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1.
This study was aimed to develop an injectable polymeric drug delivery system for tamoxifen citrate (TC) using poly(sebacic acid‐co‐ricinoleic acid) [poly(SA‐RA) 70 : 30 w/w] as a drug carrier for the treatment of estrogen receptor positive breast cancer. Injectable biodegradable microparticles of TC were produced by solvent displacement technique of microencapsulation and were characterized by surface morphology (scanning electron microscopy), particle size, size distribution, physical and chemical interaction (Fourier transform infrared), nature and physical state of drug [DSC and X‐ray diffraction (XRD)], and in vitro release studies. TC loading over different concentrations was analyzed by high performance liquid chromatography (HPLC) technique. Polyanhydride microparticles obtained after lyophilization were nearly spherical in shape with smooth surface and size less than 2.5 μm. TC was dispersed in the form of amorphous state, and TC remains intact and stable during the process of microencapsulation. In vitro drug release studies demonstrated prolonged controlled release of TC with zero‐order kinetics. Stability studies revealed that the production process of microparticles itself did not affect the chemical stability of the drug and polymer forming the particle matrix. Significant difference in drug release capacity was observed in microparticles with different drug loadings, and the drug release was more sustained in microparticles prepared with high TC. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2011  相似文献   

2.
Dexamethasone‐loaded poly(lactide‐co‐glycolide) (PLGA) devices are commonly used as model systems for controlled release. In this study, PLGA nanoparticles containing dexamethasone acetate were prepared by a nanoprecipitation technique in the absence of organochlorine solvents and were characterized by their mean size, ζ potential, scanning electron microscopy, and differential scanning calorimetry to develop a controlled release system. The analytical method for the quantification of dexamethasone acetate by high‐performance liquid chromatography was validated. The results show that it was possible to prepare particles at a nanometric size because the average diameter of the drug‐loaded PLGA particles was 540 ± 4 nm with a polydispersity index of 0.07 ± 0.01 and a ζ potential of ?2.5 ± 0.3 mV. These values remained stable for at least 7 months. The drug encapsulation efficiency was 48%. In vitro tests showed that about 25% of the drug was released in 48 h. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 41199.  相似文献   

3.
Tetracycline (TC)‐loaded ionic interpenetrating polymer networks (IPNs) of carboxymethyl cellulose (CMC) and crosslinked poly(acrylic acid) (PAA) were prepared and characterized by infrared spectral analysis, differential scanning calorimetry and scanning electron microscopy techniques. The prepared IPNs were evaluated for in vitro blood compatibility by clot formation and hemolysis methods and their water imbibitions capacity was determined. Fractional release dynamics of tetracycline was also investigated from loaded IPNs of CMC and PAA. The entrapped drug was examined for antibacterial activity and structural integrity and effects of various parameters such as percentage loading of the drug, chemical composition of the carrier IPN, pH and temperature of the release medium were investigated on the release profiles of TC. The drug was also released in different simulated biological fluids. Copyright © 2005 Society of Chemical Industry  相似文献   

4.
To reach sustained drug release, a new composite drug‐delivery system consisting of poly(d,l ‐lactide‐co‐glycolide) (PLGA) nanoparticles (NPs) embedded in thermosensitive poly(N‐isopropyl acrylamide) (PNIPAAm) hydrogels was developed. The PNIPAAm hydrogels were synthesized by free‐radical polymerization and were crosslinked with poly(ethylene glycol) diacrylate, and the PLGA NPs were prepared by a water‐in‐oil‐in‐water double‐emulsion solvent‐evaporation method. The release behavior of the composite hydrogels loaded with albumin–fluorescein isothiocyanate conjugate was studied and compared with that of the drug‐loaded neat hydrogel and PLGA NPs. The results indicate that we could best control the release rate of the drug by loading it to the PLGA NPs and then embedding the whole system in the PNIPAAm hydrogels. The developed composite hydrogel systems showed near zero‐order drug‐release kinetics along with a reduction or omission of initial burst release. The differential scanning calorimetry results reveal that the lower critical solution temperature of the developed composite systems remained almost unchanged (<1°C increase only). Such a characteristic indicated that the thermosensitivity of the PNIPAAm hydrogel was not distinctively affected by the addition of PLGA NPs. In conclusion, an approach was demonstrated for the successful preparation of a new hybrid hydrogel system having improved drug‐release behavior with retained thermosensitivity. The developed systems have enormous potential for many biotechnological applications. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 40625.  相似文献   

5.
Copolymers of ε‐caprolactone and L ‐lactide (PCLLA) with different monomer ratio were synthesized by ring opening polymerization, and drug‐loaded nanoparticles of poly‐ε‐caprolactone (PCL), poly‐L ‐lactide (PLLA), and their copolymers were prepared by precipitation method, respectively. The results of differential scanning calorimetry and X‐ray diffraction indicated that the copolymerization of PCLLA decreased the crystallinity of the polymers, and the results of transmission electron micrograph and laser light scattering (LLS) revealed that the prepared nanoparticles had a spherical shape, and the size of PCLLA nanoparticles (∼ 85 nm) was smaller than that of the PCL and PLLA nanoparticles. The experiment of in vitro drug release showed that the drug release rate from PCLLA nanoparticles was slower than that from PCL and PLLA nanoparticles, and the release profile of PCL6/LA4 nanoparticles appeared to follow zero order kinetics. These results suggested that the polymer composition made a great influence on the nanoparticle size and drug release behavior. © 2000 John Wiley & Sons, Inc. J Appl Polym Sci 75: 874–882, 2000  相似文献   

6.
Methyl methacrylate (MMA), methoxy poly(ethylene glycol) monomaleate (MPEG), and acrylamidoglycolic acid (AGA) terpolymeric microgels (MGs) have been synthesized by free‐radical surfactant‐free emulsion polymerization. MPEG was synthesized from maleic anhydride and methoxy poly(ethylene glycol). The MGs were crosslinked with ethylene glycol dimethacrylate, and the chemical crosslinking was confirmed by Fourier transform infrared spectroscopy. 5‐Fluorouracil (5‐FU), a model anticancer drug, has been loaded into the MGs by in situ and adsorption methods. Empty as well as drug‐loaded MGs were then characterized by transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and X‐ray diffraction (XRD). DSC and XRD studies indicated a molecular level dispersion of the drug in PMMA MGs during in situ loading. TEM images showed the formation of spherical MGs. In vitro release of 5‐FU from the crosslinked poly(MMA‐co‐AGA‐co‐MPEG) MGs were investigated at both pH 7.4 and 1.2 buffer medium that controlled release of the drug up to ~ 18 h. Both the encapsulation efficiency and the release patterns were dependent on the amount of crosslinking agent and the amount of drug loaded. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2009  相似文献   

7.
The development of porous biodegradable scaffolds is of great interest in tissue engineering. In this regard, exploration of novel biocompatible materials is needed. Silk fibroin‐chondroitin sulfate‐sodium alginate (SF‐CHS‐SA) porous hybrid scaffolds were successfully prepared via lyophilization method and crosslinked by 1‐ethyl‐3‐(3‐dimethylaminopropyl)carbodiimide‐ethanol treatment. According to the scanning electron microscopy studies, mean pore diameters of the scaffolds were in the range of 60–187 μm. The porosity percentage of the scaffold with SF‐CHS‐SA ratio of 70 : 15 : 15 (w/w/w %) was 92.4 ± 3%. Attenuated total reflectance Fourier transform infrared spectroscopy, X‐ray diffraction, and differential scanning calorimetry results confirmed the transition from amorphous random coil to crystalline β‐sheet in treated SF‐CHS‐SA scaffold. Compressive modulus was significantly improved in hybrid scaffold with SF‐CHS‐SA ratio of 70 : 15 : 15 (3.35 ± 0.15 MPa). Cytotoxicity assay showed that the scaffolds have no toxic effects on chondrocytes. Attachment of chondrocytes was much more improved within the SF‐CHS‐SA hybrid scaffold. Real‐time polymerase chain reaction analyses showed a significant increase in gene expression of collagen type II, aggrecan, and SOX9 and decrease in gene expression of collagen type I for SF‐CHS‐SA compared with SF scaffold. This novel hybrid scaffold can be a good candidate to be utilized as an efficient scaffold for cartilage tissue engineering. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 41048.  相似文献   

8.
The venlafaxine hydrochloride (VHL)‐loaded chitosan nanoparticles were prepared by ionic gelation of chitosan (CS) using tripolyphosphate (TPP). The nanoparticles were characterized using FTIR, differential scanning calorimetry, X‐ray diffraction, dynamic light scattering, transmission electron microscopy, and X‐ray photoelectron spectroscopy. The effect of concentration of CS, polyethylene glycol (PEG), VHL and CS/TPP mass ratio on the particle size and zeta potential of nanoparticles was examined. The particle size of CS/TPP nanoparticles and VHL‐loaded CS/TPP nanoparticles was within the range of 200–400 nm with positive surface charge. In the case of VHL‐loaded nanoparticles and PEG‐coated CS/TPP nanoparticles, the particle size increases and surface charge decreases with increasing concentration of VHL and PEG. Both placebo and VHL‐loaded CS/TPP nanoparticles were observed to be spherical in nature. PEG coating on the surface of CS/TPP nanoparticles was confirmed by XPS analysis. Maximum drug entrapment efficiency (70%) was observed at 0.6 mg/mL drug concentration. In vitro drug release study at 37°C ± 0.5°C and pH 7.4 exhibited initial burst release followed by a steady release. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2009  相似文献   

9.
In this study, itaconic acid (IA) was grafted on poly(vinyl alcohol) (PVA) at two different grafting percentages, 7.0% (w/w) and 14.0% (w/w), and membranes were prepared from the grafted copolymer (PVA‐g‐IA). Performances of PVA and PVA‐g‐IA membranes for the transdermal release of salicylic acid (SA) at in vitro conditions were investigated by using 2.0 mg/mL SA solutions. Effect of the pH on the release of SA was studied by keeping pH of donor and acceptor solutions in a range of (2.1–7.4). Permeation studies were also carried on at different SA concentrations. Effect of temperature on the release of SA was investigated in the temperature range of (32–39) (±1)°C. Results showed that presence of IA decreased the release of SA from the PVA membranes and 73% SA was released at the end of 48 h at (32 ± 1)°C from the IA‐1 membranes. pH affected the release of SA through the grafted membranes and studies showed that release of SA was high with donor solution pH of 2.1. When the pH of donor and receiver solutions were kept at the same pH value, the overall SA% in permeate increased. Increase in concentration of SA decreased the release of SA for the studied membranes. Release of SA from PVA‐g‐IA membranes was temperature sensitive and increase in temperature from (32 ± 1)°C to (39 ± 1)°C increased the release percentage of SA by 24% (w/w). The overall activation energy for the permeation of SA through IA‐1 membrane was found to be 22.97 kJ/mol. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2008  相似文献   

10.
BACKGROUND: Drug‐loaded electrospun ultrafine fibers have the advantages of both nanoscale drug delivery systems and conventional solid dosage forms. To improve the control of drug release, the combined use of electrospinning and pharmaceutical polymers has attracted increasing interest recently. RESULTS: Ultrafine drug‐loaded polyvinylpyrrolidone fibers were successfully prepared using an electrospinning process with ibuprofen as the active pharmaceutical ingredient and polyvinylpyrrolidone K30 as the filament‐forming polymer. The analytical results from scanning electron microscopy, differential scanning calorimetry and Fourier transform infrared spectroscopy indicated that the drug had good compatibility with the polymer and that the drug was well distributed in the ultrafine fibers as an amorphous physical form. In vitro dissolution tests showed that the fiber mats were able to dissolve within 10 s through a polymer‐controlled mechanism. CONCLUSION: The fast dissolution of drug‐loaded fibers may lead to applications that improve dissolution rates of poorly water‐soluble drugs, or that involve the preparation of oral fast‐dissolving drug delivery systems. Copyright © 2009 Society of Chemical Industry  相似文献   

11.
In this study, acrylamide (AAm) was grafted onto poly(vinyl alcohol) (PVA) in solution with UV radiation, and membranes were prepared from the graft copolymer (PVA‐g‐AAm) for transdermal release of salicylic acid (SA) at in vitro conditions. Permeation studies were carried out using a Franz‐type diffusion cell. Release characteristics of SA through PVA and PVA‐g‐AAm membranes were studied using 2.0 mg/mL SA solutions. Effects of the presence of AAm in the copolymer, pH of donor and acceptor solution, and concentration of SA and temperature on the release of SA were investigated. Permeation of SA through the membranes was found to be pH‐dependent, and increase in pH generally increased the release percentage of SA, and the presence of AAm in the membrane positively affected the permeation. The effect of concentrations of SA on the permeation was also searched using saturated solution of SA, and permeated amount of SA was found to be less than in the case of unsaturated SA solution. Studies showed that the release of SA from PVA‐g‐AAm membranes was temperature‐sensitive and increase in temperature increased the permeation rate. 82.76% (w/w) SA was released at the end of 24 h at (39 ± 1)°C, and the overall activation energy for the permeation of SA through PVA‐g‐AAm membranes was found to be 19.65 kJ/mol. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2008  相似文献   

12.
To prepare antibacterial, polymeric catheters for preventing catheter‐induced infections, sulfathiazole was loaded into polyurethane by solubilizing with solvents and the resultant films were cast. Fourier transform infrared spectroscopy confirmed the presence of sulfathiazole in the drug‐loaded polyurethane films. The thermal and mechanical properties of the films were assessed using differential scanning calorimetry and dynamic mechanical analysis. The drug‐loaded films were immersed in constantly stirred, deionized water at 37 °C for in vitro drug release study. The experimental data obtained from the in vitro drug release study were fit into mathematical models. Antibacterial efficiency of released sulfathiazole was evaluated by Escherichia coli growth inhibition test. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018 , 135, 46467.  相似文献   

13.
Bioactive wound dressings from poly(vinyl alcohol) (PVA) and zein nanoparticles (NPs) loaded with diclofenac (DLF) were prepared successfully by the single jet electrospinning method. DLF‐loaded zein NPs with an average diameter of ~228 nm were prepared using anti‐solvent precipitation method. The formulation of zein:DLF 1:1 exhibited optimum encapsulation efficiency of 47.80%. The NPs were characterized by dynamic light scattering, zeta‐potential measurement, and differential scanning calorimetry. In vitro, drug release profiles of the DLF‐loaded zein NPs, and PVA–zein NPs were also studied within 120 h and showed the release efficiency of nearly 80% from zein NPs. A more controlled release of DLF was achieved by embedding the zein NPs in the PVA nanofibers. Fourier transform infrared spectroscopy was used to analyze possible interactions between different components of the fabricated dressings. The mechanical properties of the developed dressings were also evaluated using uniaxial tensile testing. Young's modulus (E) of the dressings decreased after inclusion of zein NPs within the PVA nanofibers. Moreover, fibroblast culturing experiments proved that the composite dressings supported better cell attachment and proliferation compared to PVA nanofibers, by exhibiting moderate hydrophilicity. The results suggested that the electrospun composite dressing of PVA nanofibers and zein NPs is a promising topical drug‐delivery system and have a great potential for wound healing application. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018 , 135, 46643.  相似文献   

14.
Three‐dimensional polymeric networks, which quickly swell by imbibing a large amount of water or deswell in response to changes in their external environment, are called hydrogels. These types of polymeric materials are good potential candidates for drug‐delivery systems. In this study, we first synthesized poly(vinyl acetate‐co‐maleic anhydride) by free‐radical copolymerization. Then, they were modified with different molar ratios of melamine to prepare hydrogels that could be used in drug‐delivery systems. The hydrogels were characterized by Fourier transform infrared spectroscopy, 1H‐NMR, differential scanning calorimetry, and scanning electron microscopy. In the second step, Ceftazidime antibiotic was loaded on selected hydrogels. The in vitro drug release was investigated and compared in three different media (HCl solution at pH = 3 and buffer solutions at pH 6.1and pH 8). © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 40389.  相似文献   

15.
Semi‐interpenetrating network (IPN) of sodium alginate (NaAlg) and N‐isopropylacrylamide (NIPAAm) microspheres were prepared by water‐in‐oil (w/o) emulsification method. The microspheres were encapsulated with 5‐fluorouracil (5‐FU) and release patterns carried in 7.4 pH at temperatures of 25 and 37°C. The semi‐IPN microspheres were characterized by Fourier transform infrared spectroscopy (FTIR). Differential scanning calorimetry (DSC) and scanning electron microscopic studies were done on the drug‐loaded microspheres to confirm the polymorphism of 5‐FU and surface morphology of microspheres. These results indicated the molecular level dispersion of 5‐FU in the semi‐IPN microspheres. Particle size and size distribution were studied by laser light diffraction technique. Microspheres exhibited release of 5‐FU up to 12 h. The swelling studies were carried in 1.2 and 7.4 pH buffer media at 25 and 37°C. Drug release from NaAlg‐NIPAAm semi‐IPN microspheres at 25 and 37°C confirmed the thermosensitive nature by in vitro dissolution. The micro domains have released in a controlled manner due the presence of NIPAAm in the matrix. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2008  相似文献   

16.
In this study, a novel paclitaxel (PTX) loaded and a crosslinked solid phospholipid nanoparticles (SLN‐PTX) with negative surface charge was prepared by UV polymerization for drug delivery. Capping of positive charge of zwitterionic lecithin with negative charge of sodium 2‐acrylamido‐2‐methyl‐1‐propanesulfonate (AMPS‐Na) through cation exchange interaction produced a lecithin‐AMPS (L‐AMPS) complex. The amphiphilic and negative charged lipid complex was emulsified in the presence of emulsifier, paclitaxel, initiator, and methacrylated poly ε‐caprolacton‐diol (PCL‐MAC) as a spacer. The colloidal system was subjected to UV‐irradiation to obtain crosslinked nanoparticles. Completion of the UV‐polymerization was monitored with differential scanning calorimetry (DSC), which indicated the disappearance of exothermic peaks of vinyl groups. The nanoparticle system, having an average size of 200 nm, exhibited high drug encapsulation (96%) with negatively charged surface (zeta potential had an average of ?70 mV). PTX release profiles of the crosslinked and uncrosslinked SLN‐PTXs were studied and their pharmacological properties were compared. The crosslinked nanoparticles exhibited more controlled release behavior with longer release time compared to the uncrosslinked ones. In vitro cytotoxicity test was conducted on MCF‐7 human breast adenocarcinoma cell line, which indicated that the crosslinked SLN‐PTXs have a potential therapeutic effect for breast cancer treatments. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 44105.  相似文献   

17.
This study describes preparation of poly (acrylic acid)‐grafted cotton fibers and release of antibiotic drug gentamicin sulfate from them under physiological conditions. Poly(acrylic acid) has been grafted onto cellulose backbone of cotton fibers via Ce(IV)‐initiated polymerization in aqueous medium. The conditions obtained for optimum grafting were as follows: initiation time 30 min; initiation temperature 37°C; monomer concentration 27.8 mM; grafting temperature 30°C; nitric acid (catalyst) concentration 0.1M. The grafted fibers were characterized by FTIR, TGA, and SEM analysis. The antibiotic drug gentamicin sulfate (GS) was loaded into the grafted fibers by equilibration method and release was studied under physiological conditions. The kinetic release data was interpreted by first‐order kinetic model. Finally, drug‐loaded fibers showed fair antibacterial action against Escherichia coli. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2011  相似文献   

18.
The crystallization and melting behavior of poly(β‐hydroxybutyrate‐co‐β‐hydroxyvalerate) (PHBV) and a 30/70 (w/w) PHBV/poly(propylene carbonate) (PPC) blend was investigated with differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR). The transesterification reaction between PHBV and PPC was detected in the melt‐blending process. The interaction between the two macromolecules was confirmed by means of FTIR analysis. During the crystallization process from the melt, the crystallization temperature of the PHBV/PPC blend decreased about 8°C, the melting temperature was depressed by 4°C, and the degree of crystallinity of PHBV in the blend decreased about 9.4%; this was calculated through a comparison of the DSC heating traces for the blend and pure PHBV. These results indicated that imperfect crystals of PHBV formed, crystallization was inhibited, and the crystallization ability of PHBV was weakened in the blend. The equilibrium melting temperatures of PHBV and the 30/70 PHBV/PPC blend isothermally crystallized were 187.1 and 179°C, respectively. The isothermal crystallization kinetics were also studied. The fold surface free energy of the developing crystals of PHBV isothermally crystallized from the melt decreased; however, a depression in the relative degree of crystallization, a reduction of the linear growth rate of the spherulites, and decreases in the equilibrium melting temperature and crystallization capability of PHBV were detected with the addition of PPC. © 2004 Wiley Periodicals, Inc. J Appl Polym Sci 92: 2514–2521, 2004  相似文献   

19.
Protein‐loaded multifilament fibers were fabricated by the wet‐spinning method. The polymers which were tested included poly(L,D ‐lactide) [P(L,D )LA], L/D ratio 96/4 and poly(L,DL ‐lactide) [P(L,DL )LA], L /DL ratio 70/30. The polymers were dissolved in dichloromethane and bovine serum albumin (BSA) was dissolved in water, respectively. The solutions were mixed together using a probe sonicator to form a polymer‐protein emulsion. This emulsion was extruded to an ethanol spin bath. The fibers possessed a distinct sheath‐core structure, where the inner core was porous and the outer sheath was smooth. The diameters of the filaments were in the range of 46 and 70 μm. The tenacity values of the filaments were between 7 and 17 MPa. In vitro drug release rate of the P(L,DL )LA 70/30 filament was faster than that of the P(L,D )LA 96/4 filament. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2010  相似文献   

20.
With bovine serum albumin (BSA) as a model drug, drug‐loaded films of chitosan (CS) and poly(vinyl alcohol) (PVA) were obtained by a casting/solvent evaporation method and crosslinked by tripolyphosphate (TPP). The films were characterized by FTIR, XRD, and SEM. The influential factors of drug‐loaded films on drug‐controlled release were studied. These factors included, primarily, the component ratio of CS and PVA, the loaded amount of BSA, the pH and ionic strength of the release solution, and the crosslinking time with TPP. The results showed that within 25 h, when the weight ratios of CS to PVA in the drug‐loaded films were 90 : 10, 70 : 30, 50 : 50, and 30 : 50, the cumulative release rates of BSA were 63.3, 72.9, 81.8, and 91.8%, respectively; when the amounts of model drug were 0.1, 0.2, and 0.3 g, the release rates were 100, 81.8, and 59.6%, respectively; when the pH values of the drug release medium were 1.0, 3.8, 5.4, and 7.4, the release rates reached 100, 100, 37.9, and 7.8%, respectively; the cumulative release rates of BSA were 78.4, 82.3, 84.3, and 91.7% when the ionic strengths of the release solution were, respectively, 0.1, 0.2, 0.3, and 0.4M; when the crosslinking times of these drug films in the TPP solution were 0, 5, 15, 30, and 60 min, the release rates attained 100, 100, 81.8, 65, and 43.3%, respectively. All the results indicated that the CS/PVA film was useful in drug delivery systems. © 2005 Wiley Periodicals, Inc. J Appl Polym Sci 96: 808–813, 2005  相似文献   

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