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...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
International Journal of Advanced Research (IJAR)
2018
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| Subjects: | |
| Online Access: | 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 |
| Summary: | 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. |
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