16 documents found, page 1 of 2
Fighting Epilepsy with Nanomedicines-Is This the Right Weapon?
Matias, Mariana; Santos, Adriana O.; Silvestre, Samuel; Alves, GilbertoEpilepsy is a chronic and complex condition and is one of the most common neurological diseases, affecting about 50 million people worldwide. Pharmacological therapy has been, and is likely to remain, the main treatment approach for this disease. Although a large number of new antiseizure drugs (ASDs) has been introduced into the market in the last few years, many patients suffer from uncontrolled seizures, dem...
New Scaffolds of Proteasome Inhibitors: Boosting Anticancer Potential by Exploi...
Guedes, Romina A.; Grilo, Jorge H.; Carvalho, Andreia N.; Fernandes, Pedro M. P.; Ressurreição, Ana S.; Brito, Vanessa; Santos, Adriana O.Cancer is a complex multifactorial disease whose pathophysiology involves multiple metabolic pathways, including the ubiquitin-proteasome system, for which several proteasome inhibitors have already been approved for clinical use. However, the resistance to existing therapies and the occurrence of severe adverse effects is still a concern. The purpose of this study was the discovery of novel scaffolds of protea...
Innovative Aqueous Nanoemulsion Prepared by Phase Inversion Emulsification with...
Pires, Patrícia C.; Fernandes, Mariana; Nina, Francisca; Gama, Francisco; Gomes, Maria F; Rodrigues, Lina E; Meirinho, Sara; Silvestre, SamuelFormulating low-solubility or low-permeability drugs is a challenge, particularly with the low administration volumes required in intranasal drug delivery. Nanoemulsions (NE) can solve both issues, but their production and physical stability can be challenging, particularly when a high proportion of lipids is necessary. Hence, the aim of the present work was to develop a NE with good solubilization capacity for...
C-Ring Oxidized Estrone Acetate Derivatives: Assessment of Antiproliferative Ac...
Canário, Catarina; Matias, Mariana; Brito, Vanessa; Pires, Patrícia; Santos, Adriana O.; Falcão, Amílcar; Silvestre, Samuel; Alves, GilbertoC-Ring oxidized estrone acetate derivatives as antiproliferative agents were prepared and tested against five cancer cell lines by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Flow cytometry assays to evaluate cell viability and modifications in cell cycle phases and molecular docking research against estrogen receptor α, steroid sulfatase, and 17β-hydroxysteroid dehydrogenase type 1 ...
Strategies to Improve Drug Strength in Nasal Preparations for Brain Delivery of...
Pires, Patrícia C.; Rodrigues, Márcio; Alves, Gilberto Lourenço; Santos, Adriana O.Intranasal administration is a promising route for brain drug delivery. However, it can be difficult to formulate drugs that have low water solubility into high strength intranasal solutions. Hence, the purpose of this work was to review the strategies that have been used to increase drug strength in intranasal liquid formulations. Three main groups of strategies are: the use of solubilizers (change in pH, comp...
Antimicrobial and antitumor activity of S-methyl dithiocarbazate Schiff base zi...
Gomes, Filipa Ramilo; Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel; Campos, Débora L.; Pavan, Fernando R.; Gomes, Clara S.B.; Brito, VanessaSchiff bases (SB) obtained from S-methyl dithiocarbazate and aromatic aldehydes: salicylaldehyde (H2L1), o-vanillin (H2L2), pyridoxal (H2L3) and 2,6-diformyl-4-methylphenol (H3L4), and their corresponding Zn(II)-complexes (1-4), are synthesized. All compounds are characterized by elemental analyses, infrared, UV-Vis, nuclear magnetic resonance spectroscopy and mass spectrometry. The structures of H2L2 and [Zn2(...
New Estrone Oxime Derivatives: Synthesis, Cytotoxic Evaluation and Docking Studies
Canário, Catarina; Matias, Mariana; Brito, Vanessa; Santos, Adriana O.; Falcão, Amílcar; Silvestre, Samuel; Alves, GilbertoThe interest in the introduction of the oxime group in molecules aiming to improve their biological effects is increasing. This work aimed to develop new steroidal oximes of the estrane series with potential antitumor interest. For this, several oximes were synthesized by reaction of hydroxylamine with the 17-ketone of estrone derivatives. Then, their cytotoxicity was evaluated in six cell lines. An estrogenici...
Antimicrobial and antitumor activity of S-methyl dithiocarbazate Schiff base zi...
Ramilo-Gomes, Filipa; Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel; Campos, Débora L. [UNESP]; Pavan, Fernando R. [UNESP]; Gomes, Clara S.B.Made available in DSpace on 2021-06-25T11:09:35Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-03-01; Schiff bases (SB) obtained from S-methyl dithiocarbazate and aromatic aldehydes: salicylaldehyde (H2L1), o-vanillin (H2L2), pyridoxal (H2L3) and 2,6-diformyl-4-methylphenol (H3L4), and their corresponding Zn(II)-complexes (1–4), are synthesized. All compounds are characterized by elemental analyses, inf...
Antimicrobial and antitumor activity of S-methyl dithiocarbazate Schiff base zi...
Ramilo-Gomes, Filipa; Alemu, Yemataw; Tekamo, Israel; Cavaco, Isabel; Campos, Débora L.; Pavan, Fernando R.; Gomes, Clara S.B.; Brito, VanessaSchiff bases (SB) obtained from S-methyl dithiocarbazate and aromatic aldehydes: salicylaldehyde (H2L1), o-vanillin (H2L2), pyridoxal (H2L3) and 2,6-diformyl-4-methylphenol (H3L4), and their corresponding Zn(II)-complexes (1-4), are synthesized. All compounds are characterized by elemental analyses, infrared, UV-Vis, nuclear magnetic resonance spectroscopy and mass spectrometry. The structures of H2L2 and [Zn2(...
Nanoemulsions and thermosensitive nanoemulgels of phenytoin and fosphenytoin fo...
Pires, Patrícia C.; Peixoto, Diana; Teixeira, Isaura; Rodrigues, Márcio; Alves, Gilberto; Santos, Adriana O.Phenytoin is a low solubility anticonvulsant drug. It has, nonetheless, other possible therapeutic indications, such as neuropathic pain, including trigeminal neuralgia, or wound healing. Its use has decreased due to side effects, but nasal/intranasal administration could significantly increase drug safety and efficacy. The aim of this work was to develop and study nanoemulsions and thermosensitive nanoemulgels...