Vanessa R R Cunha1, Viviane A Guilherme2, Eneida de Paula2, Daniele R de Araujo3, Renan O Silva4, Jand V R Medeiros4, José R S A Leite4, Philippe A D Petersen5, Marianna Foldvari6, Helena M Petrilli5, Vera R L Constantino1. 1. Departamento de Química Fundamental, Instituto de Química, Universidade de São Paulo, USP, Av. Prof. Lineu Prestes 748, 05508-000 São Paulo, São Paulo, Brazil. 2. Departamento de Bioquímica, Instituto de Biologia, Universidade Estadual de Campinas, 13083-970, Campinas, São Paulo, Brazil. 3. Departamento de Bioquímica, Instituto de Biologia, Universidade Estadual de Campinas, 13083-970, Campinas, São Paulo, Brazil; Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, 09210-170 Santo André, São Paulo, Brazil. 4. Núcleo de Pesquisa em Biodiversidade e Biotecnologia, BIOTEC, Campus de Parnaíba, Universidade Federal do Piauí, UFPI, 64202020 Parnaíba, Piauí, Brazil. 5. Departamento de Física dos Materiais e Mecânica, Instituto de Física, Universidade de São Paulo, USP, 05315-970 São Paulo, São Paulo, Brazil. 6. School of Pharmacy, University of Waterloo, N2L 3G1 Waterloo, Ontario, Canada.
Abstract
PURPOSE: The anionic form of the drug mefenamic acid intercalated into the nanocarrier layered double hydroxide (LDH-Mef) was evaluated by anti-inflammatory and antinociceptive assays. METHODS: The LDH-Mef material was characterized by a set of physicochemical techniques, which was supported by Density Functional Theory calculations. The pharmacological effects of LDH-Mef (40 wt% of drug) were evaluated by hemolytic, anti-inflammatory activity and antinociceptive assays. RESULTS: In vivo assays were conducted for the first time in order to assess the LDH-Mef potential. The hemolytic effects decreased for the intercalated Mef as demonstrated by the higher tolerated hemolytic concentration (1.83 mM) compared to mefenamic acid (MefH), 0.48 mM. Pretreatment of animals with MefH or LDH-Mef reduced carrageenan-, dextran sulfate- and PGE2-induced paw edema. MefH or LDH-Mef also decrease total leucocytes and neutrophil counts of the peritoneal cavity after inflammation induction with carrageenan. In the nociception model, oral pretreatment with LDH-Mef reduced mechanical hypernociception carrageenan-induced after 3-4h and also the number of writhings induced by acetic acid. CONCLUSIONS: This work shows the increase of the anti-inflammatory and antinociceptive potential of the drug confined into the LDH, as well as, its hemolytic effect.
PURPOSE: The anionic form of the drug mefenamic acid intercalated into the nanocarrier layered double hydroxide (LDH-Mef) was evaluated by anti-inflammatory and antinociceptive assays. METHODS: The LDH-Mef material was characterized by a set of physicochemical techniques, which was supported by Density Functional Theory calculations. The pharmacological effects of LDH-Mef (40 wt% of drug) were evaluated by hemolytic, anti-inflammatory activity and antinociceptive assays. RESULTS: In vivo assays were conducted for the first time in order to assess the LDH-Mef potential. The hemolytic effects decreased for the intercalated Mef as demonstrated by the higher tolerated hemolytic concentration (1.83 mM) compared to mefenamic acid (MefH), 0.48 mM. Pretreatment of animals with MefH or LDH-Mef reduced carrageenan-, dextran sulfate- and PGE2-induced paw edema. MefH or LDH-Mef also decrease total leucocytes and neutrophil counts of the peritoneal cavity after inflammation induction with carrageenan. In the nociception model, oral pretreatment with LDH-Mef reduced mechanical hypernociceptioncarrageenan-induced after 3-4h and also the number of writhings induced by acetic acid. CONCLUSIONS: This work shows the increase of the anti-inflammatory and antinociceptive potential of the drug confined into the LDH, as well as, its hemolytic effect.
Authors: Viviane A Guilherme; Vanessa R R Cunha; Eneida de Paula; Daniele R de Araujo; Vera R L Constantino Journal: Pharmaceutics Date: 2022-04-25 Impact factor: 6.525
Authors: Samar M Mahgoub; Mohamed R Shehata; Fatma L Abo El-Ela; Ahmed Farghali; Amal Zaher; Rehab K Mahmoud Journal: RSC Adv Date: 2020-07-23 Impact factor: 4.036
Authors: Vanessa Roberta Rodrigues Cunha; Rodrigo Barbosa de Souza; Ana Maria Cristina Rebello Pinto da Fonseca Martins; Ivan Hong Jun Koh; Vera Regina Leopoldo Constantino Journal: Sci Rep Date: 2016-08-02 Impact factor: 4.379