Evaluation of Emulgel and Nanostructured Lipid Carrier-Based Gel Formulations for Transdermal Administration of Ibuprofen: Characterization, Mechanical Properties, and Ex-Vivo Skin Permeation
In transdermal applications of nonsteroidal anti-inflammatory drugs, the rheological and mechanical properties of the dosage form affect the performance of the drug. The aim of this study to develop emulgel and nanostructured lipid carrier NLC-based gel formulations containing ibuprofen, evaluate th...
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| Veröffentlicht in: | AAPS PharmSciTech 2024-05, Vol.25 (5), p.124, Article 124 |
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| creator | Yılmaz Usta, Duygu Teksin, Zeynep Safak Tugcu-Demiroz, Fatmanur |
| description | In transdermal applications of nonsteroidal anti-inflammatory drugs, the rheological and mechanical properties of the dosage form affect the performance of the drug. The aim of this study to develop emulgel and nanostructured lipid carrier NLC-based gel formulations containing ibuprofen, evaluate their mechanical properties, bioadhesive value and
ex-vivo
rabbit skin permeability. All formulations showed non-Newtonian pseudoplastic behavior and their viscosity values are suitable for topical application. The particle size of the nanostructured lipid carrier system was found to be 468 ± 21 nm, and the encapsulation efficiency was 95.58 ± 0.41%. According to the index of viscosity, consistency, firmness, and cohesiveness values obtained as a result of the back extrusion study, E2 formulation was found to be more suitable for transdermal application. The firmness and work of shear values of the E2 formulation, which has the highest viscosity value, were also found to be the highest and it was chosen as the most suitable formulation in terms of the spreadability test. The work of bioadhesion values of NLC-based gel and IBU-loaded NLC-based gel were found as 0.226 ± 0.028 and 0.181 ± 0.006 mJ/cm2 respectively. The percentages of IBU that penetrated through rabbit skin from the Ibuactive-Cream and the E2 were 87.4 ± 2.11% and 93.4 ± 2.72% after 24 h, respectively. When the penetration of ibuprofen through the skin was evaluated, it was found that the E2 formulation increased penetration due to its lipid and nanoparticle structure. As a result of these findings, it can be said that the NLC-based gel formulation will increase the therapeutic efficacy and will be a good alternative transdermal formulation.
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| doi_str_mv | 10.1208/s12249-024-02831-9 |
| format | Article |
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ex-vivo
rabbit skin permeability. All formulations showed non-Newtonian pseudoplastic behavior and their viscosity values are suitable for topical application. The particle size of the nanostructured lipid carrier system was found to be 468 ± 21 nm, and the encapsulation efficiency was 95.58 ± 0.41%. According to the index of viscosity, consistency, firmness, and cohesiveness values obtained as a result of the back extrusion study, E2 formulation was found to be more suitable for transdermal application. The firmness and work of shear values of the E2 formulation, which has the highest viscosity value, were also found to be the highest and it was chosen as the most suitable formulation in terms of the spreadability test. The work of bioadhesion values of NLC-based gel and IBU-loaded NLC-based gel were found as 0.226 ± 0.028 and 0.181 ± 0.006 mJ/cm2 respectively. The percentages of IBU that penetrated through rabbit skin from the Ibuactive-Cream and the E2 were 87.4 ± 2.11% and 93.4 ± 2.72% after 24 h, respectively. When the penetration of ibuprofen through the skin was evaluated, it was found that the E2 formulation increased penetration due to its lipid and nanoparticle structure. As a result of these findings, it can be said that the NLC-based gel formulation will increase the therapeutic efficacy and will be a good alternative transdermal formulation.
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ex-vivo
rabbit skin permeability. All formulations showed non-Newtonian pseudoplastic behavior and their viscosity values are suitable for topical application. The particle size of the nanostructured lipid carrier system was found to be 468 ± 21 nm, and the encapsulation efficiency was 95.58 ± 0.41%. According to the index of viscosity, consistency, firmness, and cohesiveness values obtained as a result of the back extrusion study, E2 formulation was found to be more suitable for transdermal application. The firmness and work of shear values of the E2 formulation, which has the highest viscosity value, were also found to be the highest and it was chosen as the most suitable formulation in terms of the spreadability test. The work of bioadhesion values of NLC-based gel and IBU-loaded NLC-based gel were found as 0.226 ± 0.028 and 0.181 ± 0.006 mJ/cm2 respectively. The percentages of IBU that penetrated through rabbit skin from the Ibuactive-Cream and the E2 were 87.4 ± 2.11% and 93.4 ± 2.72% after 24 h, respectively. When the penetration of ibuprofen through the skin was evaluated, it was found that the E2 formulation increased penetration due to its lipid and nanoparticle structure. As a result of these findings, it can be said that the NLC-based gel formulation will increase the therapeutic efficacy and will be a good alternative transdermal formulation.
Graphical Abstract</description><subject>Administration, Cutaneous</subject><subject>Animals</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - administration & dosage</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - chemistry</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics</subject><subject>Biochemistry</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotechnology</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>Drug Carriers - chemistry</subject><subject>Gels - chemistry</subject><subject>Ibuprofen - administration & dosage</subject><subject>Ibuprofen - chemistry</subject><subject>Ibuprofen - pharmacokinetics</subject><subject>Lipids - chemistry</subject><subject>Nanostructures - chemistry</subject><subject>Novel Advances in 3-D Printing Technology in Drug Delivery</subject><subject>Particle Size</subject><subject>Permeability</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Rabbits</subject><subject>Research Article</subject><subject>Rheology</subject><subject>Skin - metabolism</subject><subject>Skin Absorption - drug effects</subject><subject>Skin Absorption - physiology</subject><subject>Viscosity</subject><issn>1530-9932</issn><issn>1530-9932</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid>C6C</sourceid><sourceid>EIF</sourceid><recordid>eNp9kc9u1DAQxiMEoqXwAhyQjxwa8L9kHW5ltS2VFqhE4Wo59qR1SexlHFfAy_FqmGypOHGwxvJ832_G-qrqOaOvGKfqdWKcy66mXJajBKu7B9UhawStu07wh__cD6onKd1QygXrxOPqQCjFOZPisPq1uTVjNrOPgcSBbKY8XsFITHDkgwkxzZjtnBEc2fqdd2RtED1g_dak8nZWpKcRi2khJDJEJJdoQnKAkxnJiZt88IVyP-G8zzuMA4Q3ZH1t0NgZ0P9c2sfkPdhrE7wtzguMO8DZQzpettl8r7_420g-ffWBXBQ6LJ6n1aPBjAme3dWj6vPp5nL9rt5-PDtfn2xrKySf68Y61dtWcglWlLqS7dDYdtUPSvWdZYo73rJBAljT0ZUz0ja9pBQa03AplDiqXu65ZflvGdKsJ58sjKMJEHPSgrZCts2K0SLle6nFmBLCoHfoJ4M_NKP6T3B6H5wuweklON0V04s7fu4ncPeWv0kVgdgLUmmFK0B9EzOG8uf_YX8Dx3en8Q</recordid><startdate>20240531</startdate><enddate>20240531</enddate><creator>Yılmaz Usta, Duygu</creator><creator>Teksin, Zeynep Safak</creator><creator>Tugcu-Demiroz, Fatmanur</creator><general>Springer International Publishing</general><scope>C6C</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>7X8</scope><orcidid>https://orcid.org/0000-0002-9468-3329</orcidid><orcidid>https://orcid.org/0000-0003-4035-7656</orcidid><orcidid>https://orcid.org/0000-0001-6359-5935</orcidid></search><sort><creationdate>20240531</creationdate><title>Evaluation of Emulgel and Nanostructured Lipid Carrier-Based Gel Formulations for Transdermal Administration of Ibuprofen: Characterization, Mechanical Properties, and Ex-Vivo Skin Permeation</title><author>Yılmaz Usta, Duygu ; Teksin, Zeynep Safak ; Tugcu-Demiroz, Fatmanur</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c342t-5cd8bc6424ec3c64746f5c67bf88b9c182d261f4eeca907da4c5b400e5a524383</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Administration, Cutaneous</topic><topic>Animals</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - administration & dosage</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - chemistry</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics</topic><topic>Biochemistry</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Biotechnology</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>Drug Carriers - chemistry</topic><topic>Gels - chemistry</topic><topic>Ibuprofen - administration & dosage</topic><topic>Ibuprofen - chemistry</topic><topic>Ibuprofen - pharmacokinetics</topic><topic>Lipids - chemistry</topic><topic>Nanostructures - chemistry</topic><topic>Novel Advances in 3-D Printing Technology in Drug Delivery</topic><topic>Particle Size</topic><topic>Permeability</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Rabbits</topic><topic>Research Article</topic><topic>Rheology</topic><topic>Skin - metabolism</topic><topic>Skin Absorption - drug effects</topic><topic>Skin Absorption - physiology</topic><topic>Viscosity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yılmaz Usta, Duygu</creatorcontrib><creatorcontrib>Teksin, Zeynep Safak</creatorcontrib><creatorcontrib>Tugcu-Demiroz, Fatmanur</creatorcontrib><collection>Springer Nature OA Free Journals</collection><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>AAPS PharmSciTech</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Yılmaz Usta, Duygu</au><au>Teksin, Zeynep Safak</au><au>Tugcu-Demiroz, Fatmanur</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evaluation of Emulgel and Nanostructured Lipid Carrier-Based Gel Formulations for Transdermal Administration of Ibuprofen: Characterization, Mechanical Properties, and Ex-Vivo Skin Permeation</atitle><jtitle>AAPS PharmSciTech</jtitle><stitle>AAPS PharmSciTech</stitle><addtitle>AAPS PharmSciTech</addtitle><date>2024-05-31</date><risdate>2024</risdate><volume>25</volume><issue>5</issue><spage>124</spage><pages>124-</pages><artnum>124</artnum><issn>1530-9932</issn><eissn>1530-9932</eissn><abstract>In transdermal applications of nonsteroidal anti-inflammatory drugs, the rheological and mechanical properties of the dosage form affect the performance of the drug. The aim of this study to develop emulgel and nanostructured lipid carrier NLC-based gel formulations containing ibuprofen, evaluate their mechanical properties, bioadhesive value and
ex-vivo
rabbit skin permeability. All formulations showed non-Newtonian pseudoplastic behavior and their viscosity values are suitable for topical application. The particle size of the nanostructured lipid carrier system was found to be 468 ± 21 nm, and the encapsulation efficiency was 95.58 ± 0.41%. According to the index of viscosity, consistency, firmness, and cohesiveness values obtained as a result of the back extrusion study, E2 formulation was found to be more suitable for transdermal application. The firmness and work of shear values of the E2 formulation, which has the highest viscosity value, were also found to be the highest and it was chosen as the most suitable formulation in terms of the spreadability test. The work of bioadhesion values of NLC-based gel and IBU-loaded NLC-based gel were found as 0.226 ± 0.028 and 0.181 ± 0.006 mJ/cm2 respectively. The percentages of IBU that penetrated through rabbit skin from the Ibuactive-Cream and the E2 were 87.4 ± 2.11% and 93.4 ± 2.72% after 24 h, respectively. When the penetration of ibuprofen through the skin was evaluated, it was found that the E2 formulation increased penetration due to its lipid and nanoparticle structure. As a result of these findings, it can be said that the NLC-based gel formulation will increase the therapeutic efficacy and will be a good alternative transdermal formulation.
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| subjects | Administration, Cutaneous Animals Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics Biochemistry Biomedical and Life Sciences Biomedicine Biotechnology Chemistry, Pharmaceutical - methods Drug Carriers - chemistry Gels - chemistry Ibuprofen - administration & dosage Ibuprofen - chemistry Ibuprofen - pharmacokinetics Lipids - chemistry Nanostructures - chemistry Novel Advances in 3-D Printing Technology in Drug Delivery Particle Size Permeability Pharmacology/Toxicology Pharmacy Rabbits Research Article Rheology Skin - metabolism Skin Absorption - drug effects Skin Absorption - physiology Viscosity |
| title | Evaluation of Emulgel and Nanostructured Lipid Carrier-Based Gel Formulations for Transdermal Administration of Ibuprofen: Characterization, Mechanical Properties, and Ex-Vivo Skin Permeation |
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