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Lung inflammation caused by fine particulate matter (PM), particularly PM2.5, poses a significant public health challenge, with oxidative stress and inflammation playing central roles in its pathophysiology. This study evaluates the protective effects of phytosome-encapsulated extract of purple waxy corn tassel (PPT) against PM2.5-induced lung inflammation. Male Wistar rats received PPT at doses of 100, 200, and 400 mg/kg BW for 21 days prior to exposure and continued to receive the same doses for 27 days during PM2.5 exposure. Significant reductions in inflammatory markers, including cyclooxygenase-2 (COX-II), various interleukins (IL-1β, IL-6, IL-8), tumor necrosis factor-alpha (TNF-α), and nuclear factor kappa B (NF-κB), were observed, indicating that PPT effectively regulates the inflammatory response. Additionally, PPT improved oxidative stress markers by reducing malondialdehyde (MDA) levels and enhancing antioxidant enzyme activities such as superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px), thereby restoring lung antioxidant defenses. Notably, the study revealed that PPT modulates epigenetic mechanisms, as evidenced by decreased histone deacetylase (HDAC) activity and upregulation of sirtuins in lung tissue. These epigenetic modifications likely contribute to the reduction in inflammation and oxidative stress, suggesting a multifaceted protective role of PPT that involves both direct biochemical pathways and epigenetic regulation. The interplay between reduced inflammatory signaling, enhanced antioxidant capacity, and epigenetic modulation underscores PPT's potential as a therapeutic agent for managing respiratory inflammation-related diseases and its promise for the development of future functional food products. [ABSTRACT FROM AUTHOR]

Background: α-Mangostin is a major xanthone in Garcinia mangostana L. (Clusiaceae) pericarps. It has promising anti-proliferative potential in different cancer cells; however, it has poor oral bioavailability. Phytosomes are used as a novel nano-based drug delivery system. The aim of this research was to enhance the anti-proliferative potency of α-mangostin by formulating it as α-mangostin-phytosome (α-M-PTMs) and assessing its impact on SKOV-3 ovarian cancer cells in comparison to pure α-mangostin. Results: The size and entrapment efficiency of the proposed formulation were optimized using Box–Behnken statistics. The optimized formula was characterized using transmission electron microscope. The binding of α-mangostin to phospholipids was confirmed using Fourier-transform infrared (FTIR) spectroscopy. The optimized α-mangostin-phytosomes formula exhibited enhanced anti-proliferative activity with reference to raw α-mangostin. This was further substantiated by assessing the cell cycle phases that indicated an accumulation of SKOV-3 cells in the sub-G1 phase. Annexin-V staining revealed enhanced apoptotic activity in α-mangostin-phytosome-treated cells. This was associated with upregulation of CASP3 (Caspase-3), BAX (BCL2 Associated X, Apoptosis Regulator) and TP53 as well as down-regulation of BCL2 mRNA (B-Cell Leukemia/Lymphoma 2). Moreover, our data indicated enhanced ROS (Reactive oxygen species) production, cytochrome-C release, and disturbed MMP (mitochondrial membrane potential). Conclusion: Encapsulation of α-mangostin in a phytosome nano-formula enhances its anti-proliferative effects in SKOV-3 cells via, at least in part, inducing mitochondrial apoptotic cell death. [ABSTRACT FROM AUTHOR]

(1) Background: Methyl jasmonate-treated D. morbifera adventitious root extract (MeJA-DMARE), enriched with phenolics, has enhanced bioactivities. However, phenolics possess low stability and bioavailability. Substantial evidence indicates that plant extract–phospholipid complex assemblies, known as phytosomes, represent an innovative drug delivery system. (2) Methods: The phytosome complex was created by combining MeJA-DMARE with Soy-L-α-phosphatidylcholine (PC) using three different ratios through two distinct methods (co-solvency method: A1, A2, and A3; thin-layer film method: B1, B2, and B3). (3) Results: Initial evaluation based on UV-Vis, entrapment efficiency (EE%), and loading content (LC%) indicated that B2 exhibited the highest EE% (79.98 ± 1.45) and LC% (69.17 ± 0.14). The phytosome displayed a spherical morphology with a particle size of 210 nm, a notably low polydispersity index of 0.16, and a superior zeta potential value at −25.19 mV. The synthesized phytosome exhibited superior anti-inflammatory activities by inhibiting NO and ROS production (reduced to 8.9% and 55.1% at 250 μg/mL) in RAW cells and adjusting the expression of related inflammatory cytokines; they also slowed lung tumor cell migration (only 2.3% of A549 cells migrated after treatment with phytosomes at 250 μg/mL), promoting ROS generation in A549 cell lines (123.7% compared to control) and stimulating apoptosis of lung cancer-related genes. (4) Conclusions: In conclusion, the MeJA-DMARE phytosome offers stable, economically efficient, and environmentally friendly nanoparticles with superior inflammation and lung tumor inhibition properties. Thus, the MeJA-DMARE phytosome holds promise as an applicable and favorable creation for drug delivery and lung cancer treatment. [ABSTRACT FROM AUTHOR]

Manjusha Bhange, Darshan R Telange Department of Pharmaceutics, Datta Meghe College of Pharmacy, Datta Meghe Institute of Higher Education & Research (DU), Wardha, Maharashtra, IndiaCorrespondence: Manjusha Bhange, Department of Pharmaceutics, Datta Meghe College of Pharmacy, Datta Meghe Institute of Higher Education & Research (DU), Sawangi Meghe, Wardha, 442001, Maharashtra, India, Tel +91-9503985404, Email manjusha.pharmacy@dmiher.edu.inAbstract: Hepatocellular carcinoma is the fifth leading cancer in related diseases most commonly in men and women. The curative treatments of liver cancer are short-listed, associated with toxicities and therapeutically. Emerging nanotechnologies exhibited the possibility to treat or target liver cancer. Over the years, to phytosome solid lipid nanoparticles, gold, silver, liposomes, and phospholipid nanoparticles have been produced for liver cancer therapy, and some evidence of their effectiveness has been established. Ideas are limited to the laboratory scale, and in order to develop active targeting of nanomedicine for the clinical aspects, they must be extended to a larger scale. Thus, the current review focuses on previously and presently published research on the creation of phytosomal nanocarriers for the treatment of hepatocellular carcinoma. In hepatocellular carcinoma (HCC), phytosomal nanotherapeutics improve the targeted delivery and bioavailability of phytochemicals to tumor cells, thereby reducing systemic toxicity and increasing therapeutic efficacy. In order to address the intricate molecular processes implicated in HCC, this strategy is essential. Keywords: hepatocellular carcinoma, liver cancer, phytosome, nanocarrier, clinical trials

Abstract Background α-Mangostin is a major xanthone in Garcinia mangostana L. (Clusiaceae) pericarps. It has promising anti-proliferative potential in different cancer cells; however, it has poor oral bioavailability. Phytosomes are used as a novel nano-based drug delivery system. The aim of this research was to enhance the anti-proliferative potency of α-mangostin by formulating it as α-mangostin-phytosome (α-M-PTMs) and assessing its impact on SKOV-3 ovarian cancer cells in comparison to pure α-mangostin. Results The size and entrapment efficiency of the proposed formulation were optimized using Box–Behnken statistics. The optimized formula was characterized using transmission electron microscope. The binding of α-mangostin to phospholipids was confirmed using Fourier-transform infrared (FTIR) spectroscopy. The optimized α-mangostin-phytosomes formula exhibited enhanced anti-proliferative activity with reference to raw α-mangostin. This was further substantiated by assessing the cell cycle phases that indicated an accumulation of SKOV-3 cells in the sub-G1 phase. Annexin-V staining revealed enhanced apoptotic activity in α-mangostin-phytosome-treated cells. This was associated with upregulation of CASP3 (Caspase-3), BAX (BCL2 Associated X, Apoptosis Regulator) and TP53 as well as down-regulation of BCL2 mRNA (B-Cell Leukemia/Lymphoma 2). Moreover, our data indicated enhanced ROS (Reactive oxygen species) production, cytochrome-C release, and disturbed MMP (mitochondrial membrane potential). Conclusion Encapsulation of α-mangostin in a phytosome nano-formula enhances its anti-proliferative effects in SKOV-3 cells via, at least in part, inducing mitochondrial apoptotic cell death.

Mayang Kusuma Dewi,1 Muhaimin Muhaimin,2 I Made Joni,3,4 Faizal Hermanto,5 Anis Yohana Chaerunisaa6 1Doctoral Program in Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, Indonesia; 2Department of Pharmaceutical Biology, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, Indonesia; 3Functional Nano Powder University Center of Excellence (FiNder U CoE), Universitas Padjadjaran, Sumedang, Indonesia; 4Department of Physics, Faculty of Mathematics and Natural Science, Universitas Padjadjaran, Sumedang, Indonesia; 5Department of Pharmacology and Toxicology, Faculty of Pharmacy, Universitas Jenderal Achmad Yani, Cimahi, Indonesia; 6Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, IndonesiaCorrespondence: Anis Yohana Chaerunisaa, Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, Indonesia, Email anis.yohana.chaerunisaa@unpad.ac.idIntroduction: Sonneratia alba extract exhibits antimalarial activity, mainly due to its secondary metabolites—naphthoquinones, flavonoids, tannins, and saponins—where naphthoquinone is the primary active component. However, its low bioavailability limits its effectiveness. To improve this, a phytosome-based vesicular system was proposed. This study focused on formulating a phytosome with S. alba and developing a predictive model to enhance its antimalarial activity.Methods: Phytosomes were produced using antisolvent precipitation and optimized with 3-factor, 3-level Box-behnken model. Particle size, zeta potential, and entrapment efficiency were assessed. The optimized phytosomes were characterized by their physical properties and release profiles. Their antimalarial activity was tested in white BALB/c mice infected with Plasmodium berghei using Peter’s 4-day suppressive test.Results: The optimal phytosome formulation used a phospholipid-to-extract ratio of 1:3, reflux temperature of 50°C, and a duration of 2.62 hours. The phytosomes had a particle size of 471.8 nm, a zeta potential of − 54.1 mV, and an entrapment efficiency (EE) of 82.4%. In contrast, the phytosome-fraction showed a particle size of 233.4 nm, a zeta potential of − 61.5 mV, and an EE of 87.08%. TEM analysis confirmed both had a spherical shape. In vitro release rates at 24 hours were 86.2 for the phytosome-extract and 95.9% for the phytosome-fraction, compared to 46.9% and 37.7% for the extract and fraction alone. Overall, the phytosome formulation demonstrated good stability. The actual experimental values closely matched the predicted values from the Box–Behnken model, indicating a high degree of accuracy in the model. Additionally, the phytosomes exhibited significantly greater antimalarial activity than the S. alba extract and fraction alone.Conclusion: The findings indicated that the vesicular formulation in phytosomes can enhance the antimalarial activity of S. alba extract and fraction.Keywords: antimalarial S.alba, phytosome, box-behnken, extract, fraction

Background: Papaya seeds are a rich source of proteins, fat, fibers, vitamins, minerals, monounsaturated fatty acids, polyphenols, and powerful antioxidants like flavonoids. Low solubility limits the absorption and bioavailability of herbal constituents. Hence, phytosomes of Papaya seed extract were formulated to enhance its solubility and bioavailability. Methodology: Papaya seeds were extracted using ethanol as solvent, and all the phytoconstituents present in the extract were assessed during the phytochemical screening and LC-MS analysis. In-vitro antidiabetic activity pure extract was determined by alpha-amylase and alpha-glucosidase enzyme inhibitory assay. The phytosomes of extract were formulated using the lipid thin film formation method and Soya lecithin and Cholesterol as lipids. The formulated phytosomes were analyzed for parameters such as particle size, zeta potential, encapsulation efficiency, percent drug content, and In-vitro dissolution study. The chemical nature of the formulation was studied using FTIR analysis and powder X-ray diffractometry. Thermal stability of phytosomes analyzed with the help of Differential Scanning calorimetry. Results: LC-MS identified 16 phytoconstituents. In-vitro antidiabetic activity showed 59.97% and 51.17% inhibition of enzymes alpha-amylase and alpha-glucosidase, respectively. The encapsulation efficiency of the optimized formulation was 88.41±0.91% with a particle size of 188.0±53.7nm. TEM images of formulation confirm the formation of phytosomes. FTIR, DSC, and Powder X-ray diffractometry showed no unwanted peaks. The in vitro dissolution study showed 89.26±1.05% CDR of phytosome, while the extract showed 47.78±0.59% CDR. Conclusion: Evaluation results of phytosomes suggest that this formulation can be used as an effective herbal antidiabetic formulation

This study aimed to investigate the nutritional effects of phytosomal green tea on growth performance, lipid parameters, immune responses, antioxidant status, ileum bacterial population, and gamma interferon gene expression in compared to green tea extract. 375 male broiler chickens (ROSS 308)were randomly assigned to 5 treatments, with 5 replications and 15 chickens per cage. Treatments included 1- basal diet (negative control), 2- basal diet + 0.10 g/kg avilamycin, 3- basal diet + 0.60 g/kg salinomycin, 4- basal diet + 400 ml/kg green tea extract and 5-basal diet + 300 ml/kg green tea phytosome. Experimental treatments did not affect growth and carcass performance (P>0.05). Malondialdehyde, triglycerides, low density lipoprotein cholesterol in plasma affected by phytosomal extract decreased compared to control (P<0.05). Antibody levels against red blood cells, immunoglobulin G and immunoglobulin M increased in chickens fed phytosome supplement in comparison to the form of green tea extract at 28 days (P<0.05). The use of green tea extract reduced the population of Escherichia coli in comparison to avilamycin and increased the population of lactobacilli cmpared to salinomycin (P<0.05). The expression of interferon gamma gene in the spleen of chickens that received the phytosomal green tea extract was higher compared to the consumption of green tea extract (P<0.05). Conclusion is that, green tea extract -phospholipid complexes showed the same efficiency compared to green tea extract on the evaluated parameters and can be considered as an alternative in order to reduce the consumption of plant extracts in poultry nutrition. [ABSTRACT FROM AUTHOR]

Studies have reported the potential role of Boswellic acids (BAs), bioactive pentacyclic triterpenes from Boswellia serrata (BS), in treating rheumatoid arthritis (RA). However, poor water solubility and limited oral absorption are restricting factors for its better therapeutic efficacy. Based on these assumptions, the current study aimed to develop naturosomal delivery of BAs to boost their extremely low bioavailability, colloidal stability, and water solubility. Nanonized naturosomes were developed and subsequently analyzed to show their physicochemical and functional features employing the quality-by-design approach. The solubility analysis of Boswellic acid naturosomes revealed a 16 times improvement in aqueous solubility compared to BS extract (BSE). The zeta potential and dynamic light scattering findings of BSE naturosomes (BSENs) have demonstrated their colloidal stability with regulated nano-size particles. Additionally, compared to BSE (⁓31%), in-vitro dissolution experiments showed that >99% of pentacyclic triterpenes were released from BSENs. Studies on ex-vivo permeation showed that BSENs' permeation (>79%) significantly improved over BSE's (⁓20%). In-vivo efficacy studies using CFA-prompted arthritis in rodents showed a critical expansion in body wt and an undeniable reduction in paw thickness, paw volume, and TNF-α treated with BSEN compared to the arthritis control and BSE-treated group. These findings suggest that BSENs can help treat RA drugs by demonstrating their efficacy in further clinical research to validate the significant improvements.

(1) Background: Methyl jasmonate-treated D. morbifera adventitious root extract (MeJA-DMARE), enriched with phenolics, has enhanced bioactivities. However, phenolics possess low stability and bioavailability. Substantial evidence indicates that plant extract–phospholipid complex assemblies, known as phytosomes, represent an innovative drug delivery system. (2) Methods: The phytosome complex was created by combining MeJA-DMARE with Soy-L-α-phosphatidylcholine (PC) using three different ratios through two distinct methods (co-solvency method: A1, A2, and A3; thin-layer film method: B1, B2, and B3). (3) Results: Initial evaluation based on UV-Vis, entrapment efficiency (EE%), and loading content (LC%) indicated that B2 exhibited the highest EE% (79.98 ± 1.45) and LC% (69.17 ± 0.14). The phytosome displayed a spherical morphology with a particle size of 210 nm, a notably low polydispersity index of 0.16, and a superior zeta potential value at −25.19 mV. The synthesized phytosome exhibited superior anti-inflammatory activities by inhibiting NO and ROS production (reduced to 8.9% and 55.1% at 250 μg/mL) in RAW cells and adjusting the expression of related inflammatory cytokines; they also slowed lung tumor cell migration (only 2.3% of A549 cells migrated after treatment with phytosomes at 250 μg/mL), promoting ROS generation in A549 cell lines (123.7% compared to control) and stimulating apoptosis of lung cancer-related genes. (4) Conclusions: In conclusion, the MeJA-DMARE phytosome offers stable, economically efficient, and environmentally friendly nanoparticles with superior inflammation and lung tumor inhibition properties. Thus, the MeJA-DMARE phytosome holds promise as an applicable and favorable creation for drug delivery and lung cancer treatment.

Lung inflammation caused by fine particulate matter (PM), particularly PM2.5, poses a significant public health challenge, with oxidative stress and inflammation playing central roles in its pathophysiology. This study evaluates the protective effects of phytosome-encapsulated extract of purple waxy corn tassel (PPT) against PM2.5-induced lung inflammation. Male Wistar rats received PPT at doses of 100, 200, and 400 mg/kg BW for 21 days prior to exposure and continued to receive the same doses for 27 days during PM2.5 exposure. Significant reductions in inflammatory markers, including cyclooxygenase-2 (COX-II), various interleukins (IL-1β, IL-6, IL-8), tumor necrosis factor-alpha (TNF-α), and nuclear factor kappa B (NF-κB), were observed, indicating that PPT effectively regulates the inflammatory response. Additionally, PPT improved oxidative stress markers by reducing malondialdehyde (MDA) levels and enhancing antioxidant enzyme activities such as superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px), thereby restoring lung antioxidant defenses. Notably, the study revealed that PPT modulates epigenetic mechanisms, as evidenced by decreased histone deacetylase (HDAC) activity and upregulation of sirtuins in lung tissue. These epigenetic modifications likely contribute to the reduction in inflammation and oxidative stress, suggesting a multifaceted protective role of PPT that involves both direct biochemical pathways and epigenetic regulation. The interplay between reduced inflammatory signaling, enhanced antioxidant capacity, and epigenetic modulation underscores PPT’s potential as a therapeutic agent for managing respiratory inflammation-related diseases and its promise for the development of future functional food products.

The aim of this work was to evaluate the hepatoprotective potential of fractions and phytosomal complexes of Telfairia occidentalis leaf extracts on ethanol-induced hepatotoxicity in rat models. Phytosomal complexes of ethanol extract fractions were prepared by the thin film hydration technique. Hepatoprotective activities were evaluated by biochemical assays and histopathological examination of liver sections. Intoxication of animals with pure ethanol significantly (p < 0.05) elevated their liver enzyme titers, whereas co-administration with various extracts and phytosomal complexes reversed the increases. Histopathological findings revealed liver tissue protective effects of the extracts with the phytosomal complexes exhibiting greater effects (p < 0.05). Significant differences at p ≤ 0.05 were observed in the liver indices of animals treated with co-administered ethanol and extract fractions or phytosomes complexes versus the positive control group. T. occidentalis leaf extract formulated as phytosomes, therefore, has good potential of enhancing the hepatoprotective activities of the extract. [ABSTRACT FROM AUTHOR]

Background: Berberine is a poorly absorbed natural alkaloid widely used as nutraceutical to counteract diarrhoea and to lower cholesterol and hyperglycaemia. It has also been reported to reduce signs and symptoms of polycystic ovary syndrome (PCOS). Objective: To explore, through a multi-centric, randomized, controlled and prospective study, the possible role played by a form berberine that is more easily absorbed (Berberine Phytosome®, BP) in 130 Pakistani women with a diagnosis of PCOS and fertility problems due to menstrual and ovary abnormalities. Results: Ninety days of supplementation with BP, administered at 550 mg x2/die, determined (i) resumption of regular menstruation in about 70% of women (versus 16% in the control group; p < 0.0001), (ii) normalization of the ovaries anatomy in more than 60% of women (versus 13% in the control group; p < 0.0001), (iii) acne improvement in 50% of women (versus 16% in the control group; p = 0.0409) and (iv) hirsutism reduction in 14% of women (versus 0% in the control group; p = 0.0152). The metabolic and the hormonal profiles of the women in the two groups did not significantly differentiate at the end of the study. BP was well-tolerated and no specific side-effects were registered. Respectively after one, two and 8 years of trying, three women supplemented with BP became and are currently pregnant. Conclusion: Our study showed the positive effects of BP supplementation in women with PCOS and confirmed the high safety profile of this nutraceutical. [ABSTRACT FROM AUTHOR]

Ahmed Mowafy Tafish,1,2 Mohamed El-Sherbiny,3,4 Ahmed A Al‐Karmalawy,5,6 Osama Abd El-Azeem Soliman,1 Noha Mohamed Saleh1 1Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt; 2Department of Pharmaceutical Technology, Faculty of Pharmacy, Horus University, New Damietta, 34518, Egypt; 3Department of Basic Medical Sciences, College of Medicine, AlMaarefa University, Riyadh, Saudi Arabia; 4Department of Anatomy, Faculty of Medicine, Mansoura University, Mansoura, 35516, Egypt; 5Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Horus University, New Damietta, 34518, Egypt; 6Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ahram Canadian University, 6th of October City, Giza, 12566, EgyptCorrespondence: Noha Mohamed Saleh, Associate Professor of Pharmaceutics, Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt, Tel +2 01064536677, Fax +2 050 2247496, Email nunu_ramy@mans.edu.egBackground: Despite recent advances in wound healing products, phytochemicals have been considered promising and attractive alternatives. Carvacrol (CAR), a natural phenolic compound, has been reported to be effective in wound healing.Purpose: This work endeavored to develop novel CAR-loaded phytosomes for the enhancement of the wound healing process.Methods: Molecular docking was performed to compare the affinities of the different types of phospholipids to CAR. Phytosomes were prepared by three methods (thin-film hydration, cosolvency, and salting out) using Lipoid S100 and Phospholipon 90H with three levels of saturation percent (0%, 50%, and 100%), and three levels of phospholipid molar percent (66.67%, 75%, and 80%). The optimization was performed using Design Expert where particle size, polydispersity index, and zeta potential were chosen as dependent variables. The optimized formula (F1) was further investigated regarding entrapment efficiency, TEM, 1H-NMR, FT-IR, DSC, X-RD, in vitro release, ex vivo permeation, and stability. Furthermore, it was incorporated into a hydrogel formulation, and an in vivo study was conducted to investigate the wound-healing properties of F1.Results: F1 was chosen as the optimized formula prepared via the thin-film hydration method with a saturation percent and a phospholipid molar percent of zero and 66.67, respectively. TEM revealed the spherical shape of phytosomal vesicles with uniform size, while the results of 1H-NMR, FT-IR, DSC, and X-RD confirmed the formation of the phytosomal complex. F1 demonstrated a higher in vitro release and a slower permeation than free CAR. The wound area of F1-treated animals showed a marked reduction associated with a high degree of collagen fiber deposition and enhanced cellular proliferation.Conclusion: F1 can be considered as a promising remedy for the enhancement of wound healing and hence it would be hoped to undergo further investigation.Graphical Abstract: Keywords: carvacrol, phospholipids, docking, phytosome, release, topical, wound healing

Introduction: Silymarin proved to be a beneficial herbal medicine against many hepatic disorders such as alcoholic liver disease (ALD). However, its application is restricted due to its low bioavailability and consequently decreased efficacy. We herein used a nano-based approach known as "phytosome", to improve silymarin bioavailability and increase its efficacy. Methods: Phytosome nanoparticles (NPs) were synthesized using thin film hydration method. NPs size, electrical charge, morphology, stability, molecular interaction, entrapment efficiency (EE %) and loading capacity (LC %) were determined. Moreover, in vitro toxicity of NPs was investigated on mesenchymal stem cells (MSCs) viability using MTT assay. In vivo experiments were performed using 24 adult rats that were divided into four groups including control, ethanol (EtOH) treatment, silymarin/EtOH treatment and silymarin phytosome/EtOH, with 6 mice in each group. Experimental groups were given 40% EtOH, silymarin (50 mg/kg) and silymarin phytosome (200 mg/kg) through the gastric gavage once a day for 3 weeks. Biochemical parameters, containing ALP, ALT, AST, GGT, GPx and MDA were measured before and after experiment to investigate the protective effect of silymarin and its phytosomal form. And histopathological examination was done to evaluate pathological changes. Results: Silymarin phytosome NPs with the mean size of 100 nm were produced and were well tolerated in cell culture. These NPs showed a considerable protective effect against ALD through inverting the biochemical parameters (ALP, ALT, AST, GGT, GPx) and histopathological alterations Conclusion: Silymarin phytosomal NPs can be used as an efficient treatment for ALD.

Ethnopharmacological evidence has demonstrated that Terminalia chebula Retz is traditionally employed for the management of hepatic ailments. Presently, a significant number of prevalent diseases and nutritional disorders are managed through the utilization of natural remedies. The efficacy of herbal medications relies on the administration of a sufficient dosage of the therapeutically active component. However, there is a significant constraint in terms of their bioavailability when taken via oral or topical routes. Phytosomes are a novel class of herbal formulations that have been recently introduced. These formulations exhibit enhanced absorption properties, leading to improved bioavailability and efficacy compared to traditional phyto compounds or botanical extracts. The objective of the current investigation was to assess the qualitative and quantitative phytochemical analysis, high-performance liquid chromatography, optical microscopic research, and in vitro antioxidant properties of Terminalia chebula Retz leaves obtained from the Bhopal region of Madhya Pradesh. The hydroalcoholic extract of phytosome was prepared using a mixture of phospholipids and cholesterol. The characterization of phytosome was conducted using various analytical techniques, including Fourier-transform infrared spectroscopy, determination of entrapment efficiency, measurement of particle size and size distribution, examination under an optical microscope, high-performance liquid chromatography analysis. The concurrent utilization of phospholipids and Terminalia chebula Retz has the potential to produce a synergistic outcome. This synergistic effect can be assessed by evaluating the free radical scavenging activity using the DPPH model. [ABSTRACT FROM AUTHOR]

Background: Berberine is a poorly absorbed natural alkaloid widely used as nutraceutical to counteract diarrhoea and to lower cholesterol and hyperglycaemia. It has also been reported to reduce signs and symptoms of polycystic ovary syndrome (PCOS).Objective: To explore, through a multi-centric, randomized, controlled and prospective study, the possible role played by a form berberine that is more easily absorbed (Berberine Phytosome®, BP) in 130 Pakistani women with a diagnosis of PCOS and fertility problems due to menstrual and ovary abnormalities.Results: Ninety days of supplementation with BP, administered at 550 mg x2/die, determined (i) resumption of regular menstruation in about 70% of women (versus 16% in the control group; p < 0.0001), (ii) normalization of the ovaries anatomy in more than 60% of women (versus 13% in the control group; p < 0.0001), (iii) acne improvement in 50% of women (versus 16% in the control group; p = 0.0409) and (iv) hirsutism reduction in 14% of women (versus 0% in the control group; p = 0.0152). The metabolic and the hormonal profiles of the women in the two groups did not significantly differentiate at the end of the study. BP was well-tolerated and no specific side-effects were registered. Respectively after one, two and 8 years of trying, three women supplemented with BP became and are currently pregnant.Conclusion: Our study showed the positive effects of BP supplementation in women with PCOS and confirmed the high safety profile of this nutraceutical.Clinical Trial Registration:https://clinicaltrials.gov/, identifier NCT05480670

Introduction: Silymarin proved to be a beneficial herbal medicine against many hepatic disorders such as alcoholic liver disease (ALD). However, its application is restricted due to its low bioavailability and consequently decreased efficacy. We herein used a nano-based approach known as "phytosome", to improve silymarin bioavailability and increase its efficacy. Methods: Phytosome nanoparticles (NPs) were synthesized using thin film hydration method. NPs size, electrical charge, morphology, stability, molecular interaction, entrapment efficiency (EE %) and loading capacity (LC %) were determined. Moreover, in vitro toxicity of NPs was investigated on mesenchymal stem cells (MSCs) viability using MTT assay. In vivo experiments were performed using 24 adult rats that were divided into four groups including control, ethanol (EtOH) treatment, silymarin/EtOH treatment and silymarin phytosome/EtOH, with 6 mice in each group. Experimental groups were given 40% EtOH, silymarin (50 mg/kg) and silymarin phytosome (200 mg/kg) through the gastric gavage once a day for 3 weeks. Biochemical parameters, containing ALP, ALT, AST, GGT, GPx and MDA were measured before and after experiment to investigate the protective effect of silymarin and its phytosomal form. And histopathological examination was done to evaluate pathological changes. Results: Silymarin phytosome NPs with the mean size of 100 nm were produced and were well tolerated in cell culture. These NPs showed a considerable protective effect against ALD through inverting the biochemical parameters (ALP, ALT, AST, GGT, GPx) and histopathological alterations Conclusion: Silymarin phytosomal NPs can be used as an efficient treatment for ALD. [ABSTRACT FROM AUTHOR]

Hyperglycemia, a common metabolic abnormality associated with diabetes mellitus, is primarily brought on by insufficient insulin synthesis at the cellular level or/and errors in insulin action. Such an endocrine condition causes major health issues and is spreading rapidly around the globe. The widespread control of diabetes with oral drug administration without producing any side effects is still regarded as a difficult undertaking, and the rising cost of traditional treatment in developing nations is another issue of concern. Traditional preparations of herbal plant extracts in the form of medications have already drawn a lot of attention in an effort to treat these problems. Locals use the crude extract of Swertia chirayita and Zizyphus mauritiana, two prominent Nepalese medicinal plants, for a variety of ailments, including type 2 diabetes. The current study's objectives were hydroalcoholic extract extraction of plant material, phytochemical analysis of Swertia chirayita and Zizyphus mauritiana, and formulation, development, and assessment of phytosomes. This study confirms the glucose tolerance activity with help of phytosomes containing the extracts of Swertia chirayita and Zizyphus mauritiana. The increase in blood glucose level can be controlled with help of phytosomes containing these extracts, along with it phytosomes showed a sustained release activity that best fitted with Korsmeyer peppas model. [ABSTRACT FROM AUTHOR]

Background: To enhance the therapeutic potential of Tinospora cordifolia phytosomes, a chloroform extract was prepared. Objectives: The goal of this study was to create and test the therapeutic potential of a phytosome containing T. cordifolia extract. Materials and Methods: The extraction of nonpolar compounds was carried out using chloroform as solvent. The active constituent of the extract was subjected to phytochemical and Gas Chromatography–Mass Spectrometry (GC–MS) analyses. Docking studies against multiple targeted proteins confirmed the anti-diabetic, anti-inflammatory, and analgesic properties of T. cordifolia extract. The phytosomes of T. cordifolia extract were prepared by solvent evaporation technique. The phytosomes were characterized for vesicle size, entrapment efficiency, surface morphology, FTIR, in vitro drug release and in vivo anti-diabetic, anti-inflammatory, and analgesic activities. Results: The highest concentration was found to be 16.58% for epiyangambin. The reported compound inhibits GLUT1 and COX2 with 9.25 and 8.34 kcal/mol binding scores. The optimized TCP4 exhibited 454.2 ± 8.1 nm of vesicle size, –43.1 ± 7.5 mV of zeta potential, and 0.33 of polydispersity index (PDI). The phytosomes exhibited a spherical shape confirmed by TEM analysis. The formulation TCP4 showed a significantly higher release (94.7% ± 1.7%) than pure extract. TCP4 exhibited potent therapeutic potential for anti-diabetic, anti-inflammatory, and analgesic activity. Conclusion: Chloroform extract loaded phytosomes with cholesterol as lipids exhibited significant therapeutic potential due to the presence of epiyangambin. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

Prostate cancer (PC) is emerging as one of the leading causes of mortality and morbidity worldwide. Curcumin (CUR) is a well-known phytochemical, and scorpion venom (SV) is a natural peptide with proven anticancer properties. However, these natural bioactive agents are limited by low solubility, low bioavailability, poor thermal stability, and short half-lives. Therefore, the aim of this study was to fabricate SV-conjugated CUR phytosomes as promising functionalized nanovesicles and assess their anticancer efficacy in human prostatic cancer PC3 cells. CUR-Phytosome-SV was fabricated using experimental design software in which the zeta potential and particle sizes were used as dependent variables. The anticancer effect of the fabricated formulation was determined by performing a tetrazolium (MTT) assay, cell cycle analysis, annexin V staining, and examining the expression levels of Bcl-associated X-protein (Bax), p53, caspase-3, B-cell lymphoma 2 (Bcl-2), nuclear factor kappa beta (NF-kB), and tumor necrosis factor alpha (TNF-α). The particle size of the nanoconjugates was found to be in the range of 137.5 ± 7.9 to 298.4 ± 11.9 nm, and the zeta potential was 2.9 ± 0.1 to 26.9 ± 1.2 mV. The outcome of the MTT assay showed that curcumin–Phospholipon®–scorpion venom (CUR–PL–SV) exhibited a satisfactory level of cytotoxicity, and the IC50 was found to be lower than CUR and PL-SV individually. Cell cycle analysis showed predominantly cell cycle arrest at the G2-M and pre-G1 phases. In contrast, annexin V staining showed significant early and late apoptosis events in addition to increased necrosis when PC3 cells were treated with CUR–PL–SV. Reverse-transcriptase polymerase chain reaction (RT-PCR) analysis showed a reduction in expression of Bax, p53, caspase-3, NF-kB, TNF-α, and an increase in Bcl-2 expression. Moreover, a MMP analysis showed a reduction in mitochondrial permeability and hence confirmed the superior anticancer potential of CUR–PL–SV. Thus, the present study showed significant anticancer potency of SV-conjugated CUR phytosomes against human prostatic cancer PC3 cells, making it a novel treatment approach for PC.

Human diseases are characterized by the perpetuation of an inflammatory condition in which the levels of Reactive Oxygen Species (ROS) are quite high. Excessive ROS production leads to DNA damage, protein carbonylation and lipid peroxidation, conditions that lead to a worsening of inflammatory disorders. In particular, compromised mitochondria sustain a stressful condition in the cell, such that mitochondrial dysfunctions become pathogenic, causing human disorders related to inflammatory reactions. Indeed, the triggered inflammation loses its beneficial properties and turns harmful if dysregulation and dysfunctions are not addressed. Thus, reducing oxidative stress with ROS scavenger compounds has proven to be a successful approach to reducing inflammation. Among these, natural compounds, in particular, polyphenols, alkaloids and coenzyme Q10, thanks to their antioxidant properties, are capable of inhibiting the activation of NF-κB and the expression of target genes, including those involved in inflammation. Even more, clinical trials, and in vivo and in vitro studies have demonstrated the antioxidant and anti-inflammatory effects of phytosomes, which are capable of increasing the bioavailability and effectiveness of natural compounds, and have long been considered an effective non-pharmacological therapy. Therefore, in this review, we wanted to highlight the relationship between inflammation, altered mitochondrial oxidative activity in pathological conditions, and the beneficial effects of phytosomes. To this end, a PubMed literature search was conducted with a focus on various in vitro and in vivo studies and clinical trials from 2014 to 2022. [ABSTRACT FROM AUTHOR]

Abstract Background This research was performed to synthesize nanophytosome-loaded high phenolic fraction (HPF) from Juniperus polycarpos fruit extract and investigate its antiproliferation effects against breast cancer in mice model. Results The nanophytosome-loaded HPF from Juniperus polycarpos fruit extract was synthesized. The mice trial was conducted to determine the possible toxic effects of the synthesized nanophytosomes. The anticancer, pro-apoptotic, and antioxidative activities of the nanophytosomes were determined. The nanophytosome-loaded HPF had a spherical structure with a size of 176 nm and a polydispersity index coefficient of 0.24. The in vivo study manifested that nanophytosome-loaded HPF significantly improved weight gain and food intake compared to the negative control group (p

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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. [ABSTRACT FROM AUTHOR]

Prostate cancer (PC) is emerging as one of the leading causes of mortality and morbidity worldwide. Curcumin (CUR) is a well-known phytochemical, and scorpion venom (SV) is a natural peptide with proven anticancer properties. However, these natural bioactive agents are limited by low solubility, low bioavailability, poor thermal stability, and short half-lives. Therefore, the aim of this study was to fabricate SV-conjugated CUR phytosomes as promising functionalized nanovesicles and assess their anticancer efficacy in human prostatic cancer PC3 cells. CUR-Phytosome-SV was fabricated using experimental design software in which the zeta potential and particle sizes were used as dependent variables. The anticancer effect of the fabricated formulation was determined by performing a tetrazolium (MTT) assay, cell cycle analysis, annexin V staining, and examining the expression levels of Bclassociated X-protein (Bax), p53, caspase-3, B-cell lymphoma 2 (Bcl-2), nuclear factor kappa beta (NFkB), and tumor necrosis factor alpha (TNF-a). The particle size of the nanoconjugates was found to be in the range of 137.5 ± 7.9 to 298.4 ± 11.9 nm, and the zeta potential was 2.9 ± 0.1 to 26.9 ± 1.2 mV. The outcome of the MTT assay showed that curcumin-PhospholiponVR -scorpion venom (CUR-PL-SV) exhibited a satisfactory level of cytotoxicity, and the IC50 was found to be lower than CUR and PL-SV individually. Cell cycle analysis showed predominantly cell cycle arrest at the G2-M and pre-G1 phases. In contrast, annexin V staining showed significant early and late apoptosis events in addition to increased necrosis when PC3 cells were treated with CUR-PL-SV. Reverse-transcriptase polymerase chain reaction (RT-PCR) analysis showed a reduction in expression of Bax, p53, caspase-3, NF-kB, TNF-a, and an increase in Bcl-2 expression. Moreover, a MMP analysis showed a reduction in mitochondrial permeability and hence confirmed the superior anticancer potential of CUR-PL-SV. Thus, the present study showed significant anticancer potency of SV-conjugated CUR phytosomes against human prostatic cancer PC3 cells, making it a novel treatment approach for PC. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

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

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.

Background: This research was performed to synthesize nanophytosome-loaded high phenolic fraction (HPF) from Juniperus polycarpos fruit extract and investigate its antiproliferation effects against breast cancer in mice model. Results: The nanophytosome-loaded HPF from Juniperus polycarpos fruit extract was synthesized. The mice trial was conducted to determine the possible toxic effects of the synthesized nanophytosomes. The anticancer, pro-apoptotic, and antioxidative activities of the nanophytosomes were determined. The nanophytosome-loaded HPF had a spherical structure with a size of 176 nm and a polydispersity index coefficient of 0.24. The in vivo study manifested that nanophytosome-loaded HPF significantly improved weight gain and food intake compared to the negative control group (p < 0.05). The nanophytosome-loaded HPF significantly enhanced the expression of bax (3.4-fold) and caspase-3 (2.7-fold) genes, but reduced bcl2 (3.6-fold) gene expression in tumor cells. The average tumor size was significantly decreased in mice treated with nanophytosome-loaded HPF (p < 0.05). The expression of GPX (2.3-fold) and SOD (2.7-fold) antioxidants in the liver of mice supplemented with nanophytosome-loaded HPF was significantly developed compared to the negative control (p < 0.05). The nanophytosome-loaded HPF did not show toxicity on normal cells. Conclusion: Our results indicated that nanophytosome-loaded HPF might be a potential anticancer agent for the breast cancer treatment. [ABSTRACT FROM AUTHOR]

[Display omitted] • Development of a GE-PL complex with promising in vitro and in vivo oral bioavailability enhancements. • The GE-PL complex exhibits optimal physical–chemical characteristics. • GE-PL complex formulation prolongs the presence of EA in the bloodstream, leading to higher oral bioavailability and improved pharmacokinetics. Geraniin (GE), an ellagitannin (ET) renowned for its promising health advantages, faces challenges in its practical applications due to its limited bioavailability. This innovative and novel formulation of GE and soy-phosphatidylcholine (GE-PL) complex has the potential to increase oral bioavailability, exhibiting high entrapment efficiency of 100.2 ± 0.8 %, and complexation efficiency of 94.6 ± 1.1 %. The small particle size (1.04 ± 0.11 μm), low polydispersity index (0.26 ± 0.02), and adequate zeta potential (−26.1 ± 0.12 mV), indicate its uniformity and stability. Moreover, the formulation also demonstrates improved lipophilicity, reduced aqueous and buffer solubilities, and better partition coefficient. It has been validated by various analytical techniques, including Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) studies. Oral bioavailability and pharmacokinetics of free GE and GE-PL complex investigated in rabbits demonstrated enhanced plasma concentration of ellagic acid (EA) compared to free GE. Significantly, GE, whether in its free form or as part of the GE-PL complex, was not found in the circulatory system. However, EA levels were observed at 0.5 h after administration, displaying two distinct peaks at 2 ± 0.03 h (T1 max) and 24 ± 0.06 h (T2 max). These peaks corresponded to peak plasma concentrations (C1 max and C2 max) of 588.82 ng/mL and 711.13 ng/mL respectively, signifying substantial 11-fold and 5-fold enhancements when compared to free GE. Additionally, it showed an increased area under the curve (AUC), the elimination half-life (t 1/2 , el) and the elimination rate constant (K el). The formulation of the GE-PL complex prolonged the presence of EA in the bloodstream and improved its absorption, ultimately leading to a higher oral bioavailability. In summary, the study highlights the significance of the GE-PL complex in overcoming the bioavailability limitations of GE, paving the way for enhanced therapeutic outcomes and potential applications in drug delivery and healthcare. [ABSTRACT FROM AUTHOR]

Human diseases are characterized by the perpetuation of an inflammatory condition in which the levels of Reactive Oxygen Species (ROS) are quite high. Excessive ROS production leads to DNA damage, protein carbonylation and lipid peroxidation, conditions that lead to a worsening of inflammatory disorders. In particular, compromised mitochondria sustain a stressful condition in the cell, such that mitochondrial dysfunctions become pathogenic, causing human disorders related to inflammatory reactions. Indeed, the triggered inflammation loses its beneficial properties and turns harmful if dysregulation and dysfunctions are not addressed. Thus, reducing oxidative stress with ROS scavenger compounds has proven to be a successful approach to reducing inflammation. Among these, natural compounds, in particular, polyphenols, alkaloids and coenzyme Q10, thanks to their antioxidant properties, are capable of inhibiting the activation of NF-κB and the expression of target genes, including those involved in inflammation. Even more, clinical trials, and in vivo and in vitro studies have demonstrated the antioxidant and anti-inflammatory effects of phytosomes, which are capable of increasing the bioavailability and effectiveness of natural compounds, and have long been considered an effective non-pharmacological therapy. Therefore, in this review, we wanted to highlight the relationship between inflammation, altered mitochondrial oxidative activity in pathological conditions, and the beneficial effects of phytosomes. To this end, a PubMed literature search was conducted with a focus on various in vitro and in vivo studies and clinical trials from 2014 to 2022.

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. [ABSTRACT FROM AUTHOR]

Background and purpose: Vasicine is a potential bronchodilator and can be used for the effective management of asthma and bronchitis. It has low absorption in the gastrointestinal tract due to its poor solubility thereby low bioavailability. The objective of this research was to develop a novel drug delivery system of vasaka extract to improve its bioavailability by enhancing the solubility and absorption of vasicine. Experimental approach: Vasaka-loaded phytosomes were developed and optimized by thin-layer hydration technique using systematic quality by design approach. Box-Behnken design (32 factorial design) using Design-Expert software was employed to optimize phytosome wherein phosphatidylcholine concentration (X1), stirring temperature (X2), and stirring time (X3) were selected as independent variables. Yield (%), particle size (nm), and entrapment efficiency (%) were evaluated as responses. The optimized phytosome was characterized by studying the surface morphology such as FE-SEM and TEM analysis, thermal characteristics by thermal gravimetric analysis and spectral and diffraction studies by FTIR and XRD analysis and studying the dissolution behaviour of phytosome by in vitro release study. Findings/Results: The percentage yield, particle size, and entrapment efficiency values of the phytosomes were found in the range of 30.03-97.03%, 231.0-701.4 nm, and 20.02-95.88% w/w, respectively. The optimized phytosome showed the zeta potential of -23.2 mV exhibited good stability and SEM and TEM analysis revealed the spherical shape and smooth particles with the uniform particle size distribution of phytosomes. The comparative in vitro drug release study of vasaka extract and phytosome revealed the sustained release characteristics of phytosome which reached 68.80% at 8 h compared to vasaka extract reached a maximum of 45.08% at 4 h. Conclusion and implication: The results highlighted the importance of optimization of formulation development using quality by design strategy to achieve consistent quality of pharmaceutical products.

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

Transdermal drug delivery aims to create a safe and effective method of administering drugs through the skin that attracts a lot of attention and investment due to the constant progress in the field. Transferosomes are flexible or malleable vesicles (having almost the same structure as liposomes but with better skin penetration properties) discovered initially in the early 90s. The name transferosomes, which means "carrying bodies," is coined from the Latin phrase "Transferee," which means "to carry through," and the Greek term "soma," meaning "body." In comparison to typical herbal extracts, phytosomes (Transferosomes) are created by attaching specific herbal extracts to phosphatidylcholine, resulting in a formulation with increased solubility and, hence, better absorption, resulting in improved pharmacokinetic and pharmacodynamic features of the entrapped drugs. We are using the word phytosomes and transferosomes interchangeably as we have consolidated vesicular delivery of herbal drugs through skin. In this mini-review, we have demonstrated the enormous potential of developing nanotechnology to deliver bioactive phytochemicals, with a special emphasis on phytosomes (Transferosomes) as a unique lipid-based nanocarrier for transdermal drug delivery. [ABSTRACT FROM AUTHOR]

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 /cm2/hour. To sum up, phytosomes can inhibit weight gain and are better than to green tea extracts (p < 0.05).

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.

Transdermal drug delivery aims to create a safe and effective method of administering drugs through the skin that attracts a lot of attention and investment due to the constant progress in the field. Transferosomes are flexible or malleable vesicles (having almost the same structure as liposomes but with better skin penetration properties) discovered initially in the early 90s. The name transferosomes, which means “carrying bodies,” is coined from the Latin phrase “Transferee,” which means “to carry through,” and the Greek term “soma,” meaning “body.” In comparison to typical herbal extracts, phytosomes (Transferosomes) are created by attaching specific herbal extracts to phosphatidylcholine, resulting in a formulation with increased solubility and, hence, better absorption, resulting in improved pharmacokinetic and pharmacodynamic features of the entrapped drugs. We are using the word phytosomes and transferosomes interchangeably as we have consolidated vesicular delivery of herbal drugs through skin. In this mini-review, we have demonstrated the enormous potential of developing nanotechnology to deliver bioactive phytochemicals, with a special emphasis on phytosomes (Transferosomes) as a unique lipid-based nanocarrier for transdermal drug delivery.