β-Caryophyllene-Loaded Microemulsion-Based Topical Hydrogel: A Promising Carrier to Enhance the Analgesic and Anti-Inflammatory Outcomes
Musculoskeletal pain and inflammation can vary from localised pain like pain in the shoulders and neck to widespread pain like fibromyalgia, and as per estimates, around 90% of humans have experienced such pain. Oral non-steroidal anti-inflammatory drugs (NSAIDs) are frequently prescribed for such c...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-08-01
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| Series: | Gels |
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| Online Access: | https://www.mdpi.com/2310-2861/9/8/634 |
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| author | Sitah Alharthi Zyta Maria Ziora Gulam Mustafa Pramila Chaubey Ahmed Farag El Kirdasy Ghallab Alotaibi |
| author_facet | Sitah Alharthi Zyta Maria Ziora Gulam Mustafa Pramila Chaubey Ahmed Farag El Kirdasy Ghallab Alotaibi |
| author_sort | Sitah Alharthi |
| collection | DOAJ |
| description | Musculoskeletal pain and inflammation can vary from localised pain like pain in the shoulders and neck to widespread pain like fibromyalgia, and as per estimates, around 90% of humans have experienced such pain. Oral non-steroidal anti-inflammatory drugs (NSAIDs) are frequently prescribed for such conditions but are associated with concerns like gastric irritation and bleeding. In the present study, a microemulsion-based gel comprising β-caryophyllene, isopropyl myristate, Tween 80, and normal saline was prepared as a topical option for managing topical pain and inflammation. The globules of the microemulsion were below 100 nm with a zetapotential of around −10 mV. The drug entrapment was >87% with a drug loading of >23%. The permeation studies established better skin permeation (20.11 ± 0.96 μg cm<sup>−2</sup> h<sup>−1</sup>) and retention of the drug (4.96 ± 0.02%) from the developed system vis-à-vis the conventional product (9.73 ± 0.35 μg cm<sup>−2</sup> h<sup>−1</sup>; 1.03 ± 0.01%). The dermatokinetic studies established the better pharmacokinetic profile of the bioactive in the epidermis and dermis layers of the skin. The anti-inflammatory potential in carrageenan-induced rat paw oedema was more pronounced than the conventional product (~91% vis-à-vis ~77%), indicating a better pharmacodynamic outcome from the developed system. The nanotechnology-based natural bioactive product with improved efficacy and drug loading can provide a better alternative for the management of musculoskeletal pain. |
| first_indexed | 2024-03-10T23:55:47Z |
| format | Article |
| id | doaj.art-de549a3490a546838c74f306e6c098a9 |
| institution | Directory Open Access Journal |
| issn | 2310-2861 |
| language | English |
| last_indexed | 2024-03-10T23:55:47Z |
| publishDate | 2023-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Gels |
| spelling | doaj.art-de549a3490a546838c74f306e6c098a92023-11-19T01:13:33ZengMDPI AGGels2310-28612023-08-019863410.3390/gels9080634β-Caryophyllene-Loaded Microemulsion-Based Topical Hydrogel: A Promising Carrier to Enhance the Analgesic and Anti-Inflammatory OutcomesSitah Alharthi0Zyta Maria Ziora1Gulam Mustafa2Pramila Chaubey3Ahmed Farag El Kirdasy4Ghallab Alotaibi5Department of Pharmaceutical Sciences, College of Pharmacy, Shaqra University, Al-Dawadmi Campus, Al-Dawadmi 11961, Saudi ArabiaInstitute for Molecular Bioscience, University of Queensland, St. Lucia, QL 4072, AustraliaDepartment of Pharmaceutical Sciences, College of Pharmacy, Shaqra University, Al-Dawadmi Campus, Al-Dawadmi 11961, Saudi ArabiaDepartment of Pharmaceutical Sciences, College of Pharmacy, Shaqra University, Al-Dawadmi Campus, Al-Dawadmi 11961, Saudi ArabiaDepartment of Biochemistry, College of Veterinary Medicine, Sadat City University, Sadat City 32897, EgyptDepartment of Pharmaceutical Sciences, College of Pharmacy, Shaqra University, Al-Dawadmi Campus, Al-Dawadmi 11961, Saudi ArabiaMusculoskeletal pain and inflammation can vary from localised pain like pain in the shoulders and neck to widespread pain like fibromyalgia, and as per estimates, around 90% of humans have experienced such pain. Oral non-steroidal anti-inflammatory drugs (NSAIDs) are frequently prescribed for such conditions but are associated with concerns like gastric irritation and bleeding. In the present study, a microemulsion-based gel comprising β-caryophyllene, isopropyl myristate, Tween 80, and normal saline was prepared as a topical option for managing topical pain and inflammation. The globules of the microemulsion were below 100 nm with a zetapotential of around −10 mV. The drug entrapment was >87% with a drug loading of >23%. The permeation studies established better skin permeation (20.11 ± 0.96 μg cm<sup>−2</sup> h<sup>−1</sup>) and retention of the drug (4.96 ± 0.02%) from the developed system vis-à-vis the conventional product (9.73 ± 0.35 μg cm<sup>−2</sup> h<sup>−1</sup>; 1.03 ± 0.01%). The dermatokinetic studies established the better pharmacokinetic profile of the bioactive in the epidermis and dermis layers of the skin. The anti-inflammatory potential in carrageenan-induced rat paw oedema was more pronounced than the conventional product (~91% vis-à-vis ~77%), indicating a better pharmacodynamic outcome from the developed system. The nanotechnology-based natural bioactive product with improved efficacy and drug loading can provide a better alternative for the management of musculoskeletal pain.https://www.mdpi.com/2310-2861/9/8/634analgesiananocarrierskin permeationsafetybioavailabilitymicroemulsion |
| spellingShingle | Sitah Alharthi Zyta Maria Ziora Gulam Mustafa Pramila Chaubey Ahmed Farag El Kirdasy Ghallab Alotaibi β-Caryophyllene-Loaded Microemulsion-Based Topical Hydrogel: A Promising Carrier to Enhance the Analgesic and Anti-Inflammatory Outcomes Gels analgesia nanocarrier skin permeation safety bioavailability microemulsion |
| title | β-Caryophyllene-Loaded Microemulsion-Based Topical Hydrogel: A Promising Carrier to Enhance the Analgesic and Anti-Inflammatory Outcomes |
| title_full | β-Caryophyllene-Loaded Microemulsion-Based Topical Hydrogel: A Promising Carrier to Enhance the Analgesic and Anti-Inflammatory Outcomes |
| title_fullStr | β-Caryophyllene-Loaded Microemulsion-Based Topical Hydrogel: A Promising Carrier to Enhance the Analgesic and Anti-Inflammatory Outcomes |
| title_full_unstemmed | β-Caryophyllene-Loaded Microemulsion-Based Topical Hydrogel: A Promising Carrier to Enhance the Analgesic and Anti-Inflammatory Outcomes |
| title_short | β-Caryophyllene-Loaded Microemulsion-Based Topical Hydrogel: A Promising Carrier to Enhance the Analgesic and Anti-Inflammatory Outcomes |
| title_sort | β caryophyllene loaded microemulsion based topical hydrogel a promising carrier to enhance the analgesic and anti inflammatory outcomes |
| topic | analgesia nanocarrier skin permeation safety bioavailability microemulsion |
| url | https://www.mdpi.com/2310-2861/9/8/634 |
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