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The aim of this research was to evaluate the potential of the nanospray drier as a novel apparatus for the manufacturing of a dry powder for inhalation containing ketoprofen lysinate, a nonsteroidal anti-inflammatory drug able to control the inflammation in cystic fibrosis patients. We produced several ketoprofen lysinate and leucine powder batches by means of nanospray dryer, studying the influence of process parameters on yield, particle properties (size distribution and morphology), and, mainly, aerodynamic properties of powders. Micronized particles were prepared from different hydroalcoholic solutions (alcohol content from 0 to 30% v/v) using ketoprofen in its lysine salt form and leucine as dispersibility enhancer in different ratios (from 5 to 15% w/w) with a total solid concentration ranging from 1 to 7% w/v. Results indicated that the spray head equipped with a 7 µm nozzle produced powders too big to be inhaled. The reduction of nozzle size from 7 to 4 µm led to smaller particles suitable for inhalation but, at the same time, caused a dramatic increase in process time. The selection of process variables, together with the nozzle pretreatment with a surfactant solution, allowed us to obtain a free flowing powder with satisfying aerosol performance, confirming the usefulness of the nanospray drier in the production of powder for inhalation.

Propolis is an attractive natural ingredient to design health products due to its pharmacological effects. Our chemical investigation of a polar extract of Nigerian propolis (NP) led the isolation and identification of five isoflavonoids (1-4, 6), one diarylpropane (5) and one prenylated flavanone (7) by the combination of chromatographic and spectroscopic techniques. Compounds 1, 4 and 7 were found to be the main markers in NP (8.0, 5.0 and 4.0 mg/g of dry extract, respectively). Moreover, NP and its phenolic constituents exhibited in vitro free radical scavenging activity together with a promising antidiabetic effect against α-amylase and α-glucosidase enzymes. Finally, NP showed also a moderate inhibition of Helicobacter pylori growth. These results suggested that NP could be a good candidate in nutraceuticals and food products. [ABSTRACT FROM AUTHOR]

Featured Application: The technological approach can help the health industry access new upcycled plant extracts that the industry could not access before because of the poor sensoriality or difficulty of use, with great sustainability profiles that consumers value very much. The obtained ingredient is stable both under process and harsh storage conditions, is readily water-soluble and easy handling, demonstrating versatility for multiple applications in various industries from cosmetic to nutrition and much more. Grape harvesting generates a high amount of wastes, mostly leaves, which represent an economic and ecological problem for farmers. New products can be generated through these wastes, giving environmental, social, and economic advantages while also meeting the industry demand for novel natural ingredients. In this study, aqueous leaf-extracts from two cultivars of Vitis vinifera Aglianico (Agl) and Greco di Tufo (Gre) were produced by microwave-assisted extraction (MAE) and evaluated in composition by ATR- FTIR and HPLC to identify the main phenolic compounds, especially quercetin and kaempferol. The results showed that leaves extracts confirm to be a potential source of phenolic compounds. Dry extracts, although highly functional, show critical handling characteristics, being sticky and unstable in normal post-processing conditions. A stable and easy handling microparticulate ingredient was produced by spray drying containing the most phenolic-rich obtained extract (AGL-28). The microparticle powder form based on pectin/maltodextrin matrix was produced with high process efficiency. The microstructures were able to confer functional and chemical stability to the extract while also showing good technological characteristics (high water dissolution rate and flow properties), transforming the extract into a handling ingredient able to meet new industrial uses. [ABSTRACT FROM AUTHOR]

Considered as a superfood of the future, Spirulina platensis matrix has been extensively used because of its beneficial effect on the management of cardiovascular diseases. However, its nutraceutical properties, bioactive compounds, and molecular mechanisms are unknown. Here, we demonstrate that S platensis matrix processed in vitro by simulated gastrointestinal digestion induces direct endothelial nitric oxide (NO)-mediated vasorelaxation of resistance vessels in mice. To gain insight into the bioactive compounds responsible for this effect, we used a complex multistep peptidomic approach to fractionate the crude digest: of the 5 peptide fractions identified (A-E), only fraction E evoked vasorelaxation. High-resolution mass spectrometry-based screening revealed in E the presence of 4 main peptides (SP3-SP6 [spirulina peptides]), of which only SP6 (GIVAGDVTPI) exerted direct endothelium-dependent vasodilation of ex vivo vessels, an effect occurring via a PI3K (phosphoinositide-3-kinase)/AKT (serine/threonine kinase Akt) pathway converging on NO release. In vivo, administration of SP6 evoked a significant hemodynamic effect, reducing blood pressure, an action absent in eNOS (endothelial NO synthase)-deficient mice. Of note, although lower doses of SP6 had no hemodynamic effects, it still enhanced endothelial NO vasorelaxation. Finally, in an experimental model of arterial hypertension, SP6 exerted an antihypertensive effect, improving endothelial vasorelaxation associated with enhanced serum nitrite levels. Based on our results, this novel decameric peptide may extend the possible fields of application for spirulina-derived peptides and could be developed into a promising nonpharmacological approach for the containment of pathologies associated with vascular NO misregulation. [ABSTRACT FROM AUTHOR]

Many natural compounds having antioxidant and anti-inflammatory activity are a potential target for new therapies against chronic inflammatory syndromes. The oral administration of functional herbal supplements may become a prevention strategy or therapy adjuvant for susceptible patients. A case study is our milk thistle (Silybum marianum) extract rich in silymarin complex. A water-soluble microencapsulated powder system was developed by a spray drying technique to improve the poor silymarin bioactivity after oral administration. Sodium carboxymethylcellulose (NaCMC) was employed as coating/swelling polymer matrix and sodium lauryl sulfate (SLS) as the surfactant (1:1:0.05 w/w/w). A H2O/EtOH/acetone (50/15/35 v/v/v) solvent system was used as liquid feed. The microsystems were capable of improving the in vitro dissolution and permeation rates, suggesting an enhancement of bioactivity after oral administration. The microsystems protect the antioxidant activity of silymarin after harsh storage conditions period and do not affect the anti-inflammatory properties of the raw extract (efficient already at lower concentrations of 0.312 mg/mL) to reduce dendritic cells (DCs) inflammatory cytokine secretion after lipopolysaccharide administration. This approach allows managing particle size, surface properties and release of bioactive agents improving the bioactivity of a herbal supplement and is also possibly applicable to many other similar natural products. [ABSTRACT FROM AUTHOR]

Hazelnut shells, a by-product of the kernel industry processing, are reported to contain high amount of polyphenols. However, studies on the chemical composition and potential effects on human health are lacking. A methanol hazelnut shells extract was prepared and dried. Our investigation allowed the isolation and characterization of different classes of phenolic compounds, including neolignans, and a diarylheptanoid, which contribute to a high total polyphenol content (193.8 - 3.6 mg of gallic acid equivalents (GAE)/g of extract). Neolignans, lawsonicin and cedrusin, a cyclic diarylheptanoid, carpinontriol B, and two phenol derivatives, C-veratroylglycol, and β-hydroxypropiovanillone, were the main components of the extract (0.71%-2.93%, w/w). The biological assays suggested that the extract could be useful as a functional ingredient in food technology and pharmaceutical industry showing an in vitro scavenging activity against the radical 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) (EC50 = 31.7 µg/mL with respect to α-tocopherol EC50 = 10.1 µg/mL), and an inhibitory effect on the growth of human cancer cell lines A375, SK-Mel-28 and HeLa (IC50 = 584, 459, and 526 µg/mL, respectively). The expression of cleaved forms of caspase-3 and poly(ADP-ribose) polymerase-1 (PARP-1) suggested that the extract induced apoptosis through caspase-3 activation in both human malignant melanoma (SK-Mel-28) and human cervical cancer (HeLa) cell lines. The cytotoxic activity relies on the presence of the neolignans (balanophonin), and phenol derivatives (gallic acid), showing a pro-apoptotic effect on the tested cell lines, and the neolignan, cedrusin, with a cytotoxic effect on A375 and HeLa cells. [ABSTRACT FROM AUTHOR]

The aim of this study was to produce a hydro-alcoholic safe antioxidant Malus pumila Miller cv Annurca peel extract (APE) useful as functional ingredient in an oil-in-water emulsion. Results showed that APE contains a hydroxycinnamic acid (chlorogenic acid), flavonol glycosides (quercetin derivatives) and a dihydrochalcone, phloridzin (phloretin-2-O-glucoside). The isoquercitrin (quercetin-3-O-glucoside) content was quantified in 0.3% w/w of extract. APE showed a significant and concentration-dependent free-radical scavenging activity correlated to its polyphenols content. No cytotoxic effect was observed in primary human epidermal keratinocyte adults and dermal fibroblast cell lines. The formulative approach led to produce a stable emulsion able to load a high amount of APE, up to 6.0% w/w. The homogenous distribution of APE in the emulsion was clearly demonstrated by fluorescence microscopy analysis. The emulsion resulted able to enhance the in vitro release rate of APE through synthetic membranes with respect to the raw material. [ABSTRACT FROM AUTHOR]

Thymelaea microphylla Coss. et Dur. (Thymelaeaceae) is a rare medicinal plant endemic to Algeria. In order to continue our studies on this species, herein we report the isolation and characterisation of 20 compounds from a hydroalcoholic extract (EtOH–H2O 7:3) of the aerial parts. They include monoterpene glucosides (1–3), phenolic acid derivatives (4, 8 and 9), phenylpropanoid glucosides (5 and 6), flavonoids (7, 10 and 11), a benzyl alcohol glucoside (12), ionol glucosides (13–16), lignans (17–19) and a bis-coumarin (20). All the structures were elucidated by spectroscopic methods including 1D and 2D NMR experiments, as well as ESI-MS analysis. Moreover, the extract of T. microphylla showed a significant and concentration-dependent free radical-scavenging activity in vitro, correlated to the presence of phenolic and chlorogenic acid derivatives (8, 9 and 4). [ABSTRACT FROM AUTHOR]

The study focused on the development and characterization of an O/W emulsion for skincare containing Castanea sativa spiny burs extract (CSE) as functional agent. The emulsion was stable and had suitable physicochemical and technological properties for dermal application and CSE showed no cytotoxicity in spontaneously immortalized keratinocytes (HaCaT) at active concentrations. A single-blind, placebo-controlled, monocentric study was designed to evaluate the skin tolerability and the skin performance of the CSE-loaded emulsion on healthy human volunteers. An improvement was observed in skin biomechanical properties such as hydration, skin elasticity and a reduction in the periorbital wrinkles in 30 days without altering the skin barrier function, sebum, pH, and erythema values. A significant skin moisturizing effect was detected while the skin barrier function was preserved. The selected natural ingredient combined with the designed formulation and the optimized preparation method has led to a final product that satisfies the physico-chemical and technological requirements underlying the safety of use and the formulative stability over time. With no negative skin reactions and highly significant effects on skin elasticity, wrinkles, and moisturization, the CSE-based emulsion achieved very satisfying outcomes representing a promising functional formulation for skin care. [ABSTRACT FROM AUTHOR]

Cancer is one of the main causes of death globally and considered as a major challenge for the public health system. The high toxicity and the lack of selectivity of conventional anticancer therapies make the search for alternative treatments a priority. In this review, we describe the main plant-derived natural products used as anticancer agents. Natural sources, extraction methods, anticancer mechanisms, clinical studies, and pharmaceutical formulation are discussed in this review. Studies covered by this review should provide a solid foundation for researchers and physicians to enhance basic and clinical research on developing alternative anticancer therapies. [ABSTRACT FROM AUTHOR]

The administration of natural antioxidants is considered to be a prevention strategy for chronic diseases and a useful tool for the healthcare system to reduce the administration of expensive and often not effective treatments. The chemical characterization of a methanolic extract (AJ) of Ajuga reptans L. was performed, and its antioxidant activity was evaluated. AJ and the major compounds, characterized by chromatographic techniques as phenylpropanoids and iridoids, were able to reduce the Reactive Oxygen Species levels in cancer cell lines (melanoma, A375, cervical cancer, HeLa, and alveolar adenocarcinoma, A549), stimulated by E. coli lipopolysaccharide. However, a clinical translation of these results encountered a significant limitation represented by the poor water solubility and bioavailability of the extract and compounds. Consequently, a hydro-soluble powder system (AJEP3) was developed by spray-drying encapsulating AJ into a multi-component solid matrix that is based on L-proline and hydroxyethylcellulose as loading and coating agents, and lecithin as solubility enhancer. The technological approach led to a satisfactory process yield (71.5%), encapsulation efficiency (99.9%), and stability. The in vitro water dissolution rate of the bioactive compounds appeared to be improved with respect to the extract, suggesting higher feasibility in the manufacturing and administration; even the in vitro biological activity of the produced multi-component AJEP3 was clearly enhanced. [ABSTRACT FROM AUTHOR]

Spirulina platensis contains several compounds showing nutritional and therapeutic benefits. Recently, a series of peptides able to reduce the blood pressure level and to enhance the endothelial vasorelaxation was isolated from the hydrolyzed highly water-soluble Spirulina extract (HSE). However, HSE shows critical organoleptic characteristics also having poor intestinal permeability, limiting absorption when orally delivered. This research aims to overcome the critical issues through the encapsulation of HSE in Chitosan/Mannitol—(CM)-based microparticles by spray drying. The produced powders (CM-HSE) showed good process yield (≈70%) and encapsulation efficiency (≈100%) also having good derived flow properties as well as stability up to six months storage. The microparticles constituting the spray-dried powder resulted in an amorphous micrometric state (d50 ≈ 14 µm) able to retain dark colour and unpleasant smell of raw HSE. Moreover, the in vitro permeation study by Franz cell indicated that the engineered microparticles are able to enhance the permeation of HSE through an intestinal biomimetic barrier (551.13 μg/cm2 CM-HSE vs. 315.46 μg/cm2 HSE at 270 min). [ABSTRACT FROM AUTHOR]

An extract obtained from hazelnut shells by-products (HSE) has antioxidant and chemopreventive effects on human melanoma and cervical cancer cell lines, inducing apoptosis by caspase-3 activation. A clinical translation is limited by poor water solubility and low bioavailability. Dried plant extracts often show critical characteristics such as sticky/gummy appearance, unpleasant smell, and instability involving practical difficulties in processing for industrial use. A spray drying method has been applied to transform raw HSE in a microparticulate powder. The biopolymeric matrix was based on l-proline as loading carrier, hydroxyethylcellulose in combination with pectin as coating polymers; lecithin and ethanol were used as solubility enhancers. A Hot-Cold-Hot method was selected to prepare the liquid feed. The thus prepared powder showed good technological properties (solid-state, particle dimensions, morphology, and water dissolution rate), stability, and unchanged chemopreventive effects with respect to the unprocessed HSE. [ABSTRACT FROM AUTHOR]

The choice of formulation is often of crucial importance in order to obtain a pharmaceutical product for the administration of poorly soluble drugs. Recently, a new water-soluble microparticulate powder form (MTE-mp) for the oral administration of a high functionality/low solubility silymarin rich milk thistle extract (MTE) has been developed. Findings showed that extract-loaded microparticles by spray-drying were produced with high and reproducible yields and encapsulation efficiency. The in vitro dissolution and permeation rates of silymarin were dramatically improved with respect to the raw material, and also enhanced the silymarin anti-inflammatory abilities. Given these successful results, the new MTE-mp delivery system has been proposed as an active ingredient for dermal applications. The aim of this research was the design and development of two topical formulations, hydrogel and emulgel (O/W emulsion), containing the MTE-mp delivery system or MTE raw extract. All the formulations were compared to each other in terms of handling and incorporation amount of the active ingredient during the productive process. Moreover, the addition to the emulgel of lecithin (L) as enhancer of permeation was tested. The MTE-mp ingredient that resulted was stable and more-easily incorporated both in hydrogel and emulgel than raw MTE extract, obtaining the best permeation profile for MTE-mp from emulgel with the addition of L. The obtained results confirm that the MTE-mp system could be used as a stable, water-soluble, and easy-handling functional ingredient, giving the opportunity to develop new strategies for MTE delivery in health products. [ABSTRACT FROM AUTHOR]

Chestnut (Castanea sativa Miller.) burs (CSB) represent a solid waste produced during the edible fruit harvesting. Their usual disposal in the field increases the environmental and economic impact of the agricultural process. HPLC-UV-HRMS profiling revealed that CSB organic and aqueous extracts (CSB-M, CSB-H, CSB-A) contain several hydrolyzable tannins, mainly ellagitannins, and glycoside flavonols. Ellagic acid (EA) and chestanin are predominant components (5–79 and 1–13 mg/g dry extract, respectively). NMR analysis confirmed the chemical structures of the major constituents from CSB-M. The extracts displayed a significant scavenging activity against DPPH• (EC50 12.64–24.94 µg/mL) and ABTS•+ radicals (TEAC value 2.71–3.52 mM Trolox/mg extract). They were effective in inhibiting the mycelial growth (EC50 6.04–15.51 mg/mL) and spore germination (EC50 2.22–11.17 mg/mL) of Alternaria alternata and Fusarium solani. At the highest concentration, CSB-M was also active against Botrytis cinerea both in mycelium and spore form (EC50 64.98 and 16.33 mg/mL). The EA contributed to the antifungal activity of extracts (EC50 on spore germination 13.33–112.64 µg/mL). Our results can support the upgrading of chestnut burs from agricultural wastes to a resource of natural fungicides for managing fruit and vegetable diseases. [ABSTRACT FROM AUTHOR]

Arthrospira platensis, better known as Spirulina, is one of the most important microalgae species. This cyanobacterium possesses a rich metabolite pattern, including high amounts of natural pigments. In this study, we applied a combined strategy based on Fourier Transform Ion Cyclotron Resonance Mass Spectrometry (FT-ICR-MS) and Ultra High-Performance Liquid Chromatography (UHPLC) for the qualitative/quantitative characterization of Spirulina pigments in three different commercial dietary supplements. FT-ICR was employed to elucidate the qualitative profile of Spirulina pigments, in both direct infusion mode (DIMS) and coupled to UHPLC. DIMS showed to be a very fast (4 min) and accurate (mass accuracy ≤ 0.01 ppm) tool. 51 pigments were tentatively identified. The profile revealed different classes, such as carotenes, xanthophylls and chlorophylls. Moreover, the antioxidant evaluation of the major compounds was assessed by pre-column reaction with the DPPH radical followed by fast UHPLC-PDA separation, highlighting the contribution of single analytes to the antioxidant potential of the entire pigment fraction. β-carotene, diadinoxanthin and diatoxanthin showed the highest scavenging activity. The method took 40 min per sample, comprising reaction. This strategy could represent a valid tool for the fast and comprehensive characterization of Spirulina pigments in dietary supplements, as well as in other microalgae-based products. [ABSTRACT FROM AUTHOR]

Abstract: Ethnopharmacological relevance: The genus Paeonia (Paeoniaceae), is one of the most important source of crude drugs in traditional Chinese medicine and investigation on many species is large. Up to now studies on Paeonia rockii, one of the eight species recognized in the section Moutan, are very limited. Aim of the study: This research aimed to investigate the composition of Paeonia rockii roots and to evaluate the in vitro free-radical scavenging and antifungal activities of a polar extract (PPR) and its major constituents. Materials and methods: PPR was obtained from defatted dried roots of Paeonia rockii using MeOH as extraction solvent. Its n-BuOH soluble portion (PPR-B) was purified by Sephadex LH-20 followed by RP-HPLC to give nineteen compounds belonging to the classes polyphenols, monoterpenes and triterpenes. Their structure were spectrally characterized (UV, 1D and 2D NMR, MS). The polyphenols content of PPR and PPR-B was examined by the Folin–Ciocalteau colorimetric assay and HPLC method. Both extracts (PPR and PPR-B) and their major constituents were tested for the free-radical scavenging activity by DPPH-test, and for the antifungal activity by three methods (micro-broth dilution method, XTT assay and Candida albicans morphological analysis). Results: 5-Butylhydroxy-γ-lactone (1), and ethyl-arabinopyranoside (2) have been isolated for the first time as naturally occurring compounds and taxifolin (3) was reported for the first time in Paeonia spp. Nine polyphenols, four monoterpenes and three triterpenes were also identified. Both the extracts PPR and PPR-B had high polyphenol content, and high concentration of gallic acid derivatives and paeoniflorin, chemotaxonomic characteristic markers of the genus. PPR, gallic acid and methyl-gallate displayed high potency in scavenging free-radicals (DPPH test, EC50 13.3, 1.2, 1.9μg/ml, respectively). Both the extracts and gallic acid individually showed an interesting antifungal property (MIC50 at 24h 25, 0.9 and 30μg/ml, respectively) and notably, a combination of paeoniflorin/gallic acid (MIC50 =0.5+20μg/ml, respectively) was more active than the single compound in inhibiting Candida growth. Conclusion: The polar methanolic extract (PPR), its n-BuOH soluble fraction and constituents of Paeonia rockii were extensively investigated. Both extracts and some of their compounds have the ability to scavenge free-radicals and to inhibit Candida albicans growth. [Copyright &y& Elsevier]

Graphical abstract Abstract Fused deposition modeling by 3D-printing is a rapid technique for the production of personalized drug dosage forms. One of the most delicate step of the whole process is the drug loading onto the thermoplastic polymer to obtain the drug-loaded filament used as feedstock for 3D FDM printers. With the aim of improving the drug loading, a systematic study on the influence of polymer size distribution on the quantity of drug able to adhere onto the polymer surface was conducted. Several solid mixtures were prepared, using five PVA batches (4000–5000 µm, 1000–2000 µm, 600–1000 µm, 250–600 µm, <250 µm) and Ciprofloxacin hydrochloride as active compound in different ratios. Operative specifics and printer's parameters were tuned for an optimal print of drug-loaded filaments into the desired dosage forms, i.e. cylindrical printlets , fully characterized in terms of homogeneity, process efficiency, physical properties, drug content and release kinetics. The PVA particle size affected the polymer ability to form homogeneous mixture with the drug and the efficiency of the extrusion process. In particular, finest PVA batches showed better processability and reduced the drug loss during the drug/polymer mixing and the extrusion process. Drug-loaded filaments with different drug concentrations were successfully printed and the obtained printlets dissolution profiles were almost superimposable, taking an important step for the future application of 3D-printing manufacturing process to obtain personalized galenic formulations. [ABSTRACT FROM AUTHOR]

BioActive Compounds (BACs) recovered from food or food by-product matrices are useful in maintaining well being, enhancing human health, and modulating immune function to prevent or to treat chronic diseases. They are also generally seen by final consumers as safe, non-toxic and environment-friendly. Despite the complex process of production, chemical characterization, and assessment of health effects, BACs must also be manufactured in stable and bioactive ingredients to be used in pharmaceutical, food and nutraceutical industry. Generally, vegetable derivatives occur as sticky raw materials with pervasive smell and displeasing flavor. Also, they show critical water solubility and dramatic stability behavior over time, involving practical difficulties for industrial use. Therefore, the development of novel functional health products from natural sources requires the design of a suitable formulation to delivery BACs at the site of action, preserve stability during processing and storage, slow down the degradation processes, mask lousy tasting or smell, and increase the bioavailability, while maintaining the BACs functionality. The present review focuses on human health benefits, BACs composition, and innovative technologies or formulation approaches of natural ingredients from some selected foods and by-products from industrial food transformations., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Fresh juice from bergamot (Citrus bergamia Risso) has been studied to evaluate the polyphenolic composition by HPLC-DAD analysis and total polyphenols content by UV method. The main constituent, Naringin, has been selected as analytical and biological marker of the juice. Juice has been loaded onto maltodextrin matrix by spray-drying. The produced maltodextrin/juice powder (BMP) showed neither significant change in total polyphenols content nor decrease in antioxidant properties with respect to fresh juice. Moreover, BMP displayed high in vitro dissolution rate of the bioactive constituents in water and in simulated biological fluids. BMP appears as promising functional raw material for food, nutraceutical and pharmaceutical products. With this aim, a formulation study to develop tablets (BMT) for oral administration has been also performed. The produced solid oral dosage form preserved high polyphenols content, showed complete disaggregation in few minutes and satisfying dissolution rate of the bioactive constituents in simulated biological fluids.