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1.
《Ceramics International》2017,43(6):4957-4964
Magnetic nanoparticles are attractive carriers for drug delivery and layered materials intercalated by drug molecules exhibit improved safety and effectiveness of drug delivery. In this work, we report the loading of a model anticancer drug, 5-fluorouracil (5FU), into a magnetic layered nanohydroxyapatite (ML-HAP) by intercalation technique. The as-prepared ML-HAP nanoparticles with loaded 5FU were characterized using transmission electron microscopy (TEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), and vibrating sample magnetometer. We find that, within a certain drug concentration, the drug molecules can be intercalated into the gallery of ML-HAP without breaking its lamellar structure. The drug loading capacity of ML-HAP is extremely large. The drug release profiles display pH-dependent behavior and the drug release mechanisms are a combination of drug diffusion and HAP dissolution. Furthermore, ML-HAP/5FU shows strong superparamagnetism and good biocompatibility. The ML-HAP can be an efficient platform for targeted anticancer drug delivery.  相似文献   

2.
Silk fibroin (SF) is a protein-based biomacromolecule with excellent biocompatibility, biodegradability and low immunogenicity. The development of SF-based nanoparticles for drug delivery have received considerable attention due to high binding capacity for various drugs, controlled drug release properties and mild preparation conditions. By adjusting the particle size, the chemical structure and properties, the modified or recombinant SF-based nanoparticles can be designed to improve the therapeutic efficiency of drugs encapsulated into these nanoparticles. Therefore, they can be used to deliver small molecule drugs (e.g., anti-cancer drugs), protein and growth factor drugs, gene drugs, etc. This paper reviews recent progress on SF-based nanoparticles, including chemical structure, properties, and preparation methods. In addition, the applications of SF-based nanoparticles as carriers for therapeutic drugs are also reviewed.  相似文献   

3.
The effective and locally sustained delivery of hydrophobic drug with hydrogels as carriers is still a challenge owing to the inherent incompatibility of hydrophilic hydrogel network and hydrophobic drug. One promising approach is to use porous hydrogels to encapsulate and deliver hydrophobic drug in the form of nanoparticles to the disease sites. However, this approach is currently limited by the inability to load concentrated hydrophobic drug nanoparticles into the hydrogels because of the severe nanoparticle aggregation during the loading process. In this article, we firstly designed and fabricated efficient drug nanoparticles embedded hydrogels for hydrophobic drug delivery by incorporating monodisperse silybin (hydrophobic drug for liver protection) nanoparticles into acrylated hyaluronic acid (HA‐AC) based hydrogels through in situ cross‐linking. The silybin nanoparticles embedded hydrogel scaffolds proved to be a good sustained release system with a long period of 36 h. The drug release from this hybrid hydrogels could be modulated by tuning HA‐AC concentration, cross‐linking ratio, chain length of cross‐linker and drug loading amount. The different kinetic models were applied, and it was observed that the release profile of silybin best followed the Hixson‐Crowell model for the release of drug from the hydrogels embedding silybin nanoparticles. It could be envisioned that this process would significantly advance the potential applications of hydrogel scaffolds mediated hydrophobic drug delivery in clinical therapies. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 43111.  相似文献   

4.
水溶性壳聚糖纳米粒子的制备及其BSA载药性能   总被引:3,自引:0,他引:3  
王春  杨连生  扶雄 《化工进展》2006,25(12):1431-1435
为了避免高分子量壳聚糖水溶性差以及增溶剂乙酸可能带来的负面作用,本文选择低分子量水溶性壳聚糖 (WSC)作研究对象,采用三聚磷酸(TPP)作交链剂制备不同WSC/TPP比率的WSC纳米粒子,并用于牛血清白蛋白 (BSA)的释放载体。经测得为球形形貌的纳米粒子空载和载药时粒径、Zeta电位分别在35~190 nm、35~42 mV。红外光谱及X–射线衍射证实了纳米粒子中WSC的氨基与TPP的磷酸基团发生了交联反应。纳米粒子载药性能试验表明在0.05~1 mg/mL范围内随着BSA浓度的增大,纳米粒子的载药量增加而负载率降低。体外释放实验表明水溶性壳聚糖纳米载体对蛋白质药物具有缓释特征。因此,水溶性壳聚糖有望成为新的载体应用于蛋白质药物的控制释放。  相似文献   

5.
Amphiphilic copolymers with cationic hydrophilic moieties and different ratios of hydrophobic portion to hydrophilic portion were designed and synthesized via the combination of hydrosilylation reactions and quaternization reactions. The structures were characterized through Fourier transform infrared spectroscopy, 1H NMR , 13C NMR and gel permeation chromatography. The measurements of critical micelle concentrations, electrical conductivities and zeta potentials indicated that the copolymers could self‐assemble into nanoparticles with charges around the surface in aqueous solution. The sizes of the micelles were between 67 nm and 104 nm detected by dynamic light scattering. The self‐assembled micelles were used as drug carriers to encapsulate a model drug (tocopherol), and their drug‐loading content (DLC ) and efficiency (DLE ) were determined by UV ?visible spectra, resulting in considerable drug‐loading capacity to a tocopherol maximum up to 17.2% (DLC ) and 80.3% (DLE ) with a size of 90 nm. The blank micelles and drug‐loaded micelles displayed a spherical shape detected by transmission electron microscopy, which demonstrated not only the self‐assembly behaviors but also the drug‐loading performances of the cationic amphiphilic copolymers. All the results demonstrated that the cationic amphiphilic copolymers could be used as potential electric‐responsive drug carriers. © 2017 Society of Chemical Industry  相似文献   

6.
To investigate the delivery of hydrophobic therapeutic agents, a new class of polymer carriers was synthesized. These carriers are composed of two components: (i) a pH‐responsive hydrogel composed of methacrylic acid grafted with poly(ethylene glycol) tethers, P(MAA‐g‐EG), and (ii) hydrophobic poly(methyl methacrylate) (PMMA) nanoparticles. Before the P(MAA‐g‐EG) hydrogel was crosslinked, PMMA nanoparticles were added to the solution and upon exposure to UV light they were photoencapsulated throughout the P(MAA‐g‐EG) hydrogel structure. The pH‐responsive behavior of P(MAA‐g‐EG) is capable of triggered release of a loaded therapeutic agent, such as a low molecular weight drug or protein, when it passes from the stomach (low pH) to upper small intestine (neutral pH). The introduction of PMMA nanoparticles into the hydrogel structure affected the swelling behavior, therapeutic agent loading efficiency, and solute release profiles. In equilibrium swelling conditions the swelling ratio of nanoparticle‐containing hydrogels decreased with increasing nanoparticle content. Loading efficiencies of the model therapeutic agent fluorescein ranged from 38% to 51% and increased with increasing hydrophobic content. Release studies from neat P(MAA‐g‐EG) and the ensuing P(MAA‐g‐EG) hydrogels containing nanoparticles indicated that the transition from low pH (2.0) to neutral pH (7.0) triggered fluorescein release. Maximum fluorescein release depended on the structure and hydrophobicity of the carriers used in these studies. Copyright © 2012 Society of Chemical Industry  相似文献   

7.
Doxorubicin (Dox) is a widely used fluorescent chemotherapy drug. Its primary delivery systems, based on physical adsorption to silica nanoparticles, can lead to low drug loading. Direct loading of Dox via covalent bonds during the formation of silica nanoparticles has never been reported. In this work, we designed and synthesized a silane-borate precursor, which contains not only an alkoxysilane moiety to form organosilica nanoparticles but also a phenylboronic acid moiety to react with diol-containing compounds. Using this compound, the covalent loading of Dox during the preparation of organosilica nanoparticles was effectively realized with a high drug loading content up to 22.4 %. Further modification by hyaluronic acid (HA) bestowed the Si-Dox@HA nanoparticles with the ability to target CD44-overexpressing cancer cells. The Si-Dox@HA nanoparticles exhibited H2O2-responsive release of about 80 % Dox and displayed seven-fold selectivity for killing cancer cells over normal cells, relative to Dox and Si-Dox nanoparticles. Moreover, these Si-Dox@HA nanoparticles are also suitable for targeted fluorescence imaging of CD44-overexpressing cancer cells.  相似文献   

8.
The aim of this work was to explore the capacity to load an anticancer agent Doxorubicin (Dox) on new poly(alkylcyanoacrylate) (PACA) nanoparticles prepared by redox radical emulsion polymerization (RREP). These nanoparticles present several advantages compared with the previously described PACA nanoparticles obtained by anionic emulsion polymerization (AEP). Their cytotoxicity was lower and because they do not activate the complement system, they are believed to behave like stealth nanoparticles after intravenous administration. Dox was incorporated during the preparation of the nanoparticles. However, the drug molecules were degraded by cerium IV, which is a strong oxidant agent. To avoid drug degradation, Dox must be loaded by adsorption on preformed nanoparticles. Optimal loading capacity was deduced from a Scatchard's analysis of the Dox adsorption pattern. The loading performance [Loading efficiency (LE) 74%, Loading content (LC) 3.7%], the Dox release and the amount of Dox retained by the new nanoparticles 75% were similar to those of the already well described PACA nanoparticles obtained by AEP (LE 79% and LC 4.2%, drug retention capacity 75%). It can be concluded that the loading and releasing properties make the new nanoparticles an interesting carrier candidate for the in vivo delivery of Dox. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2011  相似文献   

9.
Optomagnetic multifunctional composite based on upconversion luminescence nanomaterial is regarded as a promising strategy for bioimaging,disease diagnosis and targeted delivery of drugs.To explore a mesoporous nanostructure with excellent water dispersibility and high drug-loading capacity,a novel nanorattle-structured Fe3O4@SiO2@NaYF4∶Yb,Er magnetic upconversion nanorattle (MUCNR) was suc-cessfully designed by using Fe3O4 as core and NaYF4∶Yb,Er nanocrystals as shell.The microstructures and crystal phase of the as-prepared MUCNRs were evaluated by transmission electron microscopy,X-ray powder diffraction and N2 adsorption/desorption isotherms.The Kirkendall effect was adapted to explain the formation mechanism of the MUCNRs.The loading content and encapsulation efficiency of doxorubicin hydrochloride (DOX) could reach as high as 18.2% and 60.7%,respectively.Moreover,the DOX loading MUCNR (DOX-MUCNR) system showed excellent sustained drug release and strong pH-dependent performance,which was conducive to drug release at the slightly acidic microenvironment of tumor.Microcalorimetry was used to quantify the interactions between the carrier structure and drug release rate directly.The heat release rates in the heat-flow diagrams are basically consistent with the DOX release rate,thereby showing that microcalorimetry assay not only provides a unique thermody-namic explanation for the structure-activity relationship of Fe3O4@SiO2@NaYF4∶Yb,Er MUCNRs but also provides powerful guidance to avoid the blind selection or design of drug carriers.Therefore,our work firmly provided a comprehensive perspective for using Fe3O4@SiO2@NaYF4∶Yb,Er MUCNRs as a remark-able magnetic targeted drug carrier.  相似文献   

10.
Functionalized amphiphilic block copolymers poly(N‐isopropyl acrylamide)‐b‐poly(stearyl methacrylate) (PNIPAM‐PSMA) are synthesized. Their self‐assembled core‐shell nanoparticles have the hydrophilic thermosensitive shell and hydrophobic crystallizable core. Nanoparticles exhibit volume phase transition at temperature of 38 °C and its poly(stearyl methacrylate) (PSMA) moiety could form nano size crystals to retain drugs, making them good carriers for drug co‐delivery system. Thermosensitivity and crystallinity of nanoparticles are characterized with dynamic light scattering (DLS), differential scanning calorimetry (DSC), small‐angle X‐ray scattering (SAXS), and atomic force microscopy (AFM). The interactions and relationship between chemical structures of copolymer nanoparticles and loading drugs are discussed. Different loading techniques and combined loading of hydrophobic/hydrophilic drugs are studied. Nanoparticles show a good and controllable drug loading capacity (DL) of hydrophilic/hydrophobic drugs. The drugs release kinetics is analyzed with Fick's law and Weibull model. A general method for analyzing drug release kinetics from nanoparticles is proposed. Weibull model is well fitted and the parameters with definite physical meaning are analyzed. PNIPAM‐PSMA nanoparticles show a quite different thermal response, temporal regulation, and sustained release effect of hydrophilic and hydrophobic drugs, suggesting a promising application in extended and controlled co‐delivery system of multi‐drug. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 44132.  相似文献   

11.
In this work, the near-infrared (NIR) light-responsive shape memory scaffolds with hierarchical porous structures are designed and facilely formed by freeze drying of 3D printed viscous gel-like pickering emulsions, which are stabilized by hydrophobically modified graphene oxide (g-GO) and silica nanoparticles, and contain thermo-responsive poly(d , l -lactic acid-co-trimethylene carbonate) (PLMC) in the oil phase. The prepared scaffolds display an interconnected filament structure with hierarchical pores and high porosity. The incorporation of g-GO nanoparticles into PLMC matrix prompts that the scaffold shape memory can be triggered by NIR light with fast shape recovery. Moreover, the in vitro mineralization experiment shows that the scaffolds have biological activity, and the drug release study demonstrates that the scaffolds can be used as drug carriers with efficient drug release capacity. Furthermore, cell culture assays based on mouse bone mesenchymal stem cells exhibit that the scaffolds own good cytocompatibility. Therefore, the facile preparation and remote activation of the shape memory nanocomposite scaffolds with hierarchical porous structure and multifunctionality represents a highly attractive candidate as minimally invasive implantation scaffolds for bone tissue engineering applications.  相似文献   

12.
Medical nanoplatforms based on clusters of superparamagnetic nanoparticles decorated with a PNIPAM thermo-responsive shell have been synthesized and used as drug carriers for doxorubicin (DOXO), a common chemotherapeutic agent. The nanosystem here developed has a total diameter below 200 nm and exploits the temperature responsive behaviour of the PNIPAM polymeric shell for the controlled loading and release of DOXO. The system has been tested in vitro on tumour cells and it clearly demonstrates the effectiveness of drug polymer encapsulation and time-dependent cell death induced by the doxorubicin release. Comparative cellular studies of the DOXO loaded nanoplatform in the presence or absence of an external magnet (0.3 T) showed the synergic effect of accumulation and enhanced toxicity of the system, when magnetically guided, resulting in the enhanced efficacy of the system.  相似文献   

13.
The aim of this study was to prepare arsenic trioxide (ATO)-loaded stealth PEGylated PLGA nanoparticles (PEG-PLGA-NPs) and to assess the merits of PEG-PLGA-NPs as drug carriers for ATO delivery. PEG-PLGA copolymer was synthesized with methoxypolyethyleneglycol (Mw=5000), D, L-lactide, and glycolide by the ring-opening polymerization method. Amorphous ATO was transformed into cubic crystal form to increase its solu-bility in the organic solvent. ATO-loaded PEG-PLGA-NPs were prepared by the modified spontaneous emulsification solvent diffusion (SESD) method, and the main experimental factors influencing the characteristics of nanopar- ticles were investigated, to optimize the preparation. To confirm the escape of PEG-PLGA-NPs from phagocytosis by phagocytes, PEG-PLGA-NPs labeled rhodamine B uptake by murine peritoneal macrophages (MPM) were analyzed by flow cytometry. The results showed that the physicochemical characteristics of PEG-PLGA-NPs were affected by the type and concentration of the emulsifiers, polymer concentration, and drug concentration. ATO-loaded PEG-PLGA-NPs, with particle size of 120.8nm, zeta potential of-10.73mV, encapsulation efficiency of 73.6%, and drug loading of 1.36%, were prepared under optimal conditions. The images of transmission electron micros-copy (TEM) indicated that the optimized nanoparticles were near spherical and without aggregation or adhesion. The release experiments in vitro showed the ATO release from PEG-PLGA-NPs exhibited consequently sustained release for more than 26d, which was in accordance with Higuchi equation. The uptake of PEG-PLGA-NPs by MPM was found to decrease markedly compared to PLGA-NPs. The experimental results showed that PEG-PLGA-NPs were potential nano drug delivery carriers for ATO.  相似文献   

14.
Novel amphiphilic star‐shaped terpolymers comprised of hydrophobic poly(?‐caprolactone), pH‐sensitive polyaminoester block and hydrophilic poly(ethylene glycol) (Mn = 1100, 2000 g mol?1) were synthesized using symmetric pentaerythritol as the core initiator for ring‐opening polymerization (ROP) reaction of ?‐caprolactone functionalized with amino ester dendrimer structure at all chain ends. Subsequently, a second ROP reaction was performed by means of four‐arm star‐shaped poly(?‐caprolactone) macromer with eight ‐OH end groups as the macro‐initiator followed by the attachment of a poly(ethylene glycol) block at the end of each chain via a macromolecular coupling reaction. The molecular structures were verified using Fourier transform infrared and 1H NMR spectroscopies and gel permeation chromatography. The terpolymers easily formed core–shell structural nanoparticles as micelles in aqueous solution which enhanced drug solubility. The hydrodynamic diameter of these agglomerates was found to be 91–104 nm, as measured using dynamic light scattering. The hydrophobic anticancer drug curcumin was loaded effectively into the polymeric micelles. The drug‐loaded nanoparticles were characterized for drug loading content, encapsulation efficiency, drug–polymer interaction and in vitro drug release profiles. Drug release studies showed an initial burst followed by a sustained release of the entrapped drug over a period of 7days at pH = 7.4 and 5.5. The release behaviours from the obtained drug‐loaded nanoparticles indicated that the rate of drug release could be effectively controlled by pH value. Altogether, these results demonstrate that the designed nanoparticles have great potential as hydrophobic drug delivery carriers for cancer therapy. © 2015 Society of Chemical Industry  相似文献   

15.
Zhen Tian 《Polymer》2008,49(2):446-454
In the present study we describe a synthesis and self-assembly and an in vitro evaluation of a kind of novel amphiphilic glycopeptide block copolymers as carriers for controlled drug release. Initially, an amphiphilic ABA triblock copolymer comprising polytetrahydrofuran (PTHF) as a central hydrophobic block flanked by poly(l-lysine)s (PLLs) as outer hydrophilic blocks was synthesized through the ring-opening polymerization of ?-benzyloxycarbonyl-l-lysine N-carboxyanhydride with a distal amine-terminated PTHF as a macroinitiator, followed by removal of the protecting group. Afterwards the resulting triblock copolymer was allowed to react with d-gluconolactone and lactobionolactone in the varying feeding ratios in the presence of diisopropylethylamine leading to the target glycopeptide block copolymers with high yields. They were found to easily self-assemble into nano-sized aggregates in water. The critical aggregation concentrations (CACs) were assessed by fluorescence measurement with N-phenyl-1-naphthylamine employed as a molecular probe. The particle sizes of the aggregates before and after doxorubicin loading were determined by dynamic light scattering (DLS) and the aggregate morphologies were evidenced by transmission electron microscopy (TEM) measurements. Finally, the in vitro doxorubicin loading capacity and release behavior were investigated with these glycopeptide copolymers as carriers for controlled release.  相似文献   

16.
Amino-modified polylactic acid (EPLA) nanofibre microspheres with a high porosity, large specific surface area, strong adsorption capacity, and rich in active amino groups were developed for drug delivery applications. Alendronate, a well-known antiresorptive agent, was chosen as a model drug to evaluate the loading capacity and release properties of the prepared EPLA microspheres. SEM micrographs clearly showed that the drug was loaded into the microspheres within the pores between the nanofibers and as well as being adsorbed on their surface. XRD and FTIR spectra analyses also confirmed drug loading. UV/Vis-absorption spectrophotometry was used to study the impact of various parameters, including adsorption time and initial concentration and pH value of the alendronate solution, on the microsphere drug-loading capacity. Under optimum conditions, EPLA microspheres exhibited a high alendronate adsorption capacity of up to 503?mg/g. In vitro release studies showed that alendronate-loaded EPLA nanofibre microspheres exhibited a perfect release performance, with alendronate being released in a sustained manner for approximately 15 days without any obvious initial burst. Therefore, EPLA nanofibre microspheres hold great potential as efficient, controlled release drug delivery carriers of alendronate.  相似文献   

17.
Gelatin (Type A) nanoparticles were prepared by a single W/O emulsion technique and characterized by infrared (IR) spectra, scanning electron microscopy (SEM), and particle size analysis. The IR spectra clearly confirmed the presence of gelatin and cytarabine in the loaded nanoparticles while the scanning electron micrograph (SEM) image depicts smooth surface, spherical shape and uneven size of nanoparticles (100–300 nm). The prepared nanoparticles were loaded with cytarabine, a well‐known anticancer drug, and the release dynamics of entrapped drug was investigated as a function of various experimental factors, such as percent loading of the drug, chemical architecture of the nanocarriers, and pH, temperature, ionic strength, and nature of the release medium. The nanoparticles were also studied for their water sorption capacity by optical microscopic method taking advantage of the aggregation of nanoparticles. The drug release process was analyzed kinetically using Ficks power law, and a correlation was established between the quantity of released drug and swelling of the nanoparticles. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 101: 2320–2332, 2006  相似文献   

18.
杨薇  朱圆芳 《安徽化工》2018,44(3):52-54
对所制备的二氧化硅纳米粒子(MS NPs)的载药性能、生物相容性和pH响应的药物释放性能进行了系统研究。实验结果显示,该MS NPs对化疗药物阿霉素(Dox)的负载量可达30μg·mg~(-1),具有很好的药物载运能力。此外,这种MS NPs具有pH响应性,能够对肿瘤微环境发生响应并精准释放药物对肿瘤细胞进行治疗。细胞MTT实验结果表明,所制得的MS NPs具有良好的生物相容性以及载药后很好的抗肿瘤能力,72h后可杀灭约82%的肿瘤细胞。因此,所制备的MS NPs在抗肿瘤领域有着巨大的应用潜力。  相似文献   

19.
To develop a nontoxic system for targeting therapy, a new highly ordered hierarchical mesoporous calcium carbonate nanospheres (CCNSs) as small drug carriers has been synthesized by a mild and facile binary solvent approach under the normal temperature and pressure. The hierarchical structure by multistage self-assembled strategy was confirmed by TEM and SEM, and a possible formation process was proposed. Due to the large fraction of voids inside the nanospheres which provides space for physical absorption, the CCNSs can stably encapsulate the anticancer drug etoposide with the drug loading efficiency as high as 39.7 wt.%, and etoposide-loaded CCNS (ECCNS) nanoparticles can dispersed well in the cell culture. Besides, the drug release behavior investigated at three different pH values showed that the release of etoposide from CCNSs was pH-sensitive. MTT assay showed that compared with free etoposide, ECCNSs exhibited a higher cell inhibition ratio against SGC-7901 cells and also decreased the toxicity of etoposide to HEK 293 T cells. The CLSM image showed that ECCNSs exhibited a high efficiency of intracellular delivery, especially in nuclear invasion. The apoptosis test revealed that etoposide entrapped in CCNSs could enhance the delivery efficiencies of drug to achieve an improved inhibition effect on cell growth. These results clearly implied that the CCNSs are a promising drug delivery system for etoposide in cancer therapy.  相似文献   

20.
A wide number of drug nanocarriers have emerged to improve medical therapies, and in particular to achieve controlled delivery of drugs, genes or gene expression-modifying compounds, or vaccine antigens to a specific target site. Of the nanocarriers, lipid-based and polymeric nanoparticles are the most widely used. Lipid-based systems like niosomes and liposomes are non-toxic self-assembly vesicles with an unilamellar or multilamellar structure, which can encapsulate hydrophobic/hydrophilic therapeutic agents. Polymeric nanoparticles, usually applied as micelles, are colloidal carriers composed of biodegradable polymers. Characteristics such as loading capacity, drug release rate, physical and chemical stability, and vesicle size are highly dependent on experimental conditions, and material and method choices at the time of preparation. To be able to develop effective methods for large scale production and to meet the regulatory requirements for eventual clinical implementation of nanocarriers, one needs to have in-depth knowledge of the principles of nanoparticle preparation. This review paper presents an overview of different preparation methods of polymeric and novel lipid-based (niosome and solid lipid) nanoparticles.  相似文献   

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