Topical co-delivery of indomethacin and nigella sativa L. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity

Indomethacin is a potent, nonselective Non-steroidal Antiinflammatory Drug (NSAID) but its low water-solubility precludes its use as topical dosage form. As with other NSAIDs, the systemic delivery is associated with high risk of serious gastrointestinal adverse events including bleeding, ulcera...

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Main Authors: Badri, Waisudin, Mohamed, Farahidah, Mohd Shafri, Mohd Affendi, El Asbahani, A., Miladi, Karim, Nazari, Qand Agha, Viennet, Celine, Robin, Sophie, Fessi, Hatem, Elaissari, Abdelhamid
Format: Article
Language:English
Published: International Journal of Advanced Research (IJAR) 2018
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Online Access:http://irep.iium.edu.my/66791/
http://irep.iium.edu.my/66791/
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http://irep.iium.edu.my/66791/1/443_IJAR%20indomethacin%20microparticles.pdf
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spelling iium-667912018-10-19T08:22:01Z http://irep.iium.edu.my/66791/ Topical co-delivery of indomethacin and nigella sativa L. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity Badri, Waisudin Mohamed, Farahidah Mohd Shafri, Mohd Affendi El Asbahani, A. Miladi, Karim Nazari, Qand Agha Viennet, Celine Robin, Sophie Fessi, Hatem Elaissari, Abdelhamid RM Therapeutics. Pharmacology RS Pharmacy and materia medica Indomethacin is a potent, nonselective Non-steroidal Antiinflammatory Drug (NSAID) but its low water-solubility precludes its use as topical dosage form. As with other NSAIDs, the systemic delivery is associated with high risk of serious gastrointestinal adverse events including bleeding, ulceration and perforation of stomach and intestines. Here we demonstrate a safer way of administration i.e via topical demonstrating synergistic effects when co-delivered with Nigella sativa L. seeds essential oil (NSSEO) in the form of coencapsulated particles (~200 nm) of poly--caprolactone. The particles showed penetrability across stratum corneum to dermis layer in ex-vivo human skin. Further study in the xyline-induced ear edema in mice was performed, and co-encapsulated particles demonstrated highest antiinflammatory effect compared to indomethacin particles and indomethacin gels. Despite slower onset compared to indomethacin gels, the inflamed ear continued to show reduction in thickness over 8 hours of observation demonstrating synergistic and pro-longed effect contributed by NSSEO. In immunohistochemistry study of CD45+, the mice ears treated with co-encapsulated particles showed considerable reduction in lesions, epidermal-dermal separation and inflammatory cells (lymphocytes and neutrophils) infiltration as compared to other formulation. Based on microscopic evaluation, the anti-inflammatory inhibition effect of co-encapsulated particles is the highest (90%) followed by indomethacin particles (79%) and indomethacin gel (49%). The findings suggest not only skin permeability of indomethacin significantly improved but also the therapeutic effects, all provided by the presence of NSSEO in the particles. This study paves the way to more co-encapsulation of any other contemporary medicines in combination with this wholesome natural oil, NSSEO. International Journal of Advanced Research (IJAR) 2018-04 Article PeerReviewed application/pdf en http://irep.iium.edu.my/66791/1/443_IJAR%20indomethacin%20microparticles.pdf Badri, Waisudin and Mohamed, Farahidah and Mohd Shafri, Mohd Affendi and El Asbahani, A. and Miladi, Karim and Nazari, Qand Agha and Viennet, Celine and Robin, Sophie and Fessi, Hatem and Elaissari, Abdelhamid (2018) Topical co-delivery of indomethacin and nigella sativa L. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity. International Journal of Advanced Research, 6 (4). pp. 801-816. ISSN 2320-5407 http://www.journalijar.com/uploads/443_IJAR-22995.pdf 10.21474/IJAR01/6916
repository_type Digital Repository
institution_category Local University
institution International Islamic University Malaysia
building IIUM Repository
collection Online Access
language English
topic RM Therapeutics. Pharmacology
RS Pharmacy and materia medica
spellingShingle RM Therapeutics. Pharmacology
RS Pharmacy and materia medica
Badri, Waisudin
Mohamed, Farahidah
Mohd Shafri, Mohd Affendi
El Asbahani, A.
Miladi, Karim
Nazari, Qand Agha
Viennet, Celine
Robin, Sophie
Fessi, Hatem
Elaissari, Abdelhamid
Topical co-delivery of indomethacin and nigella sativa L. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity
description Indomethacin is a potent, nonselective Non-steroidal Antiinflammatory Drug (NSAID) but its low water-solubility precludes its use as topical dosage form. As with other NSAIDs, the systemic delivery is associated with high risk of serious gastrointestinal adverse events including bleeding, ulceration and perforation of stomach and intestines. Here we demonstrate a safer way of administration i.e via topical demonstrating synergistic effects when co-delivered with Nigella sativa L. seeds essential oil (NSSEO) in the form of coencapsulated particles (~200 nm) of poly--caprolactone. The particles showed penetrability across stratum corneum to dermis layer in ex-vivo human skin. Further study in the xyline-induced ear edema in mice was performed, and co-encapsulated particles demonstrated highest antiinflammatory effect compared to indomethacin particles and indomethacin gels. Despite slower onset compared to indomethacin gels, the inflamed ear continued to show reduction in thickness over 8 hours of observation demonstrating synergistic and pro-longed effect contributed by NSSEO. In immunohistochemistry study of CD45+, the mice ears treated with co-encapsulated particles showed considerable reduction in lesions, epidermal-dermal separation and inflammatory cells (lymphocytes and neutrophils) infiltration as compared to other formulation. Based on microscopic evaluation, the anti-inflammatory inhibition effect of co-encapsulated particles is the highest (90%) followed by indomethacin particles (79%) and indomethacin gel (49%). The findings suggest not only skin permeability of indomethacin significantly improved but also the therapeutic effects, all provided by the presence of NSSEO in the particles. This study paves the way to more co-encapsulation of any other contemporary medicines in combination with this wholesome natural oil, NSSEO.
format Article
author Badri, Waisudin
Mohamed, Farahidah
Mohd Shafri, Mohd Affendi
El Asbahani, A.
Miladi, Karim
Nazari, Qand Agha
Viennet, Celine
Robin, Sophie
Fessi, Hatem
Elaissari, Abdelhamid
author_facet Badri, Waisudin
Mohamed, Farahidah
Mohd Shafri, Mohd Affendi
El Asbahani, A.
Miladi, Karim
Nazari, Qand Agha
Viennet, Celine
Robin, Sophie
Fessi, Hatem
Elaissari, Abdelhamid
author_sort Badri, Waisudin
title Topical co-delivery of indomethacin and nigella sativa L. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity
title_short Topical co-delivery of indomethacin and nigella sativa L. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity
title_full Topical co-delivery of indomethacin and nigella sativa L. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity
title_fullStr Topical co-delivery of indomethacin and nigella sativa L. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity
title_full_unstemmed Topical co-delivery of indomethacin and nigella sativa L. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity
title_sort topical co-delivery of indomethacin and nigella sativa l. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity
publisher International Journal of Advanced Research (IJAR)
publishDate 2018
url http://irep.iium.edu.my/66791/
http://irep.iium.edu.my/66791/
http://irep.iium.edu.my/66791/
http://irep.iium.edu.my/66791/1/443_IJAR%20indomethacin%20microparticles.pdf
first_indexed 2023-09-18T21:34:51Z
last_indexed 2023-09-18T21:34:51Z
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