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1.
New carrier platforms have been designed for an electrospun pyridinium calixarene nanofiber for controlled drug delivery. First, 5,11,17,23-tetra-tert-butyl-25,27-bis(3-aminomethyl-pyridineamido)-26,28-dihydroxycalix[4]arene (3-AMP) scaffold was produced by electrospinning. AMP scaffold was modified by human serum albumin (HSA), folic acid (FA), and glutathione (GSH). Doxorubicin (DOX) was loaded to surfaces of the AMP, AMP-HSA, AMP-HSA-FA, and AMP-HSA-GSH nanofibers by using DOX solution in different buffers with, 2.2, 4.0, 6.0, and 7.4 pH. The release studies DOX from four different nanofibers was also done in a various amount microenviroments by changing pH values. The loading and release amount of DOX was estimated from the calibration curve drawn at 480 and 560 nm of excitation and emission wavelengths by using a fluorescence spectrophotometer. The loading studies were confirmed by Fourier transforms infrared, atomic force microscopy, transmission electron microscopy, scanning electron microscope, and energy-dispersive X-ray (EDX) analysis.  相似文献   

2.
In this study, a novel type of macromolecular prodrug, N‐galactosylated chitosan (GC)?5‐fluorouracil acetic acid (FUA) conjugate based nanoparticles, was designed and synthesized as a carrier for hepatocellular carcinoma drug delivery. The GC–FUA nanoparticles were produced by an ionic crosslinking method based on the modified ionic gelation of tripolyphosphate with GC–FUA. The structure of the as‐prepared GC–FUA was characterized by Fourier transform infrared and 1H‐NMR analyses. The average particle size of the GC–FUA nanoparticles was 160.1 nm, and their drug‐loading content was 21.22 ± 2.7% (n = 3). In comparison with that of the freshly prepared nanoparticles, this value became larger after 7 days because of the aggregation of the GC–FUA nanoparticles. An in vitro drug‐release study showed that the GC–FUA nanoparticles displayed a sustained‐release profile compared to 5‐fluorouracil‐loaded GC nanoparticles. All of the results suggest that the GC–FUA nanoparticles may have great potential for anti‐liver‐cancer applications. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 42625.  相似文献   

3.
The aim of this work was to prepare an erythromycin (EM) microemulsion (EM‐ microemulsion) for transdermal EM delivery using isotropic mixtures of oil and aqueous phases. The prepared EM‐microemulsion is a white dispersion, with a suitable viscosity for transdermal delivery. In stability experiments, the EM‐microemulsion showed no marked change in appearance for up to 3 weeks at 25°C. In accelerated stability experiments at 37 and 60°C, however, precipitated crystalline EM particles were observed in the EM‐microemulsion. Diffusion of EM into the skin exhibited a first order release profile. Fluorescein (FL)‐microemulsion penetrated to the dermis layer of skin. In conclusion, we confirmed that EM‐microemulsion could serve as an excellent transdermal carrier of EM. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2013  相似文献   

4.
Microgels (MGs) are synthetic colloidal hydrogel particles made of three dimensional polymer networks. Their chemical composition is crucial for their use as intelligent drug release systems operated by temperature control. Herein, several MGs using N-isopropylacrylamide (Nipam)/N-isopropylmethacrylamide (Nipmam), chitosan and acrylic/methacrylic acid have been synthesized by free radical polymerization reactions (NC MGs) and the effects of surfactants and different reaction times on size and swelling properties have been investigated. MGs have been identified and characterized by dynamic light scattering and atomic force microscopy, and finally used to optimize the encapsulation protocol of the hydrophobic drug sorafenib. The drug delivery system here described has encapsulation efficiency of 40% and releases 10% of the entrapped drug over about 16 h after the temperature is raised above the volume phase transition temperature. Data suggest that MGs with optimized composition may act as properly instructed entities able to trap and release biomolecules following external stimuli.  相似文献   

5.
The core-shell structured polymer microgels were synthesized by coating the hydrophobic poly(methyl methacrylate) (PMMA) sphere cores with hydrophilic nonlinear poly(ethylene glycol)-based gel shell layer. The uniqueness of these core-shell microgels lies in the integration of the PMMA core microsphere with strong hydrophobicity and the novel oligo(ethylene glycol)-based gel layer with well-defined thermosensitivity for improving loading/release efficacy of two detoxification drugs (chlorpromazine and diltiazem). The hydrophilic shell is composed of hydrophilic copolymer of 2-(2-methoxyethoxy)ethyl methacrylate (MEO2MA) with oligo(ethylene glycol) methyl ether methacrylates (MEO5MA). It was found that the molar ratio of two shell monomers n(MEO2MA)/n(MEO5MA) of 1:6 was an ideal matching value for production of the P(MEO2MA)/P(MEO2MA-co-MEO5MA) core-shell microgels with tunable volume phase transition temperature and excellent colloidal stability across the physiologically important temperature range. Moreover, chlorpromazine- and diltiazem-loaded microgels can show an obvious thermosensitive release and in vitro sustained-release characteristic up to 80 h.  相似文献   

6.
In this work, we present a new type of glutathione (GSH)-responsive polyurethane-based core‑shell nanogels (RS-CS-PUNGs) with hydrophilic methoxypolyethylene glycols (mPEG) shell, which was prepared by a one-pot synthetic method. The obtained RS-CS-PUNGs not only show a good size distribution with the hydrodynamic radii around of 20 nm, but also exhibit good stability in the organic solvent. The results demonstrate that GSH (10 mM) trigger the nanogel swelling and accelerate the loaded drug release in PBS (pH = 7.4). Although the RS-CS-PUNGs loaded with DOX show a slower cellular uptake behavior than the free doxorubicin (DOX), which is likely caused by the controlled drug release property of the nanocarrier, the enhanced cellular uptake fluorescence intensity of RS-CS-PUNGs loaded with DOX is still observed compared to the control group. Both MTT and CCK-8 assay indicate that although an obvious lower initial cytotoxicity is observed compared to free DOX at 24 h postincubation, the cytotoxicity of the RS-CS-PUNGs loaded with DOX is obvious enhanced after treated 72 h, which stayed at the similar level with free DOX. Attributing to the easy preparation progress and GSH-responsive property, RS-CS-PUNGs maybe hold the potential for further application in the field of drug delivery. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2020 , 137, 48473.  相似文献   

7.
'Plate-like-coral' shaped polymer capsule (PC-PLCDB) with dendritic network structure and porous channels has been synthesized and used for therapeutic purposes. First di-block copolymer [(PEG)-b-(L-AspA)n] has been synthesized from PEG (polyethylene glycol) and aspartic acid (AspA). Then the biocompatible PC-PLCDB has been achieved by homogeneous mixing of [(PEG)-b-(L-AspA)n] and poly-N-isopropyl acrylamide (PNIPAM) followed by reprecipitation. Only H-bonding is responsible for the foundation of self-assembly of the polymer chains and to form PC-PLCDB. A huge extent of loading anticancer drug, for example, doxorubicin (DOX) in PC-PLCDB is possible. in vitro study has been performed to check the therapeutic efficacy of PC-PLCAD-DOX formulation on chronic myeloid leukemia cells (K562). The IC50 has been calculated to be 0.405 (±0.014) ng μg−1 of the formulation. PC-PLCAD-DOX inhibits 80% of the cancer cell only by 1.0 μg mL−1 of the formulation. This study reveals that the PC-PLCAD could be a promising candidate for therapeutic applications.  相似文献   

8.
A novel stimuli‐responsive magnetite nanohydrogel (MNHG), namely [poly(ethylene glycol)‐block‐poly(N‐isopropylacrylamide‐co‐maleic anhydride)2]‐graft‐poly(ethylene glycol)/Fe3O4 [PEG‐b‐(PNIPAAm‐co‐PMA)2]‐g‐PEG/Fe3O4, was successfully developed. For this purpose, NIPAAm and MA monomers were block copolymerized onto PEG‐based macroinitiator through atom transfer radical polymerization technique to produce PEG‐b‐(PNIPAAm‐co‐PMA)2. The synthesized Y‐shaped terpolymer was crosslinked through the esterification of maleic anhydride units using PEG chains to afford a hydrogel. Afterward, magnetite nanoparticles were incorporated into the synthesized hydrogel through the physical interactions. The chemical structures of all synthesized samples were characterized using Fourier transform infrared and proton nuclear magnetic resonance spectroscopies. Morphology, thermal stability, size, and magnetic properties of the synthesized MNHG were investigated. In addition, the doxorubicin hydrochloride loading and encapsulation efficiencies as well as stimuli‐responsive drug release ability of the synthesized MNHG were also evaluated. The drug‐loaded MNHG at physiological condition exhibited negligible drug release values. In contrast, at acidic (pH 5.3) condition and a little bit higher temperature (41 °C) the developed MNHG showed higher drug release values, which qualified it for cancer chemotherapy due to especial physiology of cancerous tissue in comparison with the surrounding normal tissue. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018 , 135, 46657.  相似文献   

9.
Zein is the major storage protein from corn with strong hydrophobicity and unique solubility and has been considered as a versatile food biopolymer. Due to the special tertiary structures, zein can self‐assemble to form micro‐ and nano‐particles through liquid–liquid dispersion or solvent evaporation approaches. Zein‐based delivery systems have been particularly investigated for hydrophobic drugs and nutrients. Recently, increasing attention has been drawn to fabricate zein‐based advanced drug delivery systems for various applications. In this review, the molecular models of zein tertiary structure and possible mechanisms involved in zein self‐assembly micro‐ and nano‐particles are briefly introduced. Then, a state‐of‐the‐art introduction and discussion are given in terms of preparation, characterization, and application of zein‐based particles as delivery systems in the fields of food science, pharmaceutics, and biomedicine. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 40696.  相似文献   

10.
Maltose, a natural disaccharide, was crosslinked with divinyl sulfone to prepare poly(maltose) (p(MAL)) micro/nanoparticles via one step microemulsion system with ≥90% ± 5% yield in a size rage of 0.5–100 μm for the first time. P(MAL) was modified (m-p(MAL)) with ethylenediamine (EDA), polyethyleneimine (PEI), and taurine (TA) to render additional functionalities, that is, amine and sulfate groups. The isoelectronic point of bare p(MAL) particles were calculated at pH 2.2 ± 0.5 and was changed to 1.3 ± 0.5, 4.3 ± 1.0, and 8.1 ± 0.7 for TA (p(MAL)/TA), EDA (p(MAL)/EDA), and PEI (p(MAL)/PEI) modification, respectively. Bare p(MAL) particles were found to be biocompatible up to 2 mg/ml with hemolysis and blood clotting tests, whereas the modified p(MAL) particles were found to be biocompatible at 1 mg/ml concentration. Additionally, it was found that TA- and PEI-modified p(MAL) particles induced blood clotting mechanisms. Sodium diclofenac as model drug was released at proportions of 8.7% ± 1.3%, 3.9% ± 0.2%, 8.8% ± 0.9%, and 31.6% ± 0.4% of the loaded drug in phosphate buffered saline solution from p(MAL), p(MAL)/TA, p(MAL)/EDA, and p(MAL)/PEI, respectively. The inhibition of antimicrobial activity of p(MAL)/PEI particles at 20 mg/ml concentration for Escherichia coli and Staphylococcus aureus strain was determined as 99.86% ± 0.3% and 99.79% ± 0.25%, respectively.  相似文献   

11.
Carvedilol is a drug with low oral bioavailability due to its high first‐pass metabolism. The purpose of the present study was to prepare a mucoadhesive dry powder inhaler of this drug loaded in poly(ethylene‐co‐vinyl acetate)(PEVA) nanoparticles for pulmonary delivery. PEVA nanoparticles were prepared by an O/W solvent evaporation method and coated with different concentrations of chitosan as a mucoadhesive polymer. Encapsulation efficiency, particle size, zeta potential, release efficiency, and mucoadhesive properties of the different formulations were evaluated on mucin substrate. The optimized formulation of nanoparticles was spray dried using lactose and mannitol as carrier powders. The flowability of the obtained powders was checked by Carr's Index and Hausner ratio and the in vitro deposition of the aerosolized drug was investigated using a Next Generation Impactor. Increasing in the particle size and zeta potential of nanoparticles confirmed the settling of the chitosan coating layer on the surface of nanoparticles. The in vitro drug release from coated nanoparticles decreased with increasing of chitosan concentration. Mucoadhesive property of chitosan‐coated PEVA nanoparticles was higher than noncoated ones. Spray‐dried powders had different aerosilization behavior. Mannitol‐based formulation was found to have low density, better flow ability, smaller aerodynamic diameter (daer) and higher fine powder fraction. The results of the present study allow concluding that mannitol spray dried, mucoadhesive nanoparticles of PEVA are suitable inhaler powder for pulmonary delivery of carvedilol. © 2013 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 39694.  相似文献   

12.
Non‐porous poly(2‐hydroxyethyl methacrylate) [p(HEMA)] nanoparticles were prepared by surfactant free emulsion polymerization. The p(HEMA) nanoparticles was about 200 nm diameter, spherical form, and non‐porous. Reactive Red 120 (RR 120) was covalently attached to the p(HEMA) nanoparticles and Ni(II) ions were incorporated to attach dye molecules. Urease was immobilized onto RR120‐Ni(II) attached p(HEMA) nanoparticles via adsorption. The maximum urease adsorption capacity of RR120‐Ni(II) attached p(HEMA) nanoparticles was 480.01 mg g?1 nanoparticles at pH 7.0 in phosphate buffer. It was observed that urease could be repeatedly adsorbed and desorbed without significant loss in adsorption amount. Km values were 21.50 and 34.06 mM for the free and adsorbed enzyme. The Vmax values were 4 U for the free enzyme and 3.3 U for the adsorbed enzyme. The optimum pH was 25 mM pH 7 phosphate buffer for free and adsorbed enzyme. The optimum temperature was determined at 35°C and 55°C for the free and adsorbed enzyme, respectively. These findings show considerable promise for this material as an adsorption matrix in biotechnological applications. © 2013 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 39757.  相似文献   

13.
Porous chitosan (CS)/graphene oxide (GO) composite xerogels were prepared through a simple and “green” freeze‐drying method. Scanning electron microscopy, Fourier transform infrared spectrometry, powder X‐ray diffraction, and compressive strength measurements were performed to characterize the microstructures and mechanical properties of as‐prepared composite xerogels. The results show that the incorporation of GO resulted in an observable change in the porous structure and an obvious increase in the compressive strength. The abilities of the composite xerogels to absorb and slowly release an anticancer drug, doxorubicin hydrochloride (DOX), in particular, the influence of different GO contents, were investigated systematically. The porous CS/GO composite xerogels exhibited efficient DOX‐delivery ability, and both the adsorption and slow‐release abilities increased obviously with increasing GO content. Additionally, the best adsorption concentration of DOX was 0.2 mg/mL, and the cumulative release percentage of DOX from the xerogels at pH4 much higher than that at pH 7.4. Therefore, such porous CS/GO composite xerogels could be promising materials as postoperation implanting stents for the design of new anticancer drug‐release carriers. © 2013 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2014 , 131, 40006.  相似文献   

14.
Electrospun scaffolds of the biodegradable and biocompatible poly-4-hydroxybutyrate (P4HB) polyester have been prepared using horizontal and vertical set-up configurations of electrospinning. Specifically, it has been evaluated the influence of solvent, polymer concentration, and processing parameters, such as applied voltage, flow rate, and needle tip-collector distance. Scaffolds obtained under the most favorable conditions were characterized in terms of crystallinity, lamellar supramolecular order, thermal (including calorimetric and thermogravimetric data), mechanical, and surface properties. Results pointed out significant differences with respect to commercial sutures (based in P4HB, e.g., MonoMax®) and demonstrated that electrospun scaffolds were constituted by crystalline microfibers with a tangled distribution that leads to high modulus Young modulus (4 MPa), maximum strength (28 MPa), and elongation (360%). Furthermore, new scaffolds had thermal stability and a rough surface that led to a hydrophobic character (105°). Scaffolds could also be successfully loaded during the electrospinning process with a peptide analog to the fibroblast growth factor (e.g., CYRSRKYSSWYVALKRC), giving rise to fully biocompatible samples with a clear acceleration in wound healing.  相似文献   

15.
This study was designed to develop a drug delivery system based on poly(N-isopropylacrylamide) (pNIPAM) hydrogel and a suitable solvent to enhance solubility and local release of curcumin. pNIPAM hydrogel was synthesized by radical polymerization. The chemical, mechanical and physical properties and biocompatibility of pNIPAM hydrogel were investigated as an implantable and rechargeable drug reservoir. Curcumin was loaded within pNIPAM hydrogel during swelling by using two different solvents; methanol, an organic solvent, and low molecular weight polyethylene glycol (PEG200), a polymeric solvent. The results of drug solubility showed that using PEG200 can increase curcumin solubility more than commonly used organic solvents such as methanol. Also, the release profile of drug-loaded hydrogels demonstrated that PEG200 has a superior effect on the cumulative amount of released curcumin (33.163 ± 0.319 μg/ml) compared to methanol (8.765 ± 0.544 μg/ml) during 1 week. Based on our results, curcumin-loaded hydrogels did not show any cytotoxicity, and pNIPAM/PEG combination represented an antibacterial effect within 12 hours. Accordingly, it can be concluded that pNIPAM hydrogel in combination with low molecular weight PEG200 could be used as an efficient drug delivery system to preserve and provide sustained release of curcumin as a hydrophobic drug.  相似文献   

16.
In order to reduce the toxic side effects of chemotherapeutic drugs and improve the targeting and efficiency of cancer treatment, the development of drug delivery system has received great attention. In this study, second generation polyglutamic acid dendrimers (G2) are used as basic materials to produce porous nanoparticles through cross link by crosslinkers containing disulfide bonds. The crosslinked products (G2)n have negative electricity and abundant voids, which enable them to adsorb the electronegative anticancer drug DOX. At the same time, in order to transport DOX to the tumor site, we modified FA on DOX and encapsulated it in magnetic mesoporous silica (FA-DOX-MSNs). Therefore, the final nanoparticles (FA-DOX-MSNs/(G2)n) not only have dual targeting ability to transport DOX to the tumor site, but also have reductive responsiveness that can release drugs responsively in the tumor cells. In addition, it has good biocompatibility and endocytosis ability.  相似文献   

17.
The inflammation and pain associated with osteoarthritis are treated with nonsteroidal anti‐inflammatory drugs (NSAIDs). This treatment is accompanied by several side effects; therefore local intra articular (IA) NSAID injection can be more efficient and safe than systemic administration or topical use. In this study, alginate?chitosan?pluronic nanoparticles were considered as a new vehicle for IA meloxicam delivery. These novel nanoparticles were prepared using an ionotropic gelation method and were optimized for variables such as alginate to chitosan mass ratio, pluronic concentration, and meloxicam concentration using a 3‐factor in 3‐level Box‐Behnken design. To optimize the formulation, the dependent variables considered were particle size, zeta potential, entrapment efficiency, and mean dissolution time (MDT). The nanoparticles morphology was characterized by FESEM and AFM. The potential interactions of the drug‐polymers were investigated by ATR‐FTIR and DSC, and the delivery profile of meloxicam from the nanoparticles was obtained. The average particle size of the optimized nanoparticles was 283 nm, the zeta potential was ?16.9 mV, the meloxicam entrapment efficiency was 55%, and the MDT was 8.9 hours. The cumulative released meloxicam amount from the composite nanoparticles was 85% at pH 7.4 within 96 h. The release profile showed an initial burst release followed by a sustained release phase. The release mechanism was non‐Fickian diffusion. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 42241.  相似文献   

18.
In this work, nanofiber scaffolds for surface drug delivery applications were obtained by electrospinning poly(N-vinylcaprolactam) (PNVCL) and its blends with poly(ε-caprolactone) and poly(N-vinylcaprolactam)-b-poly(ε-caprolactone). The process parameters to obtain smooth and beadless PNVCL fibers were optimized. The average fibers diameter was less than 1 μm, and it was determined by scanning electron microscopy analyses. Their affinity toward water was evaluated by measuring the contact angle with water. The ketoprofen release behavior from the fibers was analyzed using independent and model-dependent approaches. The low values of the release exponent (n < 0.5) obtained for 20 and 42 °C, indicating a Fickian diffusion mechanism for all formulations. Dissolution efficiencies (DEs) revealed the effect of polymer composition, methodology used in the electrospinning process, and temperature on the release rate of ketoprofen. PNVCL/poly(N-vinylcaprolactam)-b-poly(ε-caprolactone)-based nanofibers showed greater ability to control the in vitro release of ketoprofen, in view of reduced kinetic constant and DE, making this material promising system for controlling release of hydrophobic drugs. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2020 , 137, 48472.  相似文献   

19.
Surface‐modified poly(d , l ‐lactide)/polycaprolactone/β‐tricalcium phosphate complex scaffold was fabricated in this study and we hypothesized that pliable and mechanical strong scaffold would be achieved by regulation of ternary compositions; while superficial modification strategy conduced to preserve and controlled‐release of bioactive growth factors. Properties of the composite scaffolds were systematically investigated, including mechanical properties, surface morphology, porosity, wettability, and releasing behavior. Moreover, the representative cytokine, recombinant human bone morphogenetic protein‐2 (rhBMP‐2), was loaded and implanted into muscular pouch of mouse to assess bone formation in vivo. Improved osteogenesis was achieved ascribed to both amplified β‐tricalcium phosphate (β‐TCP) content and retarded initial burst release. Particularly, scaffold doped with hydroxypropyl methylcellulose (HPMC) displayed optimal osteogenic capability. The results indicated that the PDLLA/PCL/β‐TCP complex scaffold along with HPMC‐coating and rhBMP‐2 loading was a promising candidate for bone regeneration. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 40951.  相似文献   

20.
In this paper, we have evaluated the incorporation of a drug model and its release from silk fibroin (SF) membranes, analyzing the morphological, chemical, barrier, and biological properties. SF self-assembled into stable globular structures, encapsulating the drug, when diclofenac sodium (DS) was incorporated into SF solution prior to membranes preparation. The membranes showed biostatic action and prevented microorganism permeation. Kinetic studies indicate that DS was released in 120 min, with Fickian diffusion as the main mechanism of release. Results of this paper emphasize the potential of SF in wound healing, with good barrier and biological properties. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2020 , 137, 48763.  相似文献   

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