Pharmacological effects of a complex α-bisabolol/β-cyclodextrin in a mice arthritis model with involvement of IL-1β, IL-6 and MAPK

• Published in: Biomedicine & pharmacotherapy Vol. 151; p. 113142
• Main Authors: Heimfarth, Luana, Rezende, Marília Matos, Pereira, Erik Willyame Menezes, Passos, Fabiolla Rocha Santos, Monteiro, Brenda Souza, Santos, Tiffany Karoline Barroso, Lima, Natália Teles, Souza, Isana Carla Leal, de Albuquerque Junior, Ricardo Luiz Cavalcanti, de Souza Siqueira Lima, Pollyana, de Souza Araújo, Adriano Antunes, Quintans Júnior, Lucindo José, Kim, Bonglee, Coutinho, Henrique D.M., de Souza Siqueira Quintans, Jullyana
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 01-07-2022; Elsevier
• Subjects: Arthritis; Cyclodextrin; Inflammation; Nociception; Oxidative stress; Terpene; Nociception; Oxidative stress; Terpene; Cyclodextrin; Arthritis; Inflammation
• ISSN: 0753-3322; 1950-6007
• DOI: 10.1016/j.biopha.2022.113142

Inflammatory arthritis is the most prevalent chronic inflammatory disease worldwide. The pathology of the disease is characterized by increased inflammation and oxidative stress, which leads to chronic pain and functional loss in the joints. Conventional anti-arthritic drugs used to relieve pain and other arthritic symptoms often cause severe side effects. α-bisabolol (BIS) is a sesquiterpene that exhibits high anti-inflammatory potential and a significant antinociceptive effect. This study evaluates the anti-arthritic, anti-inflammatory and antihyperalgesic effects of BIS alone and in a β-cyclodextrin (βCD/BIS) inclusion complex in a CFA-induced arthritis model. Following the intra-articular administration of CFA, male mice were treated with vehicle, BIS and βCD/BIS (50 mg/kg, p.o.) or a positive control and pain-related behaviors, knee edema and inflammatory and oxidative parameters were evaluated on days 4, 11, 18 and/or 25. Ours findings shows that the oral administration of BIS and βCD/BIS significantly attenuated spontaneous pain-like behaviors, mechanical hyperalgesia, grip strength deficit and knee edema induced by repeated injections of CFA, reducing the joint pain and functional disability associated with arthritis. BIS and βCD/BIS also inhibited the generation of inflammatory and oxidative markers in the knee and blocked MAPK in the spinal cord. In addition, ours results also showed that the incorporation of BIS in cyclodextrin as a drug delivery system improved the pharmacological profile of this substance. Therefore, these results contribute to the pharmacological knowledge of BIS and demonstrated that this terpene appears to be able to mitigate deleterious symptoms of arthritis.