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Synthesis, In Vitro Biological Evaluation of Antiproliferative and Neuroprotect...

Brito, Vanessa; Marques, Mariana; Esteves, Marta; Serra-Almeida, Catarina; Alves, Gilberto; Almeida, Paulo; Bernardino, Liliana; Silvestre, Samuel

Steroids constitute an important class of pharmacologically active molecules, playing key roles in human physiology. Within this group, 16E-arylideneandrostane derivatives have been reported as potent anti-cancer agents for the treatment of leukemia, breast and prostate cancers, and brain tumors. Additionally, 5α,6α-epoxycholesterol is an oxysterol with several biological activities, including regulation of cel...


Fighting Epilepsy with Nanomedicines-Is This the Right Weapon?

Matias, Mariana; Santos, Adriana O.; Silvestre, Samuel; Alves, Gilberto

Epilepsy 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...


Intranasal Microemulsion as an Innovative and Promising Alternative to the Oral...

Meirinho, Sara; Rodrigues, Márcio; Santos, Adriana O; Falcão, Amílcar; Alves, Gilberto

Stiripentol (STP) is a new-generation antiepileptic only available for oral administration. However, it is extremely unstable in acidic environments and undergoes gastrointestinal slow and incomplete dissolution. Thus, STP intranasal (IN) administration might overcome the high oral doses required to achieve therapeutic concentrations. An IN microemulsion and two variations were herein developed: the first conta...


Nanoformulations for the Delivery of Dietary Anthocyanins for the Prevention an...

Nunes, Ana R.; Costa, Elisabete C.; Alves, Gilberto; Silva, Luís R.

Diabetes mellitus (DM) is a metabolic disease characterized by abnormal blood glucose levels-hyperglycemia, caused by a lack of insulin secretion, impaired insulin action, or a combination of both. The incidence of DM is increasing, resulting in billions of dollars in annual healthcare costs worldwide. Current therapeutics aim to control hyperglycemia and reduce blood glucose levels to normal. However, most mod...


Exploring the Antioxidant, Antidiabetic, and Antimicrobial Capacity of Phenolic...

Gonçalves, Ana C.; Nunes, Ana R.; Meirinho, Sara; Ayuso-Calles, Miguel; Roca-Couso, Rocío; Rivas, Raúl; Falcão, Amílcar; Alves, Gilberto; Silva, Luís R.

(1) Background: Nowadays, special attention has been paid to red and purple fruits, including blueberries and sweet cherries, since they are highly attractive to consumers due to their organoleptic properties, standing out due to their vibrant red and purple colours and sweet flavour, and nutritional value. (2) Methods: The present study evaluated the phenolic profile of phenolic-enriched extracts from blueberr...


Blackberries and Mulberries: Berries with Significant Health-Promoting Properties

Martins, Mariana S.; Gonçalves, Ana C.; Alves, Gilberto; Silva, Luís R.

Blackberries and mulberries are small and perishable fruits that provide significant health benefits when consumed. In reality, both are rich in phytochemicals, such as phenolics and volatile compounds, and micronutrients, such as vitamins. All the compounds are well-known thanks to their medicinal and pharmacological properties, namely antioxidant, anti-inflammatory, anti-cancer, antiviral, and cardiovascular ...


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, Samuel

Formulating 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...


Strategies to Improve Drug Strength in Nasal Preparations for Brain Delivery of...

Pires, Patrícia; Rodrigues, Márcio; Alves, Gilberto; Santos, Adriana

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...


Intranasal delivery of lipid-based nanosystems as a promising approach for brai...

Meirinho, Sara; Rodrigues, Márcio; Ferreira, Catarina; Caetano Oliveira, Rui; Fortuna, Ana; Santos, Adriana; Falcão, Amílcar; Alves, Gilberto

Perampanel (PER), a new-generation antiepileptic drug effective against different types of seizures, has already demonstrated a potential in status epilepticus therapy. Considering the growing interest of intranasal (IN) administration for nose-to-brain delivery, PER could be envisioned as a good candidate for this route, especially if formulated in a lipid-based nanosystem. With that purpose, a hydrophobic for...


Study of the metabolic stability profiles of perampanel, rufinamide and stiripe...

Meirinho, Sara; Rodrigues, Márcio; Fortuna, Ana; Falcão, Amílcar; Alves, Gilberto

New-generation antiepileptic drugs as perampanel, rufinamide and stiripentol emerged as alternatives in chronic epilepsy polytherapy. Hence, their metabolic stability and potential involvement in relevant drug-drug interactions (DDI) are of great clinical interest, being HepaRG cells herein used as an in vitro human model. To characterize their metabolic stability profiles, HepaRG cells were incubated with pera...


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