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1.
Cell Mol Biol (Noisy-le-grand) ; 70(8): 235-243, 2024 Sep 08.
Artigo em Inglês | MEDLINE | ID: mdl-39262266

RESUMO

Recent research has emphasized the development of efficient drug delivery systems to facilitate the delivery of biological compounds such as polyphenols via skin absorption. Phytozomes have been employed as carriers of plant compounds in this context Hydrogen bonding between plant polyphenols and the phospholipid phosphate group enables efficient encapsulation of potent compounds for enhanced drug delivery systems. Additionally, the strong affinity of phytosomes for the skin's phospholipids enhances skin absorption. In this study, phytosomes were initially formulated using the thin-layer hydration method After optimizing the synthetic parameters, phytosomes were loaded with Resveratrol and Quercetin for enhanced delivery and skin absorption potential to assess the characteristics of the synthesized phytosomes, tests were conducted to determine particle distribution and size, zeta potential, and examine the microstructure morphology using a scanning electron microscope (SEM). Furthermore, a siloxane gel base was formulated in this study, and the stability of the physicochemical and biological properties of the final prepared nanoformulation was investigated. The results of this study indicated that the formulated phytosomes exhibit optimal characteristics for facilitating high skin penetration of resveratrol and quercetin. A high skin absorption was observed after 60 days of synthesis. Additionally, the base of the siloxane gel can play a significant role in preventing the formation of scars by reducing the passage of water vapor.


Assuntos
Cicatriz , Géis , Quercetina , Resveratrol , Siloxanas , Resveratrol/química , Resveratrol/administração & dosagem , Resveratrol/farmacocinética , Géis/química , Siloxanas/química , Quercetina/química , Quercetina/administração & dosagem , Quercetina/farmacocinética , Absorção Cutânea/efeitos dos fármacos , Tamanho da Partícula , Animais , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Pele/metabolismo , Pele/efeitos dos fármacos , Compostos Fitoquímicos/química , Fitossomas
2.
J Oleo Sci ; 73(9): 1213-1220, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39218638

RESUMO

The aim of present work was to develop and evaluate Ampelopsis Radix ethanolic extract loaded phytosomes for improved efficacy in colorectal cancer. Ampelopsis Radix ethanolic extract was prepared by Soxhlet extraction process followed by development of phytosomes using lipids and other excipients. The phytosomes were evaluated for surface morphology, particle size analysis, zeta potential, encapsulation efficiency, drug loading, in vitro drug release, Cytotoxicity assay, cellular uptake studies were performed on HCT-116 and SW480 cell lines. In vivo antitumor activity was performed. The phytosomes were found spherical shape with smooth surface characteristics. The drug loading was observed between 29.27 to 42.10 % while particle size of 85 to 130 nm was found. Phytosomes showed desired release pattern which is required for cancer treatment. Phytosomes showed maximum antiproliferative activity on cell lines over the period of 24 hours and showed highest internalization within both types of cell lines. The survival rate of animals in phytosomes treated group was found to be 100% proving the safety and efficacy. Phytosomes showed highest antitumor activity as compared to other formulations. Study confirms the potential use Ampelopsis Radix ethanolic extract loaded phytosomes for improved efficacy in colorectal cancer.


Assuntos
Ampelopsis , Neoplasias Colorretais , Etanol , Extratos Vegetais , Neoplasias Colorretais/tratamento farmacológico , Neoplasias Colorretais/patologia , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Etanol/química , Animais , Ampelopsis/química , Células HCT116 , Tamanho da Partícula , Liberação Controlada de Fármacos , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Camundongos , Proliferação de Células/efeitos dos fármacos , Fitoterapia , Fitossomas
3.
Int J Mol Sci ; 25(8)2024 Apr 09.
Artigo em Inglês | MEDLINE | ID: mdl-38673748

RESUMO

Metabolic disorders (MDs), including dyslipidemia, non-alcoholic fatty liver disease, diabetes mellitus, obesity and cardiovascular diseases are a significant threat to human health, despite the many therapies developed for their treatment. Different classes of bioactive compounds, such as polyphenols, flavonoids, alkaloids, and triterpenes have shown therapeutic potential in ameliorating various disorders. Most of these compounds present low bioavailability when administered orally, being rapidly metabolized in the digestive tract and liver which makes their metabolites less effective. Moreover, some of the bioactive compounds cannot fully exert their beneficial properties due to the low solubility and complex chemical structure which impede the passive diffusion through the intestinal cell membranes. To overcome these limitations, an innovative delivery system of phytosomes was developed. This review aims to highlight the scientific evidence proving the enhanced therapeutic benefits of the bioactive compounds formulated in phytosomes compared to the free compounds. The existing knowledge concerning the phytosomes' preparation, their characterization and bioavailability as well as the commercially available phytosomes with therapeutic potential to alleviate MDs are concisely depicted. This review brings arguments to encourage the use of phytosome formulation to diminish risk factors inducing MDs, or to treat the already installed diseases as complementary therapy to allopathic medication.


Assuntos
Doenças Metabólicas , Compostos Fitoquímicos , Animais , Humanos , Disponibilidade Biológica , Terapias Complementares/métodos , Doenças Metabólicas/tratamento farmacológico , Compostos Fitoquímicos/administração & dosagem , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Fitossomas , Polifenóis/química , Polifenóis/farmacologia , Polifenóis/administração & dosagem
4.
Recent Pat Anticancer Drug Discov ; 19(2): 154-164, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38214355

RESUMO

BACKGROUND: Multidrug resistance (MDR) of cancer cells is a major obstacle to efficient cancer chemotherapy. Combination therapy is expected to enhance the anticancer effect and reverse MDR. Numerous patents involve different kinds of nanoparticles for the co-delivery of multiple chemotherapeutics, but the FDA has approved none. OBJECTIVE: In this study, oxymatrine (OMT) and glycyrrhizin (GL) were co-loaded into phytosomes as the core of nanocarriers, and the shell was cross-linked with chitosan (CS) and hyaluronic acid (HA) with the capability for the controlled, sequential release and the targeted drug uptake. METHODS: Phospholipid complexes of OMT and GL (OGPs) were prepared by a solvent evaporation technique and could self-assemble in an aqueous solution to form phytosomes. CS and HA were sequentially coated on the surface of OGPs via electrostatic interactions to obtain CS coated OGPs (CS-OGPs) and HA modified CS-OGPs (HA-CS-OGPs), respectively. The particle size and zeta potential were measured to optimize the formulations. In vitro cytotoxicity and cellular uptake experiments on HepG2 cells were performed to evaluate the anticancer activity. RESULTS: OGPs were obtained with nano-size around 100 nm, and CS and HA coating on phytosomes could change the particle size and surface potential. The drug loading of OMT and GL showed that the nanocarriers could maintain a fixed ratio of 1:1. The in vitro release experiments indicated the release of OMT and GL was pH-dependent and sequential: the release of OMT from CS-OGPs and HA-CS-OGPs was significantly increased at pH 5.0 compared to the release at pH 7.4, while GL exhibited sustained released from CS-OGPs and HA-CS-OGPs at pH 5.0. Furthermore, in vitro cytotoxicity and cellular uptake experiments on HepG2 cells demonstrated that the co-delivery system based on phytosomes had significant synergistic anti-tumor activities, and the effects were enhanced by CS and HA modification. CONCLUSION: The delivery of OMT and GL via HA-CS-OGPs might be a promising treatment to reverse MDR in cancer therapy.


Assuntos
Quitosana , Matrinas , Nanopartículas , Humanos , Quitosana/química , Fitossomas , Ácido Hialurônico/química , Ácido Glicirrízico/farmacologia , Ácido Glicirrízico/química , Patentes como Assunto , Sistemas de Liberação de Medicamentos/métodos , Portadores de Fármacos/química
5.
Int J Biol Macromol ; 256(Pt 2): 128501, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38040148

RESUMO

Nano-carriers are well-known delivery systems to encapsulate different bioactive compounds and extracts. Such nano-systems are used in various food and drug areas to protect active ingredients, increase bioavailability, control the release, and deliver bioactive substances. This study aimed to design and fabricate a stable colloidal nano-delivery system to better preserve the antioxidant properties of pomegranate peel extract (PPE) and protect its sustained release in a gastrointestinal model. To achieve this goal, a nano-phytosomal system was fabricated with plant-based, cost-effective, and food-grade compounds, i.e., phosphatidylcholine (PC) and gamma-oryzanol (GO) for encapsulation of PPE. To fabricate the nano-phytosomes, thin film hydration/sonication method was used. The parameters of particle size, zeta potential, polydispersity index (PDI), loading capacity (LC), and encapsulation efficiency (EE) were investigated to evaluate the efficiency of the produced nano-system. In summary, the size, zeta potential, PDI, LC, and EE of homogenous spherical PC-GO-PPE nano-phytosomes (NPs) in the ratio of 8:2:2 % w/w were achieved as 60.61 ± 0.81 nm, -32.24 ± 0.84 mV, 0.19 ± 0.01, 19.13 ± 0.30 %, and 95.66 ± 1.52 %, respectively. Also, the structure of NPs was approved by Fourier transform infrared spectroscopy (FT-IR) and scanning electron microscope (SEM). The optimized NPs were stable during one month of storage at 4 °C, and changes in the size of particles and PPE retention rate were insignificant (p > 0.05). The nano-encapsulation of PPE significantly decreased the loss of its antioxidant activity during one month of storage at 4 °C. The optimized NPs exhibited prolonged and sustained release of PPE in a gastrointestinal model, so that after 2 h in simulated gastric fluid (SGF) and 4 h in simulated intestinal fluid (SIF), 22.66 ± 2.51 % and 69.33 ± 4.50 % of initially loaded PPE was released, respectively. Optimized NPs had considerable cytotoxicity against the Michigan Cancer Foundation-7 cell line (MCF7) (IC50 = 103 µg/ml), but not against Human Foreskin Fibroblast cell line (HFF-2) (IC50 = 453 µg/ml). In conclusion, spherical PC-GO-PPE NPs were identified as a promising delivery system to efficiently encapsulate PPE, as well as protect and preserve its bioactivity, including antioxidant and cytotoxicity against cancer cell line.


Assuntos
Neoplasias , Fenilpropionatos , Punica granatum , Humanos , Punica granatum/química , Antioxidantes/química , Polifenóis/farmacologia , Polifenóis/metabolismo , Fitossomas , Fosfatidilcolinas/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier , Preparações de Ação Retardada , Extratos Vegetais/química
6.
Curr Pharm Des ; 29(38): 3073-3086, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37961864

RESUMO

AIM: This work aimed to elucidate the mechanisms of Se@Tri-PTs in alleviating podocyte injury via network pharmacology and in vitro cellular assay. BACKGROUND: Selenized tripterine phytosomes (Se@Tri-PTs) have been confirmed to undertake synergistic and sensitized effects on inflammation, which may be curatively promising for diabetic nephropathy (DN). However, the mechanisms of Se@Tri-PTs in alleviating podocyte injury, a major contributor to DN, still remain unclear. OBJECTIVE: The objective of the study was to find out the underlying mechanisms of Se@Tri-PTs in alleviating podocyte injury in diabetic nephropathy. METHODS: The key components and targets of Tripterygium wilfordii (TW) significant for DN as well as the signaling pathways involved have been identified. A high glucose-induced podocyte injury model was established and verified by western blot. The protective concentration of Se@Tri-PTs was screened by CCK-8 assay. Podocytes cultured with high glucose were treated with Se@Tri-PTs under protective levels. The expression of key protective proteins, nephrin and desmin, in podocytes, was assayed by western blot. Further, autophagy- related proteins and factors, like NLRP3, Beclin-1, LC3II/LC3, P62, and SIRT1, were analyzed, which was followed by apoptosis detection. RESULTS: Network pharmacology revealed that several monomeric components of TW, especially Tri, act on DN through multiple targets and pathways, including the NLRP3-mediated inflammatory pathway. Se@Tri-PTs improved the viability of podocytes and alleviated their injury induced by high glucose at 5 µg/L or above. High-glucose induction promoted the expression of NLRP3 in podocytes, while a low concentration of Se@Tri-PTs suppressed the expression. A long-term exposure of high glucose significantly inhibited the autophagic activity of podocytes, as manifested by decreased Beclin-1 level, lower ratio of LC3 II/LC3 I, and up- regulation of P62. This abnormality was efficiently reversed by Se@Tri-PTs. Importantly, the expression of SIRT1 was up-regulated and podocyte apoptosis was reduced. CONCLUSION: Se@Tri-PTs can alleviate podocyte injury associated with DN by modulating NLRP3 expression through the pathway of SIRT1-mediated autophagy.


Assuntos
Diabetes Mellitus , Nefropatias Diabéticas , Podócitos , Humanos , Podócitos/metabolismo , Nefropatias Diabéticas/tratamento farmacológico , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Fitossomas , Sirtuína 1/metabolismo , Proteína Beclina-1/farmacologia , Farmacologia em Rede , Glucose/metabolismo , Diabetes Mellitus/metabolismo
7.
Int J Nanomedicine ; 18: 5749-5780, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37849641

RESUMO

Background: 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.


Assuntos
Fitossomas , Cicatrização , Animais , Simulação de Acoplamento Molecular , Espectroscopia de Infravermelho com Transformada de Fourier , Fosfolipídeos , Tamanho da Partícula
8.
Genes (Basel) ; 14(8)2023 07 28.
Artigo em Inglês | MEDLINE | ID: mdl-37628599

RESUMO

The application of nano drug delivery systems, particularly those utilizing natural bioactive compounds with anticancer properties, has gained significant attention. In this study, a novel nano-phytosome-loaded phenolic rich fraction (PRF) derived from Allium ampeloprasum L. was developed. The antitumor activity of the formulation was evaluated in BALB/c mice with TUBO colon carcinoma. The PRF-loaded nano-phytosome (PRF-NPs) exhibited a sphere-shaped structure (226 nm) and contained a diverse range of phenolic compounds. Animal trials conducted on TUBO tumor-bearing mice demonstrated that treatment with PRF-NPs at a dosage of 50 mg TPC/Kg/BW resulted in significant improvements in body weight and food intake, while reducing liver enzymes and lipid peroxidation. The expression of apoptosis-related genes, such as Bax and caspase-3, was upregulated, whereas Bcl2 was significantly downregulated (p < 0.05). Furthermore, the expression of GPx and SOD genes in the liver was notably increased compared to the control group. The findings suggest that the phytosomal encapsulation of the phenolic rich fraction derived from Allium ampeloprasum L. can enhance the bioavailability of natural phytochemicals and improve their antitumor properties. The development of PRF-NPs as a nano drug delivery system holds promise for effective breast cancer treatment.


Assuntos
Allium , Regulação da Expressão Gênica , Allium/química , Apoptose/efeitos dos fármacos , Antioxidantes/farmacologia , Fitossomas , Extratos Vegetais/farmacologia , Fenóis/farmacologia , Nanoestruturas , Feminino , Animais , Camundongos , Camundongos Endogâmicos BALB C , Peroxidação de Lipídeos , Fígado/efeitos dos fármacos , Fígado/enzimologia , Peso Corporal , Antineoplásicos/farmacologia , Regulação da Expressão Gênica/efeitos dos fármacos
9.
Cells ; 12(15)2023 08 04.
Artigo em Inglês | MEDLINE | ID: mdl-37566078

RESUMO

Extracellular vesicle (EV) research has expanded substantially over the years. EVs have been identified in all living organisms and are produced and released as a means of intercellular communication or as a defense mechanism. Recently, nano-scaled vesicles were successfully isolated from edible plant sources. Plant-derived EVs, referred to here as phytosomes, are of a size reported to range between 30 nm and 120 nm in diameter, similar to small mammalian extracellular vesicles, and carry various bioactive molecules such as mRNA, proteins, miRNA and lipids. Due to the availability of many plants, phytosomes can be easily isolated on a large scale. The methods developed for EV isolation from mammalian cells have been successfully applied for isolation and purification of phytosomes. The therapeutic effects of phytosomes on different disease models, such as inflammation and autoimmune disease, have been reported, and a handful of studies have suggested their therapeutic effects on cancer diseases. Overall, the research on phytosomes is still in its infancy and requires more exploration. This review will narrate the anti-cancer activity and characteristics of phytosomes derived from edible plants as well as describe studies which have utilized phytosomes as drug delivery vehicles for cancer with the ultimate objective of significantly reducing the adverse effects associated with conventional therapeutic approaches.


Assuntos
Exossomos , Vesículas Extracelulares , MicroRNAs , Neoplasias , Animais , Exossomos/metabolismo , Fitossomas , Vesículas Extracelulares/metabolismo , MicroRNAs/metabolismo , Sistemas de Liberação de Medicamentos/métodos , Mamíferos/genética , Neoplasias/metabolismo
10.
Int J Pharm ; 644: 123332, 2023 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-37625602

RESUMO

Rheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease associated with progressive articular damage, functional loss and comorbidity. Conventional RA therapy requires frequent dosing and prolonged use, and usually results in poor efficacy and severe toxicity. In the current study, for the first time, we describe a combination strategy using phytosomes co-loaded with curcumin (CUR) and leflunomide (LEF) to improve the clinical outcomes of RA therapy. Exploiting 23 factorial design, various compositions of CUR and LEF co-loaded phytosomes (CUR/LEF-phytosomes) were successfully prepared and were extensively characterized (e.g., particle size, zeta potential, drugs encapsulation efficiency, morphology, DSC, FTIR and release kinetics). The optimal CUR/LEF-loaded phytosomes (F2) demonstrated high stability and spherical morphology with a particle size of ca. 760 nm and negative zeta potential value of - 55.7, high entrapment for both drugs, and sustained release profile of the entrapped medications. In vivo, oral administration of the CUR/LEF-phytosomes (F2) in arthritic rats resulted in significant reduction of paw swelling and inflammatory markers, compared to the free drugs and their physical mixture. Histopathological examination revealed significant improvement in phytosomes-treated animal group with no signs of arthritis. CUR/LEF-loaded phytosomes provide an auspicious strategy for alleviation of RA.


Assuntos
Artrite Reumatoide , Curcumina , Animais , Ratos , Fitossomas , Artrite Reumatoide/tratamento farmacológico , Leflunomida , Administração Oral
11.
Eur J Pharm Biopharm ; 189: 174-188, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37343893

RESUMO

Nowadays, fisetin (FIS) is extensively studied as potent anticancer surrogate with a multitarget actions against various types of cancers including breast cancer. However, its poor aqueous solubility handicapped its clinical utility. The current work endeavored, for the first time, to develop FIS phytosomes (FIS-PHY) for improving its physicochemical properties and subsequently its anticancer activity. Optimization of FIS- phytosomes involved different preparation techniques (Thin film hydration and ethanol injection) and different FIS: phospholipid molar ratios (1:1, 1:2, and 1:3). Complex formation was confirmed by complexation efficiency, infrared spectroscopy (IR), solubility studies and transmission electron microscope. The optimized FIS-PHY of 1:1 M ratio (PHY1) exhibited a nanometric particle size of 233.01 ± 9.46 nm with homogenous distribution (PDI = 0.27), negative zeta potential of - 29.41 mV, 100% complexation efficiency and controlled drug release over 24 h. In-vitro cytotoxicity study showed 2.5-fold decrease in IC50 of PHY1 compared with free FIS. Also, pharmacodynamic studies confirmed the promoted cytotoxicity of PHY1 against breast cancer through modulating TGF-ß1/MMP-9 molecular pathways of tumorigenesis. Overall, overcoming FIS drawbacks were successfully achieved through development of innovative biocompatible phytosomal system.


Assuntos
Neoplasias da Mama , Fosfolipídeos , Humanos , Feminino , Fosfolipídeos/química , Fitossomas , Neoplasias da Mama/tratamento farmacológico , Flavonóis
12.
Molecules ; 28(6)2023 Mar 17.
Artigo em Inglês | MEDLINE | ID: mdl-36985711

RESUMO

Nephrotoxicity is a serious complication that limits the clinical use of gentamicin (GEN). Parthenolide (PTL) is a sesquiterpene lactone derived from feverfew with various therapeutic benefits. However, PTL possesses low oral bioavailability. This study aimed to evaluate the therapeutic protective effects of PTL-phytosomes against GEN-induced nephrotoxicity in rats. The PTL was prepared as phytosomes to improve the pharmacological properties with a particle size of 407.4 nm, and surface morphology showed oval particles with multiple edges. Rats were divided into six groups: control, nano-formulation plain vehicle, PTL-phytosomes (10 mg/kg), GEN (100 mg/kg), GEN + PTL-phytosomes (5 mg/kg), and GEN + PTL-phytosomes (10 mg/kg). The administration of PTL-phytosomes alleviated GEN-induced impairment in kidney functions and histopathological damage, and decreased kidney injury molecule-1 (KIM-1). The anti-oxidative effect of PTL-phytosomes was demonstrated by the reduced malondialdehyde (MDA) concentration and increased superoxide dismutase (SOD) and catalase (CAT) activities. Furthermore, PTL-phytosomes treatment significantly enhanced sirtuin 1 (Sirt-1), nuclear factor erythroid-2-related factor-2 (Nrf2), NAD(P)H quinone dehydrogenase 1 (NQO1), and heme oxygenase-1 (HO-1). Additionally, PTL-phytosomes treatment exhibited anti-inflammatory and anti-apoptotic properties in the kidney tissue. These findings suggest that PTL-phytosomes attenuate renal dysfunction and structural damage by reducing oxidative stress, inflammation, and apoptosis in the kidney.


Assuntos
Gentamicinas , Sesquiterpenos , Ratos , Animais , Gentamicinas/efeitos adversos , Fator 2 Relacionado a NF-E2/metabolismo , Fitossomas , Sirtuína 1/metabolismo , Rim , Antioxidantes/farmacologia , Sesquiterpenos/farmacologia , Sesquiterpenos/metabolismo , Estresse Oxidativo , NAD(P)H Desidrogenase (Quinona)/metabolismo
13.
Poult Sci ; 102(5): 102627, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36996511

RESUMO

This research examined the effects of feeding phytosomal green tea on broilers infected with coccidia. To provide phytosome, green tea extract was loaded into soy lecithin. Groups of chicks included uninfected and untreated control (NC), infected and untreated control (PC), infected and treated with salinomycin control (SC), infected and treated with 300 and 400 mL of green tea extract (GTE300, GTE400), infected and treated with 200, 300, 400 and 500 mL of green tea phytosome (GTP200, GTP300, GTP400, and GTP500). At 14-days posthatch, chickens were orally gavaged, except the NC group with a coccidia vaccine 30 times larger than the approved dose. Body weight (BW), feed intake (FI), and feed conversion ratio (FCR) were determined at 7, 14, 20, 28, 35, and 42 d. The characteristics of the carcass, internal organs and intestinal morphology were assessed on d 42. Applying overdose of coccidiosis vaccine showed experimental Eimeria infection, led to decrease in FI and BW, and increased FCR compared to PC group (P < 0.001). Meanwhile salinomycin, green tea extract, and green tea phytosome compensated the negative effects of Eimeria infection on growth performance. The treatments did not affect carcass, breast, and thigh relative weights. Interestingly, abdominal fat percent was significantly lower in chickens fed GTP300, GTP400, and GTP500 than in those fed GTE300, GTE300, and GTP200 (P < 0.0001). In comparison to the basal diet plus green tea extract forms and NC groups, the PC group increased the relative weights of the liver, spleen, bursa, and pancreas (P < 0.05). The highest values of villus height and villus height to crypt ratio were obtained in duodenum, jejunum and ileum in GTP300 group (P < 0.0001), while, villi diameter in duodenum and ileum decreased the most in GTP300 and GTP500, respectively (P < 0.0001). Consequently, as natural anticoccidial drug delivery systems, 300 mL of green tea phytosome can be introduced as the optimal dose to maximize the benefits of phytosome for intestinal integrity and reduce the consumption of green tea extract.


Assuntos
Coccidiose , Eimeria , Doenças das Aves Domésticas , Animais , Galinhas , Suplementos Nutricionais , Fitossomas , Chá , Coccidiose/prevenção & controle , Coccidiose/veterinária , Coccidiose/tratamento farmacológico , Dieta/veterinária , Peso Corporal , Ração Animal/análise , Doenças das Aves Domésticas/tratamento farmacológico , Doenças das Aves Domésticas/prevenção & controle
14.
J Microencapsul ; 40(3): 186-196, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36880280

RESUMO

PURPOSE: The study was aimed to encapsulate Hedyotis corymbosa extract (HCE) into phytosomes to improve its therapeutic efficacy in neuropathic pain by enhancing the bioavailability of chief chemical constituent Hedycoryside -A (HCA). METHODS: For preparing phytosomes complexes (F1, F2, and F3), HCE and phospholipids were reacted in disparate ratio. F2 was chosen to assess its therapeutic efficacy in neuropathic pain induced by partial sciatic nerve ligation. Nociceptive threshold and oral bioavailability were also estimated for F2. RESULTS: Particle size, zeta potential and entrapment efficiency for F2 were analysed as 298.1 ± 1.1 nm, -3.92 ± 0.41 mV and 72.12 ± 0.72% respectively. F2 gave enhanced relative bioavailability (158.92%) of HCA along with a greater neuroprotective potential showing a significant antioxidant effect and augmentation (p < 0.05) in nociceptive threshold with the diminution in damage to nerves. CONCLUSION: F2 is an optimistic formulation for enhancing the HCE delivery for the effective treatment of neuropathic pain.


Assuntos
Hedyotis , Neuralgia , Animais , Fitossomas , Roedores , Neuralgia/tratamento farmacológico
15.
Sci Rep ; 13(1): 2501, 2023 02 13.
Artigo em Inglês | MEDLINE | ID: mdl-36781871

RESUMO

Although nature is a rich source of potential drugs and drug leads, the widespread application of natural products (NPs) is limited due to their poor absorption when administered orally. A strategy of using phytosome has emerged as a promising technique to increase the bioavailability of NPs. Here, a comprehensive computational investigation is performed to explore the nature of interactions in the formation of phytosomes between phosphatidylcholine (PC) and a series of polyphenols (PP), including epigallocatechin-3-gallate (Eg), luteolin (Lu), quercetin (Qu), and resveratrol (Re). Our quantum mechanical calculation revealed that the intermolecular hydrogen bonds (HBs) of phosphate and glycerol parts of PC with the polyphenol compounds are the main driving force in the formation of phytosomes. The strongest HB (with energy HB = - 108.718 kJ/mol) is formed between the Eg molecule and PC. This hydrogen bond results from the flexible structure of the drug which along with several van der Waals (vdW) interactions, makes Eg-PC the most stable complex (adsorption energy = - 164.93 kJ/mol). Energy decomposition analysis confirms that the electrostatic interactions (hydrogen bond and dipole-diploe interactions) have a major contribution to the stabilization of the studied complexes. The obtained results from the molecular dynamics simulation revealed that the formation of phytosomes varies depending on the type of polyphenol. It is found that the intermolecular hydrogen bonds between PP and PC are a key factor in the behavior of the PP-PC complex in the self-aggregation of phytosome. In Eg-PC, Lu-PC, and Qu-PC systems, the formation of strong hydrogen bonds (HBCP < 0 and ∇2ρBCP > 0) between PP and PC protects the PP-PC complexes from degradation. The steered molecular dynamics simulation results have a good agreement with experimental data and confirm that the phytosome platform facilitates the penetration of PP compounds into the membrane cells.


Assuntos
Produtos Biológicos , Polifenóis , Fosfolipídeos , Fitossomas , Lecitinas
16.
J Diet Suppl ; 20(1): 55-67, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-34632933

RESUMO

In this preliminary pilot registry study, we investigated the effects of the oral supplementation of a standardized cranberry extract (Anthocran® Phytosome®, Indena) delivered by a lecithin-based system, for the prophylactic management of recurrent-urinary tract infections (R-UTIs). We included 64 otherwise healthy subjects who underwent a surgical procedure and required post-surgical urinary catheterization for high-risk UTIs or a previous history of R-UTIs. Patients were given supplementation with the standardized cranberry extract at the dose of either 120 mg/day (n = 12) or 240 mg/day (n = 12) or assigned to a control group consisting of standard management (SM; n = 18) or nitrofurantoin administration (n = 22) for 4 weeks. After 4 weeks, patients receiving the standardized cranberry supplementation reported to have a more effective reduction in UTI symptoms, as assessed on the visual analogue scale, compared with patients in the SM or nitrofurantoin groups. The occurrence of hematuria and urine bacterial contamination were decreased among patients treated with the supplement compared with controls (p < 0.05). The cranberry extract was also superior to the control management in terms of recurrence of signs/symptoms, with none of the patients in this group suffering from a R-UTI in the 3 months following the study end (p < 0.05). The supplementation showed an optimal safety profile, with no significant adverse events and no drop-outs in the supplement group. This registry shows that this cranberry extract is effective as a supplementary, preventive management in preventing post-operative, post-catheter UTIs; the product has a good tolerability profile.


Assuntos
Infecções Urinárias , Vaccinium macrocarpon , Humanos , Fitoterapia/métodos , Fitossomas , Nitrofurantoína/uso terapêutico , Extratos Vegetais/uso terapêutico , Infecções Urinárias/etiologia , Infecções Urinárias/prevenção & controle , Infecções Urinárias/tratamento farmacológico , Cateterismo
17.
Pharm Nanotechnol ; 11(1): 44-55, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36121090

RESUMO

BACKGROUND: Herbal preparations with low oral bioavailability have a fast first-pass metabolism in the gut and liver. To offset these effects, a method to improve absorption and, as a result, bioavailability must be devised. OBJECTIVE: The goal of this study was to design, develop, and assess the in vivo toxicity of polyherbal phytosomes for ovarian cyst therapy. METHODS: Using antisolvent and rotational evaporation procedures, phytosomes containing phosphatidylcholine and a combination of herbal extracts (Saraca asoca, Bauhinia variegata, and Commiphora mukul) were synthesized. For a blend of Saraca asoca, Bauhinia variegata, and Commiphora mukul, Fourier-transform infrared spectroscopy (FTIR), preformulation investigations, qualitative phytochemical screening, and UV spectrophotometric tests were conducted. Scanning electron microscopy (SEM), zeta potential, ex vivo release, and in vivo toxicological investigations were used to examine phytosomes. RESULTS: FTIR studies suggested no changes in descriptive peaks in raw and extracted herbs, although the intensity of peaks was slightly reduced. Zeta potential values between -20.4 mV to - 29.6 mV suggested stable phytosomes with an accepted particle size range. Percentage yield and entrapment efficiency were directly correlated to the amount of phospholipid used. Ex vivo studies suggested that the phytosomes with low content of phospholipids showed good permeation profiles. There was no difference in clinical indications between the extract-loaded phytosomes group and the free extract group in in vivo toxicological or histopathological examinations. CONCLUSION: The findings of current research work suggested that the optimized phytosomes based drug delivery containing herbal extracts as bioenhancers has the potential to improve the bioavailability of hydrophobic extracts.


Assuntos
Fosfolipídeos , Síndrome do Ovário Policístico , Feminino , Humanos , Fosfolipídeos/química , Fitossomas , Sistemas de Liberação de Medicamentos/métodos , Fosfatidilcolinas
18.
Cell Mol Biol (Noisy-le-grand) ; 69(14): 1-8, 2023 12 20.
Artigo em Inglês | MEDLINE | ID: mdl-38279505

RESUMO

Plant extracts have been shown to be effective in treating a variety of ailments; however their hydrophilic nature and unique chemical structure have caused significant hurdles due to their low bioavailability. Phytosomes technology is used to improve the absorption of phytoconstituents that are difficult to absorb. Among the leading deaths in the society is malignancy. The aforementioned consumes remained a big issue for modern chemotherapy since it has yet to be treated in an efficient manner. The goal of this study is to outline the most recent research on the potential use of phytosome complexes for cancer therapy, as well as the formulation processes and mechanism of transportation through phytosomes.Nanotechnology has paved the way for cancer therapy by altering key features of medications and their carriers. Novel drug delivery systems are used to transfer antitumor drugs to the particular site via different nanostructures. Among several unique drug delivery systems, phytosomes are a creative way to transfer phytoactive compounds to the site of action, and several phytosomes formulations are now being used in clinical settings. Phytoconstituents' anti-cancer activities are increased by phytosomal formulations.


Assuntos
Antineoplásicos , Nanoestruturas , Neoplasias , Humanos , Fitossomas , Sistemas de Liberação de Medicamentos , Antineoplásicos/uso terapêutico , Neoplasias/tratamento farmacológico , Compostos Fitoquímicos/uso terapêutico
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