Since ancient times, folk medicine and agro-food science have benefitted from the use of plant derivatives, such as essential oils, to combat different diseases, as well as to preserve food. In Nature, essential oils play a fundamental role in protecting the plant from biotic and abiotic attacks to which it may be subjected. Many researchers have analyzed in detail the modes of action of essential oils and most of their components. The purpose of this brief review is to describe the properties of essential oils, principally as antifungal agents, and their role in blocking cell communication mechanisms, fungal biofilm formation, and mycotoxin production.

Essential Oils and Antifungal Activity

Amorphous solid dispersions: Rational selection of a manufacturing process.

Granulation, the process of particle enlargement by agglomeration technique, is one of the most significant unit operations in the production of pharmaceutical dosage forms, mostly tablets and capsules. Granulation process transforms fine powders into free-flowing, dust-free granules that are easy to compress. Nevertheless, granulation poses numerous challenges due to high quality requirement of the formed granules in terms of content uniformity and physicochemical properties such as granule size, bulk density, porosity, hardness, moisture, compressibility, etc. together with physical and chemical stability of the drug. Granulation process can be divided into two types: wet granulation that utilize a liquid in the process and dry granulation that requires no liquid. The type of process selection requires thorough knowledge of physicochemical properties of the drug, excipients, required flow and release properties, to name a few. Among currently available technologies, spray drying, roller compaction, high shear mixing, and fluid bed granulation are worth of note. Like any other scientific field, pharmaceutical granulation technology also continues to change, and arrival of novel and innovative technologies are inevitable. This review focuses on the recent progress in the granulation techniques and technologies such as pneumatic dry granulation, reverse wet granulation, steam granulation, moisture-activated dry granulation, thermal adhesion granulation, freeze granulation, and foamed binder or foam granulation. This review gives an overview of these with a short description about each development along with its significance and limitations.

Granulation techniques and technologies: recent progresses

Fabricating 3D printed orally disintegrating printlets using selective laser sintering

To describe the nutritional and health attributes of kiwifruit and the benefits relating to improved nutritional status, digestive, immune and metabolic health. The review includes a brief history of green and gold varieties of kiwifruit from an ornamental curiosity from China in the 19th century to a crop of international economic importance in the 21st century; comparative data on their nutritional composition, particularly the high and distinctive amount of vitamin C; and an update on the latest available scientific evidence from well-designed and executed human studies on the multiple beneficial physiological effects. Of particular interest are the digestive benefits for healthy individuals as well as for those with constipation and other gastrointestinal disorders, including symptoms of irritable bowel syndrome. The mechanisms of action behind the gastrointestinal effects, such as changes in faecal (stool) consistency, decrease in transit time and reduction of abdominal discomfort, relate to the water retention capacity of kiwifruit fibre, favourable changes in the human colonic microbial community and primary metabolites, as well as the naturally present proteolytic enzyme actinidin, which aids protein digestion both in the stomach and the small intestine. The effects of kiwifruit on metabolic markers of cardiovascular disease and diabetes are also investigated, including studies on glucose and insulin balance, bodyweight maintenance and energy homeostasis. The increased research data and growing consumer awareness of the health benefits of kiwifruit provide logical motivation for their regular consumption as part of a balanced diet. Kiwifruit should be considered as part of a natural and effective dietary strategy to tackle some of the major health and wellness concerns around the world.

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The nutritional and health attributes of kiwifruit: a review

A new strain, namely Lysinibacillus sp. BV152.1 was isolated from the rhizosphere of ground ivy (Glechoma hederacea L.) producing metabolites with potent ability to inhibit biofilm formation of an important human pathogens Pseudomonas aeruginosa PAO1, Staphylococcus aureus, and Serratia marcescens. Structural characterization revealed di-rhamnolipids mixture containing rhamnose (Rha)-Rha-C10-C10, Rha-Rha-C8-C10, and Rha-Rha-C10-C12 in the ratio 7:2:1 as the active principle. Purified di-rhamnolipids, as well as commercially available di-rhamnolipids (Rha-Rha-C10-C10, 93%) were used as the substrate for the chemical derivatization for the first time, yielding three semi-synthetic amide derivatives, benzyl-, piperidine-, and morpholine. A comparative study of the anti-biofilm, antibacterial and cytotoxic properties revealed that di-Rha from Lysinibacillus sp. BV152.1 were more potent in biofilm inhibition, both cell adhesion and biofilm maturation, than commercial di-rhamnolipids inhibiting 50% of P. aeruginosa PAO1 biofilm formation at 50 μg mL-1 and 75 μg mL-1, respectively. None of the di-rhamnolipids exhibited antimicrobial properties at concentrations of up to 500 μg mL-1. Amide derivatization improved inhibition of biofilm formation and dispersion activities of di-rhamnolipids from both sources, with morpholine derivative being the most active causing more than 80% biofilm inhibition at concentrations 100 μg mL-1. Semi-synthetic amide derivatives showed increased antibacterial activity against S. aureus, and also showed higher cytotoxicity. Therefore, described di-rhamnolipids are potent anti-biofilm agents and the described approach can be seen as viable approach in reaching new rhamnolipid based derivatives with tailored biological properties.

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Anti-biofilm Properties of Bacterial Di-Rhamnolipids and Their Semi-Synthetic Amide Derivatives.

Infective diseases have become health threat of a global proportion due to appearance and spread of microorganisms resistant to majority of therapeutics currently used for their treatment. Therefore, there is a constant need for development of new antimicrobial agents, as well as novel therapeutic strategies. Quinolines and quinolones, isolated from plants, animals, and microorganisms, have demonstrated numerous biological activities such as antimicrobial, insecticidal, anti-inflammatory, antiplatelet, and antitumor. For more than two centuries quinoline/quinolone moiety has been used as a scaffold for drug development and even today it represents an inexhaustible inspiration for design and development of novel semi-synthetic or synthetic agents exhibiting broad spectrum of bioactivities. The structural diversity of synthetized compounds provides high and selective activity attained through different mechanisms of action, as well as low toxicity on human cells. This review describes quinoline and quinolone derivatives with antibacterial, antifungal, anti-virulent, antiviral, and anti-parasitic activities with the focus on the last 10 years literature.

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Quinolines and quinolones as antibacterial, antifungal, anti-virulence, antiviral and anti-parasitic agents

Antibiotic resistance has become a serious global threat to public health; therefore, improved strategies and structurally novel antimicrobials are urgently needed to combat infectious diseases. Here we report a new type of highly potent 4-aminoquinoline derivatives as quorum sensing inhibitors in Serratia marcescens and Pseudomonas aeruginosa, exhibiting weak bactericidal activities (minimum inhibitory concentration (MIC) > 400 μM). Through detailed structure–activity study, we have identified 7-Cl and 7-CF3 substituted N-dodecylamino-4-aminoquinolines (5 and 10) as biofilm formation inhibitors with 50% biofilm inhibition at 69 μM and 63 μM in S. marcescens and P. aeruginosa, respectively. These two compounds, 5 and 10, are the first quinoline derivatives with anti-biofilm formation activity reported in S. marcescens. Quantitative structure–activity relationship (QSAR) analysis identified structural descriptors such as Wiener indices, hyper-distance-path index (HDPI), mean topological charge (MTC), topol...

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Long-Chain 4-Aminoquinolines as Quorum Sensing Inhibitors in Serratia marcescens and Pseudomonas aeruginosa.

Context: Considering that bitter taste of drugs incorporated in orally disintegrating tablets (ODTs) can be the main reason for avoiding drug therapy, it is of the utmost importance to achieve successful taste-masking. The evaluation of taste-masking effectiveness is still a major challenge.Objective: The objective of this study was to mask bitter taste of the selected model drugs by drug particle coating with Eudragit® E PO, as well as to evaluate taste-masking effectiveness of prepared ODTs using compendial dissolution testing, dissolution in the small-volume shake-flask assembly and trained human taste panel.Materials and methods: Model drugs were coated in fluidized bed. Disintequik™ ODT was used as a novel co-processed excipient for ODT preparation. Selected formulations were investigated in vitro and in vivo using techniques for taste-masking assessment.Results and discussion: Significantly slower drug dissolution was observed from tablets with coated drug particles during the first 3 min of...

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In vitro and in vivo investigation of taste-masking effectiveness of Eudragit E PO as drug particle coating agent in orally disintegrating tablets.

Mixed microbial infections caused by Pseudomonas aeruginosa and pathogenic fungi are commonly found in patients with chronic infections and constitute a significant health care burden. The aim of this study was to address the potential polymicrobial antibiofilm activity of pompia and grapefruit essential oils (EOs). The mechanism of antimicrobial activity of EOs was analysed. EOs of pompia and grapefruit inhibited fungal growth with MIC concentrations between 50 and 250 mg L−1, whereas no effect on P. aeruginosa growth was observed. Both citrus EOs inhibited formation of bacterial and fungal monomicrobial biofilms in concentrations of 50 mg L−1 and were efficient in potentiating the activity of clinically used antimicrobials in vitro . The concentration of 10 mg L−1 EOs inhibited mixed biofilm formation composed of P. aeruginosa and Aspergillus fumigatus or Scedosporium apiospermum . Citrus EOs affected quorum sensing in P. aeruginosa and caused fast permeabilisation of Candida albicans membrane. Pompia and grapefruit EOs potently inhibited biofilm formation and could be used for the control of common polymicrobial infections.

Ivana Aleksic

Papers

Anti-biofilm Properties of Bacterial Di-Rhamnolipids and Their Semi-Synthetic Amide Derivatives.

Quinolines and quinolones as antibacterial, antifungal, anti-virulence, antiviral and anti-parasitic agents

Long-Chain 4-Aminoquinolines as Quorum Sensing Inhibitors in Serratia marcescens and Pseudomonas aeruginosa.

In vitro and in vivo investigation of taste-masking effectiveness of Eudragit E PO as drug particle coating agent in orally disintegrating tablets.

Prevention of polymicrobial biofilms composed of Pseudomonas aeruginosa and pathogenic fungi by essential oils from selected Citrus species.