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1.
Food Chem X ; 23: 101624, 2024 Oct 30.
Artículo en Inglés | MEDLINE | ID: mdl-39100248

RESUMEN

Functional foods like probiotics offer health benefits against various diseases, and plant bioactive compounds can enhance their growth. Zein, a protein, shows biological activity upon hydrolysis, and encapsulating it in nanoparticles improves bioavailability. This study examined chitosan-coated nanoliposomes as carriers for hydrolyzed and unhydrolyzed maize zein to fortify kashk. Combining chitosan and hydrolyzed zein in a 1:2 ratio achieves the highest encapsulation efficiency, antioxidant activity, smallest particle size, polydispersity index, and zeta potential. FTIR and XRD analyses confirm hydrolyzed zein's entrapment and crystalline nature post-encapsulation. Optimized nanoliposomes release hydrolyzed zein faster in simulated intestinal fluid than in gastric fluid, indicating high bioavailability and stability. When used to fortify kashk, these nanoliposomes slightly lower acidity but maintain standard pH over 60-day cold storage, improve elastic properties, and enhance probiotic viability. At the same time, sensory attributes remain comparable to the control, highlighting their functional food potential.

2.
Curr Pharm Des ; 2024 Jul 11.
Artículo en Inglés | MEDLINE | ID: mdl-38994614

RESUMEN

INTRODUCTION: Esophageal-Squamous Cell Carcinoma (ESCC) is often diagnosed at the middle or late stage, thus requiring more effective therapeutic strategies. Pharmacologically, the anti-tumor activity of the principal active constituent of Sophora flavescens, matrine (MA), has been explored widely. Notwithstanding, it is significant to nanotechnologically enhance the anti-tumor activity of MA in view of its potential to distribute non-tumor cells. METHODS: Herein, MA-loaded Nano-Liposomes (MNLs) were prepared to enhance the effect of anti-ESCC. The MNL showed a smaller sized particle (25.95 ± 1.02 nm) with a low polydispersed index (PDI = 0.130 ± 0.054), uniform spherical morphology, good solution stability, and encapsulated efficiency (65.55% ± 2.47). Furthermore, we determined the characteristics of KYSE-150 cells by cell viability assay, IC50, Mitochondrial Membrane Potential (MMP), Western blot, and apoptotic analysis, which indicated that MNLs down-regulated the cell viability and IC50 in a concentration-dependent manner and induced a significant change in JC-1 fluorescence from red to green. RESULTS: The above observations resulted in increased Bax and Caspase-3 levels, coupled with a substantial decrease in Bcl-2 and apoptotic promotion at the advanced stage compared with MA. CONCLUSION: Based on these results, MNLs may serve as a more effective and promising therapeutic option for ESCC.

3.
Colloids Surf B Biointerfaces ; 241: 113992, 2024 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-38833960

RESUMEN

In order to reduce the cardiotoxicity of doxorubicin (DOX) and improve its antitumor effect, dihydroartemisinin (DHA) and DOX prodrug (DOX-S-DHA) synthesized via a single sulfur bond was used with TEPP-46 to prepare nano-liposomes (DOX-S-DHA@TEPP-46 Lips). In which, TEPP-46 was expected to exert p53 bidirectional regulation to promote the synergistic antitumor effect of DOX and DHA while reducing cardiotoxicity. DOX-S-DHA@TEPP-46 Lips exhibited uniform particle size, good stability, and excellent redox-responsive activity. DOX-S-DHA@TEPP-46 Lips could significantly inhibit the proliferation of tumor cells, but had less cytotoxicity on normal cells. The presence of TEPP-46 increased the content of p53 protein, which further induced tumor cell apoptosis. DOX-S-DHA@TEPP-46 Lips had satisfactory long circulation to enhance the antitumor efficacy and reversed the cardiotoxicity of DOX in B16-F10 tumor-bearing mice. In conclusion, DOX-S-DHA@TEPP-46 Lips provides a new insight on creating sophisticated redox-sensitive nano-liposomes for cancer therapy as well as the decreased cardiotoxicity of DOX.


Asunto(s)
Artemisininas , Cardiotoxicidad , Doxorrubicina , Liposomas , Profármacos , Animales , Artemisininas/química , Artemisininas/farmacología , Artemisininas/administración & dosificación , Doxorrubicina/farmacología , Doxorrubicina/química , Doxorrubicina/administración & dosificación , Profármacos/química , Profármacos/farmacología , Ratones , Liposomas/química , Cardiotoxicidad/prevención & control , Proliferación Celular/efectos de los fármacos , Apoptosis/efectos de los fármacos , Antineoplásicos/farmacología , Antineoplásicos/química , Antineoplásicos/administración & dosificación , Tamaño de la Partícula , Nanopartículas/química , Sistemas de Liberación de Medicamentos , Ratones Endogámicos C57BL , Melanoma Experimental/tratamiento farmacológico , Melanoma Experimental/patología , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Línea Celular Tumoral
4.
Food Sci Biotechnol ; 33(7): 1707-1714, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38623436

RESUMEN

Attempts to improve low absorption and rapid metabolic conversion of curcumin were made by developing curcumin-loaded bilayer nanoliposomes coated with chitosan and alginate for intestinal-specific drug delivery. A curcumin-loaded nano-liposome was prepared with optimized formulations with phosphatidylcholine, curcumin, chitosan, and alginate. The particle size of the optimized formulation was approximately 400 nm, and the encapsulation efficiency was more than 99%. In the in vitro release study, curcumin release from the curcumin-loaded nanoliposome with double layers of chitosan/alginate (CNL-CH/AL) was suppressed in the simulated gastric fluid (SGF, pH 1.2) and enhanced in the simulated intestinal fluid (SIF, pH 6.8). In the in vivo pharmacokinetic study in rats, the CNL-CH/AL-treated group showed a prolonged absorption pattern of curcumin and the area under the plasma concentration-time curve from 0 to 24 h (AUC0-24) was improved 109-fold compared to the control group treated with a curcumin solution without a nanocarrier.

5.
Nanomaterials (Basel) ; 13(19)2023 Sep 22.
Artículo en Inglés | MEDLINE | ID: mdl-37836259

RESUMEN

Liposomes are microspheres produced by placing phospholipids in aqueous solutions. Liposomes have the advantage of being able to encapsulate both hydrophilic and hydrophobic functional substances and are thus important mediators used in cosmetics and pharmaceuticals. It is important for liposomes to have small sizes, uniform particle size distribution, and long-term stability. Previously, liposomes have been prepared using a homo mixer, microfluidizer, and horn and bath types of sonicators. However, it is difficult to produce liposomes with small sizes and uniform particle size distribution using these methods. Therefore, we have developed a focused ultrasound method to produce nano-sized liposomes with better size control. In this study, the liposome solutions were prepared using the focused ultrasound method and conventional methods. The liposome solutions were characterized for their size distribution, stability, and morphology. Results showed that the liposome solution prepared using focused ultrasonic equipment had a uniform particle size distribution with an average size of 113.6 nm and a polydispersity index value of 0.124. Furthermore, the solution showed good stability in dynamic light scattering measurements for 4 d and Turbiscan measurements for 1 week.

6.
Pharmaceutics ; 15(9)2023 Sep 16.
Artículo en Inglés | MEDLINE | ID: mdl-37765299

RESUMEN

Inflammatory bowel disease (IBD), which includes ulcerative colitis (UC) and Crohn's disease, is known to increase the risk of colitis-associated cancer (CAC). CAC has been found to be unresponsive to standard chemotherapy regimens, and the current treatments do not utilize effective small-molecule drugs and colon-targeted delivery systems. Previous studies indicated that the M13-nano-liposome (NL) formulation can effectively target the colon and reshape the gut microbiota in ex vivo cultures, generating altered microbial metabolites that can efficiently prevent chronic UC. In this study, we tested the cancer cell uptake ability of the NL formulation and investigated the potential of the M13-NL formulation to prevent CAC in the azoxymethane (AOM)-exposed IL10-/- mouse model. Our findings demonstrate that oral administration of M13-NL prevents tumor development in AOM-exposed IL10-/- mice, suggesting that M13-NL is a promising oral drug formulation for preventing CAC.

7.
Neurosci Lett ; 812: 137367, 2023 08 24.
Artículo en Inglés | MEDLINE | ID: mdl-37419304

RESUMEN

Chemotherapy-induced peripheral neuropathy (CIPN) is an important adverse effect of treatment with oxaliplatin (OXA). We have developed PEGylated nanoliposomal oxaliplatin (OXA-LIP) and tested its activity in an animal model of CIPN. OXA-LIPs were prepared using a combination of egg yolk lecithin, cholesterol, and DSPE-mPEG2000 (at ratios 400, 80, and 27 mg). These liposomes were characterized using several different methods (e.g., polydispersity index (PDI), and zeta potential, FESEM). The in vivo study was performed in 15 male rats comprising three groups: a negative control (normal saline) OXA, and OXA-LIP. These were injected intraperitoneally at a concentration of 4 mg/kg on two consecutive days every week, for 4 weeks. After that, CIPN was assessed using the hotplate and acetonedropmethods. Oxidative stress biomarkers such as SOD, catalase, MDA, and TTG were measured in the serum samples. The functional disturbances of the liver and kidney were assessed by measuring the serum levels of ALT, AST, creatinine, urea, and bilirubin. Furthermore, hematological parameters were determined in the three groups. The OXA-LIP had an average particle size, PDI, and zeta potential of 111.2 ± 1.35 nm, 0.15 ± 0.045, and -52.4 ± 17 mV, respectively. The encapsulation efficiency of OXA-LIP was 52% with low leakage rates at 25 °C.Thermal hyperalgesia changes showed OXA has significant effects in the induction of neuropathy on days 7, 14, and 21 compared to the control group. OXA had a significantly greater sensitivity than the OXA-LIP and control groups in the thermal allodynia test (P < 0.001). OXA-LIP administration did not show significant effects on the changes of oxidative stress, biochemical factors, and cell count. Our findings provide a proof of concept on the potential application of oxaliplatin encapsulated with PEGylated nanoliposome to ameliorate the severity of neuropathy, supporting further studies in clinical phases to explore the value of this agent for Chemotherapy-induced peripheral neuropathy.


Asunto(s)
Antineoplásicos , Enfermedades del Sistema Nervioso Periférico , Masculino , Ratas , Animales , Oxaliplatino/efectos adversos , Antineoplásicos/toxicidad , Enfermedades del Sistema Nervioso Periférico/inducido químicamente , Enfermedades del Sistema Nervioso Periférico/tratamiento farmacológico , Hiperalgesia/inducido químicamente , Hiperalgesia/tratamiento farmacológico , Polietilenglicoles/efectos adversos
8.
Foods ; 12(12)2023 Jun 14.
Artículo en Inglés | MEDLINE | ID: mdl-37372581

RESUMEN

Melon seed oil (MSO) possesses plenty of long-chain fatty acids (LFCAs, oleic-linoleic acid 90%), remarkable antioxidant activity (DPPH (0.37 ± 0.40 µmol TE/g), ABTS (4.98 ± 0.18 µmol TE/g), FRAP (0.99 ± 0.02 µmol TE/g), and CUPRAC (4.94 ± 0.11 µmol TE/g)), and phenolic content (70.14 ± 0.53 mg GAE/100 g). Encapsulation is a sound technology to provide thermal stability and controlled release attributes to functional compounds such as plant seed oil. Nano-sized and micro-sized capsules harboring MSO were generated by utilizing thin film dispersion, spray drying, and lyophilization strategies. Fourier infrared transform analysis (FTIR), scanning electron microscopy (SEM), and particle size analyses were used for the authentication and morphological characterization of the samples. Spray drying and lyophilization effectuated the formation of microscale capsules (2660 ± 14 nm, 3140 ± 12 nm, respectively), while liposomal encapsulation brought about the development of nano-capsules (282.30 ± 2.35 nm). Nano-liposomal systems displayed significant thermal stability compared to microcapsules. According to in vitro release studies, microcapsules started to release MSO in simulated salivary fluid (SSF) and this continued in gastric (SGF) and intestinal (SIF) environments. There was no oil release for nano-liposomes in SSF, while limited release was observed in SGF and the highest release was observed in SIF. The results showed that nano-liposomal systems featured MSO thermal stability and controlled the release attributes in the gastrointestinal system (GIS) tract.

9.
Pharmaceutics ; 15(2)2023 Feb 06.
Artículo en Inglés | MEDLINE | ID: mdl-36839861

RESUMEN

Epigallocatechin gallate (EGCG), the main ingredient in green tea, holds promise as a potential treatment for pulmonary arterial hypertension (PAH). However, EGCG has many drawbacks, including stability issues, low bioavailability, and a short half-life. Therefore, the purpose of this research was to develop and optimize an inhalable EGCG nano-liposome formulation aiming to overcome EGCG's drawbacks by applying a design of experiments strategy. The aerodynamic behaviour of the optimum formulation was determined using the next-generation impactor (NGI), and its effects on the TGF-ß pathway were determined using a cell-based reporter assay. The newly formulated inhalable EGCG liposome had an average liposome size of 105 nm, a polydispersity index (PDI) of 0.18, a zeta potential of -25.5 mV, an encapsulation efficiency of 90.5%, and a PDI after one month of 0.19. These results are in complete agreement with the predicted values of the model. Its aerodynamic properties were as follows: the mass median aerodynamic diameter (MMAD) was 4.41 µm, the fine particle fraction (FPF) was 53.46%, and the percentage of particles equal to or less than 3 µm was 34.3%. This demonstrates that the novel EGCG liposome has all the properties required to be inhalable, and it is expected to be deposited deeply in the lung. The TGFß pathway is activated in PAH lungs, and the optimum EGCG nano-liposome inhibits TGFß signalling in cell-based studies and thus holds promise as a potential treatment for PAH.

10.
Chem Biodivers ; 19(10): e202200397, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-36097678

RESUMEN

Nanoencapsulation of essential oils (EOs) in drug delivery systems leads to their capability of improving their solubility, stability, and bioavailability of them. The aim of this study was preparation, optimization, and characterization of nano-liposomes/nano-niosomes containing Achillea millefolium essential oils (A. millefolium EOs) and comparison of their properties. In the experimental study, characteristics of nanoparticles including size, zeta potential, Fourier Transform Infrared Spectroscopy (FTIR), % encapsulation efficiency (EE%) and the release amount of essential oils from nano-liposome or niosome were assessed using different techniques. Then to determine cell viability at different concentrations, the MTT assay was used. Also, the dilution method was used to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of antimicrobial agents. The optimized formulations provided potential advantages, including an appropriate nano-size scale, and a negative charge, and also showed a continuous drug release behavior, which successfully encapsulated essential oil with high entrapment efficiency. In terms of size and release amount, nano-niosome had superiority to nano-liposome with smaller size and also slower release but nano-liposome could encapsulate essential oils in a higher percentage compared to nano-niosome. Also, there was a significant difference between the toxicity of encapsulated EOs and free EOs in terms of viability (P<0.05). In addition, the antimicrobial effect of liposomal and niosomal EO was greater than free EO. In conclusion, the designed nano-based systems were determined as promising lipid-based nano-carriers for essential oil delivery that proffered a novel, high potential therapy for breast cancer and favorable antimicrobial effects.


Asunto(s)
Achillea , Antiinfecciosos , Neoplasias , Aceites Volátiles , Liposomas/química , Aceites Volátiles/farmacología , Antibacterianos/farmacología , Línea Celular
11.
Int J Mol Sci ; 23(12)2022 Jun 20.
Artículo en Inglés | MEDLINE | ID: mdl-35743311

RESUMEN

(1) Background: Curcumin (CUR) and tetrandrine (TET) are natural compounds with various bioactivities, but have problems with low solubility, stability, and absorption rate, resulting in low bioavailability, and limited applications in food, medicine, and other fields. It is very important to improve the solubility while maintaining the high activity of drugs. Liposomes are micro-vesicles synthesized from cholesterol and lecithin. With high biocompatibility and biodegradability, liposomes can significantly improve drug solubility, efficacy, and bioavailability. (2) Methods: In this work, CUR and TET were encapsulated with nano-liposomes and g DSPE-MPEG 2000 (DP)was added as a stabilizer to achieve better physicochemical properties, biosafety, and anti-tumor effects. (3) Results: The nano-liposome (CT-DP-Lip) showed stable particle size (under 100 nm) under different conditions, high solubility, drug encapsulation efficiency (EE), loading capacity (LC), release rate in vitro, and stability. In addition, in vivo studies demonstrated CT-DP-Lip had no significant toxicity on zebrafish. Tumor cytotoxicity test showed that CT-DP-Lip had a strong inhibitory effect on a variety of cancer cells. (4) Conclusions: This work showed that nano-liposomes can significantly improve the physical and chemical properties of CUR and TET and make them safer and more efficient.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas , Curcumina , Neoplasias , Animales , Bencilisoquinolinas , Curcumina/química , Curcumina/farmacología , Portadores de Fármacos/química , Liposomas/química , Neoplasias/tratamiento farmacológico , Tamaño de la Partícula , Pez Cebra
12.
J Control Release ; 348: 893-910, 2022 08.
Artículo en Inglés | MEDLINE | ID: mdl-35760233

RESUMEN

Cancer cells have various immune evasion mechanisms that resist the immune cells by reprogramming the tumor microenvironment (TME), such as programmed death-ligand 1 (PD-L1) and indoleamine 2,3-dioxygenase-1 (IDO1) overexpression. One of the approaches to restore antitumor immune response by T-cells is through induction of immunogenic cell death (ICD). Thus, drug carrier containing IDO1 siRNA and ICD inducer would be effective anticancer regimen to modulate the immunosuppressive TME by reversing the IDO1-mediated immunosuppression in a synergistic combination with ICD induction. However, numerous nanocarrier platforms for co-delivery of multiple drugs mostly depend on the enhanced permeation and retention (EPR), which is insufficient to achieve selectivity in tumor sites harboring various types of cells. We designed a targeted drug delivery system using nano-sized liposomes functionalized with anti-CD44 and anti-PD-L1 DNA aptamers, which target breast cancer cells and inhibit PD-1/PD-L1 interaction between cancer cells and T-cells. To reverse immunosuppressive TME and reactivate immune response, cancer-targeting nano-liposomes were prepared to contain immunogenic cell death inducer (Doxorubicin, DOX) and IDO1 siRNA, namely Aptm[DOX/IDO1]. The Aptm[DOX/IDO1] specifically delivered the loaded DOX and IDO1 siRNA into target breast cancer cells through aptamer-mediated endocytosis. Cancer-targeted DOX/IDO1 siRNA delivery enhanced ICD and suppressed IDO1 expression with significantly high toxicity in cancer cells. We demonstrated that Aptm[DOX/IDO1] could achieve synergistic antitumor effects by facilitating ICD response and simultaneous reversal of the immunosuppressive TME with IDO1 knockdown in the subcutaneous breast cancer model mice, thus reducing tumor size. These antitumor effects were exerted with intratumoral infiltration of CD8+ cytotoxic T lymphocyte as well as attenuation of regulatory T-cell recruitment in the tumor sites. We further proved that our Aptm[DOX/IDO1] strategy significantly reduced tumor metastasis in tumor-xenograft mice through a synergistic combination of cancer cell-targeted ICD induction and reversal of the IDO1-mediated immunosuppressive TME. Our nanocarrier platform based on cationic liposomes containing DOX and IDO1 siRNA, which are conjugated with two DNA aptamers targeting the cancer cell surface, accomplished synergistic chemoimmunotherapy through tumor-specific immune modulation into immune-favorable TME in vivo.


Asunto(s)
Antineoplásicos , Aptámeros de Nucleótidos , Animales , Línea Celular Tumoral , Doxorrubicina , Humanos , Terapia de Inmunosupresión , Liposomas , Ratones , Ratones Endogámicos BALB C , ARN Interferente Pequeño/genética
13.
Assay Drug Dev Technol ; 19(7): 453-462, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-34435891

RESUMEN

This study aimed to assess the effect of voriconazole (VCZ)-loaded nano-liposomes on biological activity and expression of ERG11, CDR1, and CDR2 genes in fluconazole (FCZ)-resistant Candida albicans. In this study, 5 resistant isolates of C. albicans and 3 susceptible clinical isolates to FCZ were scrutinized from 60 patients suspected of candidiasis. The liposomal formulation of VCZ was produced. After that, the minimum biofilm inhibitory concentration (MBIC) testing was performed and the percentage of growth inhibition was determined. Finally, ERG11, CDR1, and CDR2 mRNA levels were amplified by the quantitative reverse transcription PCR (qRT-PCR) instrument. The obtained results unveiled that VCZ-loaded nano-liposome reduction of minimum inhibitory concentration in C. albicans isolates was remarkable. The results of the MBIC in the most optimum inhibitory concentration of VCZ-loaded nano-liposome were determined to be 4.54 and 4.88 µg/mL for susceptible isolate and resistant isolate, respectively. The ERG11 gene expression in FCZ-resistant C. albicans strains in VCZ-treated, liposomal formulation of VCZ-treated, and nontreated specimens stood at 91%, 63%, and 100%, respectively. Expression levels of CDR1 genes in FCZ-resistant C. albicans were shown to be 91%, 88%, and 100%, respectively. Concerning CDR2 genes, this rate varied to 91%, 78%, and 100% in FCZ resistant, respectively. What our study unveiled was that the use of liposomal VCZ formulation could further reduce the expression of azole-resistant genes compared to VCZ itself. In addition, thanks to more efficacious penetration of the liposomal form, the rate of growth inhibition was considerably higher.


Asunto(s)
Candida albicans , Fluconazol , Antifúngicos/farmacología , Candida albicans/genética , Farmacorresistencia Fúngica/genética , Fluconazol/farmacología , Proteínas Fúngicas/genética , Expresión Génica , Humanos , Liposomas , Pruebas de Sensibilidad Microbiana , Voriconazol/farmacología
14.
Adv Pharm Bull ; 11(2): 295-300, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33880351

RESUMEN

Purpose: Enoxaparin has been widely used as a choice drug for treatment and prevention of different coagulation disorders. Orally administered enoxaparin encounters with gastrointestinal barrier because of its high water solubility, high molecular weight and significant negative charge. Since, the nano-liposomes has gained great interest for oral drug delivery, we decided to introduce the best protocol for preparing enoxaparin nano-liposomes through in vitro characterization. Methods: Nano-liposomes were prepared by ethanol injection, thin film hydration, and double emulsion/solvent evaporation methods. Size distribution, zeta potential, loading efficiencies, and in vitro drug release of nano-liposomes were also studied. Results: The mean vesicle size was obtained under 100 nm, and the zeta potential was highly negative through all preparation methods. Nano-liposomes prepared by double emulsion/ solvent evaporation (DE) technique could entrap more of this hydrophilic drug (43 ± 7.1 %), but through thin layer hydration (TL) and ethanol injection (EI) only 28.4± 3.2% and 17.3 ± 2.5% of drug could be loaded into synthesized carriers. Drug release from these carriers was also obtained 42.17±1.72%, 29.43±0.34% and 32.27±0.14%, in 24 hours for EI, TL, and DE methods, respectively. Conclusion: Here, we can introduce double emulsion/solvent evaporation method as an acceptable method for enoxaparin loading, although some toxicity and in-vivo tests are also necessary to fully understand the potential of this formulation.

15.
Cell Cycle ; 19(24): 3581-3594, 2020 12.
Artículo en Inglés | MEDLINE | ID: mdl-33300430

RESUMEN

Gefitinib (GEB) is one of the drugs used for patients with epidermal growth factor receptor (EGFR)-positive mutations in non-small cell lung cancer (NSCLC). However, application of GEB is limited by its low water solubility, stability, and utilization rate, especially the side effects while GEB is given by oral. In this study, nanoliposome was used as a carrier to prepare nanoliposome compound drug (GL) by embedding GEB in the nanoliposome perfectly combined with green nontoxic solvent and thin-film dispersion method. The nanoliposome structure was expected to improve the water solubility and biocompatibility of GEB, thus improving the effect of cancer treatment. The surface electronegative nanoliposomes can effectively avoid protein adsorption and prolong the circulation time in vivo. Meanwhile, the ratio of lecithin to cholesterol (LE/CH) was explored to maximize the encapsulation efficiency of nanoliposome. Subsequent test results showed that GL exhibited better stability, smaller particle size and higher encapsulation efficiency. In addition, in vitro drug release curve also further confirmed that GL had a promising drug sustained-release effect. In particular, a series of in vitro tests such as cell activity, apoptosis, colony formation, scratch, invasion, and cell cycle assays were performed. The results indicated that GL significantly enhanced the pro-apoptotic effect on A549 cells. Most cell cycles of A549 cells were blocked in the G0/G1 phase influenced by GL, thus inhibiting the proliferation of cancer cells. In vivo anti-tumor studies showed that compared with pure GEB, GL had a significant inhibiting effect on NSCLC. In conclusion, the GL which was synthesized by a simple method in this study significantly improved the treatment effect of cancer cells, which proved that the nanoliposome carrier had an excellent application prospect in the treatment of lung cancer.


Asunto(s)
Antineoplásicos/administración & dosificación , Carcinoma de Pulmón de Células no Pequeñas/tratamiento farmacológico , Carcinoma de Pulmón de Células no Pequeñas/metabolismo , Sistemas de Liberación de Medicamentos/métodos , Gefitinib/administración & dosificación , Neoplasias Pulmonares/tratamiento farmacológico , Neoplasias Pulmonares/metabolismo , Nanoestructuras/química , Células A549 , Animales , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Cápsulas , Carcinoma de Pulmón de Células no Pequeñas/patología , Ciclo Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Liberación de Fármacos , Estabilidad de Medicamentos , Gefitinib/química , Humanos , Liposomas , Neoplasias Pulmonares/patología , Ratones , Ratones Endogámicos BALB C , Ratones Desnudos , Tamaño de la Partícula , Solubilidad , Resultado del Tratamiento , Carga Tumoral/efectos de los fármacos , Ensayos Antitumor por Modelo de Xenoinjerto
16.
J Drug Target ; 26(4): 365-372, 2018 04.
Artículo en Inglés | MEDLINE | ID: mdl-28972792

RESUMEN

E75 (HER-2/neu-369-377), is an immunogenic peptide which is highly expressed in breast cancer patients. The purpose of this study was to develop an effective vaccine delivery/adjuvant system by attachment of this peptide to the surface of liposomes consisting of phospholipids including distearoylphosphocholine (DSPC) and distearoyl phosphoglycerol (DSPG) with high transition temperature (Tm) and dioleoylphosphatidylethanolamine (DOPE) (a pH-sensitive lipid for cytosolic antigen delivery) to improve antitumour immune activity against the E75 peptide. For this purpose, the E75 peptide was incorporated into liposomes consisting of DSPC/DSPG/cholesterol (Chol)/DOPE (15/2/3/5 molar ratio) through conjugation with distearoylphosphoethanolamine-N-[maleimide(polyethylene glycol)-2000] (maleimide-PEG2000-DSPE). Immunization of BALB/c mice was performed three times with different forms of liposomal formulations at 2-week intervals and antitumour immunity responses were evaluated. Results of ELISpot and flow cytometry analysis showed that mice vaccinated with DSPC/DSPG/Chol/DOPE/E75 have significantly enhanced the antigen-specific IFN-γ response of CD8+ T cells and generated cytotoxic T lymphocytes (CTL) antitumour responses. CTL responses induced by this formulation resulted in inhibition of tumour progression and longer survival time in the mice TUBO tumour model. The results revealed that the liposomes consist of DSPC/DSPG/Chol/DOPE could be suitable candidates for vaccine delivery of E75 peptide for the prevention and therapy of HER2-positive breast cancer and merit further investigation.


Asunto(s)
Neoplasias de la Mama/tratamiento farmacológico , Vacunas contra el Cáncer/administración & dosificación , Fragmentos de Péptidos/administración & dosificación , Fosfolípidos/química , Receptor ErbB-2/administración & dosificación , Animales , Neoplasias de la Mama/inmunología , Linfocitos T CD8-positivos/inmunología , Vacunas contra el Cáncer/inmunología , Progresión de la Enfermedad , Femenino , Interferón gamma/inmunología , Liposomas , Ratones , Ratones Endogámicos BALB C , Nanopartículas , Fragmentos de Péptidos/inmunología , Receptor ErbB-2/inmunología , Tasa de Supervivencia , Linfocitos T Citotóxicos/inmunología , Temperatura de Transición
17.
Artículo en Chino | WPRIM (Pacífico Occidental) | ID: wpr-701848

RESUMEN

Objective To prepare quercetin liposome and to explore the antitumor effect of quercetin liposome.Methods The cholesterol and lecithin were used as membrane materials,quercetin nano liposome was prepared by thin film ultrasound method.The zeta potential and particle size distribution of quercetin liposome were tested by Malvern laser particle size analyzer and transmission electron microscope respectively.In order to explore the anti-tumor effect of quercetin nano-liposome,the mouse model of cervical cancer was established.After tail vein injection of quercetin and quercetin nano-liposome for 15 days,the tumor inhibitory rate,the thymus (spleen) index were analyzed,and the pathology of tumor tissues was further observed.Results Under the condition of lecithin∶cholesterol ∶ quercetin =8 ∶ 2 ∶ 1,the hydration time of 15 min and the ultrasonic time of 15 min,the quercetin nano-liposome was prepared,and the particle size distribution was uniform and the potential was-10.8.The tumor inhibitory rate of quercetin nano-liposome treatment group was 54.16%,which was significantly higher than that of the quercetin treatment group (x2 =6.477,P < 0.05).The pathology results of the tumor tissues showed that nanocrystallization of quercetin could increase the anti-cancer effect of quercetin.Conclusion Both quercetin and quercetin nano-liposome exhibit significant effect on the tumor growth,and the inhibitory rate is increased after quercetin was nanocrystallization.Our study will provide theoretical basis for the application of quercetin nano-liposome in the treatment of cervical cancer.

18.
Food Chem ; 230: 690-696, 2017 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-28407968

RESUMEN

The aim of the present research was to evaluate the application, stability and suitability of ω3 polyunsaturated fatty acids (PUFAs) incorporated nanoliposomes in food enrichment. Nanoliposomal ω3 PUFAs was prepared by Mozafari method, and their application in bread and milk was compared with unencapsulated (fish oil) and microencapsulated ω3 PUFAs. Sensory evaluation was conducted to determine the perceptible sensory difference/similarity between control, unencapsulated, microencapsulated, and nanoliposomal ω3 PUFAs enriched foods. Results showed no significant (p=0.11) detectable difference between control and nanoliposomal ω3 PUFAs enriched samples while, samples enriched with unencapsulated or microencapsulated ω3 PUFAs showed significant (p=0.02) fishy flavor. Moreover, significantly (p<0.01) higher ω3 PUFAs % recovery and lower peroxide and anisidine values were observed in nanoliposomal ω3 PUFAs enriched samples in comparison with other samples. In conclusion, an effective and reproducible method for application of ω3 PUFAs in the food system was developed.


Asunto(s)
Ácidos Grasos Omega-3/química , Liposomas/química , Alimentos Fortificados , Humanos
19.
Food Chem ; 216: 146-52, 2017 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-27596403

RESUMEN

Fish oils have many dietary benefits, but due to their strong odors and rapid deterioration, their application in food formulations is limited. For these reasons, nano-liposome was used to nano-encapsulate fish oil in this study and encapsulated fish oil was utilized in fortifying yogurt. Physicochemical properties of produced yogurt including pH, acidity, syneresis, fatty acid composition, peroxide value as well as sensory tests were investigated during three weeks storage at 4°C. Nano-liposome encapsulation resulted in a significant reduction in acidity, syneresis and peroxide value. The results of gas chromatography analyses revealed that after 21days storage, yogurt fortified with nano-encapsulated fish oil had a higher DHA and EPA contents than yogurt containing free fish oil. Overall, the results of this study indicates that adding nano-encapsulated fish oil into yogurt gave closer characteristics to control sample in terms of sensory characteristics than yogurt fortified with free fish oil.


Asunto(s)
Aceites de Pescado/química , Alimentos Fortificados/análisis , Liposomas/química , Nanopartículas/química , Nanotecnología/métodos , Yogur/análisis , Animales , Grasas Insaturadas en la Dieta , Ácidos Grasos/análisis , Humanos
20.
Front Microbiol ; 8: 2700, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-29379490

RESUMEN

Food grade micro- or nano-carrier systems (NCS) are being developed to improve the controlled release of antimicrobial agents. To augment the stability of liposomal NCS and to overcome the limitations associated with the use of free bacteriocin (nisin) in the food system, multi-component colloidosomes (MCCS) were developed by electrostatic interactions between anionic alginate and cationic chitosan (multilayer) around phospholipids based liposomes (core). Zeta-sizer results revealed the average diameter of 145 ± 2 nm, 596 ± 3 nm, and 643 ± 5 nm for nano-liposome (NL), chitosomes (chitosan coated NL) and MCCS, respectively. Zeta potential values of NCS varied from -4.37 ± 0.16 mV to 33.3 ± 6 mV, thus both chitosomes (CS) and MCCS were positively charged. Microstructure analysis by scanning electron microscope (SEM) revealed relatively higher size of MCCS with smooth and round morphology. TGA and DSC based experiments revealed that MCCS were thermally more stable than uncoated liposomes. Encapsulation efficiency of nisin in MCCS was observed to be 82.9 ± 4.1%, which was significantly higher than NL (56.5 ± 2.5%). FTIR analyses confirmed the cross-linking between sodium alginate and chitosan layer. Both qualitative (growth kinetics) and quantitative (colony forming unit) antimicrobial assays revealed that nisin loaded MCCS have superior potential to control resistant foodborne pathogens including Staphylococcus aureus, Listeria monocytogenes, and Enterococcus faecalis, (5.8, 5.4, and 6.1 Log CFUmL-1 reduction, respectively) as compared to free nisin, loaded NL or CS. Controlled release kinetics data fitted with Korsmeyer-Peppas model suggested that nisin release from MCCS followed Fickian diffusion. Cytotoxic studies on human blood cells and HepG2 cell lines revealed hemocompatibility and non-toxicity of MCCS. Thus, due to enhanced controlled release, stability and biocompatibility; these multi-component colloidosomes can be useful for incorporating antimicrobial agents into functional foods, beverages and pharmaceutical products to combat pathogenic and spoilage bacteria.

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