Antinociceptive activity of transdermal nanostructured surfactant-based systems containing duloxetine hydrochloride

Duloxetine hydrochloride (DLX) is a serotonin and norepinephrine reuptake inhibitor that is effective in the treatment of chronic pain. However, the drug has several adverse reactions and extensive hepatic first-pass effect. This study aimed at developing surfactant-based formulations such as liquid...

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Bibliographic Details
Published in:	Journal of drug delivery science and technology Vol. 101; p. 106166
Main Authors:	Seixas, Karoline Belém, Araujo, Guilherme Rodolfo Souza de, de Oliveira, Alisson Macário, Silveira Filho, Alex José, Leite, Arthur Renato Oliveira Fieto, Napoleão, Thiago Henrique, Sarmento, Victor Hugo Vitorino, Gonsalves, Joyce Kelly Marinheiro da Cunha, Bedor, Danilo César Galindo, Silva, Maria Carolina Silveira Costa, Lira, Ana Amélia Moreira, Leal, Leila Bastos, de Santana, Davi Pereira
Format:	Journal Article
Language:	English
Published:	Elsevier B.V 01-11-2024
Subjects:	Antinoceptive Duloxetine Liquid crystals Microemulsion Transdermal Antinoceptive Duloxetine Transdermal Microemulsion Liquid crystals
Online Access:	Get full text
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Summary:	Duloxetine hydrochloride (DLX) is a serotonin and norepinephrine reuptake inhibitor that is effective in the treatment of chronic pain. However, the drug has several adverse reactions and extensive hepatic first-pass effect. This study aimed at developing surfactant-based formulations such as liquid crystals (LCs) and evaluating the influence of the formulations on DLX skin permeation and in vivo antinociceptive activity. Thereafter, the formulations were obtained using PEG-40 Hydrogenated Castor Oil, Tween 80, licuri oil and water. The systems selected showed isotropy, high viscosity and rheology suggestive of LCs. The systems presented ability to permeate DLX through the skin. ATR-FTIR demonstrated that formulations promoted lipid disorganization and modification of protein conformation, facilitating the drug diffusion through the stratum corneum. Moreover, the formulation loaded with DLX showed high antinociceptive activity in mice (tests of acetic acid-induced abdominal writhing, formalin and tail immersion) via the transdermal route. The antinociceptive activity was close to that of morphine (i.p.). In conclusion, the LC obtained proved to be a promising system for transdermal delivery of DLX and pain management. [Display omitted]
ISSN:	1773-2247
DOI:	10.1016/j.jddst.2024.106166