutaneous delivery</subject><subject>Permeability</subject><subject>Pharmacology & Pharmacy</subject><subject>Phosphatidylcholines - chemistry</subject><subject>Proton Magnetic Resonance Spectroscopy</subject><subject>Science & Technology</subject><subject>Science & Technology - Other Topics</subject><subject>Serum Albumin, Bovine - chemistry</subject><subject>Skin</subject><subject>Skin - drug effects</subject><subject>Skin diseases</subject><subject>Soybeans</subject><subject>Spectrum analysis</subject><subject>Static Electricity</subject><subject>Transdermal drug delivery systems</subject><issn>1178-2013</issn><issn>1176-9114</issn><issn>1178-2013</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><sourceid>AOWDO</sourceid><sourceid>EIF</sourceid><sourceid>8G5</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><sourceid>GUQSH</sourceid><sourceid>M2O</sourceid><recordid>eNqNks1vEzEQxVcIREvhxB2txBEl-HPtvSBVoUBQUypBz5bXO5t1tLGD7U3pf49pQtpIHJAPHo1_73lsvaJ4jdGUYCbez79eTb8TjhnFT4pTjIWcEITp00f1SfEixhVCXMiqfl6cUMKZQJicFv7C9doZaMtrCGZM2oEfY_kRBruFcFf6rlxA6n0K8EsnKG-idctyYQ0MA8TyOsBGh6y-takvr_wWhnKmk_XOmvJ8ventRqc-14ssDlYPL4tnnR4ivNrvZ8XNp4sfsy-Ty2-f57Pzy4nhjKRJ3bSStm1NqOSiYbqioqobxLAxhhhZaSQJtBpD3XDNGixRQ4HWtCN1Y9qG07NivvNtvV6pTbBrHe6U11bdN3xYKh2SNQMoYzpGgHKOpGD5IllJRqtWSM07gWmXvT7svDZjs4bWgEtBD0emxyfO9mrpt0oQxhkX2eDt3iD4nyPEpFZ-DC6_XxGGGaorhtgDtdR5Kuu6_OnarG006rwiVU1kTatMTf9B5dXC2hrvoLO5fyR4txOY4GMM0B0Gx0j9CZDKAVL7AGX6zeO3Hti_icmA3AG30PguGgs5PQcM5YxRyiQWuUJ4ZtN9GGZ-dOlhkv-R0t_4g-D4</recordid><startdate>20200101</startdate><enddate>20200101</enddate><creator>Zhao, Yun-Chun</creator><creator>Zheng, Hai-Li</creator><creator>Wang, Xiao-Rong</creator><creator>Zheng, Xiao-Ling</creator><creator>Chen, Yue</creator><creator>Fei, Wei-Dong</creator><creator>Zheng, Yong-Quan</creator><creator>Wang, Wen-Xi</creator><creator>Zheng, Cai-Hong</creator><general>Dove Medical Press Ltd</general><general>Dove Medical Press Limited</general><general>Taylor & Francis Ltd</general><general>Dove</general><general>Dove Medical Press</general><scope>AOWDO</scope><scope>BLEPL</scope><scope>DTL</scope><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>3V.</scope><scope>7X7</scope><scope>7XB</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>8G5</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>GUQSH</scope><scope>K9.</scope><scope>M0S</scope><scope>M2O</scope><scope>MBDVC</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>Q9U</scope><scope>5PM</scope></search><sort><creationdate>20200101</creationdate><title>Enhanced Percutaneous Delivery of Methotrexate Using Micelles Prepared with Novel Cationic Amphipathic Material</title><author>Zhao, Yun-Chun ; Zheng, Hai-Li ; Wang, Xiao-Rong ; Zheng, Xiao-Ling ; Chen, Yue ; Fei, Wei-Dong ; Zheng, Yong-Quan ; Wang, Wen-Xi ; Zheng, Cai-Hong</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c542t-9bd83dd923857b4a63769b041ccc2c86a082eda1e9b5a4b180b3e393f29bcdb53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>3-diaminopropane</topic><topic>Administration, Cutaneous</topic><topic>Adsorption</topic><topic>Animals</topic><topic>Cations</topic><topic>Cattle</topic><topic>Chemical weapons</topic><topic>Dermatologic agents</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Delivery Systems</topic><topic>Electrolytes</topic><topic>Experiments</topic><topic>Humans</topic><topic>Life Sciences & Biomedicine</topic><topic>Lipids</topic><topic>Mass spectrometry</topic><topic>Methotrexate</topic><topic>Methotrexate - administration & dosage</topic><topic>Methotrexate - chemistry</topic><topic>Mice</topic><topic>micelle</topic><topic>Micelles</topic><topic>Morphology</topic><topic>n-dimethyl-(n</topic><topic>Nanoscience & Nanotechnology</topic><topic>NMR</topic><topic>Nuclear magnetic resonance</topic><topic>Nuclear magnetic resonance spectroscopy</topic><topic>n′-di-stearoyl-1-ethyl)1</topic><topic>Original Research</topic><topic>Osmolar Concentration</topic><topic>Particle Size</topic><topic>percutaneous delivery</topic><topic>Permeability</topic><topic>Pharmacology & Pharmacy</topic><topic>Phosphatidylcholines - chemistry</topic><topic>Proton Magnetic Resonance Spectroscopy</topic><topic>Science & Technology</topic><topic>Science & Technology - Other Topics</topic><topic>Serum Albumin, Bovine - chemistry</topic><topic>Skin</topic><topic>Skin - drug effects</topic><topic>Skin diseases</topic><topic>Soybeans</topic><topic>Spectrum analysis</topic><topic>Static Electricity</topic><topic>Transdermal drug delivery systems</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Zhao, Yun-Chun</creatorcontrib><creatorcontrib>Zheng, Hai-Li</creatorcontrib><creatorcontrib>Wang, Xiao-Rong</creatorcontrib><creatorcontrib>Zheng, Xiao-Ling</creatorcontrib><creatorcontrib>Chen, Yue</creatorcontrib><creatorcontrib>Fei, Wei-Dong</creatorcontrib><creatorcontrib>Zheng, Yong-Quan</creatorcontrib><creatorcontrib>Wang, Wen-Xi</creatorcontrib><creatorcontrib>Zheng, Cai-Hong</creatorcontrib><collection>Web of Science - Science Citation Index Expanded - 2020</collection><collection>Web of Science Core Collection</collection><collection>Science Citation Index Expanded</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>Research Library (Alumni Edition)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>Research Library Prep</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Research Library</collection><collection>Research Library (Corporate)</collection><collection>Access via ProQuest (Open Access)</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>ProQuest Central Basic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>International journal of nanomedicine</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Zhao, Yun-Chun</au><au>Zheng, Hai-Li</au><au>Wang, Xiao-Rong</au><au>Zheng, Xiao-Ling</au><au>Chen, Yue</au><au>Fei, Wei-Dong</au><au>Zheng, Yong-Quan</au><au>Wang, Wen-Xi</au><au>Zheng, Cai-Hong</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Enhanced Percutaneous Delivery of Methotrexate Using Micelles Prepared with Novel Cationic Amphipathic Material</atitle><jtitle>International journal of nanomedicine</jtitle><stitle>INT J NANOMED</stitle><addtitle>Int J Nanomedicine</addtitle><date>2020-01-01</date><risdate>2020</risdate><volume>15</volume><spage>3539</spage><epage>3550</epage><pages>3539-3550</pages><issn>1178-2013</issn><issn>1176-9114</issn><eissn>1178-2013</eissn><abstract>Background: Methotrexate (MTX) is an antiproliferative drug widely used to treat inflammatory diseases and autoimmune diseases. The application of percutaneous administration is hindered due to its poor transdermal penetration. To reduce side effects and enhanced percutaneous delivery of MTX, novel methotrexate (MTX)-loaded micelles prepared with a amphiphilic cationic material, N,N-dimethyl-(N',N'-di-stearoyl-1-ethyl)1,3-diaminopropane (DMSAP), was designed.
Materials and Methods: DMSAP was synthesized via three steps using simple chemical agents. H nuclear magnetic resonance and mass spectroscopy were used to confirm the successful synthesis of DMSAP. A safe and non-toxic phosphatidylcholine, soybean phosphatidylcholine (SPC), was added to DMSAP at different ratios to form P/D-micelles. Then, MTX-entrapped micelles (M/P/D-micelles) were prepared by electrostatic adsorption. The physicochemical properties and blood stability of micelles were examined thoroughly. In addition, the transdermal potential of the micelles was evaluated by permeation experiments.
Results: In aqueous environments, DMSAP conjugates could self-assemble spontaneously into micelles with a low critical micelle concentration (CMC) of 0.056 mg/mL. Stable, spherical MTX-entrapped micelles (M/P/D-micelles) with a size of 100-120 nm and high zeta potential of +36.26 mV were prepared. In vitro permeation studies showed that M/P/D-micelles exhibited superior skin permeability and deposition of MTX in the epidermis and dermis compared with that of free MTX.
Conclusion: These special novel cationic M/P/D-micelles can enhance the permeability of MTX and are expected to be a promising percutaneous delivery system for therapy skin diseases.</abstract><cop>ALBANY</cop><pub>Dove Medical Press Ltd</pub><pmid>32547012</pmid><doi>10.2147/IJN.S251431</doi><tpages>12</tpages><oa>free_for_read</oa></addata></record> |
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| identifier | ISSN: 1178-2013 |
| ispartof | International journal of nanomedicine, 2020-01, Vol.15, p.3539-3550 |
| issn | 1178-2013 1176-9114 1178-2013 |
| language | eng |
| recordid | cdi_proquest_journals_2414096404 |
| source | MEDLINE; DOVE Medical Press Journals; DOAJ Directory of Open Access Journals; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central Open Access; Web of Science - Science Citation Index Expanded - 2020<img src="https://exlibris-pub.s3.amazonaws.com/fromwos-v2.jpg" />; Access via Taylor & Francis (Open Access Collection); PubMed Central |
| subjects | 3-diaminopropane Administration, Cutaneous Adsorption Animals Cations Cattle Chemical weapons Dermatologic agents Drug Carriers - chemistry Drug Delivery Systems Electrolytes Experiments Humans Life Sciences & Biomedicine Lipids Mass spectrometry Methotrexate Methotrexate - administration & dosage Methotrexate - chemistry Mice micelle Micelles Morphology n-dimethyl-(n Nanoscience & Nanotechnology NMR Nuclear magnetic resonance Nuclear magnetic resonance spectroscopy n′-di-stearoyl-1-ethyl)1 Original Research Osmolar Concentration Particle Size percutaneous delivery Permeability Pharmacology & Pharmacy Phosphatidylcholines - chemistry Proton Magnetic Resonance Spectroscopy Science & Technology Science & Technology - Other Topics Serum Albumin, Bovine - chemistry Skin Skin - drug effects Skin diseases Soybeans Spectrum analysis Static Electricity Transdermal drug delivery systems |
| title | Enhanced Percutaneous Delivery of Methotrexate Using Micelles Prepared with Novel Cationic Amphipathic Material |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-04T01%3A56%3A47IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-gale_proqu&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Enhanced%20Percutaneous%20Delivery%20of%20Methotrexate%20Using%20Micelles%20Prepared%20with%20Novel%20Cationic%20Amphipathic%20Material&rft.jtitle=International%20journal%20of%20nanomedicine&rft.au=Zhao,%20Yun-Chun&rft.date=2020-01-01&rft.volume=15&rft.spage=3539&rft.epage=3550&rft.pages=3539-3550&rft.issn=1178-2013&rft.eissn=1178-2013&rft_id=info:doi/10.2147/IJN.S251431&rft_dat=%3Cgale_proqu%3EA626928936%3C/gale_proqu%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=2414096404&rft_id=info:pmid/32547012&rft_galeid=A626928936&rft_doaj_id=oai_doaj_org_article_ccf42e3550874637868436d78a5f713f&rfr_iscdi=true |