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Development and Pharmacological Evaluation of Liposomes and Nanocapsules Containing Paroxetine Hydrochloride.

Raquel Chiarentin, Dienifer Pereira Bottcher, Bruna Zeni, Carolina Grave, Fernanda Neutzling Kaufmann,Thalia Emmanoella Sebulsqui Saraiva,Gabriel da Costa Berna, Giulia Aline Fuhr,Bruna Saraiva Hermann, Bruna Hoffmeister,Fernando Dal Pont Morisso,Mariele Feiffer Charao,Simone Gasparin Verza,Juliane Deise Fleck,Andresa Heemann Betti,Cristiane Bastos de Mattos

International journal of pharmaceutics(2024)

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摘要
Depression is one of the most common psychiatric disorders. Nanotechnology has emerged to optimize the pharmacological response. Therefore, the aim of this work was to develop and characterize liposomes and nanocapsules containing paroxetine hydrochloride and evaluate their antidepressant-like effect using the open field and tail suspension tests in mice. Liposomes and nanocapsules were prepared using the reverse-phase evaporation and nanoprecipitation methods, respectively. The particle size of the formulation ranged from 121.81 to 310.73 nm, the polydispersity index from 0.096 to 0.303, the zeta potential from -11.94 to -34.50 mV, the pH from 5.31 to 7.38, the drug content from 80.82 to 94.36 %, and the association efficiency was 98 %. Paroxetine hydrochloride showed slower release when associated with liposomes (43.82 %) compared to nanocapsules (95.59 %) after 10 h. In Vero cells, in vitro toxicity showed a concentration-dependent effect for paroxetine hydrochloride nanostructures. Both nanostructures decreased the immobility time in the TST at 2.5 mg/kg without affecting the number of crossings in the open field test, suggesting the antidepressant-like effect of paroxetine. In addition, the nanocapsules decreased the number of groomings, reinforcing the anxiolytic effect of this drug. These results suggest that the nanostructures were effective in preserving the antidepressant-like effect of paroxetine hydrochloride even at low doses.
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关键词
Major Depressive Disorder,Paroxetine Hydrochloride,Liposomes,Nanocapsules,Pharmacological Evaluation
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