Dermatopharmacokinetic and pharmacodynamic evaluation of a novel nanostructured formulation containing capsaicinoids for treating neuropathic pain

Autor(es)

Lorenzoni, Ricardo ^{[1, 2]} ; Contri, Renata Vidor ^{[1, 3]} ; Freitas de Lima, Cleverton Kleiton ^[4] ; Barreto, Fabiano ^[5] ; de Araujo, Bibiana Verlindo ^[1] ; Pohlmann, Adriana Raffin ^[1] ; Palhares de Miranda, Ana Luisa ^[4] ; Dalla Costa, Teresa ^[1] ; Guterres, Silvia Staniscuaski ^[1]

Afiliação do(s) autor(es)

^[1] Univ Fed Rio Grande do Sul, Coll Pharm, Pharmaceut Sci Grad Program, Porto Alegre, RS - Brazil

^[2] Univ Coimbra, Fac Med, Ctr Neurosci & Cell Biol, Rua Larga, P-3004504 Coimbra - Portugal

^[3] Univ Fed Rio Grande do Sul, Coll Pharm, Porto Alegre, RS - Brazil

^[4] Univ Fed Rio de Janeiro, Fac Pharm, Rio De Janeiro, RJ - Brazil

^[5] Lab Nacl Agropecuario Rio Grande LANAGRO RS, Porto Alegre, RS - Brazil

• Tipo de documento: Artigo Científico
• Fonte: International Journal of Pharmaceutics; v. 596, MAR 1 2021.
• Citações Web of Science: 0

Resumo

The in vivo skin penetration by dermal microdialysis and the pharmacological efficacy of a chitosan hydrogel containing capsaicinoids-loaded nanocapsules (CHNCcaps) was evaluated in this study. Such gel has previously been proven to control capsaicinoids release and decrease the drugs side effects in humans. The nanocapsules containing capsaicinoids had an average size around 150 nm, with a low polydispersity index, positive zeta potential, and high encapsulation efficiency of the drugs. The CHNC caps showed intact nanocapsules, a slightly acid pH value, and a pseudoplastic behavior suitable for topical application. Microdialysis experiments showed a 1.6-fold increase in the concentration of capsaicinoids in the dermis (after 12 h of its application) when CHNCCaps was administered compared to a chitosan hydrogel containing capsaicinoids in hydroethanolic solution (CHETcaps) and the commercial cream. The CHNC caps showed antiallodynic and antihyperalgesic effects from 6 h to 96 h after treatment initiation, whereas CHET caps and the commercial cream showed antiallodynic and antihyperalgesic effects only at 48 h and 96 h after treatment initiation, respectively. CHNC caps and the commercial cream maintained antihyperalgesic activity for 6 days after treatment interruption. For mechanical allodynia, the antinociceptive effect was maintained for 48 h after treatment interruption only with CHNCCaps. In conclusion, CHNC caps is a promising formulation for treating peripheral neuropathic pain. (AU)

• Processo FAPESP: 14/50928-2 - INCT 2014: Nanotecnologia Farmacêutica: uma abordagem transdisciplinar
• Beneficiário: Maria Vitória Lopes Badra Bentley
• Modalidade de apoio: Auxílio à Pesquisa - Temático