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1.
Pharmaceutics ; 15(12)2023 Nov 24.
Artigo em Inglês | MEDLINE | ID: mdl-38140006

RESUMO

Curcumin is known for its anti-inflammatory, neuroprotective, and antioxidant properties, but its use in biological applications is hindered by its sensitivity to light, oxygen, and temperature. Furthermore, due to its low water solubility, curcumin has a poor pharmacokinetic profile and bioavailability. In this study, we evaluated the potential application of curcumin as a neuroprotective agent encapsulated in RGD peptide-PEGylated nanoliposomes developed from salmon-derived lecithin. Salmon lecithin, rich in polyunsaturated fatty acids, was used to formulate empty or curcumin-loaded nanoliposomes. Transmission electron microscopy, dynamic light scattering, and nanoparticle tracking analysis characterizations indicated that the marine-derived peptide-PEGylated nanoliposomes were spherical in shape, nanometric in size, and with an overall negative charge. Cytotoxicity tests of curcumin-loaded nanoliposomes revealed an improved tolerance of neurons to curcumin as compared to free curcumin. Wild-type SH-SY5Y were treated for 24 h with curcumin-loaded nanoliposomes, followed by 24 h incubation with conditioned media of SH-SY5Y expressing the Swedish mutation of APP containing a high ratio of Aß40/42 peptides. Our results revealed significantly lower Aß-induced cell toxicity in cells pre-treated with RGD peptide-PEGylated curcumin-loaded nanoliposomes, as compared to controls. Thus, our data highlight the potential use of salmon lecithin-derived RGD peptide PEGylated nanoliposomes for the efficient drug delivery of curcumin as a neuroprotective agent.

2.
Foods ; 12(20)2023 Oct 22.
Artigo em Inglês | MEDLINE | ID: mdl-37893760

RESUMO

Plant-based desserts are becoming increasingly popular with and appreciated by consumers. However, they are limited by the choice of ingredients, which are often expensive and unstable with a random texture. Therefore, the aim of the research is to propose a new product that offers an advantageous texture and flavour in a fermented dessert based on a flour mix supplemented with an enzymatic hydrolysate. This study involved the development of two processes: (i) an enzymatic hydrolysis of oat flour and (ii) a fermentation of a flour mixture (oat, chickpea, and coconut) by lactic acid bacteria (Lactobacillus delbrueckii subsp. bulgaricus and Streptococcus thermophilus). The result of the oat flour hydrolysate shows a significant decrease in starch after 60 min of reaction, followed by an increase in sugar content. During 23 days of storage at 4 °C, the formulations used showed post-acidification, water retention capacity decrease, and hardness increase related to the hydrolysate rate (p < 0.05). All formulations allowed the viability of lactic bacteria (over 5 log10 CFU/mL) and verified their ability to produce exopolysaccharides (0.23-0.73 g/100 g). The prototyping of such a product represents a key step in meeting the growing demand for plant-based alternatives, with qualitative sensory characteristics without additives.

3.
Int J Mol Sci ; 24(17)2023 Aug 29.
Artigo em Inglês | MEDLINE | ID: mdl-37686165

RESUMO

There is a growing interest for complex in vitro environments that closely mimic the extracellular matrix and allow cells to grow in microenvironments that are closer to the one in vivo. Protein-based matrices and especially hydrogels can answer this need, thanks to their similarity with the cell microenvironment and their ease of customization. In this study, an experimental design was conducted to study the influence of synthesis parameters on the physical properties of gelatin methacryloyl (GelMA). Temperature, ratio of methacrylic anhydride over gelatin, rate of addition, and stirring speed of the reaction were studied using a Doehlert matrix. Their impact on the following parameters was analyzed: degree of substitution, mass swelling ratio, storage modulus (log(G')), and compression modulus. This study highlights that the most impactful parameter was the ratio of methacrylic anhydride over gelatin. Although, temperature affected the degree of substitution, and methacrylic anhydride addition flow rate impacted the gel's physical properties, namely, its storage modulus and compression modulus. Moreover, this experimental design proposed a theoretical model that described the variation of GelMA's physical characteristics as a function of synthesis conditions.


Assuntos
Gastrópodes , Hidrogéis , Animais , Projetos de Pesquisa , Gelatina , Anidridos
4.
Int J Mol Sci ; 23(22)2022 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-36430432

RESUMO

Alzheimer's disease (AD) is the most frequent case of neurodegenerative disease and is becoming a major public health problem all over the world. Many therapeutic strategies have been explored for several decades; however, there is still no curative treatment, and the priority remains prevention. In this review, we present an update on the clinical and physiological phase of the AD spectrum, modifiable and non-modifiable risk factors for AD treatment with a focus on prevention strategies, then research models used in AD, followed by a discussion of treatment limitations. The prevention methods can significantly slow AD evolution and are currently the best strategy possible before the advanced stages of the disease. Indeed, current drug treatments have only symptomatic effects, and disease-modifying treatments are not yet available. Drug delivery to the central nervous system remains a complex process and represents a challenge for developing therapeutic and preventive strategies. Studies are underway to test new techniques to facilitate the bioavailability of molecules to the brain. After a deep study of the literature, we find the use of soft nanoparticles, in particular nanoliposomes and exosomes, as an innovative approach for preventive and therapeutic strategies in reducing the risk of AD and solving problems of brain bioavailability. Studies show the promising role of nanoliposomes and exosomes as smart drug delivery systems able to penetrate the blood-brain barrier and target brain tissues. Finally, the different drug administration techniques for neurological disorders are discussed. One of the promising therapeutic methods is the intranasal administration strategy which should be used for preclinical and clinical studies of neurodegenerative diseases.


Assuntos
Doença de Alzheimer , Nanopartículas , Doenças Neurodegenerativas , Humanos , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/prevenção & controle , Doenças Neurodegenerativas/tratamento farmacológico , Sistemas de Liberação de Medicamentos/métodos , Nanopartículas/uso terapêutico , Barreira Hematoencefálica
5.
Pharmaceutics ; 14(10)2022 Oct 12.
Artigo em Inglês | MEDLINE | ID: mdl-36297607

RESUMO

Soft nanoparticles, and in particular, nanoliposomes (NL), have attracted increasing interest for their use in food, nutraceuticals, and in particular, in pharmaceutics for drug delivery. Recent data using salmon lecithin NL suggest that these NL, rich in omega-3 (n-3) fatty acids, can improve the bioavailability and transport of molecules through the blood brain barrier (BBB) to target the brain for the prevention and treatment of neurodegenerative diseases. The objective of this study was to characterize the physicochemical properties and analyze the transfer phenomena of salmon lecithin NL over time in neurons to better understand the behavior of NL in an intracellular environment. To test this, primary cultures of cortical neurons from rat embryos were incubated with salmon lecithin NL from day 3 after cell culture, for up to 104 h. The physicochemical properties of NL such as size, speed, morphology and the diffusion coefficient in the live cultures, were studied over time. Image analysis of cell morphology showed dendritic growth and neuronal arborization after 48 h of exposure to NL, for up to 104 h. Results showed an NL stability in size, speed and diffusion coefficient over time, with a peak at 48 h, and then a return to baseline value at the end of incubation. The average speed and diffusion coefficient achieved provided important information on the mode of entry of NL into neurons, and on the slow diffusion rate of NL into the cells. Analysis of videos from 2 h to 104 h showed that significant levels of NL were already internalized by neurons after 3 h incubation. NL appearance and intracellular distribution indicated that they were packed in intracellular compartments similar to endocytic vesicles, suggesting internalization by an active endocytic-like process. The results obtained here demonstrate internalization of NL by cortical neurons by an active endocytic-like process, and suggest the potential use of NL for time-release of therapeutics aimed towards prevention or treatment of neurodegenerative diseases.

6.
Int J Mol Sci ; 23(20)2022 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-36293278

RESUMO

Hop (Humulus lupulus L.) is a plant used as an ingredient in beer or employed for its anti-inflammatory properties. The cultivation of hops is currently dedicated to the brewing industry, where mainly female flowers are used, whereas aerial parts, such as leaves, are considered coproducts. Osteoarthritis is the most common musculoskeletal disease associated with low-grade cartilage inflammation. Liposomes have been shown to be promising systems for drug delivery to cartilage cells, called chondrocytes. The aim of our work was to vectorize hop extract valorized from coproducts as a therapeutic agent to alleviate inflammation in human chondrocytes in vitro. Liquid chromatography allowed the identification of oxidized bitter acids in a methanolic extract obtained from the leaves of Cascade hops. The extract was encapsulated in rapeseed lecithin nanoliposomes, and the physicochemical properties of empty or loaded nanoliposomes exhibited no difference. Increasing concentrations of the hop extract alone, empty nanoliposomes, and loaded nanoliposomes were tested on human chondrocytes to assess biocompatibility. The appropriate conditions were applied to chondrocytes stimulated with interleukin-1ß to evaluate their effect on inflammation. The results reveal that encapsulation potentiates the hop extract anti-inflammatory effect and that it might be able to improve joint inflammation in osteoarthritis. Furthermore, these results also show that a "zero waste" chain is something that can be achieved in hop cultivation.


Assuntos
Brassica napus , Brassica rapa , Humulus , Osteoartrite , Humanos , Humulus/química , Lecitinas , Interleucina-1beta , Condrócitos , Lipossomos , Extratos Vegetais/química , Inflamação/tratamento farmacológico , Osteoartrite/tratamento farmacológico
7.
Mar Drugs ; 20(4)2022 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-35447922

RESUMO

Salmon byproducts (Salmo salar) generated by the food chain represent a source of long-chain polyunsaturated fatty acids (eicosapentaenoic acid (EPA): 20:5n-3; docosahexaenoic acid (DHA): 22:6n-3) and peptides that can be used as supplements in food for nutraceutical or health applications, such as in the prevention of certain pathologies (e.g., Alzheimer's and cardiovascular diseases). The extraction of polar lipids naturally rich in PUFAs by enzymatic processes without organic solvent (controlled by pH-Stat method), coupled with the production of 1 kDa salmon peptides by membrane filtration, allowed the formulation of nanocarriers. The physicochemical properties of the nanoliposomes (size ranging from 120 to 140 nm, PDI of 0.27, zeta potential between -32 and -46 mV and encapsulation efficiency) were measured, and the bioactivity of salmon hydrolysate peptides was assessed (antioxidant and antiradical activity: ABTS, ORAC, DPPH; iron metal chelation). Salmon peptides exhibited good angiotensin-conversion-enzyme (ACE) inhibition activity, with an IC50 value of 413.43 ± 13.12 µg/mL. Cytotoxicity, metabolic activity and proliferation experiments demonstrated the harmlessness of the nanostructures in these experimental conditions.


Assuntos
Lipossomos , Salmo salar , Animais , Ácidos Docosa-Hexaenoicos/farmacologia , Ácido Eicosapentaenoico/farmacologia , Ácidos Graxos , Peptídeos/farmacologia
8.
Int J Mol Sci ; 23(5)2022 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-35270005

RESUMO

The low efficiency in transfecting rat- and human-derived chondrocytes have been hampering developments in the field of cartilage biology. Transforming growth factor (TGF)-ß1 has shown positive effects on chondrocytes, but its applications remain limited due to its short half-life, low stability and poor penetration into cartilage. Naturally derived liposomes have been shown to be promising delivery nanosystems due to their similarities with biological membranes. Here, we used agro-based rapeseed liposomes, which contains a high level of mono- and poly-unsaturated fatty acids, to efficiently deliver encapsulated TGF-ß1 to rat chondrocytes. Results showed that TGF-ß1 encapsulated in nano-sized rapeseed liposomes were safe for chondrocytes and did not induce any alterations of their phenotype. Furthermore, the controlled release of TGF-ß1 from liposomes produced an improved response in chondrocytes, even at low doses. Altogether, these outcomes demonstrate that agro-based nanoliposomes are promising drug carriers.


Assuntos
Cartilagem Articular , Condrócitos , Animais , Cartilagem/metabolismo , Cartilagem Articular/metabolismo , Células Cultivadas , Condrócitos/metabolismo , Portadores de Fármacos/farmacologia , Lipossomos/metabolismo , Ratos , Fator de Crescimento Transformador beta/metabolismo , Fator de Crescimento Transformador beta1/metabolismo
9.
Int J Mol Sci ; 22(21)2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34769291

RESUMO

Omega-3 polyunsaturated fatty acids (n-3 PUFAs) play an important role in the development, maintenance, and function of the brain. Dietary supplementation of n-3 PUFAs in neurological diseases has been a subject of particular interest in preventing cognitive deficits, and particularly in age-related neurodegeneration. Developing strategies for the efficient delivery of these lipids to the brain has presented a challenge in recent years. We recently reported the preparation of n-3 PUFA-rich nanoliposomes (NLs) from salmon lecithin, and demonstrated their neurotrophic effects in rat embryo cortical neurons. The objective of this study was to assess the ability of these NLs to deliver PUFAs in cellulo and in vivo (in mice). NLs were prepared using salmon lecithin rich in n-3 PUFAs (29.13%), and characterized with an average size of 107.90 ± 0.35 nm, a polydispersity index of 0.25 ± 0.01, and a negative particle-surface electrical charge (-50.4 ± 0.2 mV). Incubation of rat embryo cortical neurons with NLs led to a significant increase in docosahexaenoic acid (DHA) (51.5%, p < 0.01), as well as palmitic acid, and a small decrease in oleic acid after 72 h (12.2%, p < 0.05). Twenty mice on a standard diet received oral administration of NLs (12 mg/mouse/day; 5 days per week) for 8 weeks. Fatty acid profiles obtained via gas chromatography revealed significant increases in cortical levels of saturated, monounsaturated, and n-3 (docosahexaenoic acid,) and n-6 (docosapentaenoic acid and arachidonic acid) PUFAs. This was not the case for the hippocampus or in the liver. There were no effects on plasma lipid levels, and daily monitoring confirmed NL biocompatibility. These results demonstrate that NLs can be used for delivery of PUFAs to the brain. This study opens new research possibilities in the development of preventive as well as therapeutic strategies for age-related neurodegeneration.


Assuntos
Ácidos Graxos Ômega-3/administração & dosagem , Ácidos Graxos Insaturados/sangue , Lecitinas/administração & dosagem , Neurônios/citologia , Salmão/metabolismo , Administração Oral , Animais , Disponibilidade Biológica , Células Cultivadas , Cromatografia Gasosa , Ácidos Docosa-Hexaenoicos/análise , Ácidos Graxos Ômega-3/farmacocinética , Feminino , Hipocampo/química , Lecitinas/farmacocinética , Lipossomos , Fígado/química , Masculino , Camundongos , Nanoestruturas , Neurônios/química , Ácido Oleico/análise , Ácido Palmítico/análise , Tamanho da Partícula , Cultura Primária de Células , Ratos
10.
Int J Biol Macromol ; 169: 480-491, 2021 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-33352160

RESUMO

The modification of gum Arabic with ferulic acid oxidation products was performed in aqueous medium, at 30 °C and pH 7.5, in the presence of Myceliophthora thermophila laccase as biocatalyst. First, this study aimed to investigate the structures of the oxidation products of ferulic acid that could possibly be covalently grafted onto gum Arabic. HPLC analyses revealed that this reaction produced several oxidation products, whose structures were investigated using LC-MS/MS analyses (liquid chromatography-mass spectrometry with mass fragmentation analyses) and NMR experiments. The chemical structure of one intermediate reaction product was fully elucidated as the 2-(4-hydroxy-3-methoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl) methylidene] cyclobutane-1, 3-dione, called by the authors cyclobutadiferulone. Secondly, this study aimed to locate the grafting of the oxidation products onto gum Arabic by performing several NMR experiments. This study did not determine how much and specifically which oxidation products were grafted but some of them were undeniably present onto modified gum Arabic, close to the glucuronic acid C5 carbon or close to the galactose C6 carbon.


Assuntos
Ácidos Cumáricos/química , Goma Arábica/química , Lacase/química , Acacia/química , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia Líquida/métodos , Enzimas/química , Ácido Glucurônico/química , Lacase/metabolismo , Espectroscopia de Ressonância Magnética/métodos , Oxirredução , Polímeros/química , Sordariales/enzimologia , Sordariales/metabolismo , Espectrometria de Massas em Tandem/métodos , Água/química
11.
Int J Mol Sci ; 21(23)2020 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-33260309

RESUMO

Polyunsaturated fatty acids (PUFA) are important in reducing the risk for cardiovascular, metabolic and neurodegenerative diseases. Chia (Salvia hispanica L.) seeds contain high levels of omega-3 PUFA, α-linolenic acid (ALA) in particular, and are a potential source for development of omega-3 PUFA-based products. Our objective was to obtain and characterize chia seed lipids, focusing on phospholipid fraction, and to investigate their use in the formulation of nanoemulsions (NE) and nanoliposomes (NL). Solvent-based lipid extraction was performed on the ORURO variety of chia seeds, followed by lipid composition analysis using GC and LC-MS and physico-chemical characterization of chia NL and NE. Folch extraction led to a slightly higher yield of ALA as compared to Soxhlet extraction. Lipid, phospholipid, and fatty acid composition analysis of the oil and residue revealed that the residue was rich in phospholipids; these were used to prepare NE and NL. Physico-chemical characterization showed that NE and NL were generally spherical (transmission electron microscopy), with a size of <120 nm under hydrated conditions that remained stable over 5 days. In conclusion, chia oil and phospholipid-rich residue can be used to obtain stable NL or NE using a simple method that involves spontaneous emulsification during lipid hydration, which potentially may be useful in cosmetics, pharmaceutical, and other health applications.


Assuntos
Emulsões/química , Lipídeos/química , Lipossomos/química , Nanopartículas/química , Salvia/química , Sementes/química , Ácidos Graxos/análise , Lipídeos/isolamento & purificação , Nanopartículas/ultraestrutura , Tamanho da Partícula , Padrões de Referência
12.
Int J Mol Sci ; 21(19)2020 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-33019782

RESUMO

Curcumin is a hydrophobic drug gaining growing attention because of its high availability, its innocuity, and its anticancer, antitumoral, and antioxidative activity. However, its poor bioavailability in the human body, caused by its low aqueous solubility and fast degradation, presents a big hurdle for its oral administration. Here, we used nano-vesicles made of phospholipids to carry and protect curcumin in its membrane. Various curcumin amounts were encapsulated in the produced phospholipid system to form drug-loaded liposomes. Curcumin's concentration was evaluated using UV-visible measurements. The maximal amount of curcumin that could be added to liposomes was assessed. Nuclear magnetic resonance (NMR) analyses were used to determine curcumin's interactions and localization within the phospholipid membrane of the liposomes. X-ray scattering (SAXS) and atomic force microscopy (AFM) experiments were performed to characterize the membrane structure and organization, as well as its mechanical properties at the nanoscale. Conservation of the membrane's properties is found with the addition of curcumin in various amounts before saturation, allowing the preparation of a defined nanocarrier with desired amounts of the drug.


Assuntos
Antineoplásicos Fitogênicos/química , Curcumina/química , Lipossomos/química , Fosfatidilcolinas/química , Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos , Soluções , Água/química
13.
Lipids ; 55(6): 671-682, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-32770855

RESUMO

Lipid composition of liposomal bilayer should alter the cell response for permeability, transport, and uptake in small intestine. This work was done to investigate the transport and uptake of liposomes composed of docosahexaenoic acid-enriched phosphatidylcholine (PtdCho), phosphatidylserine (PtdSer), and sulfoquinovosyl diacylglycerol (SQDG) derived from marine products on multilamellar vesicles (MLV) in small intestinal epithelial cell models. The results showed that addition of PtdSer and SQDG as liposomal bilayer could improve the efficiency entrapment of liposomes. The liposomes containing PtdSer showed higher transport and uptake through both Caco-2 cell and M cell monolayers as compared to PtdCho-MLV. SQDG-containing liposomes exhibited only higher transport through M cell monolayer, while its uptake effect was higher both in Caco-2 cell and M cell monolayers. The results of experiments done with endocytosis inhibitors indicated that PtdCho-MLV must be transported via macropinocytosis and uptaken by phagocytosis in M cell monolayer model. PtdCho/PtdSer-MLV and PtdCho/SQDG-MLV might be transported and uptaken through M cell monolayer by phagocytosis. The result also indicated that PtdCho/SQDG-MLV could open the tight junction of small intestinal epithelial cell monolayers. Furthermore, our findings demonstrated that the surface status of cholesterol-containing liposomes were smooth, but they did not affect their transport and uptake through Caco-2 cell and M cell monolayers.


Assuntos
Ácidos Graxos/análise , Intestino Delgado/citologia , Lipossomos/química , Lipossomos/farmacocinética , Animais , Transporte Biológico , Células CACO-2 , Técnicas de Cocultura , Decapodiformes/química , Células Epiteliais , Corantes Fluorescentes/farmacocinética , Glicolipídeos/isolamento & purificação , Glicolipídeos/farmacocinética , Humanos , Intestino Delgado/metabolismo , Isoquinolinas/farmacocinética , Microscopia de Força Atômica , Fosfatidilcolinas/farmacocinética , Sargassum/química
14.
Molecules ; 25(13)2020 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-32605291

RESUMO

To promote the nutritional and pharmacological values of four sea cucumber species (Holothuria poli, H. tubulosa, H. arguinensis, and H. sanctori), harvested from the Algerian coast, we aimed to study their proximate composition, fatty acid profile and angiotensin-converting enzyme (ACE) inhibitory activity. Their phospholipids were also used to elaborate nanoliposomes and to encapsulate peptides obtained from the same source. After the physico-chemical characterization of nanoliposomes and peptides, in vitro analyses were realized. The four holothurian species showed a high amount of protein (49.26-69.34%), and an impressive lipid profile of 27 fatty acids, mainly composed of polar fatty acids (91.16-93.85%), with a high polyunsaturated fatty acids (PUFA) content (50.90-71.80%), particularly eicosapentaenoic acid (EPA) (5.07-8.76%) and docosahexaenoic acid (DHA) (4.86-7.25%). A high phospholipids amount was also found (55.20-69.85%), mainly composed of phosphatidylcholine (PC) (51.48-58.56%). Their peptide fractions exhibited a high ACE inhibitory activity (IC50 0.30 to 0.51 mg/mL). The results also showed that the nanoliposomes do not induce cytotoxicity and cell death in human MSCs and no perturbation of proliferation for all the times and the tested concentrations, as well as the combined nanoliposomes and hydrolysates (HTS) at a concentration of 0.1 mg/mL. All four sea cucumbers show potential as a new source for omega-3, omega-6, and bioactive peptides.


Assuntos
Inibidores da Enzima Conversora de Angiotensina/análise , Ácidos Graxos/análise , Fosfolipídeos/análise , Pepinos-do-Mar/química , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Animais , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Humanos , Hidrólise , Lipossomos , Células-Tronco Mesenquimais/citologia , Nanopartículas , Fosfolipídeos/farmacologia , Cultura Primária de Células , Pepinos-do-Mar/metabolismo
15.
Int J Mol Sci ; 21(10)2020 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-32414043

RESUMO

Investigations in cartilage biology have been hampered by the limited capacity of chondrocytes, especially in rats and humans, to be efficiently transfected. Liposomes are a promising delivery system due to their lipid bilayer structure similar to a biological membrane. Here we used natural rapeseed lecithin, which contains a high level of mono- and poly-unsaturated fatty acids, to evaluate the cytocompatibility of these phospholipids as future potential carriers of biomolecules in joint regenerative medicine. Results show that appropriate concentrations of nanoliposome rapeseed lecithin under 500 µg/mL were safe for chondrocytes and did not induce any alterations of their phenotype. Altogether, these results sustain that they could represent a novel natural carrier to deliver active substances into cartilage cells.


Assuntos
Cartilagem Articular/crescimento & desenvolvimento , Condrócitos/efeitos dos fármacos , Lipossomos/farmacologia , Nanopartículas/química , Animais , Brassica napus/química , Cartilagem Articular/efeitos dos fármacos , Membrana Celular/genética , Sistemas de Liberação de Medicamentos , Humanos , Lecitinas/química , Lecitinas/genética , Lecitinas/farmacologia , Lipossomos/química , Fosfolipídeos/genética , Ratos , Medicina Regenerativa
16.
Mar Drugs ; 18(4)2020 Apr 17.
Artigo em Inglês | MEDLINE | ID: mdl-32316578

RESUMO

Current anticancer drugs exhibit limited efficacy and initiate severe side effects. As such, identifying bioactive anticancer agents that can surpass these limitations is a necessity. One such agent, curcumin, is a polyphenolic compound derived from turmeric, and has been widely investigated for its potential anti-inflammatory and anticancer effects over the last 40 years. However, the poor bioavailability of curcumin, caused by its low absorption, limits its clinical use. In order to solve this issue, in this study, curcumin was encapsulated in chitosan-coated nanoliposomes derived from three natural lecithin sources. Liposomal formulations were all in the nanometric scale (around 120 nm) and negatively charged (around -40 mV). Among the three lecithins, salmon lecithin presented the highest growth-inhibitory effect on MCF-7 cells (two times lower growth than the control group for 12 µM of curcumin and four times lower for 20 µM of curcumin). The soya and rapeseed lecithins showed a similar growth-inhibitory effect on the tumor cells. Moreover, coating nanoliposomes with chitosan enabled a higher loading efficiency of curcumin (88% for coated liposomes compared to 65% for the non-coated liposomes) and a stronger growth-inhibitory effect on MCF-7 breast cancer cells.


Assuntos
Antineoplásicos/farmacologia , Curcumina/farmacologia , Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos/métodos , Lipossomos/farmacologia , Animais , Disponibilidade Biológica , Brassica rapa , Neoplasias da Mama/tratamento farmacológico , Quitosana , Portadores de Fármacos , Feminino , Humanos , Lecitinas , Células MCF-7 , Nanopartículas , Salmão , Células Tumorais Cultivadas/efeitos dos fármacos
17.
Mar Drugs ; 18(4)2020 Apr 13.
Artigo em Inglês | MEDLINE | ID: mdl-32295082

RESUMO

Breast cancer is the leading cause of death from cancer among women. Higher consumption of dietary marine n-3 long-chain polyunsaturated fatty acids (LC-PUFAs) is associated with a lower risk of breast cancer. Eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) are two n-3 LC-PUFAs found in fish and exert anticancer effects. In this study, natural marine- derived lecithin that is rich in various polyunsaturated fatty acids (PUFAs) was extracted from salmon heads and transformed into nanoliposomes. These nanoliposomes were characterized and cultured with two breast cancer lines (MCF-7 and MDA-MB- 231). The nanoliposomes decreased the proliferation and the stiffness of both cancer cell types. These results suggest that marine-derived lecithin possesses anticancer properties, which may have an impact on developing new liposomal delivery strategies for breast cancer treatment.


Assuntos
Antineoplásicos/química , Ácidos Docosa-Hexaenoicos/química , Ácido Eicosapentaenoico/química , Peixes , Lipossomos/química , Animais , Antineoplásicos/farmacologia , Ácidos Docosa-Hexaenoicos/farmacologia , Ácido Eicosapentaenoico/farmacologia , Feminino , Humanos , Lipossomos/farmacologia , Células MCF-7/efeitos dos fármacos
18.
Mar Drugs ; 17(7)2019 Jul 09.
Artigo em Inglês | MEDLINE | ID: mdl-31323972

RESUMO

Lipids play multiple roles in preserving neuronal function and synaptic plasticity, and polyunsaturated fatty acids (PUFAs) have been of particular interest in optimizing synaptic membrane organization and function. We developed a green-based methodology to prepare nanoliposomes (NL) from lecithin that was extracted from fish head by-products. These NL range between 100-120 nm in diameter, with an n-3/n-6 fatty acid ratio of 8.88. The high content of n-3 PUFA (46.3% of total fatty acid content) and docosahexanoic acid (26%) in these NL represented a means for enrichment of neuronal membranes that are potentially beneficial for neuronal growth and synaptogenesis. To test this, the primary cultures of rat embryo cortical neurons were incubated with NL on day 3 post-culture for 24 h, followed by immunoblots or immunofluorescence to evaluate the NL effects on synaptogenesis, axonal growth, and dendrite formation. The results revealed that NL-treated cells displayed a level of neurite outgrowth and arborization on day 4 that was similar to those of untreated cells on day 5 and 6, suggesting accelerated synapse formation and neuronal development in the presence of NL. We propose that fish-derived NL, by virtue of their n-3 PUFA profile and neurotrophic effects, represent a new innovative bioactive vector for developing preventive or curative treatments for neurodegenerative diseases.


Assuntos
Ácidos Graxos Ômega-3/administração & dosagem , Lecitinas/administração & dosagem , Neurônios/efeitos dos fármacos , Salmão , Sinapses/efeitos dos fármacos , Animais , Células Cultivadas , Córtex Cerebral/citologia , Composição de Medicamentos/métodos , Avaliação Pré-Clínica de Medicamentos , Embrião de Mamíferos , Química Verde/métodos , Lipossomos , Nanopartículas/química , Plasticidade Neuronal/efeitos dos fármacos , Cultura Primária de Células , Ratos
19.
Molecules ; 24(10)2019 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-31137865

RESUMO

Curcumin, a natural polyphenol, has many biological properties, such as anti-inflammatory, antioxidant, and anti-carcinogenic properties, yet, its sensitivity to light, oxygen, and heat, and its low solubility in water renders its preservation and bioavailability challenging. To increase its bioaccessibility, we fabricated nanoliposomes and chitosan-coated nanoliposomes encapsulating curcumin, and we evaluated the systems in terms of their physicochemical characteristics and release profiles in simulated gastrointestinal mediums. Chitosan-coating enhanced the stability of nanoliposomes and slowed the release of curcumin in the simulated gastrointestinal (GI) environment. This study demonstrates that nanoliposomes and chitosan-coated nanoliposomes are promising carriers for poorly soluble lipophilic compounds with low oral bioavailability, such as curcumin.


Assuntos
Quitosana/química , Curcumina/farmacologia , Nanopartículas/química , Animais , Liberação Controlada de Fármacos , Ácidos Graxos/análise , Cinética , Lipossomos , Salmão
20.
Mar Drugs ; 16(7)2018 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-29941790

RESUMO

Curcumin (diferuloylmethane) is a natural bioactive compound with many health-promoting benefits. However, its poor water solubility and bioavailability has limited curcumin’s biomedical application. In the present study, we encapsulated curcumin into liposomes, formed from natural sources (salmon lecithin), and characterized its encapsulation efficiency and release profile. The proposed natural carriers increased the solubility and the bioavailability of curcumin. In addition, various physico-chemical properties of the developed soft nanocarriers with and without curcumin were studied. Nanoliposome-encapsulated curcumin increased the viability and network formation in the culture of primary cortical neurons and decreased the rate of apoptosis.


Assuntos
Curcumina/química , Curcumina/metabolismo , Lipossomos/química , Nanopartículas/química , Neurônios/efeitos dos fármacos , Salmão/metabolismo , Animais , Apoptose/efeitos dos fármacos , Disponibilidade Biológica , Portadores de Fármacos/química , Lecitinas/química , Solubilidade/efeitos dos fármacos
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