Gastroprotective effect of α-terpineol-loaded polymethyl methacrylate particles on gastric injury model

• Published in: Journal of drug delivery science and technology 2022-01, Vol.67, p.102989, Article 102989
• Main Authors: de Barros Fernandes, Helio, Ciriaco, Shayara Lopes, Filgueiras, Lívia Alves, Costa Barros, Izabel, Menezes Carvalho, André Luis, Lins Rolim, Hercília Maria, Nele de Souza, Marcio, Costa da Silva Pinto, José Carlos, Mendes, Anderson Nogueira, de Cássia Meneses Oliveira, Rita
• Format: Article
• Language: English
• Subjects: Ethanol; Gastroprotective effect; PMMA particles; α-Terpineol
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2021.102989

Terpenes present in essential oils have been promising for studies of gastroprotective activity. A monoterpene constituent of Melaleuca quinquenervia (Cav.) S.F. Blake and Cedrus deodara Roxb. ex D.Don, α-terpineol, has gastric protective activity against models of acute injury in rodents. However, it is a lipophilic compound and has a short half-life in blood flow. Therefore, the objective of the present work was to propose polymeric polymethyl methacrylate particles to be loaded with α-terpineol, in order to improve the stability and half-life of the asset. Polymethyl methacrylate particles containing α-terpineol were synthesized, characterized and evaluated for the gastroprotective effect in models of acute injury in rodents. The formulation used for the gastroprotective activity test showed a diameter of 796.8 ± 88.34 nm, a polydispersity index of 0.532, a zeta potential of −52.5 ± 13.1 mV and an encapsulation rate of 74.07 ± 3.03. The incorporation of monoterpene in polymethyl methacrylate particles increased the gatroprotective efficacy of α-terpineol. The incorporation of α-terpineol in polymethyl methacrylate particles maintains the gastroprotective properties of α-terpineol, with a lower dose administered compared to carbenoxolone, a drug used in the treatment of lesions of the oral mucosa. [Display omitted] •α-Terpineol has a gastroprotective action.•The incorporation of α-terpineol in polymethyl methacrylate particles increases the gastroprotective activity.•α-Terpineol loaded polymethyl methacrylate particles have effects similar to Carbenoxolone.