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Topic Review
Biography
Topic Review
Innovations in Chewable Formulations and 3D Printing
Since their introduction, chewable dosage forms have gained traction due to their ability to facilitate swallowing, especially in paediatric, geriatric and dysphagia patients. Their benefits stretch beyond human use to also include veterinary applications, improving administration and palatability in different animal species. Despite their advantages, current chewable formulations do not account for individualised dosing and palatability preferences. In light of this, three-dimensional (3D) printing, and in particular the semi-solid extrusion technology, has been suggested as a novel manufacturing method for producing customised chewable dosage forms. This advanced approach offers flexibility for selecting patient-specific doses, excipients, and organoleptic properties, which are critical for ensuring efficacy, safety and adherence to the treatment.
599
07 Sep 2022
Topic Review
Hypoxic Tumor Environments in Photodynamic Therapy
Photodynamic therapy (PDT) has become a promising method of cancer treatment due to its unique properties, such as noninvasiveness and low toxicity. The efficacy of PDT is significantly reduced by the hypoxia tumor environments, because PDT involves the generation of reactive oxygen species (ROS), which requires the great consumption of oxygen. Moreover, the consumption of oxygen caused by PDT would further exacerbate the hypoxia condition, which leads to angiogenesis, invasion of tumors to other parts, and metastasis.
350
06 Sep 2022
Topic Review
NRF2-Activating Compounds Bearing α,β-Unsaturated Moiety
The surge of scientific interest in the discovery of Nuclear Factor Erythroid 2 (NFE2)-Related Factor 2 (NRF2)-activating molecules underscores the importance of NRF2 as a therapeutic target especially for oxidative stress. The chemical reactivity and biological activities of several bioactive compounds have been linked to the presence of α,β-unsaturated structural systems. The α,β-unsaturated carbonyl, sulfonyl and sulfinyl functional groups are reportedly the major α,β-unsaturated moieties involved in the activation of the NRF2 signaling pathway. The carbonyl, sulfonyl and sulfinyl groups are generally electron-withdrawing groups, and the presence of the α,β-unsaturated structure qualifies them as suitable electrophiles for Michael addition reaction with nucleophilic thiols of cysteine residues within the proximal negative regulator of NRF2, Kelch-like ECH-associated protein 1 (KEAP1). The physicochemical property such as good lipophilicity of these moieties is also an advantage because it ensures solubility and membrane permeability required for the activation of the cytosolic NRF2/KEAP1 system.
770
02 Sep 2022
Topic Review
Resveratrol from Dietary Supplement to a Drug Candidate
Resveratrol (RVT) is a well known phyto-chemical and is widely used in dietary supplements and botanical products. It shows a wide range of pharmacological/beneficial effects. it can be a potential candidate to be developed as phyto-pharmaceutical. Multiple diseases are reported to be treated by the therapeutic effect of RVT since it has antioxidant, anti-cancer activity and anti-inflammatory activities. It also has a major role in diabetes, arthritis, cardiac disorder and platelet aggregation etc. The major requirements are establishments regarding safety, efficacy profile and physicochemical characterization.
613
29 Aug 2022
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.
537
26 Aug 2022
Topic Review
Relevance of Crystal Forms in the Pharmaceutical Field
The existence of multiple crystal forms of an active pharmaceutical ingredients (API) is relevant not only for the selection of the best solid material to carry through the various stages of drug development, including the choice of dosage and of excipients suitable for drug development and marketing, but also in terms of intellectual property protection and/or extension. This is because the physico-chemical properties, such as solubility, dissolution rate, thermal stability, processability, etc., of the solid API may depend, sometimes dramatically, on the crystal form, with important implications on the drug’s ultimate efficacy.
972
26 Aug 2022
Topic Review
Drug Discovery Research around Tetanus Toxin Fragment C
Tetanus caused by the tetanus toxin (TT) is a fatal illness, which despite the existence of a vaccine, led to an estimated 34,684 deaths in 2019. TT is a neurotoxin produced by Clostridium tetani, a Gram-positive pathogenic bacterium, mainly found in soil and the gastrointestinal tracts of animals. TT induces the inhibition of neurotransmitter release, leading to spastic paralysis in a four-step process. First, TT binds to specific receptors, mainly composed of lipids and gangliosides, found at the neuromuscular junction (NMJ). Another receptor is reached by TT after these first bindings: a protein receptor responsible for its internalization (second step). This double receptor binding is responsible for the high affinity between TT and nerve cells. Third, TT is then transported into the cell body via axonal retrograde transport. In the last step, the proteolytic cleavage by TT of the VAMP/synaptobrevin, a neuronal substrate, leads to the inhibition of neurotransmitter release. All of these biological properties can be distinct associated parts of the TT structure. TT is a 150.7 kDa protein composed of a 52.4 kDa light chain and a 98.3 kDa heavy chain linked by a disulfide bond.
682
26 Aug 2022
Topic Review
Microfluidic Approaches for Affinity-Based Exosome Separation
As a subspecies of extracellular vesicles (EVs), exosomes have provided promising results in diagnostic and theranostic applications in recent years. The nanometer-sized exosomes can be extracted by liquid biopsy from almost all body fluids, making them especially suitable for mainly non-invasive point-of-care (POC) applications. To achieve this, exosomes must first be separated from the respective biofluid. Impurities with similar properties, heterogeneity of exosome characteristics, and time-related biofouling complicate the separation. Due to the compactness of state-of-the-art methods available for the separation of exosomes, quick analysis time and portable form factor, these microfluidic devices are particularly suitable to deliver fast and reliable results for POC applications. For these devices, new manufacturing methods (e.g., laminating, replica molding and 3D printing) that use low-cost materials and do not require clean rooms are presented. Additionally, special flow routes and patterns that increase contact surfaces, as well as residence time, and thus improve affinity purification are displayed.
271
25 Aug 2022
Topic Review
Advanced Mass Spectrometry in Service of Forensic Analysis
Mass spectrometry has been used to assist forensic investigation. Due to its unique capabilities, mainly high-resolution mass data and structural information, high sensitivity, and cooperation with separation techniques, this method provides access to many tools streamlining and accelerating sample analysis. Low analyte consumption, advanced derivatization procedures and availability of isotopically labeled standards offer opportunities to study materials previously not considered viable evidence, opening new avenues in forensic investigations.
458
25 Aug 2022
Topic Review
The Genus
Cetraria
s. str.
The genus Cetraria s. str. (Parmeliaceae family, Cetrarioid clade) consists of 15 species of mostly erect brown or greenish yellow fruticose or subfoliose thallus. These Cetraria species have a cosmopolitan distribution, being primarily located in the Northern Hemisphere, in North America and in the Eurasia area.
447
24 Aug 2022
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