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1.
The present paper reports the preparation and characterization of composite hydroxypropyl methylcellulose/polyacrylonitrile (HPMC/PAN)-medicated fibers via a wet spinning technique. Tamoxifen (TAM) was selected as a model drug. Numerous analyses were conducted to characterize the mechanical, structure and morphology properties of the composite fibers. The drug content and in vitro dissolution behavior were also investigated. SEM images showed that the TAM-loaded HPMC/PAN composite fibers had a finger-like outer skin and a porous structure. FT-IR spectra demonstrated that there was a good compatibility between polymer and drug. Results from X-ray diffraction and DSC suggested that most of the incorporated TAM was evenly distributed in the fiber matrix in an amorphous state, except for a minority that aggregated on the surface of fibers. The drug content in the fibers was lower than that in the spinning solution and about 10% of TAM was lost during spinning process. In vitro dissolution results indicated that, compared to TAM-PAN fibers, HPMC/PAN composite systems had weaker initial burst release effects and more drug-loading. The combination of hydrophilic polymer HPMC with PAN could improve the performance of polymer matrix composite fibers in regulating the drug-release profiles.  相似文献   

2.
Nanoparticles of a poorly water-soluble anti-malarial drug, artemisinin (ART), and its composite particles with a hydrophilic polymer, polyvinylpyrrolidone (PVP), were synthesized using a nanofabrication method called the evaporative precipitation of nanosuspension (EPN). ART nanoparticles and ART/PVP composite particles containing ART nanoparticles coated with PVP were successfully prepared with the aim of improving the dissolution rate of ART. The effect of polymer concentration on the physical and morphological properties, and dissolution rate of the EPN-prepared ART/PVP composite particles was investigated. The crystallinity of ART nanoparticles decreased with increasing polymer concentration, as suggested by the differential scanning calorimetry and X-ray diffraction studies. The phase solubility studies revealed an AL-type of curve, indicating a linear increase in the drug solubility with PVP concentration. The dissolution of the ART nanoparticles and ART/PVP composite particles markedly increased as compared to that of the original ART powder due to lower particle size and reduced crystallinity of the drug particles. The percent dissolution efficiency (DE), relative dissolution (RD), t 75% and similarity factor (f 2) were calculated for the statistical analysis. Various mathematical models, viz., zero-order, first-order, Korsemeyer–Peppas and Higuchi, were applied to fit the experimental drug-dissolution data and diffusion was found to be the drug release mechanism.  相似文献   

3.
The main aim of this study was to inhibit the re-crystallization of a potent antimalarial drug, artemisinin (ART), by encapsulating it in core-shell fibers via a coaxially electrospun method. The ART-infiltrated cellulose acetate (CA) solution as the core material and poly(vinyl pyrrolidone) (PVP) solution as the shell material were used to prepared ART-loaded core-shell fibers ([ART/CA]/PVP). Transmission electron microscopy images confirmed the core-shell structures of the coaxially electrospun fibers. The scanning electron microscope (SEM), X-ray diffraction, and differential scanning calorimetry were performed to characterize the physical states of ART in the fibers. It was observed that ART crystals were formed in the ART-loaded CA/PVP composite fibers (ART/CA/PVP) during the electrospinning process and increased during storage duration. While ART crystals hardly were observed in the fresh core-shell [ART/CA]/PVP fibers with high ART entrapped amount (20?wt.%) and a little was detected after 6-month storage. Fourier transform infrared spectroscopy (FTIR) results illustrated the hydrogen bonding interaction between ART and CA in the core-shell [ART/CA]/PVP fibers mainly contributed to the amorphous state of ART. Importantly, combination of the hydrophilic PVP shell and the amorphous ART in CA core, the core-shell [ART/CA]/PVP fibers provided a continued and stable ART release manner. Ex vivo permeation studies suggested the amorphous ART in the medicated core-shell fibers could permeate through the stratum corneum smoothly. Hence, the core-shell [ART/CA]/PVP fiber matrix could provide a potential application in transdermal patches.  相似文献   

4.
The present paper reports the preparation and characterization of composite hydroxypropyl methylcellulose/polyacrylonitrile (HPMC/PAN)-medicated fibers via a wet spinning technique. Tamoxifen (TAM) was selected as a model drug. Numerous analyses were conducted to characterize the mechanical, structure and morphology properties of the composite fibers. The drug content and in vitro dissolution behavior were also investigated. SEM images showed that the TAM-loaded HPMC/PAN composite fibers had a finger-like outer skin and a porous structure. FT-IR spectra demonstrated that there was a good compatibility between polymer and drug. Results from X-ray diffraction and DSC suggested that most of the incorporated TAM was evenly distributed in the fiber matrix in an amorphous state, except for a minority that aggregated on the surface of fibers. The drug content in the fibers was lower than that in the spinning solution and about 10% of TAM was lost during spinning process. In vitro dissolution results indicated that, compared to TAM–PAN fibers, HPMC/PAN composite systems had weaker initial burst release effects and more drug-loading. The combination of hydrophilic polymer HPMC with PAN could improve the performance of polymer matrix composite fibers in regulating the drug-release profiles.  相似文献   

5.
Coaxial electrospinning is a new technique to fabricate continuous composite ultrafine fibers with core/shell structure, which has a broad application perspective in the biomedical field. In this study, ultrafine fibrous membranes of core/shell poly(vinyl pyrrolidone)/poly(L-lactide-co-ε-caprolactone) (PVP/PLCL) were produced by coaxial electrospinning and the structural morphology of the obtained ultrafine fibers was observed by scanning electron microscopy and transmission electron microscopy. Electrospun PLCL and chitosan membranes were also prepared by traditional electrospinning as controls. The electrospun PVP/PLCL membranes showed the largest water absorption (501.3%) in phosphate buffer solution due to introduction of the PVP component and the core/shell fiber structure. Results of tensile tests indicated that the electrospun PVP/PLCL membranes possessed higher tensile strength and elongation-at-break, and lower Young's modulus than those of PLCL and chitosan membranes in both dry and wet states. Studies on cell adhesion, viability and morphology on the fibrous membranes showed that PVP/PLCL membranes could mimic the structure of natural extracellular matrices and positively promote cell–cell and cell–matrix interactions because of hydrophilicity/hydrophobicity balance.  相似文献   

6.
Tissue engineering of skeletal muscle using polymer fiber arrays   总被引:5,自引:0,他引:5  
The purpose of this study was to assess a new scaffold design for muscle tissue engineering: arrays of parallel-oriented polymer microfibers. First, C2C12 skeletal myoblasts were seeded onto single, laminin-coated polypropylene fibers and their growth and alignment were characterized. With the aim of creating skeletal muscle sheets, it was then investigated whether cell layers of single fibers merged when in close proximity to neighboring fibers. The optimal fiber spacing needed to achieve cell alignment with the lowest possible content of scaffold material was established. Further, it was assessed whether such a cell sheet became contractile and whether it survived in vitro for extended periods of time. C2C12 cells, cultured on fibers 10 to 15 microm in diameter, formed up to 50-microm-thick layers of longitudinally aligned cells. Four different groups based on fiber spacing (30 to 35, 50 to 55, 70 to 75, and 90 to 95 microm) were evaluated. Complete cell sheets formed between fibers that were spaced 55 microm apart or less; larger spacing led to no or incomplete sheets. C2C12 cells, seeded onto a 10 x 20 mm fiber array, formed a contractile cell sheet that was maintained in vitro for 70 days. Larger, three-dimensional structures might be created by arranging fibers in several layers or by stacking cellular sheets.  相似文献   

7.
The release behavior of poorly soluble drugs (naproxen and ketoprofen) from inert (acrylic resins) and hydrophilic swellable (high-viscosity hydroxypropylmethylcellulose) tableted matrices containing betacyclodextrin (betaCD) was investigated. The results demonstrated that, in both cases, betaCD can enhance the rate of drug release. Matrices obtained from formulations in which lactose replaced betaCD were also evaluated. BetaCD in inert matrices causes a dramatic increase in the rate of drug release, higher than that promoted by lactose which merely acts as a channelling agent. This result suggests that possible in situ formation of the drug-betaCD complex. which causes an improvement in apparent drug solubility, could have a greater influence on the rate of drug release than the possible increase of water uptake by a soluble filler. Indeed, if the opposite were true, lactose would be more effective in increasing the rate of drug release than betaCD, because of its greater solubility in water. On the contrary, in the case of hydrophilic matrices, lactose proves to be much more effective in promoting drug release than betaCD. It seems that, while the bulky interaction compound can freely diffuse through water-filled pores of inert systems, its diffusion through swollen macromolecular chains of hydrophilic matrices may be hindered. This hypothesis was supported by data obtained from binary (drug/polymer) and ternary (drug/polymer/betaCD) hydrophilic matrices using a betaCD-containing dissolution media.  相似文献   

8.
Fabrication of aligned microfiber scaffolds is critical in successful engineering of anisotropic tissues such as tendon, ligaments and nerves. Conventionally, aligned microfiber scaffolds are two dimensional and predominantly fabricated by electrospinning which is solvent dependent. In this paper, we report a novel technique, named microfiber melt drawing, to fabricate a bundle of three dimensionally aligned polycaprolactone microfibers without using any organic solvent. This technique is simple yet effective. It has been demonstrated that polycaprolactone microfibers of 10?μm fiber diameter can be directly drawn from a 2?mm orifice. Orifice diameter, temperature and take-up speed significantly influence the final linear density and fiber diameter of the microfibers. Mechanical test suggests that mechanical properties such as stiffness and breaking force of microfiber bundles can be easily adjusted by the number of fibers. In vitro study shows that these microfibers are able to support the proliferation of human dermal fibroblasts over 7?days. In vivo result of Achilles tendon repair in a rabbit model shows that the microfibers were highly infiltrated by tendon tissue as early as in 1?month, besides, the repaired tendon have a well-aligned tissue structure under the guidance of aligned microfibers. However whether these three dimensionally aligned microfibers can induce three dimensionally aligned cells remains inconclusive.  相似文献   

9.
The strength and stability of hybrid fiber delivery systems, ones that perform a mechanical function and simultaneously deliver drug, are critical in the design of surgically implantable constructs. We report the fabrication of drug-eluting microfibers where drug loading and processing conditions alone increase microfiber strength and stability partially due to solvent-induced crystallization. Poly(L-lactic acid) microfibers of 64±7 μm diameter were wet spun by phase inversion. Encapsulation of a model hydrophobic anti-inflammatory drug, dexamethasone, at high loading provided stability to microfibers which maintained linear cumulative release kinetics up to 8 weeks in vitro. In our wet spinning process, all microfibers had increased crystallinity (13-17%) in comparison to unprocessed polymer without any mechanical stretching. Moreover, microfibers with the highest drug loading retained 97% of initial tensile strength and were statistically stronger than all other microfiber formulations, including control fibers without drug. Results indicate that the encapsulation of small hydrophobic molecules (<400 Da) may increase the mechanical integrity of microfilaments whose crystallinity is also increased as a result of the process. Multifunctional drug-eluting microfibers can provide an exciting new opportunity to design novel biomaterials with mechanical stability and controlled release of a variety of therapeutics with micron-scale accuracy.  相似文献   

10.
There is a need for better wound dressings that possess the requisite angiogenic capacity for rapid in situ healing of full-thickness skin wounds. Borate bioactive glass microfibers are showing a remarkable ability to heal soft tissue wounds but little is known about the process and mechanisms of healing. In the present study, wound dressings composed of borate bioactive glass microfibers (diameter = 0.4–1.2 μm; composition 6Na2O, 8K2O, 8MgO, 22CaO, 54B2O3, 2P2O5; mol%) doped with 0–3.0 wt.% CuO were created and evaluated in vitro and in vivo. When immersed in simulated body fluid, the fibers degraded and converted to hydroxyapatite within ∼7 days, releasing ions such as Ca, B and Cu into the medium. In vitro cell culture showed that the ionic dissolution product of the fibers was not toxic to human umbilical vein endothelial cells (HUVECs) and fibroblasts, promoted HUVEC migration, tubule formation and secretion of vascular endothelial growth factor (VEGF), and stimulated the expression of angiogenic-related genes of the fibroblasts. When used to treat full-thickness skin defects in rodents, the Cu-doped fibers (3.0 wt.% CuO) showed a significantly better capacity to stimulate angiogenesis than the undoped fibers and the untreated defects (control) at 7 and 14 days post-surgery. The defects treated with the Cu-doped and undoped fibers showed improved collagen deposition, maturity and orientation when compared to the untreated defects, the improvement shown by the Cu-doped fibers was not markedly better than the undoped fibers at 14 days post-surgery. These results indicate that the Cu-doped borate glass microfibers have a promising capacity to stimulate angiogenesis and heal full-thickness skin defects. They also provide valuable data for understanding the role of the microfibers in healing soft tissue wounds.  相似文献   

11.
Drug release and its relationship with kinetic and thermodynamic parameters of drug sorption onto poly(lactic acid) (PLA) fibers have been studied using Diclofenac, 5-Fluorouracil (5-FU) and Metformin as model drugs. The sorption method is more flexible and avoids the damaged drugs, remaining toxic organic solvents and safety problems which occurred with the dissolution method. The quantitative relationship with high correlation between drug-release and drug-loading concentration, affinity and activation energy for diffusion has been established to predict the initial burst and subsequent release of the drugs. Drugs with higher activation energy for diffusion, lower diffusion coefficients and higher affinity on PLA fiber, such as Diclofenac, can achieve high loading capacity and constant drug release. It has also been found that elevated temperatures can achieve high loading capacity and constant release. In addition, the study showed that Diclofenac release profiles were similar for sorption and dissolution loading methods.  相似文献   

12.
This article describes an electrospinning process to fabricate double-layered ultrafine fibers. A bioabsorbable polymer, Polycaprolactone (PCL), was used as the outer layer or the shell and two medically pure drugs, Resveratrol (RT, a kind of antioxidant) and Gentamycin Sulfate (GS, an antibiotic), were used as the inner layers or the cores. Morphology and microstructure of the ultrafine fibers were characterized by scanning electron microscope (SEM) and transmission electron microscopy (TEM), whereas mechanical performance of them was understood through tensile test. In vitro degradation rates of the nanofibrous membranes were determined by measuring their weight loss when immersed in pH 7.4 phosphate-buffered saline (PBS) mixed with certain amount of Pseudomonas lipase for a maximum of 7 days. The drug release behaviors of the RT and GS were measured using a high performance liquid chromatography (HPLC) and ultraviolet-visible (UV-vis) spectroscopy, respectively. It has been found that the drug solutions without any fiber-forming additive could be encapsulated in the PCL ultrafine fibers, although they alone cannot be made into a fiber form. Beads on the fiber surface influenced the tensile behavior of the ultrafine fibers remarkably. When the core solvent was miscible with the shell solvent, higher drug concentration decreased the bead formation and thus favored the mechanical performance. The situation, however, became different if the two solvents were immiscible with each other. The degradation rate was closely related to hydrophilicity of the drugs in the cores. Higher hydrophilicity apparently led to faster degradation. The release profiles of the RT and GS exhibited a sustained release characteristic, with no burst release phenomenon.  相似文献   

13.
目的 研发一种可供机体埋植的长效的氟尿嘧啶载药纤维支架.方法 有机相分离法制备纤维,扫描电镜(SEM)观察纤维形态,光学显微镜测定纤维直径,红外光谱分析(FTIR)和差示扫描热分析(DSC)鉴定药物载体结合状态并测定纤维中PLLA的结晶度,紫外分光光度法(UV)测定纤维的载药量以及体外释放.结果 制备出微米级的载药纤维,载药量与载药效率均较高;药物与聚乳酸属于简单物理混合;相对应两种结构模式载药纤维呈现两种释放模式.结论 b型结构纤维适合于开发成长效的在位埋植载药纤维支架.  相似文献   

14.
Novel antibiotic-eluting composite fibers designed for use as basic wound dressing elements were developed and studied. These structures were composed of a polyglyconate core and a porous poly(dl-lactic-co-glycolic acid) shell loaded with one of three antibiotic drugs: mafenide acetate, gentamicin sulphate and ceftazidime pentahydrate. The shell was prepared by the freeze-drying of inverted emulsions. The fiber investigation focused on the effects of the emulsion’s formulation on the shell microstructure and on the resulting profile of drug release from the fibers. Albumin was found to be the most effective surfactant for stabilizing the inverted emulsions and also to have a beneficial holdup effect on the release kinetics of the hydrophilic antibiotic drugs, especially mafenide acetate, probably through a specific interaction. An increase in the organic:aqueous phase ratio, polymer content or molecular weight of the host polymer resulted in a decrease in the burst release and a more moderate release profile due to changes in shell microstructure. The first two parameters were found to be more effective than the third. The diverse release profiles obtained in the current study and the good mechanical properties indicate that our new composite fibers have good potential for use in wound healing applications.  相似文献   

15.
Cao X  Fu M  Wang L  Liu H  Deng W  Qu R  Su W  Wei Y  Xu X  Yu J 《Acta biomaterialia》2012,8(6):2104-2112
The purpose of this study was to develop porous silica nanoparticles (PSNs) as a carrier to improve oral bioavailability of poorly water-soluble drugs, using silymarin as a model. PSNs were synthesized by reverse microemulsion and ultrasonic corrosion methods. A 3-day release formulation consisting of a silymarin solid dispersion, a hydrophilic gel matrix and silymarin-loaded PSNs was prepared. In vitro release studies indicated that both the silymarin-loaded PSNs and the 3-day release formulation showed a typical sustained-release pattern over a long period, about 72 h. The in vivo studies revealed that the 3-day release formulation gave a significantly higher plasma concentration and larger area under the concentration-time curves than commercial tablets when orally administered to beagle dogs. This implies that the prepared 3-day release formulation significantly enhanced the oral bioavailability of silymarin, suggesting that PSNs can be used as promising drug carriers for oral sustained release systems. Thus providing a technically feasible approach for improving the oral bioavailability and long-term efficacy of poorly soluble drugs.  相似文献   

16.
On the basis of the bioactivity of hydroxyapatite (HA) and the excellent mechanical and biocompatible performance of polyethylene terephthalate (PET), composite microfibers made of nanograde HA with PET was designed and fabricated to mimic the structure of biological bone, which exhibits a composite of nanograde apatite crystals and natural polymer. The PET/HA nanocomposite was molded into fibers so that the bulk structures' mechanical properties can be custom tailored by changing the final 3D orientation of the fibbers. This study focused on the in vitro biocompatibility evaluation of the PET/HA composite fibers as potential bone fixation biomaterial for total hip replacement prosthesis surfaces. The MTT assay was performed with the extracts of the composite fibers in order to evaluate the short-term effects of the degradation products. The cell morphology of L929 mouse fibroblast cell line was analyzed after direct contact with the fiber scaffolds for different time periods, and the cell viability was also analyzed by the Alamar Blue assay. The release of the inflammatory cytokine, tumor necrosis factor-alpha (TNF-alpha), from RAW 264.7 macrophages in the presence of fiber extracts and fibers was used as a measure of the inflammatory response. The ability of the fiber matrices to support L929 attachment, spreading, and growth in vitro, combined with the compatible degradation extracts and low inflammation potential of the fibers and extracts, suggests potential use of these fibers as load-baring bone fixation biomaterial structures.  相似文献   

17.
This work describes the design and assembly of multifunctional and cost-efficient composite fiber nonwovens as semi-occlusive wound dressings using a simple electrospinning process to incorporate a variety of functional components into an ultrathin fiber. These components include non-hydrophilic poly(L-lactide) (PLLA) as fibrous backbone, hydrophilic poly(vinyl pyrrolidone)-iodine (PVP-I), TiO(2) nanoparticles, zinc chloride as antimicrobial, odor-controlling, and antiphlogistic agents, respectively. The process of synthesis starts with a multicomponent solution of PLLA, PVP, TiO(2) nanoparticles plus zinc chloride, in which TiO(2) nanoparticles are synthesized by in situ hydrolysis of TiO(2) precursors in a PVP solution for the sake of obtaining the particle-uniformly dispersive solution. Subsequent electrospinning generates the corresponding composite fibers. A further iodine vapor treatment to the composite fibers combines iodine with PVP to produce the PVP-I complexes. Experiments indicate that the assembled composite fibers (300-400 nm) possess the ointment-releasing characteristic and the phase-separate, core-sheath structures in which PVP-I residing in fiber surface layer becomes the sheath, and PLLA distributing inside the fiber acts as the core. Based on this design, the structural advantages combining active components endow the assembled composite nonwovens with a variety of functions, especially, the existence of PVP-I, endows the nonwoven with water absorbability, antimicrobial activity, adhesive ability, and transformable characteristic from hydrophilicity to non-hydrophilicity. The multifunctional, cost-efficient, and ointment-releasing characteristics make the multicomponent composite fibrous nonwovens potentially useful in applications such as initial stage of dressing of the cankerous or contaminated wounds.  相似文献   

18.
Endotoxin (ET) in the dialysate is known to be adsorbed by dialysis membranes made of polyether polymer alloy (PEPA) and polymethylmethacrylate (PMMA). In the present study, the effect of polyvinylpyrrolidone (PVP) localization of the PEPA dialysis membrane on the adsorption of ET was investigated. The compounding of PVP in the PEPA membrane was changed, and hydrophobic membrane in both blood side and dialysate side, and hydrophilic membrane in only the blood side were used. Adsorption was evaluated by filling the contaminated dialysate inside and outside the membrane after priming with physiological saline, and determining the ET concentration in the blood side and dialysate side of dialysis membrane during the 240 min period from the start of filling the contaminated dialysate. With the PEPA membranes investigated, ET was significantly adsorbed to the hydrophobic side and was not adsorbed to the blood side of hydrophilic type membrane. These results suggest that in addition to electrostatic action attributable to the compounding of hydrophilic agent PVP to the dialysis membrane, the distribution of PVP that was compounded and the potential of the membrane itself may cause differences in adsorption of ET.  相似文献   

19.
The function of a photocrosslinked poly(propylene fumarate) (PPF)/poly(N-vinyl pyrrolidone) (PVP) matrix for the sustained release of three ophthalmic model drugs, acetazolamide (AZ), dichlorphenamide (DP), and timolol maleate (TM), was investigated. The drugs differ in molecular weight and degree of dissociation in aqueous environments; both are parameters that significantly influence drug diffusivity. AZ, DP, and TM-loaded cylindrical rods (10 mm length, 0.6 mm diameter) were fabricated by photoinduced cross-copolymerization of PPF and N-vinyl pyrrolidone (NVP) in molds. The released amounts of AZ, DP, TM, and NVP were determined by high-performance liquid chromatography (HPLC). The effects of drug properties and loading on the release kinetics were investigated. The in vitro release of AZ, DP, and TM was well sustained from the polymer matrices over a period of approximately 210, 270, and 250 days, respectively. The release kinetics correlated with the HPLC retention profiles of the different drugs. Following a small initial burst release (<10%), a dual modality release controlled by diffusion and bulk erosion was found for all drugs. Drug release rates of up to 4 microg/day were reached. Matrix drug loading generally affected the extent of the burst release, release kinetics, as well as the matrix water content and matrix degradation that were determined gravimetrically. Microcomputed tomography was used to image structural and dimensional changes of the devices. A preliminary rabbit implantation study revealed promising ocular biocompatibility of drug-free PPF/PVP matrices. All results indicate the potential of photocrosslinked PPF-based matrices as polymeric carriers for long-term ophthalmic drug delivery.  相似文献   

20.
Han CC  Wang Y 《Inflammation》2012,35(4):1262-1268
The roots of Sophora flavescens was reported to possess many pharmacological activities including anti-inflammatory, antiashmatic, antithelmintic, free radical scavenging and antimicrobial activities. However, the low saturated solubility and dissolution velocity of S. flavescens lead to poor bioavailability. The S. flavescens nanoparticles (SFNP) were prepared by a combination of ultrasound and hydrolysis developed by the authors. The drug dissolution profiles of SFNP in both pH 6.8 and pH 2 media showed complete dissolution within 30 min. The seropharmacology study showed that oral S. flavescens absorption in the SFNP was significantly increased. Anti-inflammation assay revealed the therapeutic efficiency of S. flavescens significantly enhanced upon nanoparticle formation.  相似文献   

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