Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory Activity
The aim of this study was to encapsulate cannabidiol (CBD) extract in nanostructured lipid carriers (NLCs) to improve the chemical stability and anti-inflammatory activity of CBD for dermal delivery. CBD-loaded NLCs (CBD-NLCs) were prepared using cetyl palmitate (CP) as a solid lipid and stabilized...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-02-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/2/537 |
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| author | Boontida Morakul Varaporn Buraphacheep Junyaprasert Krisada Sakchaisri Veerawat Teeranachaideekul |
| author_facet | Boontida Morakul Varaporn Buraphacheep Junyaprasert Krisada Sakchaisri Veerawat Teeranachaideekul |
| author_sort | Boontida Morakul |
| collection | DOAJ |
| description | The aim of this study was to encapsulate cannabidiol (CBD) extract in nanostructured lipid carriers (NLCs) to improve the chemical stability and anti-inflammatory activity of CBD for dermal delivery. CBD-loaded NLCs (CBD-NLCs) were prepared using cetyl palmitate (CP) as a solid lipid and stabilized with Tego<sup>®</sup> Care 450 (TG450) or poloxamer 188 (P188) by high-pressure homogenization (HPH). The CBD extract was loaded at 1% <i>w</i>/<i>w</i>. Three different oils were employed to produce CBD-NLCs, including Transcutol<sup>®</sup> P, medium-chain triglycerides (MCT), and oleic acid (OA). CBD-NLCs were successfully prepared with an entrapment efficiency (E.E.) of 100%. All formulations showed particle sizes between 160 and 200 nm with PDIs less than 0.10. The type of surfactant and oil used affected the particle sizes, zeta potential, and crystallinity of the CBD-NLCs. CBD-NLCs stabilized with TG450 showed higher crystallinity after production and storage at 30 °C for 30 days as compared to those with P188. Encapsulation of the CBD extract in NLCs enhanced its chemical stability after exposure to simulated sunlight (1000 kJ/m<sup>2</sup>) compared to that of the CBD extract in ethanolic solution. The CBD-NLCs prepared from MCT and OA showed slower CBD release compared with that from Transcutol<sup>®</sup> P, and the kinetic data for release of CBD from CBD-NLCs followed Higuchi’s release model with a high coefficient of determination (>0.95). The extent of CBD permeation through Strat-M<sup>®</sup> depended on the oil type. The cytotoxicity of the CBD extract on HaCaT and HDF cells was reduced by encapsulation in the NLCs. The anti-inflammatory activity of the CBD extract in RAW264.7 cell macrophages was enhanced by encapsulation in CBD-NLCs prepared from MCT and OA. |
| first_indexed | 2024-03-11T08:16:46Z |
| format | Article |
| id | doaj.art-4f3f358347a149cb8ff34552c3a693de |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T08:16:46Z |
| publishDate | 2023-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-4f3f358347a149cb8ff34552c3a693de2023-11-16T22:41:16ZengMDPI AGPharmaceutics1999-49232023-02-0115253710.3390/pharmaceutics15020537Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory ActivityBoontida Morakul0Varaporn Buraphacheep Junyaprasert1Krisada Sakchaisri2Veerawat Teeranachaideekul3Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, ThailandDepartment of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, ThailandDepartment of Pharmacology, Faculty of Pharmacy, Mahidol University, Bangkok 10400, ThailandDepartment of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, ThailandThe aim of this study was to encapsulate cannabidiol (CBD) extract in nanostructured lipid carriers (NLCs) to improve the chemical stability and anti-inflammatory activity of CBD for dermal delivery. CBD-loaded NLCs (CBD-NLCs) were prepared using cetyl palmitate (CP) as a solid lipid and stabilized with Tego<sup>®</sup> Care 450 (TG450) or poloxamer 188 (P188) by high-pressure homogenization (HPH). The CBD extract was loaded at 1% <i>w</i>/<i>w</i>. Three different oils were employed to produce CBD-NLCs, including Transcutol<sup>®</sup> P, medium-chain triglycerides (MCT), and oleic acid (OA). CBD-NLCs were successfully prepared with an entrapment efficiency (E.E.) of 100%. All formulations showed particle sizes between 160 and 200 nm with PDIs less than 0.10. The type of surfactant and oil used affected the particle sizes, zeta potential, and crystallinity of the CBD-NLCs. CBD-NLCs stabilized with TG450 showed higher crystallinity after production and storage at 30 °C for 30 days as compared to those with P188. Encapsulation of the CBD extract in NLCs enhanced its chemical stability after exposure to simulated sunlight (1000 kJ/m<sup>2</sup>) compared to that of the CBD extract in ethanolic solution. The CBD-NLCs prepared from MCT and OA showed slower CBD release compared with that from Transcutol<sup>®</sup> P, and the kinetic data for release of CBD from CBD-NLCs followed Higuchi’s release model with a high coefficient of determination (>0.95). The extent of CBD permeation through Strat-M<sup>®</sup> depended on the oil type. The cytotoxicity of the CBD extract on HaCaT and HDF cells was reduced by encapsulation in the NLCs. The anti-inflammatory activity of the CBD extract in RAW264.7 cell macrophages was enhanced by encapsulation in CBD-NLCs prepared from MCT and OA.https://www.mdpi.com/1999-4923/15/2/537cannabidiol extractnanostructured lipid carriersphysicochemical propertiespermeationphotostabilitydermal delivery |
| spellingShingle | Boontida Morakul Varaporn Buraphacheep Junyaprasert Krisada Sakchaisri Veerawat Teeranachaideekul Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory Activity Pharmaceutics cannabidiol extract nanostructured lipid carriers physicochemical properties permeation photostability dermal delivery |
| title | Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory Activity |
| title_full | Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory Activity |
| title_fullStr | Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory Activity |
| title_full_unstemmed | Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory Activity |
| title_short | Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory Activity |
| title_sort | cannabidiol loaded nanostructured lipid carriers nlcs for dermal delivery enhancement of photostability cell viability and anti inflammatory activity |
| topic | cannabidiol extract nanostructured lipid carriers physicochemical properties permeation photostability dermal delivery |
| url | https://www.mdpi.com/1999-4923/15/2/537 |
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