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1.
Proc Natl Acad Sci U S A ; 120(18): e2219885120, 2023 05 02.
Artigo em Inglês | MEDLINE | ID: mdl-37094151

RESUMO

Poly(ethylene oxide) (PEO) and poloxamers, a class of poly(ethylene oxide)-b-poly(propylene oxide)-b-poly(ethylene oxide) (PEO-PPO-PEO) triblock copolymers, have many personal and medical care applications, including the stabilization of stressed cellular membranes. Despite the widespread use, the cellular transcriptional response to these molecules is relatively unknown. C2C12 myoblasts, a model muscle cell, were subjected to short-term Poloxamer 188 (P188) and PEO181 (8,000 g/mol) treatment in culture. RNA was extracted and sequenced to quantify transcriptomic impact. The addition of moderate concentrations (14 µM) of either polymer to unstressed cells caused substantial differential gene expression, including at least twofold modulation of 357 and 588 genes, respectively. In addition, evaluation of the transcriptome response to osmotic stress without polymer treatment revealed dramatic change in RNA expression. Interestingly, the addition of polymer to stressed cells-at concentrations that provide physiological protection-did not yield a significant difference in expression of any gene relative to stress alone. Genome-scale expression analysis was corroborated by single-gene quantitative real-time PCR. Changes in protein expression were measured via western blot, which revealed partial alignment with the RNA results. Collectively, the significant changes to expression of multiple genes and resultant protein translation demonstrates an unexpectedly broad biochemical response to these polymers in healthy myoblasts in vitro. Meanwhile, the lack of substantial transcriptional response to polymer treatment in stressed cells highlights the physical nature of that protective mechanism.


Assuntos
Óxido de Etileno , Poloxâmero , Poloxâmero/química , Polietilenoglicóis/química , Polímeros/química , Mioblastos , Propilenoglicóis
2.
J Environ Manage ; 365: 121611, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38959769

RESUMO

Ultrafiltration technology, separating water from impurities by the core membrane, is an effective strategy for treating wastewater to meet the ever-growing requirement of clean and drinking water. However, the similar nature of hydrophobic organic pollutants and the membrane surface leads to severe adsorption and aggregation, resulting unavoidable membrane degradation of penetration and rejection. The present study presents a novel block amphiphilic polymer, polyethersulfone-g-carboxymethyl chitosan@MWCNT (PES-g-CMC@MWCNT), which is synthesized by grafting hydrophobic polyethersulfone to hydrophilic carboxymethyl chitosan in order to suspend CMC in organic solution. A mixture of hydrophilic carboxymethyl chitosan and hydrophobic polymers (polyethersulfone), in which hydrophilic segments are bonded to hydrophobic segments, could provide hydrophilic groups, as well as gather and remain stable on membrane surfaces by their hydrophobic interaction for improved compatibility and durability. The resultant ultrafiltration membranes exhibit high water flux (198.10 L m-2·h-1), suitable hydrophilicity (64.77°), enhanced antifouling property (82.96%), while still maintains excellent rejection of bovine serum albumin (91.75%). There has also been an improvement in membrane cross-sectional morphology, resulting in more regular pores size (47.64 nm) and higher porosity (84.60%). These results indicate that amphiphilic polymer may be able to significantly promote antifouling and permeability of ultrafiltration membranes.


Assuntos
Quitosana , Interações Hidrofóbicas e Hidrofílicas , Membranas Artificiais , Polímeros , Sulfonas , Ultrafiltração , Polímeros/química , Quitosana/química , Quitosana/análogos & derivados , Sulfonas/química , Adsorção , Purificação da Água/métodos , Incrustação Biológica/prevenção & controle
3.
Anal Bioanal Chem ; 415(18): 4333-4341, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-36745239

RESUMO

Hydrogen peroxide (H2O2) is considered a significant biomarker in various diseases and could induce deleterious health problems at irregular physiological concentrations. Therefore, developing a simple, efficient biocompatible nanoprobe for trace amount H2O2 detection with high sensitivity and specificity is of great help for early diagnosis and therapeutics. Herein, we designed amphiphilic poly(styrene-co-maleic anhydride) (PMSA)-encapsulated nanoclusters composed of upconversion nanoparticles (UCNPs) and manganese dioxide nanoparticles (MnO2 NPs) at a specific ratio to produce a near-infrared (NIR) excited luminescent nanoprobe for H2O2 detection. Our results revealed that the MnO2 NPs tended to experience catalytic decomposition when exposed to H2O2, while the UCNPs were retained inside the PSMA encapsulation, causing recovery of the UCNP emission band at 470 nm in accordance with H2O2 concentration. This luminescence recovery was linearly dependent on H2O2 concentrations, yielding a limit of detection (LOD) of 20 nM. The easy-to-interpret H2O2 nanoprobe also proved high selectivity in the presence of other interfering substances, and biocompatibility and water-dispersibility, making it an ideal candidate for real-time detection of disease-related H2O2 in living organisms.


Assuntos
Nanopartículas , Óxidos , Peróxido de Hidrogênio , Compostos de Manganês , Transferência Ressonante de Energia de Fluorescência/métodos , Polímeros
4.
Molecules ; 28(4)2023 Feb 17.
Artigo em Inglês | MEDLINE | ID: mdl-36838923

RESUMO

Water treatment technology based on ultrafiltration (UF) faces the problem of severe membrane fouling due to its inherent hydrophobicity. The use of amphiphilic polymers that possess both hydrophobic and hydrophilic chain segments can be advantageous for the hydrophilic modification of UF membranes due to their excellent combination in the membrane matrix. In the present study, we examined a novel amphiphilic CA-g-AN material, constructed by grafting citric acid (CA) to aniline (AN), as a modified material to improve the hydrophilicity of a PES membrane. This material was more compatible with the polymer membrane matrix than a pure hydrophilic modified material. The polyethersulfone (PES) membranes modified by amphiphilic CA-g-AN demonstrated a higher water flux (290.13 L·m-2·h-1), which was more than eight times higher than that of the pure PES membrane. Furthermore, the flux recovery ratio (FRR) of the modified membrane could reach 83.24% and the value of the water contact angle (WCA) was 76.43°, demonstrating the enhanced hydrophilicity and antifouling ability of the modified membranes. With this study, we aimed to develop a new amphiphilic polymer to improve the antifouling property and permeability of polymer-based UF membranes to remove organic pollutants from water.


Assuntos
Incrustação Biológica , Incrustação Biológica/prevenção & controle , Membranas Artificiais , Polímeros/química , Permeabilidade
5.
Molecules ; 28(13)2023 Jul 06.
Artigo em Inglês | MEDLINE | ID: mdl-37446919

RESUMO

A heavy oil activator is an amphiphilic polymer solution that contains hydrophilic and oleophobic groups. It can enhance heavy oil recovery efficiency. This paper studied the changes in the distribution of the remaining oil after activator flooding and the performance of heavy oil's active agent. Nuclear magnetic resonance spectroscopy, laser confocal microscopy, microscopic visualization, and CT scanning techniques were used to analyze crude oil utilization, and the distribution characteristics of the remaining oil during activator flooding of heavy oil. The results showed that the heavy oil activator solution presented a dense spatial network and good viscosification ability. The activator could reduce the interfacial tension of oil and water, disassemble the heavy components of dispersed heavy oil and reduce the viscosity of heavy oil. The utilization degree of the remaining oil in small and middle pores increased significantly after activator flooding, the remaining oil associated with membranous-like and clusterlike structures was utilized to a high degree, and the decline of light/heavy fraction in heavy oil slowed down. Heavy oil activator improved the swept volume and displacement efficiency of heavy oil, playing a significant role in improving the extent of recovery of heavy oil reservoirs.


Assuntos
Petróleo , Polímeros , Campos de Petróleo e Gás , Viscosidade , Tensão Superficial
6.
Molecules ; 28(11)2023 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-37298956

RESUMO

The zwitterionic phospholipid polymer poly(2-methacryloyloxyethyl phosphorylcholine-co-n-butyl methacrylate) (PMB) is amphiphilic copolymer, and it has been reported to directly penetrate cell membranes and have good cytocompatibility. Conventional PMBs are linear-type random copolymers that are polymerized by a free radical polymerization technique. In contrast, star-shaped polymers, or simple branched-type polymers, have unique properties compared to the linear types, for example, a viscosity based on the effect of the excluded volume. In this study, a branched architecture was introduced into a PMB molecular structure, and a 4-armed star-shaped PMB (4armPMB) was synthesized by an atom transfer radical polymerization (ATRP) technique known as living radical polymerization. Linear-type PMB was also synthesized using ATRP. The effects of the polymer architecture on cytotoxicity and cellular uptake were investigated. Both 4armPMB and LinearPMB were successfully synthesized, and these polymers were verified to be water soluble. Pyrene fluorescence in the polymer solution indicated that the architecture had no effect on the behavior of the polymer aggregates. In addition, these polymers caused no cytotoxicity or cell membrane damage. The 4armPMB and LinearPMB penetrated into the cells after a short incubation period, with similar rates. In contrast, the 4armPMB showed a quicker back-diffusion from the cells than that of LinearPMB. The 4armPMB showed fast cellular internalization and exiting behaviors.


Assuntos
Metacrilatos , Polímeros , Polímeros/química , Metacrilatos/química , Estrutura Molecular , Radicais Livres , Polimerização
7.
Toxicol Appl Pharmacol ; 450: 116155, 2022 09 01.
Artigo em Inglês | MEDLINE | ID: mdl-35803437

RESUMO

To treat acute kidney injury with high efficiency and low toxicity, a novel nanoplatform was developed to remove excess reactive oxygen species (ROS). Lutein (LU) and celastrol (Cel) were loaded into low molecular weight chitosan (CS) to prepare Cel@LU-CA-CS nanomicelles. Renal tubular epithelial (HK-2) cell uptake experiments showed that the drugs could be internalized in renal tubular via the megalin receptor. In this study, the amide bond formed by the reaction of citraconic anhydride (CA) with an amino group of CS could be destroyed under acidic conditions. Therefore, the drugs were released in HK-2 cells due to the acidic environment of the lysosome. In vitro studies showed that the nanomicelles could reduce toxicity in non-target organs and enhance therapeutic efficacy in acute kidney injury (AKI). In addition, Cel@LU-CA-CS micelles had alleviated kidney oxidative stress disorder and stabilized the mitochondrial membrane potential quickly. Next, in vivo studies proved that Cel@LU-CA-CS micelles could inhibit the activation of the NF-κB p65 and p38 MAPK inflammatory signaling pathways. Therefore, the micelles further reduced the overexpression of related inflammatory factors. In conclusion, Cel@LU-CA-CS nanomicelles could treat AKI with high efficiency and low toxicity, and inhibit renal fibrosis.


Assuntos
Injúria Renal Aguda , Quitosana , Injúria Renal Aguda/induzido quimicamente , Injúria Renal Aguda/tratamento farmacológico , Injúria Renal Aguda/metabolismo , Quitosana/química , Humanos , Concentração de Íons de Hidrogênio , Luteína , Micelas , Triterpenos Pentacíclicos
8.
Skin Res Technol ; 28(1): 84-88, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34455650

RESUMO

PURPOSE: Make-up clumps, bumps and collapses are the three factors that determine how well make-up has been performed. The purpose of this study is to reduce the three factors mentioned above by using amphiphilic substances to increase the affinity between the skin and the make-up layer. In addition, it aims to evaluate the improvement of the make-up layer by developing an objective make-up layer evaluation method. METHODS: Experiments were performed in an attempt to increase the affinity between the skin and the make-up layer by minimizing the difference in surface energy between the two. Multiple types of artificial skin (leather and bio-skin) were used and treated to form the liquid foundation layer. Qualitative evaluation of the make-up layer was conducted by analyzing the surface, cross-section, and fracture area of the make-up layer, using the evaluation method proposed in this study. RESULTS: After applying this method and taking measurements by 3D surface analysis, the surface roughness of the make-up layer reduced by 46%, and the maximum thickness of the make-up layer reduced by about 50% in comparison with the control group (method not applied). In the case of the make-up layer to which this method was applied, two-dimensional cross-sectional Scanning Electron Microscope (SEM) image analysis confirmed that agglomeration was reduced, and the thickness of the make-up layer was also reduced by an average of 54%. According to this result, the technique of increasing the affinity between the skin and the make-up layer reduces the level of aggregation of make-up and encourages the formation of a uniform and thin make-up layer. Also, the fracture area after motion simulation was reduced by 33%. These results indicate that the method of increasing the affinity between skin/make-up membranes positively affects the formation of a uniform make-up layer. CONCLUSION: Increasing the affinity by reducing the surface energy between the skin and the make-up layer plays an important role in forming a thin and uniform make-up layer by improving the problems of lifting, agglomeration, and collapse of the make-up. In addition, it has been confirmed that through this method, the quality of consumer experience related to make-up satisfaction can be improved. The results show that objective analyses of make-up help the understanding of the quality of consumer experience on make-up.


Assuntos
Pele Artificial , Pele , Estudos Transversais , Derme , Humanos
9.
Int J Mol Sci ; 23(20)2022 Oct 18.
Artigo em Inglês | MEDLINE | ID: mdl-36293301

RESUMO

An amphiphilic copolymer of N-vinyl-2-pyrrolidone and acrylic acid-namely, p(VP-AA)-OD6000 (p(VP-AA))-was synthesized to prepare p(VP-AA) nanoparticles (NPs). Furthermore, the copolymer was linked with CFSE, and the so-prepared nanoparticles were loaded with the DiI dye to form D nanoparticles (DNPs). In this study, as demonstrated by immunofluorescence microscopy, immunofluorescence, and confocal microscopy, DNPs were readily taken up by human microvascular endothelial cells (HMEC-1) cells in a concentration-dependent manner. Upon uptake, both the CFSE dye (green stain) and the DiI dye (red stain) were localized to the cytoplasm of treated cells. Treatment with p(VP-AA) did not affect the viability of normal and challenged with LPS, HMEC-1 cells at 0.010 mg/mL and induced a dose-dependent decrease of these cells' viability at the higher concentrations of 0.033 and 0.066 mg/mL (p ≤ 0.01; p ≤ 0.001, respectively). Furthermore, we focused on the potential immunological activation of HMEC-1 endothelial cells upon p(VP-AA) NPs treatment by assessing the expression of adhesion molecules (E-Selectin, ICAM-1, and V-CAM). NPs treatments at concentrations utilized (p = NS) did not affect individual adhesion molecules' expression. p(VP-AA) NPs do not activate the endothelium and do not affect its viability at pharmacologically relevant concentrations.


Assuntos
Selectina E , Nanopartículas , Humanos , Molécula 1 de Adesão Intercelular , Células Endoteliais , Lipopolissacarídeos/farmacologia , Polímeros , Endotélio
10.
J Nanobiotechnology ; 19(1): 140, 2021 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-34001157

RESUMO

Synergistic chemo-photodynamic therapy has garnered attention in the field of cancer treatment. Here, a pH cascade-responsive micellar nanoplatform with nucleus-targeted ability, for effective synergistic chemo-photodynamic cancer treatment, was fabricated. In this micellar nanoplatform, 5-(4-carboxyphenyl)-10,15,20-triphenylporphyrin (Por), a photodynamic therapy (PDT) agent was utilized for carrying the novel anticancer drug GNA002 to construct a hydrophobic core, and cyclic RGD peptide (cRGD)-modified polyethylene glycol (PEG) (cRGD-PEG) connected the cell-penetrating peptide hexaarginine (R6) through a pH-responsive hydrazone bond (cRGD-PEG-N = CH-R6) to serve as a hydrophilic shell for increasing blood circulation time. After passively accumulating in tumor sites, the self-assembled GNA002-loaded nanoparticles were actively internalized into cancer cells via the cRGD ligands. Once phagocytosed by lysosomes, the acidity-triggered detachment of the cRGD-PEG shell led to the formation of R6-coated secondary nanoparticles and subsequent R6-mediated nucleus-targeted drug delivery. Combined with GNA002-induced nucleus-specific chemotherapy, reactive oxygen species produced by Por under 532-nm laser irradiation achieved a potent synergistic chemo-photodynamic cancer treatment. Moreover, our in vitro and in vivo anticancer investigations revealed high cancer-suppression efficacy of this ideal multifunctional nanoplatform, indicating that it could be a promising candidate for synergistic anticancer therapy.


Assuntos
Antineoplásicos/uso terapêutico , Portadores de Fármacos/química , Neoplasias/terapia , Fotoquimioterapia/métodos , Animais , Linhagem Celular Tumoral , Sistemas de Liberação de Medicamentos , Feminino , Humanos , Lisossomos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Nanopartículas/química , Peptídeos Cíclicos , Fármacos Fotossensibilizantes/farmacologia , Polietilenoglicóis/química , Espécies Reativas de Oxigênio
11.
Mol Pharm ; 17(11): 4212-4225, 2020 11 02.
Artigo em Inglês | MEDLINE | ID: mdl-32986447

RESUMO

Nanoparticles (NPs) produced from amphiphilic derivatives of poly-N-vinylpyrrolidone (Amph-PVP), composed of various molecular weight polymeric hydrophilic fragments linked into hydrophobic n-alkyl chains of varying lengths, were previously shown to exert excellent biocompatibility. Although routes of administration can be different, finally, most nanosystems enter the blood circulation or lymphatic vessels, and by this, they establish direct contact with endothelial cells. In this study, Amph-PVP NPs and fluorescently labeled Amph-PVP-based NPs, namely "PVP" NPs (Amph-PVP-NPs (6000 Da) unloaded) and "F"-NPs (Amph-PVP-NPs (6000 Da) loaded with fluorescent FITC), were synthesized to study Amph-PVP NPs interactions with HMEC-1 endothelial cells. PVP NPs were readily uptaken by HMEC-1 cells in a concentration-dependent manner, as demonstrated by immunofluorescence imaging. Upon uptake, the FITC dye was localized to the perinuclear region and cytoplasm of treated cells. The generation of lipopolysaccharide (LPS)-induced activated endothelium model revealed an increased uptake of PVPNPs, as shown by confocal microscopy. Both unloaded PVP NPs and F-NPs did not affect EC viability in the 0.01 to 0.066 mg/mL range. Furthermore, we focused on the potential immunological activation of HMEC-1 endothelial cells upon PVPNPs treatment by assessing the expression of their E-Selectin, ICAM-1, and VCAM-1 adhesion receptors. None of the adhesion molecules were affected by NP treatments of both activated by LPS and nonactivated HMEC-1 cells, at the utilized concentrations (p = NS). In this study, PVP (6000 Da) NPs were used to encapsulate indomethacin, a widely used anti-inflammatory drug. The synthesized drug carrier complex did not affect HMEC-1 cell growth and expression of E-selectin, ICAM-1, and VCAM-1 adhesion receptors. In summary, PVP-based NPs are safe for use on both basal and activated endothelium, which more accurately mimics pathological conditions. Amph-PVP NPs are a promising drug delivery system.


Assuntos
Anti-Inflamatórios/administração & dosagem , Materiais Biocompatíveis/química , Portadores de Fármacos/química , Células Endoteliais/efeitos dos fármacos , Indometacina/administração & dosagem , Nanopartículas/química , Polímeros/química , Pirrolidinonas/química , Anti-Inflamatórios/metabolismo , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Células Endoteliais/metabolismo , Fluoresceína-5-Isotiocianato/administração & dosagem , Corantes Fluorescentes/administração & dosagem , Corantes Fluorescentes/metabolismo , Humanos , Interações Hidrofóbicas e Hidrofílicas , Indometacina/metabolismo , Peso Molecular , Tamanho da Partícula
12.
J Nanobiotechnology ; 18(1): 13, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31941501

RESUMO

BACKGROUND: During the past few decades, drug delivery system (DDS) has attracted many interests because it could enhance the therapeutic effects of drugs and reduce their side effects. The advent of nanotechnology has promoted the development of nanosized DDSs, which could promote drug cellular uptake as well as prolong the half-life in blood circulation. Novel polymer micelles formed by self-assembly of amphiphilic polymers in aqueous solution have emerged as meaningful nanosystems for controlled drug release due to the reversible destabilization of hydrophobic domains under different conditions. RESULTS: The amphiphilic polymers presented here were composed of cholesterol groups end capped and poly (poly (ethylene glycol) methyl ether methacrylate) (poly (OEGMA)) as tailed segments by the synthesis of cholesterol-based initiator, followed by atom transfer radical polymerization (ATRP) with OEGMA monomer. FT-IR and NMR confirmed the successfully synthesis of products including initiator and polymers as well as the Mw of the polymers were from 33,233 to 89,088 g/mol and their corresponding PDI were from 1.25 to 1.55 by GPC. The average diameter of assembled polymer micelles was in hundreds nanometers demonstrated by DLS, AFM and SEM. The behavior of the amphiphilic polymers as micelles was investigated using pyrene probing to explore their critical micelle concentration (CMC) ranging from 2.53 × 10-4 to 4.33 × 10-4 mg/ml, decided by the balance between cholesterol and poly (OEGMA). Besides, the CMC of amphiphilic polymers, the quercetin (QC) feeding ratio and polarity of solvents determined the QC loading ratio maximized reaching 29.2% certified by UV spectrum, together with the corresponding size and stability changes by DLS and Zeta potential, and thermodynamic changes by TGA and DSC. More significantly, cholesterol end-capped polymer micelles were used as nanosized systems for controlled drug release, not only alleviated the cytotoxicity of QC from 8.6 to 49.9% live cells and also achieved the QC release in control under different conditions, such as the presence of cyclodextrin (CD) and change of pH in aqueous solution. CONCLUSIONS: The results observed in this study offered a strong foundation for the design of favorable polymer micelles as nanosized systems for controlled drug release, and the molecular weight adjustable amphiphilic polymer micelles held potential for use as controlled drug release system in practical application.


Assuntos
Colesterol/química , Portadores de Fármacos/química , Nanopartículas/química , Polietilenoglicóis/química , Animais , Linhagem Celular , Sobrevivência Celular , Ciclodextrinas/química , Liberação Controlada de Fármacos , Interações Hidrofóbicas e Hidrofílicas , Camundongos , Micelas , Mioblastos/citologia , Mioblastos/efeitos dos fármacos , Pirenos/química , Quercetina/administração & dosagem , Quercetina/química
13.
J Environ Sci Health B ; 55(5): 501-507, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32036766

RESUMO

Controlled release (CR) nanoformulations of Mancozeb (Manganese-zinc double salt of N, N-bisdithiocarbamic acid), a protective fungicide, have been developed using poly (ethylene glycols) (PEGs) based functionalized amphiphilic copolymers and evaluated for the management of early blight in tomato. During the field experiment, it was observed that number of infected leaflets/plants were less in developed formulation treated plants as compared to commercial products. Number of infected leaflets per plant was 2.40-4.60 and the number of fruits per plant were 6.40-9.00 at 50 mg L-1, whereas at 100 mg L-1, the corresponding numbers were 2.10-4.10 and 6.30-9.10 respectively. These formulations can be used to optimize the release of Mancozeb to achieve disease control for the desired period depending upon the matrix of the polymer used. Importantly, sufficient amount of active ingredient remains available for a reasonable period of time after application leading to reduced number of applications of pesticide.


Assuntos
Fungicidas Industriais/farmacologia , Maneb/química , Maneb/farmacologia , Nanoestruturas/química , Solanum lycopersicum/microbiologia , Zineb/química , Zineb/farmacologia , Alternaria/efeitos dos fármacos , Alternaria/patogenicidade , Fungicidas Industriais/química , Doenças das Plantas/microbiologia , Folhas de Planta/microbiologia , Polietilenoglicóis/química , Polímeros/química
14.
Mar Drugs ; 16(11)2018 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-30445668

RESUMO

Most of the methods of poly-lactic-glycolic acid (PLGA) preparation involve the passage through the emulsification of a PLGA organic solution in water followed by solvent evaporation or extraction. The choice of the droplet stabilizer during the emulsion step is critical for the dimensions and the surface characteristics of the nanoparticles (NPs). In the present work, a recently described ionic amphiphilic chitosan derivative, chitosan oleate salt (CS-OA), was proposed for the first time to prepare PLGA NPs. A full factorial design was used to understand the effect of some formulation and preparation parameters on the NP dimensions and on encapsulation efficiency (EE%) of Nile red, used as a tracer. On the basis of the DoE study, curcumin loaded NPs were prepared, having 329 ± 42 nm dimensions and 68.75% EE%. The presence of a chitosan coating at the surface was confirmed by positive zeta potential and resulted in mucoadhesion behavior. The expected improvement of the interaction of the chitosan surface modified nanoparticles with cell membrane surface was confirmed in Caco-2 cell culture by the internalization of the loaded curcumin.


Assuntos
Quitosana/química , Portadores de Fármacos/química , Nanopartículas/química , Adesividade , Células CACO-2 , Curcumina/administração & dosagem , Curcumina/química , Emulsões , Humanos , Ácido Oleico/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Solubilidade , Propriedades de Superfície
15.
Int J Mol Sci ; 19(10)2018 Oct 12.
Artigo em Inglês | MEDLINE | ID: mdl-30322014

RESUMO

The present investigation aimed to develop a tumor-targeting drug delivery system for paclitaxel (PTX). The hydrophobic deoxycholic acid (DA) and active targeting ligand folic acid (FA) were used to modify water-soluble chitosan (CS). As an amphiphilic polymer, the conjugate FA-CS-DA was synthesized and characterized by Proton nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared spectroscopy (FTIR) analysis. The degree of substitutions of DA and FA were calculated as 15.8% and 8.0%, respectively. In aqueous medium, the conjugate could self-assemble into micelles with the critical micelle concentration of 6.6 × 10-3 mg/mL. Under a transmission electron microscope (TEM), the PTX-loaded micelles exhibited a spherical shape. The particle size determined by dynamic light scattering was 126 nm, and the zeta potential was +19.3 mV. The drug loading efficiency and entrapment efficiency were 9.1% and 81.2%, respectively. X-Ray Diffraction (XRD) analysis showed that the PTX was encapsulated in the micelles in a molecular or amorphous state. In vitro and in vivo antitumor evaluations demonstrated the excellent antitumor activity of PTX-loaded micelles. It was suggested that FA-CS-DA was a safe and effective carrier for the intravenous delivery of paclitaxel.


Assuntos
Carcinoma Hepatocelular/tratamento farmacológico , Ácido Desoxicólico/química , Portadores de Fármacos/síntese química , Ácido Fólico/química , Neoplasias Hepáticas/tratamento farmacológico , Paclitaxel/administração & dosagem , Animais , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Quitosana/química , Portadores de Fármacos/química , Feminino , Humanos , Injeções Intravenosas , Células MCF-7 , Camundongos , Micelas , Transplante de Neoplasias , Paclitaxel/química , Paclitaxel/farmacologia , Tamanho da Partícula , Ensaios Antitumorais Modelo de Xenoenxerto
16.
Int J Mol Sci ; 19(6)2018 05 23.
Artigo em Inglês | MEDLINE | ID: mdl-29882845

RESUMO

Amphiphilic polymer of α-tocopherol succinate modified glycol chitosan (TS-GC) was successfully constructed by conjugating α-tocopherol succinate to the skeleton of glycol chitosan and characterized by Fourier-transform infrared (FT-IR) and proton nuclear magnetic resonance (¹H-NMR). In aqueous milieu, the conjugates self-assembled to micelles with the critical aggregation concentration of 7.2 × 10−3 mg/mL. Transmission electron microscope (TEM) observation and dynamic light scattering (DLS) measurements were carried out to determine the physicochemical properties of the micelles. The results revealed that paclitaxel (PTX)-loaded TS-GC micelles were spherical in shape. Moreover, the PTX-loaded micelles showed increased particle sizes (35 nm vs. 142 nm) and a little reduced zeta potential (+19 mV vs. +16 mV) compared with blank micelles. The X-ray diffraction (XRD) spectra demonstrated that PTX existed inside the micelles in amorphous or molecular state. In vitro and in vivo tests showed that the PTX-loaded TS-GC micelles had advantages over the Cremophor EL-based formulation in terms of low toxicity level and increased dose, which suggested the potential of the polymer as carriers for PTX to improve their delivery properties.


Assuntos
Quitosana/química , Sistemas de Liberação de Medicamentos , Micelas , Paclitaxel/administração & dosagem , Polímeros/química , Animais , Antineoplásicos/farmacologia , Quitosana/síntese química , Feminino , Glicerol/análogos & derivados , Glicerol/farmacologia , Humanos , Injeções Intravenosas , Células MCF-7 , Masculino , Camundongos , Tamanho da Partícula , Polímeros/síntese química , Espectroscopia de Prótons por Ressonância Magnética , Coelhos , Espectroscopia de Infravermelho com Transformada de Fourier , Eletricidade Estática , Difração de Raios X , alfa-Tocoferol/análogos & derivados , alfa-Tocoferol/síntese química , alfa-Tocoferol/química
17.
Macromol Rapid Commun ; 38(8)2017 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-28267231

RESUMO

A range of amphiphilic polymers with diverse macromolecular architectures has been developed and incorporated into films and coatings with potential for marine antibiofouling applications, without resorting to addition of currently used biocidal, toxic agents. Novel "green" chemical technologies employ different building blocks to endow the polymer film with surface activity, functionality, structure, and reconstruction according to the outer environment as a result of a tailored amphiphilic character of the polymer platform. We emphasise how these features can interplay and add synergistically to affect antifouling and fouling-release against common, widespread marine micro- and macro-fouling organisms.


Assuntos
Incrustação Biológica , Interações Hidrofóbicas e Hidrofílicas , Polímeros/química , Água do Mar/microbiologia , Membranas Artificiais , Microscopia de Força Atômica , Modelos Químicos , Estrutura Molecular , Polietilenoglicóis/química , Polímeros/síntese química , Propriedades de Superfície
18.
Luminescence ; 32(4): 618-624, 2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27734590

RESUMO

Physisorptions occurs everywhere and constantly in living organisms and between nanomaterials and biomolecules. In this study, one of the most important proteins, G-actin, was selected to investigate its bio-nano physisorption with a model nanoparticle coated with a amphiphilic polymer. Using a photoluminescence quenching method, both the binding constant and the Hill constant were determined as 1.79 × 107  M-1 and 0.84, respectively. Thermodynamic calculations proved that such a physisorption was a spontaneous procedure. The physisorption-mediated protein-nanoparticle conjugates were robust enough to resist gel electrophoresis, and protein conformation was kept intact, as revealed using circular dichroism. This conjugate might be a promising candidate for nanofabrication or could play a significant role in actin-related bioactivities.


Assuntos
Actinas/química , Ouro/química , Nanopartículas Metálicas/química , Actinas/metabolismo , Dicroísmo Circular , Ouro/metabolismo , Medições Luminescentes , Microscopia de Força Atômica , Microscopia Eletrônica de Transmissão , Polímeros/química , Conformação Proteica , Termodinâmica
19.
Angew Chem Int Ed Engl ; 56(13): 3516-3520, 2017 03 20.
Artigo em Inglês | MEDLINE | ID: mdl-28211226

RESUMO

We report molecular interaction-driven self-assembly of supramolecularly engineered amphiphilic macromolecules (SEAM) containing a single supramolecular structure-directing unit (SSDU) consisting of an H-bonding group connected to a naphthalene diimide chromophore. Two such SEAMs, P1-50 and P2-50, having the identical chemical structure and hydrophobic/hydrophilic balance, exhibit distinct self-assembled structures (polymersome and cylindrical micelle, respectively) due to a difference in the H-bonding group (hydrazide or amide, respectively) of the single SSDU. When mixed together, P1-50 and P2-50 adopted self-sorted assembly. For either series of polymers, variation in the hydrophobic/hydrophilic balance does not alter the morphology reconfirming that self-assembly is primarily driven by directional molecular interaction which is capable of overruling the existing norms in packing parameter-dependent morphology control in an immiscibility-driven block copolymer assembly.

20.
Beilstein J Org Chem ; 12: 939-49, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27340484

RESUMO

The topic of stimuli-responsive nanocarriers for loading guest molecules is dynamic. It has been widely studied in applications including drug controlled release, smart sensing, catalysis, and modeling. In this paper, a graft copolymer (hyperbranched polystyrene)-g-poly[2-(dimethylamino)ethyl methacrylate] (HBPS-g-PDMAEMA) was synthesized and characterized by (1)H NMR and GPC. It was observed that the star-like HBPS-g-PDMAEMA formed aggregates in aqueous solution. The influence of polymer concentration, ionic strength and pH value on the aggregates in aqueous solution was investigated by using UV-vis spectroscopy and DLS analysis. The results showed that size of aggregates was affected by a corresponding stimulus. In addition, the loading ability of HBPS-g-PDMAEMA aggregates was investigated by using pyrene or Nile red as the model guest molecules by using UV-vis and fluorescence spectroscopy. The results showed that HBPS-g-PDMAEMA aggregates were capable to encapsulate small hydrophobic molecules. These newly prepared HBPS-g-PDMAEMA nanocarriers might be used in, e.g., medicine or catalysis.

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