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Polymer nanocapsules with hydrophobic cores are promising candidates for nanoreactors to carry out (bio)chemical reactions mimicking the performance of natural cellular systems. Their architecture allows reagents to be encapsulated in the cores enabling reactions to proceed in confined environments in a controlled, and efficient manner. Polysaccharide-shell oil-core nanocapsules are proposed here as facile mergeable nanoreactors. Spontaneous fusion of oppositely charged polysaccharide capsules is demonstrated for the first time. Such capsules are formed and easily loaded with reagents by nanoemulsification of an aqueous solution of hydrophobically modified polysaccharides (chitosan, hyaluronate) and oleic acid with dissolved desired hydrophobic compounds. Efficient fusion of the formed nanocapsules dispersed in an aqueous medium at optimized conditions (pH, ionic strength) is followed using fluorescence microscopy by labeling both their cores and shells with fluorescent dyes. As a proof of concept, a model fluorogenic synthesis is also realized by fusing the capsules containing separated reagents and the catalyst. The nanocapsules and fusion process developed here establish a platform for realization of versatile reactions in a confined environment including model studies on biologically relevant processes taking place in natural systems.
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Over the last few decades, cancer has been considered a clinical challenge, being among the leading causes of mortality all over the world. Although many treatment approaches have been developed for cancer, chemotherapy is still the most utilized in the clinical setting. However, the available chemotherapeutics-based treatments have several caveats including their lack of specificity, adverse effects as well as cancer relapse and metastasis which mainly explains the low survival rate of patients. Lipid nanoparticles (LNPs) have been utilized as promising nanocarrier systems for chemotherapeutics to overcome the challenges of the currently applied therapeutic strategies for cancer treatment. Loading chemotherapeutic agent(s) into LNPs improves drug delivery at different aspects including specific targeting of tumours, and enhancing the bioavailability of drugs at the tumour site through selective release of their payload, thus reducing their undesired side effects on healthy cells. This review article delineates an overview of the clinical challenges in many cancer treatments as well as depicts the role of LNPs in achieving optimal therapeutic outcomes. Moreover, the review contains a comprehensive description of the many LNPs categories used as nanocarriers in cancer treatment to date, as well as the potential of LNPs for future applications in other areas of medicine and research.
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Nanopartículas , Neoplasias , Humanos , Lipossomos , Neoplasias/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Lipídeos , Portadores de FármacosRESUMO
Oil-core nanocapsules (NCs, also known as nanoemulsions) are of great interest due to their application as efficient carriers of various lipophilic bioactives, such as drugs. Here, we reported for the first time the preparation and characterization of NCs consisting of chondroitin sulfate (CS)-based shells and liquid oil cores. For this purpose, two amphiphilic CS derivatives (AmCSs) were obtained by grafting the polysaccharide chain with octadecyl or oleyl groups. AmCS-based NCs were prepared by an ultrasound-assisted emulsification of an oil phase consisting of a mixture of triglyceride oil and vitamin E in a dispersion of AmCSs. Dynamic light scattering and cryo-transmission electron microscopy showed that the as-prepared core-shell NCs have typical diameters in the range of 30-250 nm and spherical morphology. Since CS is a strong polyanion, these particles have a very low surface potential, which promotes their stabilization. The cytotoxicity of the CS derivatives and CS-based NCs and their impact on cell proliferation were analyzed using human keratinocytes (HaCaTs) and primary human skin fibroblasts (HSFs). In vitro studies showed that AmCSs dispersed in an aqueous medium, exhibiting mild cytotoxicity against HaCaTs, while for HSFs, the harmful effect was observed only for the CS derivative with octadecyl side groups. However, the nanocapsules coated with AmCSs, especially those filled with vitamin E, show high biocompatibility with human skin cells. Due to their stability under physiological conditions, the high encapsulation efficiency of their hydrophobic compounds, and biocompatibility, AmCS-based NCs are promising carriers for the topical delivery of lipophilic bioactive compounds.
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Sulfatos de Condroitina , Portadores de Fármacos , Nanocápsulas , Nanocápsulas/química , Humanos , Sulfatos de Condroitina/química , Portadores de Fármacos/química , Suplementos Nutricionais , Fibroblastos/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Queratinócitos/efeitos dos fármacos , Emulsões/química , Tamanho da Partícula , Vitamina E/química , Sobrevivência Celular/efeitos dos fármacos , Linhagem Celular , Células HaCaTRESUMO
This study describes the comparison between the interaction of a series of peptide-functionalized chitosan-based nanocapsules and liposomes with two cell lines, i.e., mouse macrophages RAW 264.7 and human endothelial cells EA.hy926. Both types of nanocarriers are loaded with magnetic nanoparticles and designed for anti-inflammatory therapy. The choice of these magnetic nanostructures is argued based on their advantages in terms of size, morphology, chemical composition, and the multiple possibilities of modifying their surface. Moreover, active targeting might be ensured by using an external magnetic field. To explore the impact of chitosan-based nanocapsules and liposomes on cell cytophysiology, the cell viability, using the MTT assay, and cell morphology were investigated. The results revealed low to moderate cytotoxicity of free nanocapsules and significant cytotoxicity induced by chitosan-coated liposomes loaded with dexamethasone, confirming its release from the delivery system. Thus, after 48 h of treatment with nanocapsules, the viability of RAW 264.7 cells varied between 88.18% (OCNPM-1I, 3.125 µg/mL) and 76.37% (OCNPM-1, 25 µg/mL). In the same conditions, EA.hy926 cell viability was between 99.91% (OCNPM-3, 3.125 µg/mL) and 75.15% (OCNPM-3, 25 µg/mL) at the highest dose (25 µg/mL), the values being comparable for both cell lines. Referring to the cell reactivity after dexamethasone-loaded liposome application, the lowest viability of RAW 264.7 cells was 41.25% (CLDM5CP-1, 25 µg/mL) and 58.20% (CLDMM2CP-1 1.25 µg/mL) in the endothelial cell line, proving a selective character of action of nanocarriers. The cell morphology test, performed to support and confirm the results obtained by the MTT test, revealed a differentiated response for the two types of nano-carriers. As expected, an intense cytotoxic effect in the case of dexamethasone-loaded liposomes and a lack of cytotoxicity for drug-free nanocapsules were noticed. Therefore, our study demonstrated the biocompatible feature of the studied nanocarriers, which highlights them for future research as potential drug delivery systems for pharmacological applications, including anti-inflammatory therapy.
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Anti-Inflamatórios , Sobrevivência Celular , Quitosana , Lipossomos , Nanocápsulas , Lipossomos/química , Quitosana/química , Camundongos , Nanocápsulas/química , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/administração & dosagem , Humanos , Células RAW 264.7 , Sobrevivência Celular/efeitos dos fármacos , Dexametasona/farmacologia , Dexametasona/química , Dexametasona/administração & dosagem , Linhagem Celular , Nanopartículas de Magnetita/química , Materiais Biocompatíveis/química , Materiais Biocompatíveis/farmacologiaRESUMO
Curcumin (Cur), the primary curcuminoid found in Curcuma longa L., has garnered significant attention for its potential anti-inflammatory and antibacterial properties. However, its hydrophobic nature significantly limits its bioavailability. Additionally, adipose-derived stem cells (ADSCs) possess immunomodulatory properties, making them useful for treating inflammatory and autoimmune conditions. This study aims to verify the efficacy of poly(ε-caprolactone) nanocapsules (NCs) in improving Cur's bioavailability, antibacterial, and immunomodulatory activities. The Cur-loaded nanocapsules (Cur-NCs) were characterized for their physicochemical properties (particle size, polydispersity index, Zeta potential, and encapsulation efficiency) and stability over time. A digestion test simulated the behavior of Cur-NCs in the gastrointestinal tract. Micellar phase analyses evaluated the Cur-NCs' bioaccessibility. The antibacterial activity of free Cur, NCs, and Cur-NCs against various Gram-positive and Gram-negative strains was determined using the microdilution method. ADSC viability, treated with Cur-NCs and Cur-NCs in the presence or absence of lipopolysaccharide, was analyzed using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide assay. Additionally, ADSC survival was assessed through the Muse apoptotic assay. The expression of both pro-inflammatory (interleukin-1ß and tumor necrosis factor-α) and anti-inflammatory (IL-10 and transforming growth factor-ß) cytokines on ADSCs was evaluated by real-time polymerase chain reaction. The results demonstrated high stability post-gastric digestion of Cur-NCs and elevated bioaccessibility of Cur post-intestinal digestion. Moreover, Cur-NCs exhibited antibacterial activity against Escherichia coli without affecting Lactobacillus growth. No significant changes in the viability and survival of ADSCs were observed under the experimental conditions. Finally, Cur-NCs modulated the expression of both pro- and anti-inflammatory cytokines in ADSCs exposed to inflammatory stimuli. Collectively, these findings highlight the potential of Cur-NCs to enhance Cur's bioavailability and therapeutic efficacy, particularly in cell-based treatments for inflammatory diseases and intestinal dysbiosis.
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Antibacterianos , Disponibilidade Biológica , Curcumina , Nanocápsulas , Poliésteres , Curcumina/farmacologia , Curcumina/química , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/farmacocinética , Nanocápsulas/química , Poliésteres/química , Animais , Humanos , Fatores Imunológicos/farmacologia , Fatores Imunológicos/química , Sobrevivência Celular/efeitos dos fármacos , Tamanho da Partícula , Agentes de Imunomodulação/farmacologia , Agentes de Imunomodulação/química , Materiais Biocompatíveis/química , Materiais Biocompatíveis/farmacologia , Citocinas/metabolismo , Células-Tronco/efeitos dos fármacos , Células-Tronco/metabolismoRESUMO
Feed costs present a major burden in animal production for human consumption, representing a key opportunity for cost reduction and profit improvement. Nanotechnology offers potential to increase productivity by creating higher-quality and safer products. The feed sector has benefited from the use of nanosystems to improve the stability and bioavailability of feed ingredients. The development of nanotechnology products for feed must consider the challenges raised by biological barriers as well as regulatory requirements. While some nanotechnology-based products are already commercially available for animal production, the exponential growth and application of these products requires further research ensuring their safety and the establishment of comprehensive legislative frameworks and regulatory guidelines. Thus, this article provides an overview of the current state of the art regarding nanotechnology solutions applied in feed, as well as the risks and opportunities aimed to help researchers and livestock producers.
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OBJECTIVES: Furosemide (FSM), a potent loop diuretic, is used to treat edema due to hypertension, congestive heart failure, and liver and renal failures. FSM applications are limited by its low bioavailability. Our aim is to use different nanoencapsulation strategies to control the release of FSM and enhance its pharmacokinetic properties. METHODS: Two types of FSM-loaded nanocapsules, namely FSM-loaded lipid nanocapsules (LNCs) and polymeric nanocapsules (PNCs), were developed, physicochemically characterized, and subjected to pharmacokinetic and pharmacodynamic studies. Lipid nanocapsules were prepared by the simple phase inversion method using LabrafacTM lipid, while the polymeric nanocapsules were prepared by nanoprecipitation method using polycaprolactone polymer. RESULTS: Transmission electron microscopy ascertains spherical structures, corroborating the nanometric diameter of both types of nanocapsules. The particle size of the optimized FSM-loaded LNCs and FSM-loaded PNCs was 32.19 ± 0.72 nm and 230.7 ± 5.13 nm, respectively. The percent entrapment efficiency was 63.56 ± 1.40% of FSM for the optimized PNCs. The in vitro release study indicated prolonged drug release compared to drug solutions. The two loaded nanocapsules systems succeeded in enhancing the pharmacokinetic parameters in comparison to the marketed FSM solution with superior diuretic activity (p < 0.05). The results of the stability study and the terminal sterilization by autoclave indicated the superiority of LNCs over PNCs in maintaining the physical parameters under storage conditions and the drastic conditions of sterilization. CONCLUSIONS: LNCs and PNCs are considered promising nanosysems for improving the diuretic effect of FSM.
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Diuréticos , Furosemida , Lipídeos , Nanocápsulas , Tamanho da Partícula , Polímeros , Nanocápsulas/química , Furosemida/administração & dosagem , Furosemida/farmacocinética , Furosemida/química , Furosemida/farmacologia , Animais , Diuréticos/administração & dosagem , Diuréticos/farmacocinética , Diuréticos/farmacologia , Lipídeos/química , Polímeros/química , Ratos , Masculino , Liberação Controlada de Fármacos , Administração Intravenosa , Sistemas de Liberação de Medicamentos/métodos , Ratos Wistar , Poliésteres/química , Portadores de Fármacos/química , Disponibilidade BiológicaRESUMO
Thymoquinone (TQ) is a phytochemical compound present in Nigella sativa and has potential benefits for treating dermatological conditions such as psoriasis. However, its clinical use is limited due to its restricted bioavailability, caused mainly by its low solubility and permeability. To overcome this, a new transdermal drug delivery system is required. Nanoparticles are known to enhance material solubility and permeability, and hence, this study aimed to synthesize TQ-loaded L-arginine-based polyamide (TQ/Arg PA) nanocapsules incorporated into transdermal patches for prolonged delivery of TQ. To achieve this, Eudragit E polymer, plasticizers, and aloe vera as penetration enhancer were used to develop the transdermal patch. Furthermore, novel TQ/Arg-PA was synthesized via interfacial polymerization, and the resultant nanocapsules (NCs) were incorporated into the matrix transdermal patch. The Arg-PA NCs' structure was confirmed via NMR and FTIR, and optimal TQ/Arg-PA NCs containing formulation showed high entrapment efficiency of TQ (99.60%). Molecular and thermal profiling of TQ/Arg-PA and the transdermal patch revealed the effective development of spherical NCs with an average particle size of 129.23 ± 18.22 nm. Using Franz diffusion cells and synthetic membrane (STRAT M®), the in vitro permeation profile of the prepared patches demonstrated an extended release of TQ over 24 h, with enhanced permeation by 42.64% when aloe vera was employed. In conclusion, the produced formulation has a potential substitute for corticosteroids and other drugs commonly used to treat psoriasis due to its effectiveness, safety, and lack of the side effects typically associated with other drugs.
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Benzoquinonas , Nanocápsulas , Psoríase , Humanos , Nanocápsulas/química , Nylons , Adesivo Transdérmico , Psoríase/tratamento farmacológicoRESUMO
Lipids have tremendously transformed the biomedical field, especially in the last few decades. Nanosystems, especially Lipid nanocapsules (LNCs), have emerged as the most demanding nanovehicle systems for delivering drugs, genes, and other diagnostic agents. Unique attributes and characteristic features such as higher encapsulation efficiency, stealth effect, ability to solubilize a wide range of drugs, capability to inhibit P-gp efflux pumps, and higher stability play a vital role in engaging this nanosystem. LNCs are a lipid-based nano-drug delivery method that combines the most significant traits of liposomes with polymeric nanoparticles. Structurally, LNCs have an oily core consisting of medium and long triglycerides and an aqueous phase encased in an amphiphilic shell. This manuscript crosstalks LNCs for various biomedical applications. A detailed elaboration of the structural composition, methods of preparation, and quality control aspects has also been attained, with particular emphasis on application approaches, ongoing challenges, and their possible resolution. The manuscript also expounds the preclinical data and discusses the patents atlas of LNCs to assist biomedical scientists working in this area and foster additional research. Supplementary Information: The online version contains supplementary material available at 10.1007/s12088-024-01298-3.
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Synthesis and assembly of two-dimensional (2D) polymeric materials present a tricky trade-off between the high reaction rate and precise morphology control. Here we report a nanoconfined synthesis of imine-based 2D covalent organic frameworks (COFs) at the interface of oil-in-water (O/W) emulsion droplets stabilized by cationic surfactants. Highly uniform nanocapsules (NCs) could be prepared without adding extra catalysts at room temperature in just 4.5 h at a yield of 86%. The NCs have tunable average diameters and shell thicknesses, depending on the monomer and surfactant types/concentrations. Their BET-specific surface areas are up to 139.0 m2/g, mainly contributed by narrowly-distributed mesopores at ~5.0 nm and micropores at 1.4 nm. The surfactant plays the role of a catalyst during the reaction and interestingly, it also regulates the formation of mesopores and their sizes. Both theoretical and experimental studies confirm that the reaction has been accelerated by two orders of magnitude at the microdroplet interface, compared to that without emulsification. The resulting NCs could be well dispersed in water, and they have been demonstrated to be highly efficient nanocatalysts in application of water-based hydrogen evolution. Such microdroplet interface-confined synthesis may facilitate the future development of 2D polymeric materials for more advanced applications.
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Drought and water scarcity are two of the world's major problems. Solar-powered sorption-based atmospheric water harvesting technology is a promising solution in this category. The main challenge is to design materials with high water harvesting performance while achieving fast water vapor adsorption/desorption rates. Here, a superhydrophilic photothermic hollow nanocapsule (SPHN) is represented that achieves efficient atmospheric water harvesting in outdoor climates. In SPHN, the hollow mesoporous silica (HMS) is grafted with polypyrrole (PPy) and also loaded with lithium chloride (LiCl). The hollow structure is used to store water while preventing leakage. The hydrophilic spherical nanocapsule and the trapped water produce more free and weakly adsorbed water. Significantly lower the heat of desorption compared to pure LiCl solution. Such SPHN significantly improves the adsorption/desorption kinetics, e.g., absorbs 0.78-2.01 g of water per gram of SPHN at 25 °C, relative humidity (RH) 30-80% within 3 h. In particular, SPHN has excellent photothermal properties to achieve rapid water release under natural sunlight conditions, i.e., 80-90% of water is released in 1 h at 0.7-1.0 kW m-2 solar irradiation, and 50% of water is released even at solar irradiation as low as 0.4 kW m-2 . The water collection capacity can reach 1.2 g g-1 per cycle by using the self-made atmospheric water harvesting (AWH) device. This finding provides a way to design novel materials for efficient water harvesting tasks, e.g., water engineering, freshwater generator, etc.
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The improved understanding of the connection between diet and health has led to growing interest in the development of functional foods designed to improve health and wellbeing. Many of the potentially health-promoting bioactive ingredients that food manufacturers would like to incorporate into these products are difficult to utilize because of their chemical instability, poor solubility, or low bioavailability. For this reason, nano-based delivery systems are being developed to overcome these problems. Food proteins possess many functional attributes that make them suitable for formulating various kinds of nanocarriers, including their surface activity, water binding, structuring, emulsification, gelation, and foaming, as well as their nutritional aspects. Proteins-based nanocarriers are therefore useful for introducing bioactive ingredients into functional foods, especially for their targeted delivery in specific applications.This review focusses on the preparation, properties, and applications of protein-based nanocarriers, such as nanoparticles, micelles, nanocages, nanoemulsions, and nanogels. In particular, we focus on the development and application of stimulus-responsive protein-based nanocarriers, which can be used to release bioactive ingredients in response to specific environmental triggers. Finally, we discuss the potential and future challenges in the design and application of these protein-based nanocarriers in the food industry.
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Sistemas de Liberação de Fármacos por Nanopartículas , Nanopartículas , Nanopartículas/química , Proteínas , Solubilidade , Alimento FuncionalRESUMO
The construction of an environmentally responsive drug-release system is of great significance for the treatment of special diseases. In particular, the construction of nanomaterials with pH- and thermal-responsiveness, which can effectively encapsulate drugs and control drug release, is becoming hot research. In this study, zwitterionic nanocapsules with stable core-shell structures were synthesized by inverse reversible addition-fragmentation transfer miniemulsion interfacial polymerization. To further study the structure and performance of the nanocapsules, the prepared nanocapsules were characterized by transmission electron microscopy, dynamic light dispersion, and zeta potential analysis. It was found that the nanocapsules had dual pH- and thermal- responsiveness, and the average particle size ranged from 178 to 142 nm when the temperature changed from 25 °C to 40 °C. In addition, bovine serum albumin (BSA) was encapsulated into nanocapsules, and sustained release experiments were conducted at 10 °C and 40 °C. The results showed that nanocapsules as carriers of BSA could achieve the purpose of sustained release of drugs, and showed different sustained release curves at different temperatures. Finally,in vitrocytotoxicity tests were performed to demonstrate the feasibility of their biomedical application. It is believed that the dual pH- and thermal- responsive nanocapsules are promising for drug-controlled release.
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Nanocápsulas , Nanocápsulas/química , Liberação Controlada de Fármacos , Preparações de Ação Retardada , Microscopia Eletrônica de Transmissão , Soroalbumina Bovina , Concentração de Íons de Hidrogênio , Tamanho da PartículaRESUMO
The Ugi four-component condensation in diluted liposomal suspensions was used to prepare pectin-based submicron capsules. A set of isocyanides and aldehydes was used to optimize the synthesis of capsule shells. Modified sugar beet pectin was selected as a natural polymer with pronounced surface activity to create a capsule shell. At first, liposomal composition was optimized in order to select suitable conditions for capsule formation. Then, the wide set of capsules constructed on modified sugar beet pectin scaffold has been synthesized. The choice was determined by level of substitution degree and possible chemical diversity of the modified surface. Detailed characterization of products has been performed for polysaccharide particles with liposomal core prepared with various processing parameters (concentration, cross-linking components, the density of linkage). The chemical structure, average size, polydispersity index, morphology, stability, and cytotoxicity of obtained particles have been investigated in dependence on the shell content. The obtained submicrometer cross-linked capsules (220-240 nm) with controlled colloidal properties showed high stability and low toxicity. Thus, the proposed carriers have a great potential as sustained drug delivery systems for different administration routes.
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Beta vulgaris , Pectinas , Pectinas/química , Beta vulgaris/química , Polímeros , AçúcaresRESUMO
BACKGROUND: Pharmacotherapy constitutes the first-line treatment for depression. However, its clinical use is hindered by several limitations, such as time lag, side effects, and narrow therapeutic windows. Nanotechnology can be employed to shorten the onset time by ensuring permeation across the blood brain barrier (BBB) to precisely deliver more therapeutic agents; unfortunately, formidable challenges owing to the intrinsic shortcomings of commercial drugs remain. RESULTS: Based on the extraordinary capability of monoamines to regulate the neuronal environment, we engineer a network nanocapsule for delivering serotonin (5-hydroxytryptamine, 5-HT) and catalase (CAT) to the brain parenchyma for synergistic antidepression therapy. The nanoantidepressants are fabricated by the formation of 5-HT polymerization and simultaneous payload CAT, following by surface modifications using human serum albumin and rabies virus glycoprotein. The virus-inspired nanocapsules benefit from the surface-modifying strategies and exhibit pronounced BBB penetration. Once nanocapsules reach the brain parenchyma, the mildly acidic conditions trigger the release of 5-HT from the sacrificial nanocapsule. Releasing 5-HT further positively regulate moods, relieving depressive symptoms. Meanwhile, cargo CAT alleviates neuroinflammation and enhances therapeutic efficacy of 5-HT. CONCLUSION: Altogether, the results offer detailed information encouraging the rational designing of nanoantidepressants and highlighting the potential of nanotechnology in mental health disorder therapies.
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Nanocápsulas , Humanos , Serotonina , Barreira Hematoencefálica , Encéfalo , AminasRESUMO
Chagas Disease (CD) affects around eight million people worldwide. It is considered a neglected disease that presents few treatment options with efficacy only in the acute phase. Nanoparticles have many positive qualities for treating parasite infections and may be effectively and widely employed in clinical medicine. This research aimed to evaluate the nanoencapsulated benznidazole treatment in animals experimentally infected with Trypanosoma cruzi. To analyze the treatment efficacy, we evaluated survival during thirty days, parasitemia, genotoxicity, and heart and liver histopathology. Thirty-five female Swiss mice were organized into seven groups characterizing a dose curve: A - Negative control (uninfected animals), B - Positive control (infected animals), C - Benznidazole (BNZ) 100 mg/kg (infected animals), D - 5 mg/kg Benznidazole nanocapsules (NBNZ) (infected animals), E - 10 mg/kg Benznidazole nanocapsules (infected animals), F - 15 mg/kg Benznidazole nanocapsules (infected animals), G - 20 mg/kg Benznidazole nanocapsules (infected animals). The animals were infected with the Y strain of T. cruzi intraperitoneally. The treatment was administered for eight days by oral gavage. It was possible to observe that the treatment with the highest NBNZ dose presented efficacy similar to the standard benznidazole drug. The 20 mg/kg NBNZ dose was able to reduce parasitemia, increase survival, and drastically reduce heart and liver tissue damage compared to the 100 mg/kg BNZ dose. Moreover, it showed a lower DNA damage index than the BNZ treatment. In conclusion, the nanoencapsulation of BNZ promotes an improvement in parasite proliferation control with a five times smaller dose relative to the standard dose of free BNZ, thus demonstrating to be a potential innovative therapy for CD.
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Doença de Chagas , Nanocápsulas , Nitroimidazóis , Tripanossomicidas , Trypanosoma cruzi , Camundongos , Animais , Feminino , Parasitemia/tratamento farmacológico , Parasitemia/parasitologia , Tripanossomicidas/farmacologia , Tripanossomicidas/uso terapêutico , Doença de Chagas/parasitologia , Nitroimidazóis/farmacologia , Nitroimidazóis/uso terapêuticoRESUMO
Chagas disease (CD) remains neglected and causes high morbidity and mortality. The great difficulty is the lack of effective treatment. The current drugs cause side effects and have limited therapeutic efficacy in the chronic phase. This study aims to fulfil some gaps in studies of the natural substance lychnopholide nanoencapsulated LYC-PLA-PEG-NC (LYC-NC) and free (Free-LYC): the activity in epimastigotes and amastigotes to determine its selectivity index (SI), the therapeutic efficacy in mice infected with Colombian Trypanosoma cruzi strain and insight of the mechanism of LYC-NC action on T. cruzi. The SI was obtained by calculation of the ratio between the IC50 value toward H9c2 cells divided by the IC50 value in the anti-T. cruzi test. Infected Swiss mice were treated with 2 and 12 mg/kg/day via intravenous and oral, respectively, and the therapeutic efficacy was determined. The IC50 of LYC-NC and Free-LYC for epimastigotes of T. cruzi were similar. Both were active against amastigotes in cell culture, particularly Free-LYC. The SI of LYC-NC and Free-LYC were 45.38 and 32.11, respectively. LYC-NC 2 and 12 mg/kg/day cured parasitologically, 62.5% and 80% of the animals, respectively, infected with a strain resistant to treatment. The fluorescent NC was distributed in the cardiomyocyte cytoplasm, infected or not, and interacted with the trypomastigotes. Together, these results represent advances in demonstrating LYC as a potent new therapeutic option for treating CD.
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Doença de Chagas , Nanocápsulas , Nitroimidazóis , Tripanossomicidas , Trypanosoma cruzi , Animais , Camundongos , Nifurtimox/uso terapêutico , Nitroimidazóis/farmacologia , Nitroimidazóis/uso terapêutico , Doença de Chagas/tratamento farmacológico , Poliésteres/farmacologia , Poliésteres/uso terapêutico , Tripanossomicidas/farmacologia , Tripanossomicidas/uso terapêuticoRESUMO
High-performance pesticide formulations are essential for sustainable agriculture. Among these, nano-pesticides exhibit great advantages in pest control because of their unique size effects. However, the direct effects of nano-formulation fungicides on fungal pathogens remain largely unexplored. In this study, three qualified formulations, suspension concentrate (SC), microcapsules (CS), and nanocapsules (NCS) of pyraclostrobin (PYR) were prepared and utilized to reveal their biocontrol activities against Rhizoctonia solani. Among these three formulations, NCS exhibited notable biocontrol efficacy against R. solani exemplified by an EC50 of 0.319 mg/L for mycelia, distortion of mycelia and abnormalities in cell ultrastructure. Moreover, NCS displayed excellent internalization within R. solani mycelia, contributing to severe damage to cell membrane permeability. Importantly, an equivalent quantity of NCS-PYR showed potent inhibitory effects on the target pathogen, as indicated by reduced adenosine triphosphate (ATP) content and mitochondrial Complex III activity. The NCS consistently exhibited superior in vivo protective and curative activities against R. solani compared to those of CS and SC in rice and faba bean. In summary, we uncovered the strength of rapid efficacy and biocontrol activity of NCS against R. solani and elucidated the advantages of NCS-PYR from the perspective of the target pathogen in agriculture.
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Nanocápsulas , Doenças das Plantas/prevenção & controle , Doenças das Plantas/microbiologia , RhizoctoniaRESUMO
Curcumin is an active polyphenol substance found in the highest concentrations in the roots of Curcuma longa. Its health benefits have led to recent increases in the consumption of curcumin. It has anti-inflammatory and antioxidant activities and is a potent neuroprotective against diseases of the brain. Nevertheless, its low bioavailability and its relative difficulty crossing the blood-brain barrier limit curcumin's use for these purposes. Curcumin-loaded nanoparticles may be an effective treatment for several diseases although there is a paucity of studies reporting its safety in the central nervous system (CNS). Therefore, this study aimed to identify non-neurotoxic concentrations of free curcumin and two nanoformulations of curcumin. Cell lines BV-2 and SH-SY5Y, both originating from the CNS, were evaluated after 24, 48, and 72 h of treatment with free curcumin and nanocapsules We measured viability, proliferation, and dsDNA levels. We measured levels of reactive oxygen species and nitric oxide as proxies for oxidative stress in culture supernatants. We found that free curcumin was toxic at 10 and 20 µM, principally at 72 h. Nanoformulations were more neurotoxic than the free form. Safe concentrations of free curcumin are between 1-5 µM, and these concentrations were lower for nanoformulations. We determined the ideal concentrations of free curcumin and nanocapsules serving as a basis for studies of injuries that affect the CNS.
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Curcumina , Nanocápsulas , Neuroblastoma , Humanos , Curcumina/farmacologia , Nanocápsulas/toxicidade , Linhagem Celular , Estresse OxidativoRESUMO
Some breast cancers are caused by hormonal imbalances, such as estrogen and progesterone. These hormones play a function in directing the growth of cancer cells. The hormone receptors in hormone receptor-positive breast cancer lead breast cells to proliferate out of control. Cancer therapy such as hormonal, targeted, radiation is still unsatisfactory because of these challenges namely multiple drug resistance (MDR), off-targeting, severe adverse effects. A novel aromatase inhibitor exemestane (Exe) exhibits promising therapy in breast cancer. This study aims to develop and optimize Exe-loaded lipid nanocapsules (LNCs) by using DSPC, PF68 and olive oil as lipid, surfactant and oil phase, respectively and to characterize the same. The prepared nanocapsules were investigated via in vitro cell culture and in vivo animal models. The LNCs exhibited cytotoxicity in MCF-7 cell lines and enhanced anti-cancer activity and reduced cardiotoxicity in DMBA-induced animal model when compared to the drug. Additionally, in vivo pharmacokinetics revealed a 4.2-fold increased oral bioavailability when compared with Exe suspension. This study demonstrated that oral administration of Exe-loaded LNCs holds promise for the antiestrogenic activity of exemestane in breast cancer.