Development of a novel cannabinoid-loaded microemulsion towards an improved stability and transdermal delivery
[Display omitted] The aim of this study was to develop a stable microemulsion (ME) for transdermal delivery of tetrahydrocannabinolic acid (THCA) and cannabidiolic acid (CBDA). The lipid-based vehicles were selected by screening cannabinoid solubility and the emulsifying ability of surfactants. Pseu...
Gespeichert in:
| Veröffentlicht in: | International journal of pharmaceutics 2021-07, Vol.604, p.120766-120766, Article 120766 |
|---|---|
| Hauptverfasser: | , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 120766 |
|---|---|
| container_issue | |
| container_start_page | 120766 |
| container_title | International journal of pharmaceutics |
| container_volume | 604 |
| creator | Park, Chulhun Zuo, Jieyu Somayaji, Vijay Lee, Beom-Jin Löbenberg, Raimar |
| description | [Display omitted]
The aim of this study was to develop a stable microemulsion (ME) for transdermal delivery of tetrahydrocannabinolic acid (THCA) and cannabidiolic acid (CBDA). The lipid-based vehicles were selected by screening cannabinoid solubility and the emulsifying ability of surfactants. Pseudo-ternary phase diagrams were constructed by formulation of cannabinoids with Capryol® 90 as oil phase, Tween® 80, Solutol® HS15, Procetyl® AWS, and Cremophor® RH40 as surfactants, ethanol as cosurfactant, and distilled water as the aqueous phase. A significant improvement in transmembrane flux (Jss), permeability coefficient (Kp), and enhancement ratio (ER) was found in one system compared to other formulations. This ME consisted of 1.0% (w/w) of cannabinoids, 5% (w/w) of Capryol® 90, 44% (w/w) Smix (2:1, Procetyl® AWS and Ethanol) and 50.0% (w/w) of distilled water. Additionally, the effects of pH on the permeation of the cannabinoids were investigated. Based on the pH value THCA and CBDA-loaded ME exhibited the highest permeation at pH 5.17 and pH 5.25. After storing the pH-adjusted P2 ME and the optimized P2 ME for 180 days at 4℃ and 25℃, the content of cannabinoids was over 95%. Consequently, the cannabinoid-loaded ME system is a promising option for solubilizing and stabilizing lipophilic drugs like cannabinoids and utilize them for transdermal delivery. |
| doi_str_mv | 10.1016/j.ijpharm.2021.120766 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_2537630168</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0378517321005718</els_id><sourcerecordid>2537630168</sourcerecordid><originalsourceid>FETCH-LOGICAL-c342t-53d2f4f811581e28288c86f64b4991f236bb2137ef4d816ec2b2b99027cc7b803</originalsourceid><addsrcrecordid>eNqFkEtLAzEUhYMoWB8_QcjSzdQ8ZpJ0JVKfUHCj65BJ7mBKJqnJtNJ_b0rdu7pwuOdwzofQDSVzSqi4W8_9evNl8jhnhNE5ZUQKcYJmVEne8FaKUzQjXKqmo5Kfo4tS1oQQwSifofgIOwhpM0KccBqwwTFVAVsTo-l9TN41IRkHDo_e5gTjNhSfIp7Sj8muYBOxHze5mhwuU7UEP-2r6vCUTSwO8mgCdhD8DvL-Cp0NJhS4_ruX6PP56WP52qzeX96WD6vG8pZNTccdG9pBUdopCkwxpawSg2j7drGgA-Oi72t9CUPrFBVgWc_6xYIwaa3sFeGX6PaYW5t9b6FMevTFQggmQtoWzTouBa_wVH3tjq91XSkZBr3JfjR5rynRB756rf_46gNffeRbffdHH9QdOw9ZF-shWnA-g520S_6fhF_ksIhV</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2537630168</pqid></control><display><type>article</type><title>Development of a novel cannabinoid-loaded microemulsion towards an improved stability and transdermal delivery</title><source>ScienceDirect Journals (5 years ago - present)</source><creator>Park, Chulhun ; Zuo, Jieyu ; Somayaji, Vijay ; Lee, Beom-Jin ; Löbenberg, Raimar</creator><creatorcontrib>Park, Chulhun ; Zuo, Jieyu ; Somayaji, Vijay ; Lee, Beom-Jin ; Löbenberg, Raimar</creatorcontrib><description>[Display omitted]
The aim of this study was to develop a stable microemulsion (ME) for transdermal delivery of tetrahydrocannabinolic acid (THCA) and cannabidiolic acid (CBDA). The lipid-based vehicles were selected by screening cannabinoid solubility and the emulsifying ability of surfactants. Pseudo-ternary phase diagrams were constructed by formulation of cannabinoids with Capryol® 90 as oil phase, Tween® 80, Solutol® HS15, Procetyl® AWS, and Cremophor® RH40 as surfactants, ethanol as cosurfactant, and distilled water as the aqueous phase. A significant improvement in transmembrane flux (Jss), permeability coefficient (Kp), and enhancement ratio (ER) was found in one system compared to other formulations. This ME consisted of 1.0% (w/w) of cannabinoids, 5% (w/w) of Capryol® 90, 44% (w/w) Smix (2:1, Procetyl® AWS and Ethanol) and 50.0% (w/w) of distilled water. Additionally, the effects of pH on the permeation of the cannabinoids were investigated. Based on the pH value THCA and CBDA-loaded ME exhibited the highest permeation at pH 5.17 and pH 5.25. After storing the pH-adjusted P2 ME and the optimized P2 ME for 180 days at 4℃ and 25℃, the content of cannabinoids was over 95%. Consequently, the cannabinoid-loaded ME system is a promising option for solubilizing and stabilizing lipophilic drugs like cannabinoids and utilize them for transdermal delivery.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2021.120766</identifier><language>eng</language><publisher>Elsevier B.V</publisher><subject>Acidic cannabinoids ; Cannabidiolic acid ; Cannabinoids ; Lipid-based vehicle ; Microemulsion ; Tetrahydrocannabinolic acid ; Transdermal delivery</subject><ispartof>International journal of pharmaceutics, 2021-07, Vol.604, p.120766-120766, Article 120766</ispartof><rights>2021 Elsevier B.V.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c342t-53d2f4f811581e28288c86f64b4991f236bb2137ef4d816ec2b2b99027cc7b803</citedby><cites>FETCH-LOGICAL-c342t-53d2f4f811581e28288c86f64b4991f236bb2137ef4d816ec2b2b99027cc7b803</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ijpharm.2021.120766$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3548,27922,27923,45993</link.rule.ids></links><search><creatorcontrib>Park, Chulhun</creatorcontrib><creatorcontrib>Zuo, Jieyu</creatorcontrib><creatorcontrib>Somayaji, Vijay</creatorcontrib><creatorcontrib>Lee, Beom-Jin</creatorcontrib><creatorcontrib>Löbenberg, Raimar</creatorcontrib><title>Development of a novel cannabinoid-loaded microemulsion towards an improved stability and transdermal delivery</title><title>International journal of pharmaceutics</title><description>[Display omitted]
The aim of this study was to develop a stable microemulsion (ME) for transdermal delivery of tetrahydrocannabinolic acid (THCA) and cannabidiolic acid (CBDA). The lipid-based vehicles were selected by screening cannabinoid solubility and the emulsifying ability of surfactants. Pseudo-ternary phase diagrams were constructed by formulation of cannabinoids with Capryol® 90 as oil phase, Tween® 80, Solutol® HS15, Procetyl® AWS, and Cremophor® RH40 as surfactants, ethanol as cosurfactant, and distilled water as the aqueous phase. A significant improvement in transmembrane flux (Jss), permeability coefficient (Kp), and enhancement ratio (ER) was found in one system compared to other formulations. This ME consisted of 1.0% (w/w) of cannabinoids, 5% (w/w) of Capryol® 90, 44% (w/w) Smix (2:1, Procetyl® AWS and Ethanol) and 50.0% (w/w) of distilled water. Additionally, the effects of pH on the permeation of the cannabinoids were investigated. Based on the pH value THCA and CBDA-loaded ME exhibited the highest permeation at pH 5.17 and pH 5.25. After storing the pH-adjusted P2 ME and the optimized P2 ME for 180 days at 4℃ and 25℃, the content of cannabinoids was over 95%. Consequently, the cannabinoid-loaded ME system is a promising option for solubilizing and stabilizing lipophilic drugs like cannabinoids and utilize them for transdermal delivery.</description><subject>Acidic cannabinoids</subject><subject>Cannabidiolic acid</subject><subject>Cannabinoids</subject><subject>Lipid-based vehicle</subject><subject>Microemulsion</subject><subject>Tetrahydrocannabinolic acid</subject><subject>Transdermal delivery</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><recordid>eNqFkEtLAzEUhYMoWB8_QcjSzdQ8ZpJ0JVKfUHCj65BJ7mBKJqnJtNJ_b0rdu7pwuOdwzofQDSVzSqi4W8_9evNl8jhnhNE5ZUQKcYJmVEne8FaKUzQjXKqmo5Kfo4tS1oQQwSifofgIOwhpM0KccBqwwTFVAVsTo-l9TN41IRkHDo_e5gTjNhSfIp7Sj8muYBOxHze5mhwuU7UEP-2r6vCUTSwO8mgCdhD8DvL-Cp0NJhS4_ruX6PP56WP52qzeX96WD6vG8pZNTccdG9pBUdopCkwxpawSg2j7drGgA-Oi72t9CUPrFBVgWc_6xYIwaa3sFeGX6PaYW5t9b6FMevTFQggmQtoWzTouBa_wVH3tjq91XSkZBr3JfjR5rynRB756rf_46gNffeRbffdHH9QdOw9ZF-shWnA-g520S_6fhF_ksIhV</recordid><startdate>20210715</startdate><enddate>20210715</enddate><creator>Park, Chulhun</creator><creator>Zuo, Jieyu</creator><creator>Somayaji, Vijay</creator><creator>Lee, Beom-Jin</creator><creator>Löbenberg, Raimar</creator><general>Elsevier B.V</general><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20210715</creationdate><title>Development of a novel cannabinoid-loaded microemulsion towards an improved stability and transdermal delivery</title><author>Park, Chulhun ; Zuo, Jieyu ; Somayaji, Vijay ; Lee, Beom-Jin ; Löbenberg, Raimar</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c342t-53d2f4f811581e28288c86f64b4991f236bb2137ef4d816ec2b2b99027cc7b803</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>Acidic cannabinoids</topic><topic>Cannabidiolic acid</topic><topic>Cannabinoids</topic><topic>Lipid-based vehicle</topic><topic>Microemulsion</topic><topic>Tetrahydrocannabinolic acid</topic><topic>Transdermal delivery</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Park, Chulhun</creatorcontrib><creatorcontrib>Zuo, Jieyu</creatorcontrib><creatorcontrib>Somayaji, Vijay</creatorcontrib><creatorcontrib>Lee, Beom-Jin</creatorcontrib><creatorcontrib>Löbenberg, Raimar</creatorcontrib><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Park, Chulhun</au><au>Zuo, Jieyu</au><au>Somayaji, Vijay</au><au>Lee, Beom-Jin</au><au>Löbenberg, Raimar</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development of a novel cannabinoid-loaded microemulsion towards an improved stability and transdermal delivery</atitle><jtitle>International journal of pharmaceutics</jtitle><date>2021-07-15</date><risdate>2021</risdate><volume>604</volume><spage>120766</spage><epage>120766</epage><pages>120766-120766</pages><artnum>120766</artnum><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>[Display omitted]
The aim of this study was to develop a stable microemulsion (ME) for transdermal delivery of tetrahydrocannabinolic acid (THCA) and cannabidiolic acid (CBDA). The lipid-based vehicles were selected by screening cannabinoid solubility and the emulsifying ability of surfactants. Pseudo-ternary phase diagrams were constructed by formulation of cannabinoids with Capryol® 90 as oil phase, Tween® 80, Solutol® HS15, Procetyl® AWS, and Cremophor® RH40 as surfactants, ethanol as cosurfactant, and distilled water as the aqueous phase. A significant improvement in transmembrane flux (Jss), permeability coefficient (Kp), and enhancement ratio (ER) was found in one system compared to other formulations. This ME consisted of 1.0% (w/w) of cannabinoids, 5% (w/w) of Capryol® 90, 44% (w/w) Smix (2:1, Procetyl® AWS and Ethanol) and 50.0% (w/w) of distilled water. Additionally, the effects of pH on the permeation of the cannabinoids were investigated. Based on the pH value THCA and CBDA-loaded ME exhibited the highest permeation at pH 5.17 and pH 5.25. After storing the pH-adjusted P2 ME and the optimized P2 ME for 180 days at 4℃ and 25℃, the content of cannabinoids was over 95%. Consequently, the cannabinoid-loaded ME system is a promising option for solubilizing and stabilizing lipophilic drugs like cannabinoids and utilize them for transdermal delivery.</abstract><pub>Elsevier B.V</pub><doi>10.1016/j.ijpharm.2021.120766</doi><tpages>1</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0378-5173 |
| ispartof | International journal of pharmaceutics, 2021-07, Vol.604, p.120766-120766, Article 120766 |
| issn | 0378-5173 1873-3476 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_2537630168 |
| source | ScienceDirect Journals (5 years ago - present) |
| subjects | Acidic cannabinoids Cannabidiolic acid Cannabinoids Lipid-based vehicle Microemulsion Tetrahydrocannabinolic acid Transdermal delivery |
| title | Development of a novel cannabinoid-loaded microemulsion towards an improved stability and transdermal delivery |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-13T22%3A44%3A17IST&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=Development%20of%20a%20novel%20cannabinoid-loaded%20microemulsion%20towards%20an%20improved%20stability%20and%20transdermal%20delivery&rft.jtitle=International%20journal%20of%20pharmaceutics&rft.au=Park,%20Chulhun&rft.date=2021-07-15&rft.volume=604&rft.spage=120766&rft.epage=120766&rft.pages=120766-120766&rft.artnum=120766&rft.issn=0378-5173&rft.eissn=1873-3476&rft_id=info:doi/10.1016/j.ijpharm.2021.120766&rft_dat=%3Cproquest_cross%3E2537630168%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=2537630168&rft_id=info:pmid/&rft_els_id=S0378517321005718&rfr_iscdi=true |