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The coating process for solid dosage forms is widely used in the pharmaceutical industry but presents challenges for small-scale production, needed in personalized medicine and clinical or galenic settings. This study aimed to evaluate immersion coating, a cost-effective small-scale method, for enteric-coated gelatin capsules using standard equipment. Two enteric coating polymers and different polymer concentrations were tested, along with API solubility. Results were compared with commercially available enteric capsule shells. Successful preparation of enteric coating capsules via immersion necessitates a comprehensive grasp of API and enteric polymer behavior. However, utilizing commercially available enteric capsule shells does not guarantee ease or robustness, as their efficacy hinges on the attributes of the active ingredient and excipients. Notably, coating with Eudragit S100 stands out for its superior process robustness, requiring minimal or no development time, thus representing the best option for small-scale enteric capsule production. [ABSTRACT FROM AUTHOR]

Ropinirole is a non-ergolinic dopamine agonist used to manage Parkinson's disease and it is characterized by poor oral bioavailability. This study aimed to design and develop advanced drug delivery systems composed of poloxamer 407, a non-ionic surfactant (Tween 80), and cyclodextrins (methyl-β-CD or hydroxy-propyl-β-CD) for possible brain targeting of ropinirole after nasal administration for the treatment of Parkinson's disease. The hybrid systems were formed by the thin-film hydration method, followed by an extensive physicochemical and morphological characterization. The in vitro cytotoxicity of the systems on HEK293 cell lines was also tested. In vitro release and ex vivo mucosal permeation of ropinirole were assessed using Franz cells at 34 °C and with phosphate buffer solution at pH 5.6 in the donor compartment, simulating the conditions of the nasal cavity. The results indicated that the diffusion-controlled drug release exhibited a progressive increase throughout the experiment, while a proof-of-concept experiment on ex vivo permeation through rabbit nasal mucosa revealed a better performance of the prepared hybrid systems in comparison to ropinirole solution. The encouraging results in drug release and mucosal permeation indicate that these hybrid systems can serve as attractive platforms for effective and targeted nose-to-brain delivery of ropinirole with a possible application in Parkinson's disease. Further ex vivo and in vivo studies to support the results of the present work are ongoing. [ABSTRACT FROM AUTHOR]

Industrial hemp (Cannabis sativa L.), due to its bioactive compounds (terpenes and cannabinoids), has gained increasing interest in different fields, including for medical purposes. The evaluation of the safety profile of hemp essential oil (EO) and its encapsulated form (nanoemulsion, NE) is a relevant aspect for potential therapeutic applications. This study aimed to evaluate the toxicological effect of hemp EOs and NEs from cultivars Carmagnola CS and Uso 31 on three cell lines selected as models for topical and inhalant administration, by evaluating the cytotoxicity and the cytokine expression profiles. Results show that EOs and their NEs have comparable cytotoxicity, if considering the quantity of EO present in the NE. Moreover, cells treated with EOs and NEs showed, in most of the cases, lower levels of proinflammatory cytokines compared to Etoposide used as a positive control, and the basal level of inflammatory cytokines was not altered, suggesting a safety profile of hemp EOs and their NEs to support their use for medical applications. [ABSTRACT FROM AUTHOR]

A dietary supplement potentially employed for the treatment and/or prevention of hyperlipidemia was developed. The proposed product is composed of a combination of natural macromolecules as chitosan (CH), α-cyclodextrin (α-CD), and lupin proteins (LP). First, the anti-hyperlipidemic effect of the α-CD and LP binary mixture was assessed and compared to that of the extensively utilized anti-hyperlipidemic CH, using a hyperlipidemic rat model. The anti-hyperlipidemic effect of their combination was also demonstrated. Additionally, ligand–target and protein–protein docking studies were performed. The in vivo results displayed that on intergroup comparison, blending CH, α-CD, and LP promised a superior therapeutic effect over α-CD and LP mixture, CH, and the marketed atorvastatin, potentiating a considerable reduction of serum lipid profile and the calculated atherogenic risk predictor indices. Molecular docking study revealed a weak hydrophobic cholesterol–CH and cholesterol–α-CD interactions, while protein–protein docking study showed a good lipase–LP interaction, involving eight hydrogen bonds. Then, on the base of the in vivo and docking study results, a tablet formulation was produced aimed to overcome the negative technological effects of the anti-hyperlipidemic macromolecules: long disintegration time and tablets mechanical resistance. The optimized tablet formulation has a disintegration time shorter than 15 min and a weight loss from friability test lower than 1%, which are in line with the regulatory specifications for uncoated tablets. Overall, this anti-hyperlipidemic formulation is attractive for the dietary and nutraceutical market, despite further clinical studies are required to assess the efficacy, possible side effects, and product compliance. [ABSTRACT FROM AUTHOR]

The aim of this research was to prepare novel block copolymer-surfactant hybrid nanosystems using the triblock copolymer Pluronic 188, along with surfactants of different hydrophilic to lipophilic balance (HLB ratio—which indicates the degree to which a surfactant is hydrophilic or hydrophobic) and thermotropic behavior. The surfactants used were of non-ionic nature, of which Tween 80® and Brij 58® were more hydrophilic, while Span 40® and Span 60® were more hydrophobic. Each surfactant has unique innate thermal properties and an affinity towards Pluronic 188. The nanosystems were formulated through mixing the pluronic with the surfactants at three different ratios, namely 90:10, 80:20, and 50:50, using the thin-film hydration technique and keeping the pluronic concentration constant. The physicochemical characteristics of the prepared nanosystems were evaluated using various light scattering techniques, while their thermotropic behavior was characterized via microDSC and high-resolution ultrasound spectroscopy. Microenvironmental parameters were attained through the use of fluorescence spectroscopy, while the cytotoxicity of the nanocarriers was studied in vitro. The results indicate that the combination of Pluronic 188 with the above surfactants was able to produce hybrid homogeneous nanoparticle populations of adequately small diameters. The different surfactants had a clear effect on physicochemical parameters such as the size, hydrodynamic diameter, and polydispersity index of the final formulation. The mixing of surfactants with the pluronic clearly changed its thermotropic behavior and thermal transition temperature (Tm) and highlighted the specific interactions that occurred between the different materials, as well as the effect of increasing the surfactant concentration on inherent polymer characteristics and behavior. The formulated nanosystems were found to be mostly of minimal toxicity. The obtained results demonstrate that the thin-film hydration method can be used for the formulation of pluronic-surfactant hybrid nanoparticles, which in turn exhibit favorable characteristics in terms of their possible use in drug delivery applications. This investigation can be used as a road map for the selection of an appropriate nanosystem as a novel vehicle for drug delivery. [ABSTRACT FROM AUTHOR]

BACKGROUND: Solvent‐free microwave‐assisted extraction (MAE) is a green extraction method capable of boosting the yield and quality profile of hemp essential oil when compared with other conventional extraction techniques. During this process, two by‐products are produced, namely the aqueous residue containing bioactive phenolics and the residual deterpenated biomass, which can be used for further extraction and purification of phytocannabinoids. To date, the hemp industry has not utilized these products, although they can be valuable for the food, cosmetic, nutraceutical and pharmaceutical market. RESULTS: This study assessed and optimized the variables affecting MAE efficiency, namely microwave irradiation power, extraction time and added water, which were studied using a central composite design approach, and results were used to optimize the extraction process for recovering three valuable fractions: essential oil, polyphenols and phytocannabinoids. The products obtained using the optimized conditions were characterized in terms of yield, chemical profile and antioxidant potential. Moreover, the by‐products obtained during the optimized run were further analyzed in terms of their biological activity using both enzymatic and non‐enzymatic assays. The aqueous residue demonstrated a powerful α‐glucosidase inhibition, a good activity in terms of superoxide radical scavenging activity, a modest efficacy in terms of inhibition of advanced glycation end products formation and no activity in terms of lipase inhibition. The residual deterpenated biomass did not possess significant biological activity. CONCLUSION: This work demonstrated valorization of industrial hemp essential oil and its by‐products, obtained by a sustainable and eco‐friendly extraction method, through an almost waste‐free approach. Cannabinoids as well as other valuable bioactive compounds such as glycosidic flavones may be recovered from the residues of the essential oil extraction, representing interesting substances in the pharmaceutical, cosmetic and nutraceutical fields. © 2022 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

Essential oils (EOs) represent innovative and safe botanical pesticides to be exploited in different fields, including agriculture, being often obtained by cheap and easily available plant crops. However, their use is threatened by some limits, which are mainly linked to their physico-chemical properties. In this regard, the use of nanoemulsions (NEs) usually enables to overcome these limits but often also to improve the biological activities of these products. Bunium persicum (Boiss.) B Fedtsch. and Ziziphora clinopodioides Lam. are two aromatic plants of economic interest well known for their traditional food and medical uses. Their EOs exhibited several biological properties, including a remarkable insecticidal activity against different targets. Here, the chemical analysis of the two EOs revealed the predominance of γ -terpinene (35.8%), cumin aldehyde (16.6%), γ -terpinen-7-al (14.0%), and α -terpinen-7-al (11.7%) for B. persicum , and pulegone (55.6%), piperitenone (12.8%), and iso -menthone (8.0%) for Z. clinopodioides. NEs were successfully obtained by high-pressure homogenization or ultrasonication method, using polysorbate 80 as emulsifier. The EOs and their 10% NEs were evaluated against larvae and pupae of Culex quinquefasciatus Say mosquitoes. In detail, both EOs exhibited a good larvicidal efficacy (LC 50 of 35.8 and 68.9 µL L−1 for B. persicum and Z. clinopodioides , respectively). Bunium persicum EO NE showed higher efficacy than the EO alone (LC 50 = 290.4 µL L−1), considering that only the 10% of the EO was encapsulated. Conversely, Z. clinopodioides NE showed the same efficacy than the EO alone (LC 50 of 759.8 µL L−1). In addition, both NEs displayed significantly better sublethal toxicity compared with the EOs. Moreover, even if no significant mortality was detected in the pupal stage, only 12% of the larvae pupated and emerged as adults in the case of the NE from B. persicum. In conclusion, both EOs and their NEs could be promising candidates for the development of botanical pesticides, also considering the commercial availability and affordability of these EOs. • Bunium persicum and Ziziphora clinopodioides are valuable sources of essential oils. • Their nanoemulsions were obtained by obtained by high-pressure homogenization. • Nanoemulsions evaluated for toxicity and sublethal effects on Culex quinquefasciatus. • Nanoemulsions showed same contact toxicity than essential oils alone. • Nanoemulsions showed better sublethal toxicity than essential oils. [ABSTRACT FROM AUTHOR]

High-resolution ultrasound spectroscopy (HR-US) is a spectroscopic technique using ultrasound waves at high frequencies to investigate the structural properties of dispersed materials. This technique is able to monitor the variation of ultrasound parameters (sound speed and attenuation) due to the interaction of ultrasound waves with samples as a function of temperature and concentration. Despite being employed for the characterization of several colloidal systems, there is a lack in the literature regarding the comparison between the potential of HR-US for the determination of phospholipid thermal transitions and that of other common techniques both for loaded or unloaded liposomes. Thermal transitions of liposomes composed of pure phospholipids (dimyristoylphosphatidylcholine, DMPC; dipalmitoylphosphatidylcholine, DPPC and distearoylphosphatidylcholine, DSPC), cholesterol and their mixtures were investigated by HR-US in comparison to the most commonly employed microcalorimetry (mDSC) and dynamic light scattering (DLS). Moreover, tramadol hydrochloride, caffeine or miconazole nitrate as model drugs were loaded in DPPC liposomes to study the effect of their incorporation on thermal properties of a phospholipid bilayer. HR-US provided the determination of phospholipid sol-gel transition temperatures from both attenuation and sound speed that are comparable to those calculated by mDSC and DLS techniques for all analysed liposomal dispersions, both loaded and unloaded. Therefore, HR-US is proposed here as an alternative technique to determine the transition temperature of phospholipid membrane in liposomes. [ABSTRACT FROM AUTHOR]

[Display omitted] • Microwave extraction enhanced spilanthol content in Acmella oleracea essential oil. • Spilanthol was isolated and used for comparative purposes. • The essential oil was encapsulated into a nanoemulsion. • Its acute toxicity and impact on fertility were evaluated on Culex quinquefasciatus. • Cytotoxicity and anti-inflammatory effects were determined in human cells. Acmella oleracea (L.) R.K. Jansen, also named jambù, is an edible and medicinal plant native to Brazil but extensively cultivated all over the world due to its diverse utilizations in food, cosmetics, pharmaceutics, and pest management science. Most of applications are related to the presence of active ingredients, namely alkylamides, among which spilanthol is the most important one. On the other hand, the plant biomass resulting from the large-scale cultivation of A. oleracea may yield an essential oil (EO), which can be used for some industrial purposes, for instance as larvicide against vector mosquitoes. This EO is mainly characterized by mono- and sesquiterpenes, however also spilanthol can be detected in the mixture. To maximize the content of spilanthol in the A. oleracea EO, A. oleracea aerial parts obtained from a cultivation in central Italy were subjected to microwave-assisted extraction (MAE). This procedure allowed to obtain a higher yield and spilanthol content when compared with traditional hydrodistillation (0.47 v 0.22 %, and 13.31 vs 2.24 %, respectively). The EO terpene fraction was mainly represented by β- pinene (10.8 %), myrcene (12.3 %), (E)-caryophyllene (19.4 %) and α- humulene (1.1 %). The A. oleracea EO was encapsulated into a nanoemulsion (NE) containing 6 % EO using a high-energy method. The formulation physical stability was assessed by optical microscope and DLS analyses at different timepoints showing stability up to one year of storage. The A. oleracea EO and its NE, along with the isolated spilanthol, were evaluated for acute toxicity against the 3rd instar larvae of Culex quinquefasciatus , a filariasis and arbovirus vector of public health importance, achieving LC 50 values of 16.1, 407.5, and 3.1 μL/L, respectively. The larvicidal activity seemed to be not dependent on the interaction with the cholinergic system, as shown by the high IC 50 values of A. oleracea EO and spilanthol exhibited in the anti-acetylcholinesterase (AChE) assay. Testing LC 30 values, the A. oleracea -borne products showed a significant impact on larval development, fecundity, fertility and natality of C. quinquefasciatus. Testing LC 30 values, the A. oleracea EO-NE provided a higher efficacy than spilanthol, reducing the adult fertility, in terms of egg hatchability (%) and the overall abundance of F 1 larvae. These results can be considered as promising for the development of new mosquito larvicides. The safety use of A. oleracea EO, NE and spilanthol was demonstrated in assays on mammalian fibroblasts and microglia cells, showing low level of cytotoxicity coupled with protective effects against inflammation. [ABSTRACT FROM AUTHOR]

[Display omitted] • The development of green insecticides for real-world use is a major challenge. • This review focuses on Apiaceae-borne botanicals effectiveness against mosquitoes. • Essential oils and main constituents as mosquitocidal/repellent agents are reviewed. • Modes of action of Apiaceae essential oils and their major compounds are discussed. • Toxicity on non-target species and micro/nano-formulation development is analysed. Apiaceae is a family encompassing medicinal and aromatic plants. They produce essential oils (EOs) inside oil canals, known as ducts and vittae, which occur in their vegetative and reproductive organs. Given the high EO yields and the availability of raw material from cultivations widespread all over the world, Apiaceae are exploitable for different industrial applications. An interesting perspective is their utilization in the fabrication of botanical insecticides effective against insect vectors of public importance such as mosquitoes, aiming to be eco-friendly alternatives to synthetic insecticides. On this basis, in the current review, we collected scientific evidence supporting the use of Apiaceae EOs and their major constituents as active ingredients in insecticidal formulations against larvae and adults of several mosquitoes that are important pathogen vectors (e.g., Anopheles , Aedes and Culex species). For this purpose, we analysed the published data on their larvicidal, ovicidal, oviposition deterrent, pupicidal, adulticidal, and repellent effects, using efficacy thresholds as in the case of larvicidal activity (LC 50 (lethal concentration killing 50 % of the exposed population) < 50 ppm). Toxicity to non-target organisms, including vertebrates, has also been reviewed. The major EO constituents have been highlighted, each with its spectrum of mosquitocidal activity, providing insights on their multiple modes of action. The urgent need to develop highly stable micro/nano-formulations for real-world use has been outlined. Current weaknesses and strengths in the steps toward the development of botanical insecticides have been analysed to increase awareness of the future challenges necessary to open the doors to the industrial utilization of Apiaceae EOs by agrochemical companies. [ABSTRACT FROM AUTHOR]

• mPEG-PLGA NPs, loaded with saquinavir mesylate (SQV), were incorporated inside carbopol (C974)-based hydrogel as a vaginally administered prevention or therapeutic treatment for HIV infection. • Hydrogel consistency was reduced by increasing NPs amount at a fixed C974 concentration. • mPEG-PLGA NPs had a relevant effect in promoting the incorporation of the drug inside hydrogel despite its moderate loading. • As a consequence, the incorporation NPs in the formulation led to a higher amount of the drug released from the hydrogel, using an immersion cell release apparatus. • The in vitro findings of the study could have an impact also on the in vivo bioavailability of the drug. Saquinavir mesylate (SQV) is a protease inhibitor commonly employed for the treatment of human immunodeficiency virus-1 infection. It is generally administered orally as tablets in combination with other antiviral drugs. Another promising route of administration can be represented by the vaginal one through topically applied formulations. This delivery can reduce the first-pass effect in the case of systemic drug adsorption or prevent HIV infection. We propose the formulation of a Carbopol® 974 (C974) hydrogel containing biodegradable mPEG-PL(L)GA nanoparticles (NPs) for the vaginal delivery of SQV, intended both as a prevention and a therapeutic strategy. mPEG-PL(L)GA NPs were incorporated into the C974 polymeric matrix, leading to a reduction of the hydrogel consistency dependent on NPs and C974 concentrations. Despite the moderate drug loading into NPs, the presence of the NPs had an impact on the in vitro release of the drug from the hydrogel at pH 5.5 using immersion cells. A higher amount of the drug was released, probably due to the effect of NPs in promoting the incorporation of the drug into the hydrogel at a high SQV dose. These findings can be useful for the development of topically applied hydrogels for SQV delivery, possibly having improved in vivo therapeutic outcomes. [Display omitted] [ABSTRACT FROM AUTHOR]

Formulation development and non-target effect studies are two crucial steps for the registration of new botanical insecticides. Previous reports put in evidence the potential of hemp (Cannabis sativa L.) essential oil (EO) as a new candidate ingredient for developing green insecticides. However, the validation of its target and non-target effects after proper encapsulation is missing so far. In the current work, we investigated the insecticidal efficacy of the EO obtained from the hemp variety 'Kompolti', and we optimized its formulation development into a nanoemulsion (NE). The latter was assayed against larvae of Culex quinquefasciatus Say, a well-known vector of Wuchereria bancrofti Cobbold, avian malaria, and several arboviruses, such as Western equine encephalitis virus, St. Louis encephalitis virus, West Nile virus, and Zika virus. Considering the percentage of encapsulated EO (7.5% w/w), the developed NE showed mortality on Cx. quinquefasciatus larvae, in terms of LC 50(90) values [72.2 (207.2) ppm], like those of pure EO [50.8(142.3) ppm]. Non-target toxicity experiments showed limited toxicity on the aquatic microcrustacean Daphnia magna Straus (i.e., mortality <16% after 48 h of exposure to the EO-based NE at the LC 90 estimated on mosquito larvae). Considering that the LC 50 values detected in this study are lower than those belonging to many EOs, and that the application at sublethal doses caused mortality between 39.1% and 40.8% as well as a reduction in mosquito fertility resulting in a reduction in natality of 40.4% and 45.1% for the EO and EO-based NE, respectively, both products may be considered as potential environmentally friendly and sustainable insecticides. [Display omitted] • Kompolti hemp essential oil was encapsulated in nanoemulsions. • The insecticidal efficacy of hemp essential oil and its nanoemulsion was assessed. • Both formulations had high acute toxicity on Culex quinquefasciatus larvae. • Both products had limited impact on the aquatic microcrustacean Daphnia magna. [ABSTRACT FROM AUTHOR]

[Display omitted] Lubricants are excipients used in tablet formulations to reduce friction and adhesion forces within the die or on the punches surface during the manufacturing process. Despite these excipients are always required for the tablets production, their amount must be carefully evaluated since lubricants can negatively impact on mechanical strength, disintegration and dissolution behavior of solid dosage forms. Alternative compounds have been suggested to overcome the issues of conventional lubricants and sodium lauryl sulfate (SDS) is one of the most promising one. Despite SDS has been object of several investigations, a definitive conclusion on its effectiveness cannot still be drawn. Particularly, its efficacy on tablets disaggregation and API dissolution is still unclear. Here, the effect of SDS on all the relevant features of tablets and tableting process has been evaluated on immediate release hydrophobic tablets formulations in comparison with conventional lubricants. The results of this investigation are quite outspoken: SDS has a low lubricant power while it determines only a limited improvement on tablets hardness. It greatly improves the tablets wettability but only on model formulations, the presence of superdisintegrants resets its effectiveness and any possible effect on tablets disaggregation. None of the tested formulations showed improvement on the API dissolution rate. [ABSTRACT FROM AUTHOR]

The development of effective control strategies targeting non-native ambrosia beetles (Coleoptera: Curculionidae: Scolytinae and Platypodinae) represents an emerging challenge. This is due both to their rapid spread into climatically suitable newly invaded regions rich in susceptible host plants and to the limited knowledge concerning sustainable management tools. In this context, the use of botanical insecticides, such as plant essential oils (EOs), is considered a promising option in Integrated Pest Management (IPM) strategies as an alternative to conventional insecticides for sustainable crop protection. Here, the impact of five EO nanoemulsions (Rosmarinus officinalis L. cultivar verbenone, Carlina acaulis L., Laurus nobilis L., Cupressus sempervirens L., and Betula alba L.) on the choice behavior, host colonization and progeny production by the invasive ambrosia beetle Xylosandrus compactus (Eichhoff) was evaluated under laboratory and semi-field conditions. The chemical composition of tested EOs was firstly evaluated by means of gas chromatography-mass spectrometry (GC-MS) analyses. Then, EO nanoemulsions were prepared and characterized through dynamic light scattering (DLS). Tested EO nanoemulsions showed single or bimodal droplet size distributions in the nanometric range. Results highlighted a significant repellent activity of R. officinalis cv. verbenone and C. acaulis EO nanoemulsions (at 3% EO concentration). However, the trend for repellence of the R. officinalis EO against the beetle was not confirmed at decreasing EO concentrations (i.e., 1% and 0.5%). Nanoemulsions based on C. acaulis EO significantly affected the beetle choices regardless of the tested EO concentration. Indeed, in no choice bioassays, a significantly lower number of individuals started infesting stems treated with these nanoemulsions. On the other hand, no effect of the EO treatment was found on the number of offspring produced by survived beetle females. The repellence by R. officinalis and C. acaulis EOs was confirmed in semi-field conditions. Overall, our findings provide new insights toward the use of R. officinalis and C. acaulis EOs as repellents of X. compactus , suggesting their future incorporation in non-chemical strategies, such as 'push-pull', as part of sustainable IPM packages targeting this invasive pest. [Display omitted] • Little is known about the use of plant essential oils for managing Xylosandrus ambrosia beetles. • Essential oils of Rosmarinus officinalis cv verbenone and Carlina acaulis alter host colonization by Xylosandrus compactus. • Nanoemulsions based on Carlina acaulis EO repelled the beetle regardless of the tested EO concentration. [ABSTRACT FROM AUTHOR]

Recently, plant secondary metabolites have been considered for developing new generation nematicides. Carlina acaulis L. (Asteraceae) contains an essential oil (EO) exhibiting significant insecticidal activity with limited impact on beneficial aquatic and terrestrial organisms. Herein, we report the development of a C. acaulis essential oil EO (CEO)-based nanoemulsion (CEONE) for managing the phytoparasitic nematode Meloidogyne incognita. Initially, pure C. acaulis essential oil EO (CEO) was evaluated for its toxicity against second stage juveniles (J2) of M. incognita as well as for the interruption of the nematode biological cycle into the roots of artificially inoculated tomato plants. CEO was analysed through gas chromatography-mass spectrometry (GC-MS) analysis. Therefore, CEONE was developed to ameliorate CEO efficacy, and physico-chemically characterized. GC-MS showed that the tested CEO was mainly composed by the polyacetylene carlina oxide (96%). CEO exhibited significant in vivo and in vitro activity against M. incognita. Of note, CEONE was more effective in controlling nematodes into tomato infested roots. Overall, the CEO could be practically exploited for a new class of nematicidal agents. [Display omitted] • Carlina acaulis essential oil EO (CEO)-based nanoemulsion (CEONE) controls Meloidogyne incognita. • CEO contains polyacetylene carlina oxide as the predominant component (96%). • CEO significant acts on M. incognita both in in vitro and in vivo experiments. • CEONE was more effective in controlling nematodes into tomato infested roots. • CEO could be practically exploited for a new class of nematicidal agents. [ABSTRACT FROM AUTHOR]

Carlina acaulis L., belonging to the Asteraceae (Compositae) family, is a perennial herb native to the Alps, which has a long history as a food and traditional remedy , being one of the most important medicinal plants in Europe. Its reported uses go from diuretic, cholagogic, and antibacterial agent for the treatment of gastritis, skin diseases, acne, eczema, and ulcers. Even if this plant presents a rich phytocomplex, its root essential oil (EO) is the product that surely raised most research interest. It has the exceptional feature of having as main constituent the polyacetylene carlina oxide, and is currently listed among botanicals employable in food supplements in Europe. This EO and carlina oxide showed an encouraging bioactivity on a variety of bacteria and fungi, such as Staphylococcus aureus , Escherichia coli , Klebsiella pneumoniae , Pseudomonas aeruginosa , Proteus vulgaris , Candida albicans and C. glabrata. Moreover, these products showed marked insecticidal and acaricidal activities against insect pests and vectors of medical, agricultural, and economic importance, revealing to be promising in the horizon of botanical insecticides and acaricides. Its EO as well as carlina oxide resulted to be active on vectors, e.g. Culex quinquefasciatus, urban and livestock pests e.g. Musca domestica , stored product pests e.g. Acarus siro , Trogoderma granarium and Prostephanus truncatus , and agricultural pests, e.g. Lobesia botrana , Bactrocera oleae and Ceratitis capitata, among others. These insecticidal properties are also accompanied by low-to-moderate toxicity on non-target organisms such as earthworms and aquatic microcrustaceans, as well as on vertebrate cells and mammals. Innovative formulations have been developed and tested for applying these products in real-world conditions with encouraging results. Different cultivation systems of C. acaulis have been carried out, with classic field cultivation having the greatest advantage over other systems, such as hydroponic and in vitro micropropagation in terms of insecticidal and acarcicidal compound yield. This review puts a focus for the first time on C. acaulis , its active compounds and its potential against vectors, pests, and pathogens, and on current issues related to its cultivation on a large-scale level. Moreover, its biological properties and related encapsulation techniques developed are extensively reviewed. [Display omitted] • Carlina acaulis potential as a green insecticide and acaricide was reviewed. • Carlina oxide was examined as the main responsible for the insecticidal action. • Non-target toxicity was investigated. • Challenges and perspectives for the plant cultivation were considered. • The crucial role of nanoformulations for essential oil delivery was discussed. [ABSTRACT FROM AUTHOR]

[Display omitted] The abilities of sub-cellular targeting and stimuli-responsiveness are critical challenges in pharmaceutical nanotechnology. In the present study, glyceryl monooleate (GMO)-based non-lamellar lyotropic liquid crystalline nanoparticles were stabilized by the poly(2-(dimethylamino)ethyl methacrylate)- b -poly(lauryl methacrylate) block copolymer carrying tri-phenyl-phosphine cations (TPP-QPDMAEMA- b -PLMA), either used alone or in combination with other polymers as co-stabilizers. The systems were designed to perform simultaneously sub-cellular targeting, stimuli-responsiveness and to exhibit stealthiness. The physicochemical characteristics and fractal dimensions of the resultant nanosystems were obtained from light scattering techniques, while their micropolarity and microfluidity from fluorescence spectroscopy. Their morphology was assessed by cryo-TEM, while their thermal behavior by microcalorimetry and high-resolution ultrasound spectroscopy. The analyzed properties, including the responsiveness to pH and temperature, were found to be dependent on the combination of the polymeric stabilizers. The subcellular localization was monitored by confocal microscopy, revealing targeting to lysosomes. Subsequently, resveratrol was loaded into the nanosystems, the entrapment efficiency was investigated and in vitro release studies were carried out at different conditions, in which a stimuli-triggered drug release profile was achieved. In conclusion, the proposed multi-functional nanosystems can be considered as potentially stealth, stimuli-responsive drug delivery nanocarriers, with targeting ability to lysosomes and presenting a stimuli-triggered drug release profile. [ABSTRACT FROM AUTHOR]

This study focuses on the evaluation of microfoam produced from processed dairy milk using the steaming function of the espresso machine as a function of temperature (30–80 °C), milk type (pasteurised or UHT), and whey protein contents. Foam characteristics, i.e., foam stability, viscosity, bubble size distribution noticeably varied depending on milk processing type and steam heating temperature. Foams made from pasteurised whole milk tended to be more stable. Bubbles in pasteurised milk foam were better distributed, especially at the temperature of 60 °C. It was observed that the optimal final temperature of steam frothing was in the range of 50 °C–60 °C. The results of sensory tests showed that consumers differentiated between the aroma and flavour of pasteurised and UHT milk, describing the degree of this difference from moderate to strong. [ABSTRACT FROM AUTHOR]

The essential oils (EOs) produced by a number of Apiaceae species are well known for their insecticidal efficacy against a wide spectrum of insects, including vectors, stored product and agricultural pests. In the real world, rawly formulated EOs are scarcely effective due to their low chemical stability, limited persistence into the environment, and poor hydrophilicity. Therefore, for practical applications they need to be encapsulated using nanocarriers. In the present study, we evaluated two novel EO-based nanoemulsions (NEs) derived from Pimpinella anisum and Trachyspermun ammi , two plants with documented insecticidal effectiveness, for the management of stored product insects causing economic damages, including Tribolium castaneum , Tribolium confusum , Tenebrio molitor , Trogoderma granarium adults or larvae, and Acarus siro adults or nymphs. The NEs were prepared by a high-pressure homogenization procedure and determined according to the distribution of particle size through dynamic light scattering. Pimpinella anisum EO resulted mainly dominated by the phenylpropanoid (E)-anethole, while T. ammi EO was mainly composed of thymol, p -cymene, and γ -terpinene. Each EO-based NE was tested at two concentrations (500 and 1000 ppm) on stored wheat. We evaluated mortality values of the arthropod pests after 4 h, 8 h, and 16 h, and daily from 1 to 7 days. Complete mortality was achieved for T. castaneum larvae on wheat sprayed with 1000 ppm of 4% (w/w) P. anisum EO-based NE after 6 days of exposure. Similarly, the 8% (w/w) T. ammi EO-based NE killed 100.0% of the tested T. confusum larvae after 7 days to 1000 ppm. When A. siro adults were exposed to 1000 ppm of the 8% (w/w) T. ammi EO-based NE, 89.4% of the tested individuals were killed after 7 days. Binary EO-based NE combination toxicity tests were also carried out. Almost all T. molitor adults (97.8%) died after 7 days to 1000 ppm of 3% (w/w) T. ammi + 3% (w/w) P. anisum EO-based NE. The 3% (w/w) T. ammi + 3% (w/w) P. anisum EO-based NE killed 98.6% of T. granarium adults after 7 days at 1000 ppm. Overall, the tested Apiaceae EO-based NEs exhibited relevant pesticidal efficacy under short exposure intervals, therefore they could be taken into account as auxiliary management tools towards the sustainable protection of durable commodities in storages. [Display omitted] • 4% (w/w) P. anisum EO-based NE killed all T. castaneum larvae after 6 days at 1000 ppm. • 8% (w/w) T. ammi EO-based NE killed all T. confusum larvae after 7 days at 1000 ppm. • 3% (w/w) T. ammi + 3% (w/w) P. anisum EO-based NE killed 97.8% T. molitor adults after 7 days at 1000 ppm. • 3% (w/w) T. ammi + 3% (w/w) P. anisum EO-based NE killed 98.6% T. granarium adults after 7 days at 1000 ppm. [ABSTRACT FROM AUTHOR]

Horsemint, Mentha longifolia (L.) Huds. (Lamiales: Lamiaceae), is a member of the genus Mentha , widely used for the repellent and insecticidal effectiveness of its essential oil (EO). Several chemotypes have been reported for this species. Here, the efficacy of a M. longifolia EO, belonging to the piperitenone oxide-type, and a 10% (w/w) M. longifolia EO-based nanoemulsion (NE) were examined as wheat protectants, at 500 and 1000 ppm (μL/kg). The two products were tested against four insect and a mite species, i.e., the red flour beetle, Tribolium castaneum (Herbst) (Coleoptera: Tenebrionidae), the confused flour beetle, Tribolium confusum Jacquelin du Val (Coleoptera: Tenebrionidae), the yellow mealworm beetle, Tenebrio molitor (L.) (Coleoptera: Tenebrionidae), the saw-toothed grain beetle, Oryzaephilus surinamensis (L.) (Coleoptera: Silvanidae), and the flour mite, Acarus siro L. (Sarcoptiformes: Acaridae). The NE showed a mean hydrodynamic diameter below 200 nm after preparation and no relevant changes in particle size distribution at least up to 4 months. The highest concentration of M. longifolia EO was the most effective grain protectant, causing 84.4% and 100% mortality to T. castaneum adults and larvae respectively, 42.2% and 100% mortality to T. confusum adults and larvae respectively, 100% and 34.4% mortality to T. molitor adults and larvae respectively, 100% mortality to both adults and larvae of O. surinamensis , and 87.8% and 67.8% mortality to A. siro adults and nymphs, respectively. Tribolium castaneum larvae were controlled by 500 ppm of the EO and 1000 ppm of the NE, which caused 100% and 93.3% mortality, respectively. Similarly, 1000 ppm NE caused 96.7% mortality against T. confusum larvae, while 500 ppm EO and 1000 ppm NE killed 90.0% and 91.1% of T. molitor adults, respectively. Complete mortality (100%) of O. surinamensis adults was achieved by 500 ppm EO. The findings of the current study suggest that the M. longifolia EO and the M. longifolia EO-based NE may be considered as promising alternative wheat protectants against different insect and mite storage pests, depending on their developmental stage. [Display omitted] • Mentha longifolia EO killed all Tribolium castaneum larvae after 1 day at 500 ppm. • Mentha longifolia EO killed 100% of T. confusum larvae after 4 days at 1000 ppm. • Mentha longifolia EO killed all Tenebrio molitor adults 5 days post-exposure to 1000 ppm. • All Oryzaephilus surinamensis adults and larvae were dead within 2 days at 1000 ppm EO. • Both M. longifolia EO and NE killed >80% Acarus siro adults within 7 days at 1000 ppm. [ABSTRACT FROM AUTHOR]

[Display omitted] Hand sanitizers represent a primary measure for the prevention of transmissible infections, whose use has been greatly increased during CoViD-19 pandemic. Most of the commercially available products are hydrogels, employing carbomers as thickening agents. However, few information is still available regarding performances of carbomers in hydroalcoholic media containing a percentage of alcohols ≥ 60% v/v as recommended for disinfection. The aim of this study was to investigate the colloidal behaviour of carbomer 974 and carbomer 980 in hydroalcoholic media containing from 50 to 80% w/w of alcohol (ethanol or isopropanol) and neutralised with triethanolamine or aminomethyl propanol. Both carbomers provide transparent hydrogels in water, but carbomer 980 should be preferred for the formulation of hydrogel with a percentage of alcohol ≥ 50% w/w for its better solvation. The critical alcohol concentration (CAlC), above which polymer precipitation occurs, depends on the type of alcohol and base used. Carbomer dispersions with a higher content of alcohol can be prepared using aminomethyl propanol rather than triethanolamine. The choice of the more suitable components is fundamental for the isopropanol-based dispersions since the CAlC is closer to the recommended concentrations for disinfection. Overall, these results provide helpful insights for the correct preparation of alcohol-based hand sanitizers using carbomers. [ABSTRACT FROM AUTHOR]

Quetiapine is an atypical antipsychotic approved for treating schizophrenia, bipolar depression, and mania but is frequently used in an off-label manner to control the behavioral and psychological symptoms of dementia in elderly patients with dementia. Due to the need to personalize doses for elderly patients with dementia, quetiapine tablet manipulation is widespread in hospital settings, long-term care facilities, and patient homes. The aim of this study was to assess the impact of the different splitting techniques on quetiapine fumarate tablets by analysing the obtained sub-divided tablets and to discuss compliance with the European Pharmacopoeia limits on whole and split tablets. Quetiapine fumarate tablets of two dose strengths were taken at random (in a number able to assure a power of 0.8 during statistical comparison) and were split with a kitchen knife or tablet cutter. The weight and the drug content were determined for each half tablet. The obtained data were compared to the European Pharmacopoeia limits. The differences between the different splitting techniques were statistically tested. Data showed that split tablets, independently of the dose strength and the technique employed, were not compliant with the European Pharmacopoeia specifications for both entire and subdivided tablets in terms of weight and content uniformity. Thus, such a common practice could have potential effects on treatment efficacy and toxicity, especially when also considering the fragility of the elderly target population in which polypharmacotherapy is very common. These results indicate a compelling need for flexible quetiapine formulations that can assure more accurate dose personalization. [ABSTRACT FROM AUTHOR]

[Display omitted] Cellulosic-based thickeners are commonly used in the preparation of hydro-alcoholic hand sanitisers. Yet, little is known about the behaviour of these polymeric dispersions in hydro-alcoholic mixtures. Here, we studied the dispersion ability and rheology of hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose and sodium carboxymethyl cellulose in water–ethanol mixtures. Hydroxypropyl cellulose formed transparent dispersions across the entire range of ethanol concentrations, while a critical ethanol concentration (CEC), above which dispersions became turbid, was found for all the other polymers. At and below the CEC, all the rheological parameters followed a bell-like shape profile as a function of ethanol concentration. Moreover, the molecular weight and degree of substitution of the polymers influenced the rheological properties. The CEC and rheological behaviour of the dispersions were both dependent on the ethanol/polymer and water/polymer interactions. As hand disinfectants should contain 60–95% ethanol, polymers of higher CEC, such as hydroxypropyl cellulose and hydroxypropyl methylcellulose, are recommended. [ABSTRACT FROM AUTHOR]