Floating Ricobendazole Delivery Systems: A 3D Printing Method by Co-Extrusion of Sodium Alginate and Calcium Chloride.

At present, the use of benzimidazole drugs in veterinary medicine is strongly limited by both pharmacokinetics and formulative issues. In this research, the possibility of applying an innovative semi-solid extrusion 3D printing process in a co-axial configuration was speculated, with the aim of producing a new gastro-retentive dosage form loaded with ricobendazole. To obtain the drug delivery system (DDS), the ionotropic gelation of alginate in combination with a divalent cation during the extrusion was exploited. Two feeds were optimized in accordance with the printing requirements and the drug chemical properties: the crosslinking ink, i.e., a water ethanol mixture containing CaCl2 at two different ratios 0.05 M and 0.1 M, hydroxyethyl cellulose 2% w/v, Tween 85 0.1% v/v and Ricobendazole 5% w/v; and alginate ink, i.e., a sodium alginate solution at 6% w/v. The characterization of the dried DDS obtained from the extrusion of gels containing different amounts of calcium chloride showed a limited effect on the ink extrudability of the crosslinking agent, which on the contrary strongly influenced the final properties of the DDS, with a difference in the polymeric matrix toughness and resulting effects on floating time and drug release.

Zinc and Calcium Cations Combination in the Production of Floating Alginate Beads as Prednisolone Delivery Systems.

The aim of this research was to verify the application of alginate in combination with Ca2+ and Zn2+ ions to produce a floating and prolonged release system for the oral administration of prednisolone. Hollow and floating gel-beads were designed using prilling/ionotropic gelation as the microencapsulation technique, zinc acetate in the gelling solution as the alginate external crosslinker, and calcium carbonate in the feed as the internal crosslinking agent able to generate gas when in contact with the acidic zinc acetate solution. To achieve this goal, drug/alginate solutions were opportunely combined with different amounts of calcium carbonate. The effect of the addition of calcium carbonate into the feed solution on buoyancy, encapsulation efficiency, morphology, size distribution, as well as in vitro drug release profile of the alginate particles was studied. Moreover, the ability of the floating beads to modulate in vivo the anti-inflammatory response was assayed using the carrageenan-induced acute oedema in rat paw. The proposed strategy allowed obtaining alginate beads with extremely high encapsulation efficiency values (up to 94%) and a very porous inner matrix conferring buoyancy in vitro in simulated gastric fluid up to 5 h. Moreover, in vivo, the best formulation, F4, resulted in the ability to prolong the anti-inflammatory effect up to 15 h compared with raw prednisolone.

Development of Chitosan/Mannitol Microparticles as Delivery System for the Oral Administration of a Spirulina Bioactive Peptide Extract.

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).

Design and Development of Spray-Dried Microsystems to Improve Technological and Functional Properties of Bioactive Compounds from Hazelnut Shells.

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.

Halimium halimifolium: From the Chemical and Functional Characterization to a Nutraceutical Ingredient Design.

Halimium halimifolium (Hh) is a shrub used in Algerian folk medicine to treat gastrointestinal pain. An UHPLC-PDA-ESI/MSn method was developed to identify the metabolic profile of the traditionally used infusion (Hh-A) from the aerial parts. The structures of flavanols were confirmed by NMR analysis after the isolation procedure from a hydrohalcolic extract (Hh-B) that also allowed for the identification of phenolic acids, an aryl butanol glucoside, and different derivatives of quercetin, myricetin, and kaempferol. Tiliroside isomers were the chemical markers of Hh-A and Hh-B (54.33 and 36.00 mg/g, respectively). Hh-A showed a significant scavenging activity both against the radicals 1,1-diphenyl-2-picrylhydrazyl and 2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (EC50 = 10.49 µg/mL and TEAC value = 1.98 mM Trolox/mg infusion) and the lipopolysaccharide-induced reactive oxygen species release in A375 and HeLa cells. Moreover, the antihyperglycemic properties, by inhibiting the α-amylase and α-glucosidase enzymes (IC50 = 0.82 mg/mL and 25.01 µg/mL, respectively), were demonstrated. To upgrade the therapeutic effect, a microencapsulation process is proposed as a strategy to optimize stability, handling, and delivery of bioactive components, avoiding the degradation and loss of the biological efficacy after oral intake. Hh-loaded microparticles were designed using cellulose acetate phthalate as the enteric coating material and spray drying as a production process. The results showed a satisfactory process yield (67.9%), encapsulation efficiency (96.7%), and micrometric characteristics of microparticles (laser-scattering, fluorescent, and scanning electron microscopy). In vitro dissolution studies (USPII-pH change method) showed that Hh-loaded microparticles are able to prevent the release and degradation of the bioactive components in the gastric tract, releasing them into the intestinal environment.

Design of Aerogels, Cryogels and Xerogels of Alginate: Effect of Molecular Weight, Gelation Conditions and Drying Method on Particles' Micromeritics.

Processing and shaping of dried gels are of interest in several fields like alginate aerogel beads used as highly porous and nanostructured particles in biomedical applications. The physicochemical properties of the alginate source, the solvent used in the gelation solution and the gel drying method are key parameters influencing the characteristics of the resulting dried gels. In this work, dried gel beads in the form of xerogels, cryogels or aerogels were prepared from alginates of different molecular weights (120 and 180 kDa) and concentrations (1.25, 1.50, 2.0 and 2.25% (w/v)) using different gelation conditions (aqueous and ethanolic CaCl2 solutions) and drying methods (supercritical drying, freeze-drying and oven drying) to obtain particles with a broad range of physicochemical and textural properties. The stability of physicochemical properties of alginate aerogels under storage conditions of 25 °C and 65% relative humidity (ICH-climatic zone II) during 1 and 3 months was studied. Results showed significant effects of the studied processing parameters on the resulting alginate dried gel properties. Stability studies showed small variations in aerogels weight and specific surface area after 3 months of storage, especially, in the case of aerogels produced with medium molecular weight alginate.

Chestnut (Castanea sativa Miller.) Burs Extracts and Functional Compounds: UHPLC-UV-HRMS Profiling, Antioxidant Activity, and Inhibitory Effects on Phytopathogenic Fungi.

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.

Natural polysaccharides platforms for oral controlled release of ketoprofen lysine salt.

CONTEXT: Ketoprofen lysinate (KL) is one of the most widely used non-steroidal anti-inflammatory drugs in the symptomatic treatment of some chronic inflammatory diseases. Compared to ketoprofen, KL shows better pharmacokinetics and tolerability. However, due to its short half-life of 1-2 h, a multiple dose regimen is required for oral administration. Thus, the present work deals with its encapsulation in a hydrogel-based system by prilling in order to prolong its activity. OBJECTIVE: In this paper, we propose alginate and pectin as carriers and release tailoring agent for the development of hydrogel-based beads for KL retarded and sustained release. MATERIALS AND METHODS: Beads were produced by a Nisco Encapsulator® using alginate or pectin. Operative variables were optimized to produce beads with desired morphology and size. Solid state properties were analyzed by SEM and DSC. Drug release performance was studied by Pharmacopeia pH-change assay to simulate gastrointestinal environment. RESULTS AND DISCUSSION: Prilling technique was successfully used to encapsulate high soluble drugs as KL in polysaccharides-based hydrogels. Pectin proved to be a proper polymer able to encapsulate ketoprofen lysine salt. Formulation (F8) showed good morphological properties and size, high drug content (15.6%) and encapsulation efficiency (93.5%) and promising drug release profiles. Hosting F8 in an acid-resistant capsule (DR®caps) a delivery platform has been developed to control KL release in a delayed (90 min lag time) and prolonged way (270 min complete release). CONCLUSION: The platform may be proposed as potentially useful in the oral administration of NSAIDs in chronic inflammatory diseases affected by circadian rhythm.

Fast determination of underivatized gentamicin C components and impurities by LC-MS using a porous graphitic carbon stationary phase.

Gentamicin C antibiotics are important because they are active against many multidrug-resistant Gram-negative bacilli. Unfortunately, their clinical usefulness is limited by their toxicity. Because of the difficulty involved in separating its different components, the US and European pharmacopeias both specify that the composition of gentamicin C should be determined by liquid chromatography with pulsed electrochemical detection. Here, we assess the usefulness of a porous graphitic carbon (PGC) HPLC column for separating the components of gentamicin C, and report chromatographic conditions that enable its direct characterization by PGC chromatography directly coupled to electrospray mass spectrometry. Native major components of gentamicin and impurities in commercial formulations were retained and separated on the PGC column without any need for derivatization, using mobile phases basified with ammonium hydroxide. When coupled with detection by conventional electrospray ion trap mass spectrometry (ESI-IT-MS), several previously reported impurities were detected easily, including the most polar gentamicin impurity, garamine. When operating in full-scan mode, it was possible to identify and quantitate gentamicin-related compounds using injected samples of only a few picograms. Under the described conditions, all analytes were eluted in less than 10 min and the LC-MS analyses exhibited excellent stability and linearity. The method's effectiveness was evaluated by analyzing commercial gentamicin batches and in-house formulations. When the PGC chromatographic system was coupled to an evaporative light-scattering detector, detection limits of 40-70 ng were achieved for various major gentamicin components. The chromatographic method was applied on a semi-preparative scale to purify the five major components.

Hyaluronate loaded advanced wound dressing in form of in situ forming hydrogel powders: Formulation, characterization, and therapeutic potential.

In this paper, a blend composed of alginate-pectin-chitosan loaded with sodium hyaluronate in the form of an in situ forming dressing was successfully developed for wound repair applications. This complex polymeric blend has been efficiently used to encapsulate hyaluronate, forming an adhesive, flexible, and non-occlusive hydrogel able to uptake to 15 times its weight in wound fluid, and being removed without trauma from the wound site. Calorimetric and FT-IR studies confirmed chemical interactions between hyaluronate and polysaccharides blend, primarily related to the formation of a polyelectrolytic complex between hyaluronate and chitosan. In vivo wound healing assays on murine models highlighted the ability of the loaded hydrogels to significantly accelerate wound healing compared to a hyaluronic-loaded ointment. This was evident through complete wound closure in <10 days, accompanied by fully restored epidermal functionality and no indications of the site of excision or treatment. Therefore, all these results suggest that hyaluronate-loaded powders could be a very promising conformable dressing in several wound healing applications where exudate is present.

The medieval skincare routine according to the formulations of Madgistra Trotula and the Medical School of Salerno and its reflection on cosmetology of the third millennium.

BACKGROUND: Officinal plants, minerals, animal derivatives, and miscellaneous have always been used to treat and improve appearance despite the different aesthetic canons of a specific historical and cultural context. OBJECTIVE: The aim of this work was to make a critical comparison between medieval and modern dermocosmetics analyzing the works of Trotula de Ruggiero, a female doctor of the 11th century teaching and working inside the illustrious "Medical School of Salerno," who devoted particular attention to the promotion of female care, beauty, and well-being. METHODS: We applied the historical-critical method analyzing the Latin text and the nglish translation of the standardized corpus of the main Trotula medieval manuscript De Ornatu Mulierum with a multidisciplinary scientific approach ranging from botany to pharmaceutical chemistry and technology, pharmacology and pathology. RESULTS: We identified the medicinal plants, derivatives of animal origin and minerals used in the recipes of Trotula, highlighting their biological properties in the light of current scientific knowledge. A critical comparison between medieval and modern dermocosmetics is reported also taking into consideration the chemical, pharmaceutical, and technological literature. CONCLUSION: Beyond the obvious changes in the paradigms of cosmetology and the different beauty canons of Middle Age with respect to modern times, our results emphasize the attention of Trotula to female care, beauty and well-being as well as the extraordinary combination of tradition and modernity in her work.

Couroupita guianensis bark decoction: From Amazonian medicine to the UHPLC-HRMS chemical profile and its role in inflammation processes and re-epithelialization.

ETHNOPHARMACOLOGICAL RELEVANCE: In the Amazon rainforest, the shamans of the Mayantuyacu site use the healing virtues of decoctions and teas from different parts of the Couroupita guianensis Aubl. (Lecythidaceae) trees as remedies in Ashaninka medicine. However, composition of the remedy and the underlying mechanism remain unclear. AIM OF THE STUDY: This study was designed to compare the metabolite profile of Couroupita guianensis bark decoction produced by Amazonian shamans with that obtained under standardised laboratory conditions and to investigate biological properties of both decoction and isolated constituents in skin wound healing process and inflammation. MATERIALS AND METHODS: The chemical analyses were carried out by Ultra-High-Performance Liquid Chromatography coupled with UV and High-Resolution Mass Spectrometry detectors (UHPLC-UV-HRMS). 1D and 2D-NMR experiments were performed to identify the main decoction constituents. The decoction and pure compound effect on keratinocyte migration was determined by the in vitro wound healing model; the mechanism of action was elucidated by western blot analysis. RESULTS: UHPLC-UV-HRMS analysis revealed the occurrence of polyphenolic compounds as catechins, ellagitannins and, notably, of unusual sulphated derivatives of ellagic acid isolated for the first time from Couroupita guianensis bark. A new natural sulphated molecule [4-(2″-O-sulphate- ß-D-glucuronopyranosyl) ellagic acid] was identified as the potential active compound responsible for the efficacy of bark decoction stimulating wound healing in human HaCaT keratinocytes. The molecular mechanism involved the induction of pro-migratory pathways mediated by ERK and AKT phosphorylation and the increase of MMP2 expression in HaCaT cells. At the same time, the treatment inhibited inflammation interfering with NFkB activation. CONCLUSION: Beyond identifying a new bioactive compound, the overall results scientifically validate the traditional use of Couroupita guianensis bark decoction as an anti-inflammatory remedy. Moreover, the beneficial effects on keratinocytes suggest promising therapeutic applications in skin diseases.

In Situ Hydrogel Formulation for Advanced Wound Dressing: Influence of Co-Solvents and Functional Excipient on Tailored Alginate-Pectin-Chitosan Blend Gelation Kinetics, Adhesiveness, and Performance.

Chronic skin wounds affect more than 40 million patients worldwide, representing a huge problem for healthcare systems. This study elucidates the optimization of an in situ gelling polymer blend powder for biomedical applications through the use of co-solvents and functional excipients, underlining the possibility of tailoring microparticulate powder properties to generate, in situ, hydrogels with advanced properties that are able to improve wound management and patient well-being. The blend was composed of alginate, pectin, and chitosan (APC). Various co-solvents (ethanol, isopropanol, and acetone), and salt excipients (sodium bicarbonate and ammonium carbonate) were used to modulate the gelation kinetics, rheology, adhesiveness, and water vapor transmission rate of the gels. The use of co-solvents significantly influenced particle size (mean diameter ranging from 2.91 to 5.05 µm), depending on the solvent removal rate. Hydrogels obtained using ethanol were able to absorb over 15 times their weight in simulated wound fluid within just 5 min, whereas when sodium bicarbonate was used, complete gelation was achieved in less than 30 s. Such improvement was related to the internal microporous network typical of the particle matrix obtained with the use of co-solvents, whereas sodium bicarbonate was able to promote the formation of allowed particles. Specific formulations demonstrated an optimal water vapor transmission rate, enhanced viscoelastic properties, gel stiffness, and adhesiveness (7.7 to 9.9 kPa), facilitating an atraumatic removal post-use with minimized risk of unintended removal. Microscopic analysis unveiled that porous inner structures were influencing fluid uptake, gel formation, and transpiration. In summary, this study provided valuable insights for optimizing tailored APC hydrogels as advanced wound dressings for chronic wounds, including vascular ulcers, pressure ulcers, and partial and full-thickness wounds, characterized by a high production of exudate.

3D printed macroporous scaffolds of PCL and inulin-g-P(D,L)LA for bone tissue engineering applications.

Bone repair and tissue-engineering (BTE) approaches require novel biomaterials to produce scaffolds with required structural and biological characteristics and enhanced performances with respect to those currently available. In this study, PCL/INU-PLA hybrid biomaterial was prepared by blending of the aliphatic polyester poly(ε-caprolactone) (PCL) with the amphiphilic graft copolymer Inulin-g-poly(D,L)lactide (INU-PLA) synthetized from biodegradable inulin (INU) and poly(lactic acid) (PLA). The hybrid material was suitable to be processed using fused filament fabrication 3D printing (FFF-3DP) technique rendering macroporous scaffolds. PCL and INU-PLA were firstly blended as thin films through solvent-casting method, and then extruded by hot melt extrusion (HME) in form of filaments processable by FFF-3DP. The physicochemical characterization of the hybrid new material showed high homogeneity, improved surface wettability/hydrophilicity as compared to PCL alone, and right thermal properties for FFF process. The 3D printed scaffolds exhibited dimensional and structural parameters very close to those of the digital model, and mechanical performances compatible with the human trabecular bone. In addition, in comparison to PCL, hybrid scaffolds showed an enhancement of surface properties, swelling ability, and in vitro biodegradation rate. In vitro biocompatibility screening through hemolysis assay, LDH cytotoxicity test on human fibroblasts, CCK-8 cell viability, and osteogenic activity (ALP evaluation) assays on human mesenchymal stem cells showed favorable results.

Post-COVID Syndrome: The Research Progress in the Treatment of Pulmonary sequelae after COVID-19 Infection.

Post-COVID syndrome or long COVID is defined as the persistence of symptoms after confirmed SARS-CoV-2 infection, the pathogen responsible for coronavirus disease. The content herein presented reviews the reported long-term consequences and aftereffects of COVID-19 infection and the potential strategies to adopt for their management. Recent studies have shown that severe forms of COVID-19 can progress into acute respiratory distress syndrome (ARDS), a predisposing factor of pulmonary fibrosis that can irreversibly compromise respiratory function. Considering that the most serious complications are observed in the airways, the inhalation delivery of drugs directly to the lungs should be preferred, since it allows to lower the dose and systemic side effects. Although further studies are needed to optimize these techniques, recent studies have also shown the importance of in vitro models to recreate the SARS-CoV-2 infection and study its sequelae. The information reported suggests the necessity to develop new inhalation therapies in order to improve the quality of life of patients who suffer from this condition.

Advanced printable hydrogels from pre-crosslinked alginate as a new tool in semi solid extrusion 3D printing process.

With the aim to overcome alginate shape fidelity issue during the semisolid extrusion 3D printing and matrix collapsing after drying, we speculated that a pre-crosslinking step of the alginate ink-gel with low amount of Ca+2 could improve the hydrogel performance. To verify this, the influence of pre-crosslinker concentration (10-25 mM) on the ink gel rheological properties were studied and flow behaviour and viscoelastic properties were determined. The developed ink gels were fully characterised by DSC and Magnetic Resonance Imaging (MRI). Moreover, extrudability and the shape retention of extruded forms after printing and after drying were studied. The rheological and MRI data, combined with the morphological analysis of printed forms allowed us to identify the relationship between printability, shape retention and shear thinning behaviour of gels, showing good extrudability for all the pre-crosslinked gels with a calcium concentration between 0.15 and 0.25, corresponding to both egg-box dimers and multimers interactions.

Coaxial semi-solid extrusion and ionotropic alginate gelation: A successful duo for personalized floating formulations via 3D printing.

With the aim to fulfill the patient-centered approach of precision medicine, in this research, innovative floating drug delivery systems have been developed through the use of alginate matrix and fully characterized. Particularly, to exploit the ionotropic gelation of alginate, a customized coaxial extruder for Semi-solid Extrusion 3D printing, has been used for the simultaneous dispensing of ink gel (sodium alginate 6% w/v) and crosslinking gel (hydroxyethyl cellulose 3 %w/v, calcium chloride 0.1M and Tween 85 0.1% v/v). The latter also loaded with Propranolol Hydrochloride 12.5%w/v. A novel single-step process gelation for the extemporaneous gelation of loaded oral systems has been therefore developed. These technologically advanced formulations showed high printing reproducibility in manufacturing different models (mass of a single layer 535.41 ± 40.00 mg with an average drug loading efficiency of 85% w/w) and similar release behavior, paving the way for their customization in terms of drug dosages via this pioneering process.

A Novel Three-Polysaccharide Blend In Situ Gelling Powder for Wound Healing Applications.

In this paper, alginate/pectin and alginate/pectin/chitosan blend particles, in the form of an in situ forming hydrogel, intended for wound repair applications, have been successfully developed. Particles have been used to encapsulate doxycycline in order to control the delivery of the drug, enhance its antimicrobial properties, and the ability to inhibit host matrix metalloproteinases. The presence of chitosan in the particles strongly influenced their size, morphology, and fluid uptake properties, as well as drug encapsulation efficiency and release, due to both chemical interactions between the polymers in the blend and interactions with the drug demonstrated by FTIR studies. In vitro antimicrobial studies highlighted an increase in antibacterial activity related to the chitosan amount in the powders. Moreover, in situ gelling powders are able to induce a higher release of IL-8 from the human keratinocytes that could stimulate the wound healing process in difficult-healing. Interestingly, doxycycline-loaded particles are able to increase drug activity against MMPs, with good activity against MMP-9 even at 0.5 µg/mL over 72 h. Such results suggest that such powders rich in chitosan could be a promising dressing for exudating wounds.

Pectin and Zinc Alginate: The Right Inner/Outer Polymer Combination for Core-Shell Drug Delivery Systems.

Core-shell beads loaded with betamethasone were developed using co-axial prilling as production technique and pectin plus alginate as polymeric carriers. During this study, many operative conditions were intensively investigated to find the best ones necessary to produce uniform core-shell particle systems in a reproducible way. Particularly, feed solutions' composition, polymers mass ratios and the effect of the main process parameters on particles production, micromeritics, inner structure, drug loading and drug-release/swelling profiles in simulated biological fluids were studied. The optimized core-shell formulation F5 produced with a pectin core concentration of 4.0% w/v and an alginate shell concentration of 2.0% w/v (2:1 core:shell ratio) acted as a sustained drug delivery system. It was able to reduce the early release of the drug in the upper part of the gastro-intestinal tract for the presence of the zinc-alginate gastro-resistant outer layer and to specifically deliver it in the colon, thanks to the selectivity of amidated low methoxy pectin core for this district. Therefore, these particles may be proposed as colon targeted drug delivery systems useful for inflammatory bowel disease (IBD) therapy.

Study on Ajuga reptans Extract: A Natural Antioxidant in Microencapsulated Powder Form as an Active Ingredient for Nutraceutical or Pharmaceutical Purposes.

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.