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Gymnema inodorum (GI) is a leafy green vegetable found in the northern region of Thailand. A GI leaf extract has been developed as a dietary supplement for metabolic diabetic control. However, the active compounds in the GI leaf extract are relatively nonpolar. This study aimed to develop phytosome formulations of the GI extract to improve the efficiencies of their phytonutrients in terms of anti-inflammatory and anti-insulin-resistant activities in macrophages and adipocytes, respectively. Our results showed that the phytosomes assisted the GI extract’s dispersion in an aqueous solution. The GI phytocompounds were assembled into a phospholipid bilayer membrane as spherical nanoparticles about 160–180 nm in diameter. The structure of the phytosomes allowed phenolic acids, flavonoids and triterpene derivatives to be embedded in the phospholipid membrane. The existence of GI phytochemicals in phytosomes significantly changed the particle’s surface charge from neutral to negative within the range of −35 mV to −45 mV. The phytosome delivery system significantly exhibited the anti-inflammatory activity of the GI extract, indicated by the lower production of nitric oxide from inflamed macrophages compared to the non-encapsulated extract. However, the phospholipid component of phytosomes slightly interfered with the anti-insulin-resistant effects of the GI extract by decreasing the glucose uptake activity and increasing the lipid degradation of adipocytes. Altogether, the nano-phytosome is a potent carrier for transporting GI phytochemicals to prevent an early stage of T2DM.

Kersen (Muntingia calabura L.) contains flavonoids that have the potential as antioxidants. However, its hydrophilic characteristics cause poor penetration so that its bioavailability is low. Research had been carried out on the preparation of ethanol extract of cherry leaves in ethosomal vesicle carriers. This study aimed to obtain the optimal phytosome suspension formula. Methods: Sample extraction was carried out by maceration method using ethanol as a solvent and was delipidated was by liquid-liquid method with n-hexane. The characterization of the extract included organoleptic, water-soluble extract content, ethanol soluble extract content, water content, ash content, acid insoluble ash content, and residual solvent. flavonoid contents were carried out by the TLC method and antioxidant activity was determined using DPPH method. Phytosome preparation was prepared by solvent evaporation and thin film hidration with ratio of extract and phosphatidylcholine 1:1 with concentration of 0.5% (A); 1% (B); and 1.5% (C). The characterization included observing morphology of vesicles using optical microscope, determining the size distribution of vesicles using PSA, and calculating the sorption efficiency using a spectrophotometer at max 281 nm. Results: The characteristics of extract were dark green; thick; distinctive aroma; ethanol soluble content were 70.91%; water soluble content were 32.5%; water content were 1.19%; ash content were 1.25%; acid insoluble ash content were 0.49%; and the remaining solvent was 0. The identification of flavonoids showed positive results. The extract has flavonoids and strong antioxidant activity with 62.71 g/mL for IC50. The shape is single layer large vesicle (LUV), diameter was 445.7 nm (A); 420.7 nm (B); and 419.6 nm (C). Vesicle entrapment efficiency was 5.83% (A); 47.575% (B); and 68.81% (C). It can be concluded that the optimal phytosome suspension formula is C with 1.5% phosphatidylcholine and 1.5% of extract.

Background: Quercetin, a natural polyphenol with demonstrated broad-spectrum antiviral, anti-inflammatory, and antioxidant properties, has been proposed as an adjuvant for early-stage coronavirus disease 2019 (COVID-19) infection.Objective: To explore the possible therapeutic effect of quercetin in outpatients with early-stage mild to moderate symptoms of COVID-19.Methods: This was an open-label randomized controlled clinical trial conducted at the department of medicine, King Edward Medical University, Lahore, PK. Patients were randomized to receive either standard of care (SC) plus an oral quercetin supplement (500 mg Quercetin Phytosome®, 1st week, TDS: 2nd week, BDS) (n = 50, quercetin group) or SC alone (n = 50, control group).Results: After one week of treatment, patients in the quercetin group showed a speedy recovery from COVID-19 as compared to the control group, i.e., 34 patients (vs. 12 in the control group) tested negative for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) (p = 0.0004), and 26 patients (vs. 12 in the control group) had their COVID-19-associated acute symptoms resolved (p = 0.0051). Patients in the quercetin group also showed a significant fall in the serum lactate dehydrogenase (LDH) mean values i.e., from 406.56 ± 183.92 to 257.74 ± 110.73 U/L, p = 0.0001. Quercetin was well-tolerated by all the 50 patients, and no side effects were reported.Conclusion: Our results, suggest the possible therapeutic role of quercetin in early-stage COVID-19, including speedy clearance of SARS-CoV-2, early resolution of the acute symptoms and modulation of the host’s hyperinflammatory response.Clinical Trial Registration:clinicaltrials.gov, identifier NCT04861298

Menopause is characterized by weight gain and increased visceral fat, which acts as an endocrine organ secreting proinflammatory adipocytokines, with consequent increased risk of metabolic disorders. The aim of this double-blind, placebo-controlled randomized trial was to evaluate the effects of a 60-day dietary supplementation using Camellia sinensis leaf extract on adipose tissue dysfunction in overweight or class I obese post-menopausal, sedentary women. Primary endpoints were the respiratory quotient (RQ), the percentage of carbohydrates (%CHO), the percentage of fat oxidation (%FAT), and the resting energy expenditure (REE) measured by indirect calorimetry. Secondary endpoints included body composition, by dual x-ray absorptiometry (DXA), glucose profile, lipid profile, inflammatory state, liver and kidney function, hormonal status regarding satiety, and status of catecholamines. Twenty-eight women were randomized into two groups: 14 (BMI 31.1 ± 3.5) were supplemented and 14 (BMI 31.9 ± 2.2) received placebo. In regards to the between-group differences over time (β), a statistically significant difference between the supplemented and placebo group was observed for: RQ (β = −0.04, p = 0.009), % fat oxidation (β = 11.04, p = 0.0006), insulin (β = −1.74, p = 0.009), HOMA (β = −0.31, p = 0.02), waist circumference (β = −1.07, p = 0.007), REE (β = 83.21, p = 0.009), and CRP (β = −0.14, p = 0.02). These results demonstrate that a 60-day green tea extract supplementation counteracts the dysfunction of adipose tissue in overweight post-menopausal and class I obese women.

Mahmood Barani,1 Enrico Sangiovanni,2 Marco Angarano,2 Mohammad Amin Rajizadeh,3 Mehrnaz Mehrabani,4 Stefano Piazza,2 Hosahalli Veerabhadrappa Gangadharappa,5 Abbas Pardakhty,6 Mehrzad Mehrbani,7 Mario Dell’Agli,2 Mohammad Hadi Nematollahi8 1Medical Mycology and Bacteriology Research Center, Kerman University of Medical Sciences, Kerman, 76169-13555, Iran; 2Department of Pharmacological and Biomolecular Sciences, Università degli Studi di Milano, Milan, 20133, Italy; 3Student Research Committee, Kerman University of Medical Sciences, Kerman, Iran; 4Physiology Research Center, Kerman University of Medical Sciences, Kerman, Iran; 5Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Mysuru, India; 6Pharmaceutics Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran; 7Department of Traditional Medicine, Faculty of Traditional Medicine, Kerman University of Medical Sciences, Kerman, Iran; 8Herbal and Traditional Medicines Research Center, Kerman University of Medical Sciences, Kerman, IranCorrespondence: Mario Dell’AgliDepartment of Pharmacological and Biomolecular Sciences, Università degli Studi di Milano, Via Balzaretti 9, Milan, 20133, ItalyEmail mario.dellagli@unimi.itMohammad Hadi NematollahiDepartment of Clinical Biochemistry, Kerman University of Medical Sciences, Kerman, IranEmail mh.nematollahi@yahoo.comAbstract: Nowadays, medicinal herbs and their phytochemicals have emerged as a great therapeutic option for many disorders. However, poor bioavailability and selectivity might limit their clinical application. Therefore, bioavailability is considered a notable challenge to improve bio-efficacy in transporting dietary phytochemicals. Different methods have been proposed for generating effective carrier systems to enhance the bioavailability of phytochemicals. Among them, nano-vesicles have been introduced as promising candidates for the delivery of insoluble phytochemicals. Due to the easy preparation of the bilayer vesicles and their adaptability, they have been widely used and approved by the scientific literature. The first part of the review is focused on introducing phytosome technology as well as its applications, with emphasis on principles of formulations and characterization. The second part provides a wide overview of biological activities of commercial and non-commercial phytosomes, divided by systems and related pathologies. These results confirm the greater effectiveness of phytosomes, both in terms of biological activity or reduced dosage, highlighting curcumin and silymarin as the most formulated compounds. Finally, we describe the promising clinical and experimental findings regarding the applications of phytosomes. The conclusion of this study encourages the researchers to transfer their knowledge from laboratories to market, for a further development of these products.Keywords: phytochemical, nanomedicine, phytosome, delivery, vesicle, disease

Idiopathic pulmonary fibrosis is a fatal interstitial disease characterized by fibroblast proliferation and differentiation and abnormal accumulation of extracellular matrix, with high mortality and an increasing annual incidence. Since few drugs are available for the treatment of pulmonary fibrosis, there is an urgent need for high-efficiency therapeutic drugs and treatment methods to reduce the mortality associated with pulmonary fibrosis. The interstitium, a highly efficient transportation system that pervades the body, plays an important role in the occurrence and development of disease, and can be used as a new route for disease diagnosis and treatment. In this study, we evaluated the administration of hydroxysafflor yellow A phytosomes via intervaginal space injection (ISI) as an anti-pulmonary fibrosis treatment. Our results show that this therapeutic strategy blocked the activation of p38 protein in the MAPK-p38 signaling pathway and inhibited the expression of Smad3 protein in the TGF-β/Smad signaling pathway, thereby reducing secretion of related inflammatory factors, deposition of collagen in the lungs of mice, and destruction of the alveolar structure. Use of ISI in the treatment of pulmonary fibrosis provides a potential novel therapeutic modality for the disease.

In the recent years, herbal medicines have gained worldwide attention of peoples and researchers due to their esthetic value, more patient’s compliance and prominent therapeutic effects. Novel drug delivery systems for delivery of herbal drugs possesses several advantages over conventional formulations. It includes enhancement of solubility, bioavailability, and protection from toxicity, etc. The herbal drugs can be used in a more upright course with enhanced efficacy by incorporating them into suitable dosage forms. This can be achieved by designing novel drug delivery systems for such drugs. Such systems are polymeric nanoparticles, nanocapsules, phytosomes, animations, microsphere, etc. The present article highlights the current condition of the development of novel herbal formulations and summarizes their type of active components, biological activity, and applications of novel formulations.

The objective of the present research was to formulate diammonium glycyrrhizinate (DG) into phytosomes (DG-P) to induce nasal immune responses and enhance absorption. Plackett- Burman design was used for process optimization, incorporating specific formulation and process variables to obtain the optimal parameters. Fourier transform infrared spectroscopy (FTIR), X-ray power diffraction (P-XRD), and transmission electron microscopy (TEM) were used for characterization. The adjuvant activity of the DG-P was evaluated by using bone marrow dendritic cells. In vitro nasal mucosal permeation and in situ nasal perfusion were also investigated to evaluate nasal absorption. The DG phytosomes were in the size range of 20~30 nm and zeta-potential range of −30~−40 mV. DG-P demonstrated 4.2-fold increased solubility in n-octanol. Coculturing bone marrow dendritic cells with DG-P led to enhanced dendritic cell maturation. Apparent permeability coefficient of the phytosomal formulation was almost four times higher than that of free DG determined by ex vivo permeation studies on excised porcine mucosa. In situ nasal perfusion studies in rats demonstrated that the nasal absorption of DG-P was significantly higher than that of free DG. Conclusively, the results confirmed that DG-P have potential for use as an adjuvant for nasal vaccine.

Background: The treatment of symptomatic uncomplicated colonic diverticular disease (SUDD) is still under debate, and new data show a pathogenic role of dysbiosis and low-grade inflammation in intestinal mucosa. Recent research has highlighted the anti-inflammatory effects of botanical extracts such as Curcuma longa L. and Boswellia serrata Roxb. ex Colebr. The aim of this work is to investigate the potential role of a new delivery formulation of the association of curcumin and boswellia phytosome extracts (CBP) in SUDD. Methods: In a 30-day one-group longitudinal explanatory study, patients (men and women) were treated with an innovative association of CBP standardized extracts, 500 mg bid. Results: Treatment of SUDD with the association of CBP was followed by a significant decrease in abdominal pain (p

Acute diarrhea is a frequent problem worldwide, mostly due to gastrointestinal infections or food poisoning. Boswellia serrata could be active in the treatment of acute diarrhea due to its anti-inflammatory, antispasmodic, and antimicrobial activity. In this randomized, double-blind, placebo-controlled clinical study, 49 adults with acute diarrhea were randomly allocated to receive 250 mg of a lecithin-based delivery form of Boswellia serrata (CASP) or placebo for 5 days. The time it took to become healthy with stoppage of diarrhea (primary end point) was significantly shorter in the intervention group (3.08 vs. 4.44 days: p-value < 0.0001). The probability of subjects treated with CASP to recover sooner was equal to 80.2%. A significantly lower number of stools was observed in the CASP group over time (β = −0.17, p-value < 0.0001). A significant difference was observed between the two groups for abdominal pain, nausea, and GAE (global assessment of efficacy). In conclusion, the lecithin-based delivery form of Boswellia serrata extract could be a useful addition to the treatment of acute diarrhea in adults. CASP is safe and reduces the time it takes to become healthy, the frequency of stools, the abdominal pain and nausea of subjects with acute diarrhea. Further studies are needed to confirm these promising results.

Pentaclethra macrophylla, a medicinal plant widely used for ulcer treatment in Nigeria by herbal practitioners, is limited by poor lipid solubility, resulting in poor absorption and bioavailability. Phytosomes, a novel dosage form that are better absorbed and produce better results than conventional herbal extracts, could be employed to enhance its antiulcer activity. The objective of this study was to formulate Pentaclethra macrophylla stem-bark extract as phytosomes by forming complexes with phospholipid and compare the antiulcer activity with omeprazole, a standard anti-ulcer drug. Phytosomal formulations of ethanol extract of Pentaclethra macrophylla stem-bark and Phospholipon® 90G (P90G) (extract:P90G ratios of 1:1, 1:3, 1:5) were prepared following established method. Their physicochemical properties, in vitro drug release in simulated intestinal fluid (SIF, pH=7.4) and simulated gastric fluid (SGF, pH=1.2) and anti-ulcer properties on aspirin-induced ulcer using Wistar rats were determined and compared with omeprazole. Phytosomes with spherical smooth particles with size range 0.106-0.217 µm and good encapsulation efficiencies (range = 67.61-72.8%) were obtained. Drug release increased with time irrespective of phospholipid concentration or dissolution medium. The extract possessed antiulcer activity (23.33%) which was increased to 33.33, 43.33 and 56.67% by formulating it as phytosomal formulations containing extract:P90G ratios of 1:1, 1:3, 1:5, respectively. However, omeprazole and its formulations gave significantly (p

Designing strategies for an effective transformation of food waste into high-value products is a priority to address environmental sustainability concerns. Coffee silverskin is the major by-product of the coffee roasting industry, being rich in compounds with health benefits. Such composition gives it the potential to be transformed into high-value products. In this study, coffee silverskin extracts were enriched, regarding caffeine and chlorogenic acid contents, by adsorbent column chromatography. The compounds content increased 3.08- and 2.75-fold, respectively, compared to the original extract. The enriched fractions were loaded into nano-phytosomes or cholesterol-incorporated nano-phytosomes (first coating layers) to improve the physiochemical properties and permeation rate. These nano-lipid carriers were also subjected to a secondary coating with different natural polymers to improve protection and stability against degradation. In parallel, and for comparison, different natural polymers were also used as first coating layers. The produced particles were evaluated regarding product yield, encapsulation efficiency, loading capacity, particle size, surface charge, and in vitro release simulating gastrointestinal conditions. All samples exhibited anionic surface charge. FTIR and molecular docking confirmed interactions between the phytoconstituents and lipid bilayers. The best docking score was observed for 5-caffeoylquinic acid (chlorogenic acid) exhibiting a stronger hydrogen binding to the lipid bilayer. Among several kinetic models tested, the particle release mechanism fitted well with the First-order, Korsmeyer–Peppas, and Higuchi models. Moreover, most of the formulated particles followed the diffusion-Fick law and anomalous transport.

Gunnera tinctoria, an underexplored invasive plant found in Azores, Portugal, was studied regarding its nutritional, antioxidant, and antitumoral properties. Higher antioxidant activity was found in baby leaves, followed by adult leaves and inflorescences. A phenolic fraction of the plant was enriched using adsorbent resin column chromatography (DiaionTM HP20LX, and Relite EXA90). Antitumoral effects were observed with the enriched fractions in breast (MCF-7) and pancreatic (AsPC-1) cancer cell lines, being more pronounced in the latter. To improve protection and membrane absorption rates of phenolic compounds, nano-phytosomes and cholesterol-conjugated phytosomes coated with natural polymers were loaded with the enriched fraction. The particles were characterized, and their physiochemical properties were evaluated and compared. All samples presented anionic charge and nanometer size in relation to the inner layer and micrometer size regarding the external layers. In addition, the molecular arrangement of phenolics within both types of phytosomes were studied for the first time by molecular docking. Polarity and molecular size were key factors on the molecular arrangement of the lipid bilayer. In conclusion, G. tinctoria showed to be an interesting source of nutrients and phenolic compounds with anti-tumoral potential. Moreover, phytosome loading with these compounds can increase their stability and bioavailability having in view future applications.

Gunnera tinctoria, an underexplored invasive plant found in Azores, Portugal, was studied regarding its nutritional, antioxidant, and antitumoral properties. Higher antioxidant activity was found in baby leaves, followed by adult leaves and inflorescences. A phenolic fraction of the plant was enriched using adsorbent resin column chromatography (DiaionTM HP20LX, and Relite EXA90). Antitumoral effects were observed with the enriched fractions in breast (MCF-7) and pancreatic (AsPC-1) cancer cell lines, being more pronounced in the latter. To improve protection and membrane absorption rates of phenolic compounds, nano-phytosomes and cholesterol-conjugated phytosomes coated with natural polymers were loaded with the enriched fraction. The particles were characterized, and their physiochemical properties were evaluated and compared. All samples presented anionic charge and nanometer size in relation to the inner layer and micrometer size regarding the external layers. In addition, the molecular arrangement of phenolics within both types of phytosomes were studied for the first time by molecular docking. Polarity and molecular size were key factors on the molecular arrangement of the lipid bilayer. In conclusion, G. tinctoria showed to be an interesting source of nutrients and phenolic compounds with anti-tumoral potential. Moreover, phytosome loading with these compounds can increase their stability and bioavailability having in view future applications.

Nowadays, medicinal herbs and their phytochemicals have emerged as a great therapeutic option for many disorders. However, poor bioavailability and selectivity might limit their clinical application. Therefore, bioavailability is considered a notable challenge to improve bio-efficacy in transporting dietary phytochemicals. Different methods have been proposed for generating effective carrier systems to enhance the bioavailability of phytochemicals. Among them, nano-vesicles have been introduced as promising candidates for the delivery of insoluble phytochemicals. Due to the easy preparation of the bilayer vesicles and their adaptability, they have been widely used and approved by the scientific literature. The first part of the review is focused on introducing phytosome technology as well as its applications, with emphasis on principles of formulations and characterization. The second part provides a wide overview of biological activities of commercial and non-commercial phytosomes, divided by systems and related pathologies. These results confirm the greater effectiveness of phytosomes, both in terms of biological activity or reduced dosage, highlighting curcumin and silymarin as the most formulated compounds. Finally, we describe the promising clinical and experimental findings regarding the applications of phytosomes. The conclusion of this study encourages the researchers to transfer their knowledge from laboratories to market, for a further development of these products., Graphical Abstract

Polycystic Ovary Syndrome (PCOS) is the most frequent endocrine disease in females of reproductive age and is characterized by multifactorial unhealthy conditions related to hormonal unbalance and also to dysmetabolism and inflammation. Recently, increasing evidence has shown that natural plant-based products may play a role in PCOS management. The aim of this one-group pretest–post-test explanatory study was to evaluate, in normal–overweight PCOS women with normal menses, the effectiveness of berberine on: Insulin resistance (IR) by Homeostasis Model Assessment (HOMA), Inflammation by C-Reactive Protein (CRP), Tumor Necrosis Factor α (TNF-α), Lipid metabolism, Sex hormone profile and symptoms correlated to hyperandrogenism, such as acne, by Global Acne Grading System (GAGS) and Cardiff Acne Disability Index (CADI), Body composition by DXA. Finally, adverse effects were assessed by liver and kidney functions and creatine phosphokinase (CPK). All these parameters were collected at baseline and 60 days after supplementation with a new bioavailable and safe berberine formulation. Twelve females (aged 26.6 ± 4.9, BMI 25.3 ± 3.6) were supplied for 60 days with two tablets/day (550 mg/table) of the bioavailable berberine. Results showed a statistically significant decrease in HOMA, CRP, TNF-α, Triglycerides, testosterone, Body Mass Index (BMI), Visceral Adipose Tissue (VAT), fat mass, GAGS and CADI scores, and a statistically significant increase in sex hormone-binding globulin (SHBG). Liver and kidney functions and CPK are not statistically significantly different. Therefore, berberine can represent a safe novel dietary supplement, helpful in treatment strategy for PCOS.

Coenzyme Q10 (CoQ10) is a lipid-soluble molecule with a dual role: it transfers electrons in the mitochondrial transport chain by promoting the transmembrane potential exploited by the ATPase to synthesize ATP and, in its reduced form, is a membrane antioxidant. Since the high CoQ10 hydrophobicity hinders its bioavailability, several formulations have been developed to facilitate its cellular uptake. In this work, we studied the bioenergetic and antioxidant effects in I407 and H9c2 cells of a CoQ10 phytosome formulation (UBIQSOME®, UBQ). We investigated the cellular and mitochondrial content of CoQ10 and its redox state after incubation with UBQ. We studied different bioenergetic parameters, such as oxygen consumption, ATP content and mitochondrial potential. Moreover, we evaluated the effects of CoQ10 incubation on oxidative stress, membrane lipid peroxidation and ferroptosis and highlighted the connection between the intracellular concentration of CoQ10 and its antioxidant potency. Finally, we focused on the cellular mechanism that regulates UBQ internalization. We showed that the cell lines used in this work share the same uptake mechanism for UBQ, although the intestinal cell line was less efficient. Given the limitations of an in vitro model, the latter result supports that intestinal absorption is a critical step for the oral administration of Coenzyme Q10 formulations.

Although a variety of beneficial health effects of natural flavonoids, including chrysin, has been suggested, poor solubility and bioavailability limit their practical use. As a promising delivery system, chrysin-loaded phytosomes (CPs) were prepared using egg phospholipid (EPL) at a 1:3 molar ratio and its antidiabetic effects were assessed in db/db diabetic mice. Male C57BLKS/J-db/db mice were fed a normal diet (control), chrysin diet (100 mg chrysin/kg), CP diet (100 mg chrysin equivalent/kg), metformin diet (200 mg/kg) or EPL diet (vehicle, the same amount of EPL used for CP preparation) for 9 weeks. Administration of CP significantly decreased fasting blood glucose and insulin levels in db/db mice compared with the control. An oral glucose tolerance test and homeostatic model assessment for insulin resistance were significantly improved in the CP group (p &lt, 0.05). CP treatment suppressed gluconeogenesis via downregulation of phosphoenolpyruvate carboxykinase while it promoted glucose uptake in the skeletal muscle and liver of db/db mice (p &lt, 0.05). The CP-mediated improved glucose utilization in the muscle was confirmed by upregulation of glucose transporter type 4, hexokinase2 and peroxisome proliferator-activated receptor &gamma, during treatment (p &lt, 0.05). The CP-induced promotion of GLUT4 plasma translocation was confirmed in the skeletal muscle of db/db mice (p &lt, 0.05). Based on the results, CP showed greater antidiabetic performance compared to the control by ameliorating insulin resistance in db/db mice and phytosome can be used as an effective antidiabetic agent.

The term “Phyto” means plant and “some” means cell It is also mentioned as herbosomes this is a new patented technology, where standardized plant extracts or water soluble phytoconstituents are complexed with phospholipids to produce lipid compatible molecular complexes, there by greatly increasing absorption and bioavailability. The recent development and conducted works of various researchers have been studied thoroughly to establish the transdermal route as a potential way to deliver phytoconstituents. Plant derived products or plant extracts are increasingly receiving attention as dietary supplements for the homeostatic management of inflammation, toxicities, cancers, weight loss and other chronic or acute degenerative disorders. But these products frequently face stability and bioavailability problems. Plant products after their isolation become prone to instability and are potentially unfit to cross the bio membrane as such. The phytosome technique reduces these tasks to reasonable extents. The phytosome or Herbosome technique increases the hydrophilicity of highly lipophilic drug there by making it suitable for drug delivery and increases the lipophilicity of hydrophilic phytoconstituents adequately to cross biological membrane. The topical application of phytosomes for cosmetic purpose has already been proven. This review also contains a comparative account of liposomes and phytosomes along with recent advancements in the field of phytosome technology with a special concern to transdermal drug delivery. The poor oral bioavailability of polyphenolic compound can be enhanced through the incorporation of them into phospholipid based self-assembled delivery system, i.e. popularly known as phytosome. There are number of products available in the market that contains phytosomal drug delivery system such asGinkgo biloba,Silybum marianum, andCamellia sinensis.&nbsp

Background The treatment of symptomatic uncomplicated colonic diverticular disease (SUDD) is still under debate, and new data show a pathogenic role of dysbiosis and low-grade inflammation in intestinal mucosa. Recent research has highlighted the anti-inflammatory effects of botanical extracts such as Curcuma longa L. and Boswellia serrata Roxb. ex Colebr. The aim of this work is to investigate the potential role of a new delivery formulation of the association of curcumin and boswellia phytosome extracts (CBP) in SUDD. Methods In a 30-day one-group longitudinal explanatory study, patients (men and women) were treated with an innovative association of CBP standardized extracts, 500 mg bid. Results Treatment of SUDD with the association of CBP was followed by a significant decrease in abdominal pain (p

Quercetin is one of the main dietary flavonols, but its beneficial properties in disease prevention may be limited due to its scarce bioavailability. For this purpose, delivery systems have been designed to enhance both stability and bioavailability of bioactive compounds. This study aimed at investigating the human microbial metabolism of quercetin derived from unformulated and phytosome-formulated quercetin through an in vitro model. Both ingredients were firstly characterized for their profile in native (poly)phenols, and then fermented with human fecal microbiota for 24 h. Quantification of microbial metabolites was performed by ultra-high performance liquid chromatography coupled to mass spectrometry (uHPLC-MSn) analyses. Native quercetin, the main compound in both products, appeared less prone to microbial degradation in the phytosome-formulated version compared to the unformulated one during fecal incubation. Quercetin of both products was bioaccessible to colonic microbiota, resulting in the production of phenylpropanoic acid, phenylacetic acid and benzoic acid derivatives. The extent of the microbial metabolism of quercetin was higher in the unformulated ingredient, in a time-dependent manner. This study opened new perspectives to investigate the role of delivery systems on influencing the microbial metabolism of flavonols in the colonic environment, a pivotal step in the presumed bioactivity associated to their intake.

Turmeric (Curcuma longa L.) is the only edible plant recognized as a dietary source of curcuminoids, among which curcumin, demethoxycurcumin (DMC) and bis-demethoxycurcumin (Bis-DMC) are the most representative ones. Curcumin shows a very low systemic bioavailability and for this reason, several technologies have been adopted to improve it. These technologies generally improve curcuminoid absorption in the small intestine, however, no data are available about the effect of curcuminoid formulation on colonic biotransformation. The present study aims at investigating the human colonic metabolism of curcuminoids, prepared with two different technologies, using an in vitro model. Unformulated curcuminoid and lecithin-curcuminoid botanical extracts were fermented using an in vitro fecal model and colonic catabolites were identified and quantified by uHPLC-MSn. Native compounds, mainly curcumin, DMC and bis-DMC, were metabolized by colonic microbiota within the 24-h incubation. The degradation of curcuminoids led to the formation of specific curcuminoid metabolites, among which higher concentrations of bis(demethyl)-tetrahydrocurcumin and bis(demethyl)-hexahydrocurcumin were found after lecithin-extract fermentation compared to the concentration detected after unformulated extract. In conclusion, both curcumin-based botanical extracts can be considered important sources of curcuminoids, although the lecithin-formulated extract led to a higher production of curcuminoid catabolites. Moreover, a new curcuminoid catabolite, namely bis(demethyl)-hexahydrocurcumin, has been putatively identified, opening new perspectives in the investigation of curcuminoid bioavailability and their potential metabolite bioactivity.

Lipid-based nanocarriers are attractive materials for food and pharmaceutical industries. In particular, phytosomes are platforms to target bioactive phenolics for central nervous system and to modulate pathophysiological processes underlying major chronic disorders. HPLC-DAD profiling of pennyroyal (Mentha pulegium L.) aqueous extract led to the determination of fifteen phenolic compounds (84.00 ± 4.28 mg/g lyophilized extract), of which rosmarinic acid was the major representative. In cell-free assays, the extract displayed a strong inhibitory effect against monoamine oxidase-A (hMAO-A) (IC50 = 20.11 ± 0.86 μg/mL total phenolics). Pennyroyal phytosomes, prepared with lipids extracted from egg yolks, presented a mean vesicle diameter

Multi-target drugs have gained significant recognition for the treatment of multifactorial diseases such as depression. Under a screening study of multi-potent medicinal plants with claimed antidepressant-like activity, the phenolic-rich Annona muricata aqueous extract (AE) emerged as a moderate monoamine oxidase A (hMAO-A) inhibitor and a strong hydrogen peroxide (H2O2) scavenger., This work was financed through project UID/QUI/50006/2013, receiving financial support from FCT/MEC through national funds, and co-financed by FEDER, under the Partnership Agreement PT2020. C. G. thanks FCT for the FCT Investigator(/IF/01332/2014/CP1255/CT0001). The authors would also like to acknowledge Sílvia Maia from CEMUP for her technical assistance with LTQ Orbitrap XL analyses and to Professor Michael Clifford for his advices in analyzing the MS spectra of phenolic acids.

Phytoconstituents have been utilized as medicines for thousands of years, yet their application is limited owing to major hurdles like deficit lipid solubility, large molecular size and degradation in the gastric environment of gut. Recently, phospholipid-complex technique has unveiled in addressing these stumbling blocks either by enhancing the solubilizing capacity or its potentiating ability to pass through the biological membranes and it also protects the active herbal components from degradation. Hence, this phospholipid-complex-technique can enable researchers to deliver the phytoconstituents into systemic circulation by using certain conventional dosage forms like tablets and capsules. This review highlights the unique property of phospholipids in drug delivery, their role as adjuvant in health benefits, and their application in the herbal medicine systems to improve the bioavailability of active herbal components. Also we summarize the prerequisites for phytosomes preparation like the selection of type of phytoconstituents, solvents used, various methods employed in phytosomal preparation and its characterization. Further we discuss the key findings of recent research work conducted on phospholipid-based delivery systems which can enable new directions and advancements to the development of herbal dosage forms.

Govindarajan Karthivashan,1 Mas Jaffri Masarudin,2 Aminu Umar Kura,1 Faridah Abas,3,4 Sharida Fakurazi1,5 1Laboratory of Vaccines and Immunotherapeutics, Institute of Bioscience, 2Department of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Sciences, 3Department of Food Science, Facultyof Food Science and Technology, 4Laboratory of Natural Products, Institute of Bioscience, 5Department of Human Anatomy, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Selangor, Malaysia Abstract: This study involves adaptation of bulk or sequential technique to load multiple flavonoids in a single phytosome, which can be termed as “flavonosome”. Three widely established and therapeutically valuable flavonoids, such as quercetin (Q), kaempferol(K), and apigenin(A), were quantified in the ethyl acetate fraction of Moringa oleifera leaves extract and were commercially obtained and incorporated in a single flavonosome (QKA–phosphatidylcholine) through four different methods of synthesis – bulk (M1) and serialized (M2) co-sonication and bulk (M3) and sequential (M4) co-loading. The study also established an optimal formulation method based on screening the synthesized flavonosomes with respect to their size, charge, polydispersity index, morphology, drug–carrier interaction, antioxidant potential through in vitro 1,1-diphenyl-2-picrylhydrazyl kinetics, and cytotoxicity evaluation against human hepatoma cell line (HepaRG). Furthermore, entrapment and loading efficiency of flavonoids in the optimal flavonosome have been identified. Among the four synthesis methods, sequential loading technique has been optimized as the best method for the synthesis of QKA–phosphatidylcholine flavonosome, which revealed an average diameter of 375.93±33.61nm, with a zeta potential of-39.07±3.55mV, and the entrapment efficiency was >98% for all the flavonoids, whereas the drug-loading capacity of Q, K, and A was 31.63%±0.17%, 34.51%±2.07%, and 31.79%±0.01%, respectively. The in vitro 1,1-diphenyl-2-picrylhydrazyl kinetics of the flavonoids indirectly depicts the release kinetic behavior of the flavonoids from the carrier. The QKA-loaded flavonosome had no indication of toxicity toward human hepatoma cell line as shown by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide result, wherein even at the higher concentration of 200µg/mL, the flavonosomes exert>85% of cell viability. These results suggest that sequential loading technique may be a promising nanodrug delivery system for loading multiflavonoids in a single entity with sustained activity as an antioxidant, hepatoprotective, and hepatosupplement candidate. Keywords: quercetin, kaempferol, apigenin, phytosome, antioxidant, HepaRG cell line

Medicinal plants have been a reliable source of bioactive natural products with potential pharmaceutical applications. The delivery of those bioactive agents into nanosystems is considered a promising strategy for the optimization of their pharmacologic effects. This work describes the preparation of phytosomes containing a bioactive extract from Plectranthus madagascariensis and optimization of the preparation method. Different formulations and process parameters were studied. It was observed that smaller and more uniform particles were obtained using acetone as solvent, a reaction time of two hours, and the addition of 2.5% molar concentration of cholesterol. The optimally prepared phytosomes had a diameter of 191.3 ± 75.3 nm with a polydispersity index of 0.243 ± 0.18, and a spherical shape with amorphous appearance. These nanosystems were able to encapsulate 92.8% of the extract, as evaluated by HPLC, relative to 7α,6β-dihydroxyroyleanona, the main extract component. This study suggests a future application of those phytosomes in the delivery of bioactive agents with therapeutic interest.

A phytosome is a kind of nanovesicle lipids to increase the absorption of active substances. Green tea extract was formulated into phytosome to find out its ability to inhibit weight gain. There were three formulas with thin layer hydration. Furthermore, phytosome complex formation, morphology, particle size, zeta potential, and polydispersity index, and absorption efficiency test were characterized. Phytosomes and green tea extracts were tested for absorption in vitro. A total of 25 rats were divided into five test groups, which were the normal group, placebo group, orlistat group, green tea extract group, and phytosome group. For 8 weeks they were orally induced using 10% of fructose + 2% of cholesterol, and test treatment. The best characteristics of FIII were formed complex, spherical morphology, Dv90 782.67 ± 39.7 nm, polydispersity index of 56 ± 0.11, zeta potential of -70.83 ± 1.67 mV, and adsorption efficiency of 97.77 ± 2.66 %. The test on the animals at week 8 resulted in percentage of weight gain in normal treatment of 46.47 ± 17.48%, placebo of 101.17 ± 10.37%, orlistat of 42.51 ± 25.13%, green tea extract of 92.73 ± 36.43%, and phytosomes of 45.09 ± 15.56%. Green tea extract flux was 2316.2 ± 1309.8 μg/cm2/hour, while phytosome flux was 3125.3 ± 2071.8 μg /cm 2 /hour. To sum up, phytosomes can inhibit weight gain and are better than to green tea extracts (p < 0.05).

The plant active molecules uses in home remedies have been relocated increasingly to the modern treatment. However, some of them have long side chains and high polarity that causes not to be able to pass through lipidic skin or intestine cell membranes by passive diffusion. Novel complexation technique named as ‘phytosome’ plays an important role to facilitate absorption and improve bioavailability. Drug molecules from natural sources and dietary soy phospholipids are complexed and generated cell-like structures. Up till now, the researchers have studied many phyto-phospholipid complexesas drug delivery systemcarrying out different methods (nonsolvent precipitating, supercritical fluids etc.) and provided pharmacokinetic and pharmacodynamic progresses. A lot of phytosome formulations are still under clinical trials and some of them on market. This presented review includes phytosome’s properties advantages, preparation methods, dosage forms and marketed products. In this review, introducing the most important points in phytosome and canalizing the researchers to this drug delivery system designed for herbal extracts/molecules are aimed

Curcuma longa, which contains curcumin as a major constituent, has been shown many pharmacological effects, but it is limited using in clinical due to low bioavailability. In this study, we developed a phytosome curcumin formulation and evaluated the hepatoprotective effect of phytosome curcumin on paracetamol induced liver damage in mice. Phytosome curcumin (equivalent to curcumin 100 and 200 mg/kg body weight) and curcumin (200 mg/kg body weight) were given by gastrically and toxicity was induced by paracetamol (500 mg/kg) during 7 days. On the final day animals were sacrificed and liver function markers (ALT, AST), hepatic antioxidants (SOD, CAT and GPx) and lipid peroxidation in liver homogenate were estimated. Our data showed that phytosome has stronger hepatoprotective effect compared to curcumin-free. Administration of phytosome curcumin effectively suppressed paracetamol-induced liver injury evidenced by a reduction of lipid peroxidation level, and elevated enzymatic antioxidant activities of superoxide dismutase, catalase, glutathione peroxidase in mice liver tissue. Our study suggests that phytosome curcumin has strong antioxidant activity and potential hepatoprotective effects.

The Plectranthus L’Her (Lamiaceae) genus possess a wide diversity of ethnomedicinal uses which indicate the presence of bioactive molecules. Also, natural drug delivery systems, as the phytosome, are promising strategies to improve bioactivity and stability. In this work, three plants from the Plectranthus genus were studied: P. madagascariensis, P. neochilus and P. porcatus. Several extracts were prepared by the combination of extraction methods with different polarity solvents. The obtained extracts were profiled by HPLC-DAD and the main components were identified, including polyphenols, diterpenes and flavones. Additionally, the extracts were screened for their antimicrobial (Gram positive and negative bacteria and yeasts), antioxidant (DPPH radical scavenging activity) and cytotoxic activities (MDA-MB-231 cell line). Acetonic extracts from P. madagascariensis (ultrasound and maceration) and P. neochilus (ultrasound) showed antibacterial effects against the majority of Gram positive bacteria strains tested (MIC values 1.95-250 μg/mL). The acetone ultrasound extract of P. madagascariensis showed potent antibacterial effect against Staphylococcus spp. tested, including a methicillin-resistant strain (MIC value 1.95-7.81 μg/mL). All methanolic extracts showed potent antioxidant effects at 100 ng/mL (60.8-89.0%). The maceration acetone extract from P. madagascariensis showed moderate cytotoxic effects in the MDA-MB-231 breast cancer cell line (IC50 64.52 μg/mL). These results validate the traditional uses of such plants as anti-infectious agents. The bioactive organic solvent extracts from P. madagascariensis were characterized using HPLC-DAD (major compound identification and quantification). Rosmarinic acid, 7α,6β-dihydroxyroyleanone, 7α-acetoxy-6β-hydroxyroyleanone and coleon U were identified by authentic standard overlay. 7α-Formyloxy-6β-hydroxyroyleanone was isolated from the ultrasound acetonic extract of P. madagascariensis and spectroscopically characterized (1H- and 13C-NMR). The pure compounds were tested in a battery of cancer cell lines (MDA-MB-231, MCF-7, HCT116, NCI-H460 and MCR-5) and showed moderate to potent cytotoxicity in the majority of the tested cell lines. Selectivity for cancer cell lines was observed for 7α,6β-dihydroxyroyleanone and 7α-acetoxy-6β-hydroxyroyleanone with selectivity index of 4.3 and 3.2, respectively. The combination of the observed results and literature data showed the relevance of lipophilicity and of the presence of an electron donating group at 6 and/or 7 positions to obtain high cytotoxicity in roylenanone abietanic compounds. The antibacterial acetonic ultrasound extract from P. madagascariensis was selected for incorporation in a phytosomal formulation and subsequently coated by chitosan. Phytosomes were amorphous, uniform in shape (SEM and AFM) and with an average size of 1082 ± 363 nm and zeta potential of +20.59 ± 12.02 mV. The encapsulation efficiency of the extract was determined by HPLC (57.7±0.06%). Physico-chemical interactions between formulation components were studied by DSC and DRIFTS. The phytosomes showed a sustained release and lower skin-like permeation fluxes. An up to 4-fold improvement of the anti-Staphylococci activity was verified (MIC values 0.49-31.25 μg/mL). The safety of such formulation was verified by in vitro human keratinocytes cytotoxicity and by in vivo dermal irritation tests in mice. This study showed the potential of the Plectranthus genus as a source of lead antibacterial and antiproliferative agents and thus validate the ethnomedicinal uses of the studied plants. The isolated abietane diterpenes obtained from P. madagascariensis possess promising selective cytotoxic effects in the lung cancer lines tested. Additionally, the developed phytosomal formulation containing a P. madagascariensis extract corresponds to a potent topical antibacterial candidate with a broad spectrum of activity.

Polyphenols are secondary metabolites of plants, containing in their structure the aromatic ring with one or more phenolic groups. Such molecules have great antioxidant potential. They can modulate the activity of many enzymes and cell receptors and generate specific biological effects. Several polyphenols are already in use as active ingredients of pharmaceuticals or different cosmetic products. The large size of these polycyclic molecules and poor solubility in aqueous and/or lipid media may limit development of stable formulations and their passive diffusion into and through the biological membranes. The current strategy for enhancement of solubility and permeability of biomedically relevant polyphenols is based on formation of specific complexes with phospholipids which self associate in aqueous media and form specific unilamellar vesicles often described as phytosomes or herbosomes. There is an increasing number of scientific publications in this field during the last decade and different polyphenolics (e.g., curcuminoids, silybin, silymarin, ginkgoflavonglucosides, ginkgolides, bilobalide, and dimeric flavonoids from Ginkgo biloba leaf, sericoside, polyphenols from Camellia sinensis leaf (epigallocatechin, catechin, epicatechin-3-Ogallate, epigallo catechin-3-O-gallate), Vitis Vinifera (resveratrol, quercitin, catechin, procyanidins, epicatechin), are marketed as phytosomes obtained by the patented technology Phytosome® (Indena, Italy). The chapter reviews the significance of encapsulation of poliphenolic active ingredients, properties of commercially available phytosomes (physicochemical characteristics, stability, loading capacity, solubility, dispersibility) and phytosome relevance for development of pharmaceutical preparations and personal care products. The potential for enhancement of biological effects (cardiovascular, antiinflammatory, hepatoprotective, anticancer, hypoglycemic, weight loss, antiaging), of the currently investigated phytosomes is reviewed comprehensively.

Phytosome is a complex of a natural active ingredient and phospholipids. The term ‘Phyto’ means plant while ‘some’ means cell like structure. It is claimed that phytosome increases absorption of "conventional herbal extracts" or isolated active principles both orally as well as topically. In this era phytosome gain popularity as a potential drug delivery device due to excessive demand and utility of herbs or herb based medicines. This advance technology offers amenities like improved absorption, enhanced delivery & increased bioavailability of herbal extracts. These drug-phospholipid complexes can be fabricated in the form of solution, suspension, emulsion, syrup, lotion, gel, cream, aqueous micro dispersions. Standardized plant extracts, mainly polar phytoconstituents like flavonoids, terpenoids, tannins, xanthones shall be introduced in form of phytosome.

Background: Evidences from ethnopharmacological practices have shown that combination of Abutilon indicum and Piper longum are traditionally used to treat symptoms of the liver disorder. The hypothesis is phytosomes of a combination of both crude drug extract will be more effective and safe as hepatoprotective agent. Aim: Present work is aimed at development and characterization of phytosomes containing ethanolic extract of both drugs to meet the need for better effectiveness and safety. Materials and Methods: Phytosomes were formulated by using Indena's patented process. Characterization involved following parameters: Particle size determination, percentage yield, entrapment efficiency, differential scanning calorimetry, scanning electron microscope, fourier transform infrared spectroscopy, and high performance thin liquid chromatography. Liver damage was induced in adult Charles foster rats (150 ± 10 g) with CCl4 in olive oil (1:1 v/v, i.p) 1 ml/kg once daily for 7 days. LIV 52 (1 ml/kg per oral [p.o]), ethanolic extract of A. indicum and P. longum combination (100, 200, and 400 mg/kg p.o) and phytosomes (100 mg/kg p.o.) was given 3 days prior to CCl4 administration. Estimation of liver marker enzymes and histopathological studies were done. Result was analyzed by using (analysis of variance) followed by Student-Newman–Keuls test. Result: Combined extract has shown hepatoprotective activity but phytosomal formulation has more potent hepatoprotective effect on CCl4 induced liver toxicity at very low dose comparative to a higher dose of combined extract. Conclusion: Novel approach for herbal drug delivery is more prominent than conventional which improves bioavailability of polar extract and also patient compliance. SUMMARY Standardised ethanolic extract of leaves of abutilon indicum and piper longum fruits by microwave assisted extraction was used for phytosomal complex formation and phytosomal complex was characterised by various parameters and finally the hepatoprotective activity of phytosomes and crude extract was evaluated by different biochemical markers and histopathological study. Abbreviations Used: DSC: Differential scanning calorimetry, SEM: Scanning electron microscope, FTIR: Fourier transform infrared spectroscopy, HPTLC: High performance thin liquid chromatography, p.o: Per oral, A. indicum: Abutilon indicum, P. longum: Piper longum.

Objectives Sinigrin is a major glucosinolate present in plants of the Brassicaceae family. Recently, sinigrin and its phytosome formulations have been investigated for its wound-healing actions, by our research group. The aim of this study was to demonstrate sinigrin drug release from its phytosome complex and also to determine whether the phytosome complex enhances the delivery of sinigrin into the skin when compared to free sinigrin. Methods In vitro Franz cell diffusion studies were performed on human abdominal skin. The morphology of the phytosome complex was examined by transmission electron microscopy. The in vitro drug release was determined using dialysis sacks. Key findings The in vitro drug release indicated a controlled and sustained release of sinigrin from the phytosome complex. Tape stripping results showed that the sinigrin–phytosome complex (0.5155 μg/ml) statistically significantly enhanced the delivery of sinigrin into the stratum corneum–epidermis when compared to the free sinigrin (0.0730 μg/ml). Conclusions These results suggested the possibility of utilizing sinigrin–phytosome complex, to optimally deliver sinigrin to the skin which can be further used for various skin-related diseases including wound healing.

The kind of novel herbal formulations such as polymeric nanoparticles, nanocapsules, liposomes, phytosomes, animations, microsphere, transfersomes, and ethosomes has been reported using proactive and plant selections. The novel formulations are described to have remarkable advantages over conventional formulations of plant actives and extracts which include enhancement of solubility, bioavailability, and protection from toxicity, enhancement of pharmacological activity, enhancement of stability, improved tissue macrophages distribution, sustained delivery, and protection from physical and chemical degradation. Phytosome is a patented technology developed by a leading maker of drugs and nutraceuticals, to incorporate standardized plant extracts or water-soluble phytoconstituents into phospholipids to produce lipid-compatible molecular complexes. The herbal drugs can be used in a more upright course with enhanced efficacy by incorporating them into modern dosage forms. This can be accomplished by designing novel drug delivery systems for herbal ingredients. The present review highlights the current condition of the development of novel herbal formulations and summarizes their type of active components, biological activity, and applications of novel formulations.

Sinigrin is a class of glucosinolates found naturally in plants of the Brassicaceae family. Lately, studies have shown that sinigrin possesses anticancer, antibacterial and anti-inflammatory activities. Since its efficacy has not been explored on wound healing, we examined the effect of sinigrin on HaCaT cells. We also aimed at formulating sinigrin into phytosome to form a sinigrin-phytosome complex and study the wound healing and cytotoxic activities on A-375 and HaCaT cells. Sinigrin was efficiently formulated into the phytosome with an average particle size of 153 ± 39 nm, zeta potential of 10.09 ± 0.98 mV and complex efficiency of 69.5 ± 5%. The formation of the sinigrin-phytosome complex was confirmed by DSC and FTIR analysis. The sinigrin-phytosome complex significantly exhibited wound healing effects when compared to sinigrin alone. After 42 h, the phytosome complex completely healed the wound, whereas sinigrin alone showed only 71% wound closure. The sinigrin-phytosome complex displayed minimal toxicity towards HaCaT cells and at higher concentrations, it showed potent activity towards A-375. The results indicated that sinigrin-phytosome complex augmented the therapeutic potential of sinigrin towards the wound healing activity and this approach should be explored further for cancerous wound treatment.

Among various phospholipid-mediated drug delivery systems (DDS) suitable for topic and oral administration, phytosome technology represents an advanced innovation, widely used to incorporate standardized bioactive polyphenolic phytoconstituents into phospholipid molecular complexes. In order to extend their potential therapeutic efficiency also to other routes of administration, we proposed a novel phytosome carrier-mediated vesicular system (phyto-liposome) as DDS for the flavonolignan silybin (SIL), a natural compound with multiple biological activities related to its hepatoprotective, anticancer and antioxidant (radical scavenging) effects. We screened the optimum fraction of its phytosome, available in the market as Siliphos™, into liposomes prepared by extrusion, such that vesicle sizes and charges, monitored through dynamic light scattering and laser doppler velocimetry, satisfied several quality requirements. Special emphasis was placed on the study of host-guest interaction by performing UV-vis absorption, spectrofluorimetry and NMR experiments both in aqueous and non-polar solvents to probe the effect of the presence of phospholipids on the electronic properties of SIL and its propensity to engage H bonding with the lipid headpolar groups. Finally, fluorescence microscopy observations confirmed the ability of phyto-liposomes to be internalized in human hepatoma cells, which was promising for their potential application in the treatment of acute or chronic liver diseases. © 2014 Elsevier B.V.

Francesco Di Pierro,1 Roberto Settembre2 1Scientific Department, Velleja Research, Milan, Italy; 2Neurosurgery Department, Di Venere Hospital, Bari, Italy Abstract: We conducted an 8-week, open, randomized controlled clinical trial on 141 subjects affected by neuropathic pain to investigate the role of an adjunctive therapy added to the administration of dexibuprofen (400 mg twice a day) and based on a multi-ingredient formula (Lipicur), consisting of lipoic acid plus curcumin phytosome and piperine, in patients with a diagnosis of lumbar sciatica, lumbar disk herniation, and/or lumbar canal stenosis (96 subjects), or with carpal tunnel syndrome (45 subjects). A total of 135 participants completed the study. Treatment with the multi-ingredient formula (Lipicur) reduced neuropathic pain by more than 66% in both conditions (subjects with lumbar sciatica and with carpal tunnel syndrome), and these reductions were statistically significant. Moreover, the treatment reduced dexibuprofen use by about 40%. An add-on therapy with only lipoic acid has not shown any significant results. On the basis of its safety and efficacy, Lipicur could be considered an effective complementary therapy to be added to conventional treatments to achieve better efficacy in reducing neuropathic pain. Keywords: curcumin, phytosome, piperine, dexibuprofen, neuropathic pain Erratum for this paper has been published

Irritable Bowel Syndrome (IBS) is a chronic, gastrointestinal disorder in which abdominal pain or discomfort is associated with defecation or changes in bowel habits. Its multifactorial pathophysiology leads to a variety of available treatments, mainly aimed at controlling symptoms. The management of IBS patients could be optimized by individualized strategies, including non-pharmaceutical approaches. In this study, we evaluated the efficacy and safety of a novel delivery form of Boswellia serrata extracts (BSE) (Casperome®) in patients with IBS.71 otherwise healthy subjects with idiopathic IBS were recruited. Participants were assigned to the following management strategies: hyoscine butylbromide; papaverine hydrochloride + A. belladonna extract; supplementation with Casperome®. Predominant IBS symptoms were evaluated at inclusion and at the end of the observational period (4 weeks). The numbers of subjects who needed rescue medication or medical attention/hospital admission were recorded. Adverse events were also evaluated.In all groups, the IBS symptoms investigated, namely abdominal pain, altered bowel movements, meteorism and cramps improved during the observational period. Of note, the number of subjects who needed medical attention significantly decreased only in Casperome®-supplemented group. In addition, Casperome® supplementation was related to a lower incidence of side effects (mainly stypsis).This preliminary study suggests that Casperome® supplementation could represent a promising alternative approach to manage symptoms associated with IBS in otherwise healthy subjects.