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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International Journal of Advanced Research (IJAR)
2018
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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 |
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RM Therapeutics. Pharmacology RS Pharmacy and materia medica |
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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 |
_version_ |
1777412752758800384 |