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Topic Review
Formulation Strategies to Improve Pharmacokinetics Profile
The oral route is the most common and practical means of drug administration, particularly from a patient’s perspective. However, the pharmacokinetic profile of oral drugs depends on the rate of drug absorption through the intestinal wall before entering the systemic circulation. However, the enteric epithelium represents one of the major limiting steps for drug absorption, due to the presence of efflux transporters on the intestinal membrane, mucous layer, enzymatic degradation, and the existence of tight junctions along the intestinal linings. These challenges are more noticeable for hydrophilic drugs, high molecular weight drugs, and drugs that are substrates of the efflux transporters. Another challenge faced by oral drug delivery is the presence of first-pass hepatic metabolism that can result in reduced drug bioavailability. Over the years, a wide range of compounds have been investigated for their permeation-enhancing effect in order to circumvent these challenges. There is also a growing interest in developing nanocarrier-based formulation strategies to enhance the drug absorption.
  • 538
  • 26 Aug 2022
Topic Review
Food–Drug Interactions with Fruit Juices
Fruit juices contain a large number of phytochemicals that, in combination with certain drugs, can cause food–drug interactions that can be clinically significant and lead to adverse events. The mechanisms behind such interactions are in most cases related to phytochemical interference with the activity of cytochrome P450 metabolizing enzymes (CYPs) or drug transporters. Moreover, alterations in their activity can have a clinical relevance if systemic exposure to the drug is decreased or increased, meaning that the pharmacological drug effects are suboptimal, or the drug will cause toxicity. In general, the common pharmacokinetic parameters found to be altered in food–drug interactions regarding fruit juices are the area under the concentration–time curve, bioavailability, and maximum plasma concentration. In most cases, the results from the drug interaction studies with fruit juices provide only limited information due to the small number of subjects, which are also healthy volunteers. Moreover, drug interactions with fruit juices are challenging to predict due to the unknown amounts of the specific phytochemicals responsible for the interaction, as well as due to the inter-individual variability of drug metabolism, among others. Therefore, this work aims to raise awareness about possible pharmacological interactions with fruit juices. 
  • 1.3K
  • 29 May 2021
Topic Review
Food Polyphenols and Type II Diabetes Mellitus
Type II diabetes mellitus and its related complications are growing public health problems. Many natural products present in our diet, including polyphenols, can be used in treating and managing type II diabetes mellitus and different diseases, owing to their numerous biological properties. Anthocyanins, flavonols, stilbenes, curcuminoids, hesperidin, hesperetin, naringenin, and phenolic acids are common polyphenols found in blueberries, chokeberries, sea-buckthorn, mulberries, turmeric, citrus fruits, and cereals. These compounds exhibit antidiabetic effects through different pathways.
  • 609
  • 22 May 2023
Topic Review
Fluoroquinolones Used in Therapy
Antibacterial fluoroquinolones (FQs) are frequently used in treating infections. However, the value of FQs is debatable due to their association with severe adverse effects (AEs). The Food and Drug Administration (FDA) issued safety warnings concerning their side-effects in 2008, followed by the European Medicine Agency (EMA) and regulatory authorities from other countries.
  • 454
  • 17 Mar 2023
Topic Review
Fluoride Toxicity
The practice of community water fluoridation used prophylactically against dental caries increased concern of adverse fluoride effects. Millions of people living in endemic fluorosis areas suffer from various pathological disturbances. Authors assessed the publications on fluoride toxicity until June 2020. Authors present evidence that fluoride is an enzymatic poison, inducing oxidative stress, hormonal disruptions, and neurotoxicity. Fluoride in synergy with aluminum acts as a false signal in G protein cascades of hormonal and neuronal regulations in much lower concentrations than fluoride acting alone. Our review shows the impact of fluoride on human health. We suggest focusing the research on fluoride toxicity to the underlying integrative networks. Ignorance of the pluripotent toxic effects of fluoride might contribute to unexpected epidemics in the future.
  • 939
  • 27 Oct 2020
Topic Review
Fluorescence Microscopy Techniques and DDS
In the latest years, fluorescence microscopy-related techniques have exhibited continuous developments and progresses, both from technical and applicative perspectives, holding the promise to provide unprecedented tools for drug delivery research.We have revised the major fluorescence microscopy-related experimental techniques available for the characterization of drug delivery systems （DDS）from static and dynamic points of view in different media, with a particular focus on the investigation within biological environments and in vivo. Indeed, the opportunities provided by fluorescence microscopy-related techniques to disentangle scientific issues typical of drug delivery research (spanning from the colloidal characterization of a DDS to its adhesion to biological membranes, its interaction with biomolecules, and its intracellular behavior) are countless and exponentially growing, allowing for the expectation that in the next few years the development of completely new tools and protocols will truly advance drug delivery research.
  • 299
  • 22 Jun 2021
Topic Review
Flecainide in Ventricular Arrhythmias
Flecainide is an IC antiarrhythmic drug (AAD) that received in 1984 Food and Drug Administration approval for the treatment of sustained ventricular tachycardia (VT) and subsequently for rhythm control of atrial fibrillation (AF). Currently, flecainide is mainly employed for sinus rhythm maintenance in AF and the treatment of idiopathic ventricular arrhythmias (IVA) in absence of ischaemic and structural heart disease on the basis of CAST data. Recent studies enrolling patients with different structural heart diseases demonstrated good effectiveness and safety profile of flecainide.
  • 860
  • 10 Sep 2021
Topic Review
Flecainide
Flecainide is an IC antiarrhythmic drug approved in 1984 from Food and Drug Administration for the suppression of sustained ventricular tachycardia and later for acute cardioversion of atrial fibrillation (AF) and for sinus rhythm maintenance. It is categorized as a Vaughn-Williams Class IC agent based upon its properties of causes a strong degree of sodium channel blockage with slowing cardiac conduction and a minimal effect on ventricular repolarization. Currently, flecainide is mostly used for sinus rhythm maintenance in atrial fibrillation patients without structural cardiomyopathy although recent studies enrolling different patient population demonstrated a good effectiveness and safety profile. 
  • 970
  • 13 Nov 2021
Topic Review
Flavonoids as CYP3A4 Inhibitors In Vitro
CYP enzymes are a group of heme-containing enzymes that play important roles in the metabolism of many drugs and other xenobiotics. They are located in the endoplasmic reticulum of cells throughout the body, but they are most abundant in the liver.
  • 119
  • 22 Mar 2024
Topic Review
Flavocoxid, a Nutraceutical Approach to Blunt Inflammatory Conditions
Flavonoids, from Scutellaria baicalensis (Chinese skullcap) and Acacia catechu (black catechu), have been shown to exert a variety of therapeutic effects, including anti-inflammatory, antiviral, antibacterial, and anticancer activities. Flavocoxid is a mixed extract containing baicalin and catechin and it acts as a dual balanced inhibitor of cyclooxygenase-1 (COX-1) and COX-2 peroxidase enzyme activities with a significant inhibition of 5-lipoxygenase (5-LOX) enzyme activity in vitro. Flavocoxid downregulates gene or protein expression of several inflammatory markers and exerts also strong antioxidant activity in several experimental models. Controlled clinical trials and a postmarketing study have clearly shown that flavocoxid is as effective as naproxen in managing the signs and symptoms of osteoarthritis of the knee and it has better upper gastrointestinal, renal, and respiratory safety profile than naproxen. Flavocoxid may therefore provide a potential therapeutic approach to the treatment of chronic inflammatory conditions.
  • 710
  • 01 Nov 2020
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