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Topical Nano-Vesicular Spanlastics of Celecoxib: Enhanced Anti-Inflammatory Effect and Down-Regulation of TNF-α, NF-кB and COX-2 in Complete Freund’s Adjuvant-Induced Arthritis Model in Rats

Authors Alaaeldin E, Abou-Taleb HA, Mohamad SA, Elrehany M, Gaber SS, Mansour HF

Received 1 November 2020

Accepted for publication 18 December 2020

Published 8 January 2021 Volume 2021:16 Pages 133—145

DOI https://doi.org/10.2147/IJN.S289828

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 4

Editor who approved publication: Prof. Dr. Thomas J. Webster


Eman Alaaeldin,1,2 Heba A Abou-Taleb,3 Soad A Mohamad,1 Mahmoud Elrehany,4,5 Shereen S Gaber,5 Heba F Mansour2

1Department of Pharmaceutics, Faculty of Pharmacy, Deraya University, Minia, Egypt; 2Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Nahda University (NUB), Beni-Suef, Egypt; 4Department of Biochemistry, Faculty of Pharmacy, Deraya University, Minia, Egypt; 5Department of Biochemistry, Faculty of Medicine, Minia University, Minia, Egypt

Correspondence: Eman Alaaeldin
Department of Pharmaceutics, Faculty of Pharmacy, Minia University, P.O. Box: 61111, Minia, Egypt
Email Eman_alaa_eldin@yahoo.com

Background: Rheumatoid arthritis (RA) is an autoimmune disease that underlies chronic inflammation of the synovial membrane. Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly used to treat RA. However, a long list of adverse events associated with long-term treatment regimens with NSAIDs negatively influences patient compliance and therapeutic outcomes.
Aim: The aim of this work was to achieve site-specific delivery of celecoxib-loaded spanlastic nano-vesicle-based delivery system to the inflamed joints, avoiding systemic administration of large doses.
Methodology: To develop spanlastic nanovesicles for transdermal delivery of celecoxib, modified injection method was adopted using Tween 80 or Brij as edge activators. Entrapment efficiency, vesicle size, ex vivo permeation, and morphology of the prepared nano-vesicles were characterized. Carbopol-based gels containing the selected formulations were prepared, and their clarity, pH, rheological performance, and ex vivo permeation were characterized. Celecoxib-loaded niosomes and noisome-containing gels were developed for comparison. The in vivo efficacy of the selected formulations was evaluated in a rat model of Freund’s complete adjuvant-induced arthritis. Different inflammatory markers including TNF-α, NF-кB and COX-2 were assessed in paw tissue before and after treatment.
Results: The size and entrapment efficiency of the selected spanlastic nano-vesicle formulation were 112.5 ± 3.6 nm, and 83.6 ± 2.3%, respectively. This formulation has shown the highest transdermal flux and permeability coefficient compared to the other investigated formulations. The spanlastics-containing gel of celecoxib has shown transdermal flux of 6.9 ± 0.25 μg/cm2/hr while the celecoxib niosomes-containing gel and unprocessed celecoxib-loaded gel have shown 5.2 ± 0.12 μg/cm2/hr and 0.64 ± 0.09 μg/cm2/hr, respectively. In the animal model of RA, the celecoxib-loaded spanlastics-containing gel significantly reduced edema circumference and significantly suppressed TNF-α, NF-кB and COX-2 levels compared to the niosomes-containing gel, the marketed diclofenac sodium gel, and unprocessed celecoxib-loaded gel.
Conclusion: The spanlastic nano-vesicle-containing gel represents a more efficient site-specific treatment for topical treatment of chronic inflammation like RA, compared to commercial and other conventional alternatives.

Keywords: nano-vesicles, spanlastics, celecoxib, niosomes, arthritis

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