Therapeutic effects of lornoxicam-loaded nanomicellar formula in experimental models of rheumatoid arthritis

• Published in: International journal of nanomedicine 2017-01, Vol.12, p.7015-7023
• Main Authors: Helmy, Hebatullah Samy, El-Sahar, Ayman E, Sayed, Rabab H, Shamma, Rehab Nabil, Salama, Alaa Hamed, Elbaz, Eman Maher
• Format: Article
• Language: English
• Subjects: Analgesics; Analysis; Anti-inflammatory agents; Brownian motion; Care and treatment; Drug delivery systems; Edema; Health aspects; Inflammation; inflammatory mediators; Laboratory animals; lornoxicam; Morphology; nano-carriers; Nonsteroidal anti-inflammatory drugs; Original Research; Pain; Pathogenesis; Pharmacokinetics; Pharmacy; polymeric micelles; Rheumatoid arthritis; Rheumatology; Smokers
• ISSN: 1178-2013; 1176-9114; 1178-2013
• DOI: 10.2147/IJN.S147738

Rheumatoid arthritis (RA) is a chronic inflammatory disease treated by nonsteroidal anti-inflammatory drugs (NSAIDs) including lornoxicam (LX). Nanocarriers have been used to increase the efficacy and reduce the side effects of various drugs. The objective of the present study was to compare the therapeutic efficacy of systemic administration of lornoxicam-loaded nanomicellar formula (LX-NM) with that of free LX. The LX-loaded mixed polymeric nanomicellar formula was prepared by direct equilibrium technique. Two rat models were used in the study: carrageenan-induced acute edema and Freund's complete adjuvant (FCA)-induced chronic arthritis. The inhibitory effect of LX-NM on carrageenan-induced edema was higher than free LX for the same dose (1.3 mg/kg, i.p.). LX-NM (0.325 mg/kg, i.p.) produced effects comparable to that of diclofenac, which served as a standard. In the FCA model, daily treatment with LX-NM (0.325 mg/kg, i.p.) starting on day 14 significantly reduced the percentage of edema and increased weight growth. However, the same dose of LX failed to confer any significant change. Additionally, LX-NM significantly attenuated the rise of tumor necrosis factor-α (TNF-α), interleukin-1β, prostaglandin E2, nuclear factor-κβ, malondialdehyde and nitric oxide serum levels. In contrast, LX failed to show any significant reduction in elevated serum biomarkers except for TNF-α. LX-NM is an alternative delivery system that is simply prepared at low costs. It showed a superior therapeutic efficacy against RA compared to free LX. Thus, LX-NM can be considered as a promising candidate for treatment of RA and similar inflammatory disorders.