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1.
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   

2.
The objective of the present work was to study the release behavior of plain and blend microspheres (MS) of PLGA and Pluronic F68/127. In this study, a novel blend MS of poly(D ,L ‐lactic‐co‐glycolic acid) (PLGA) and Pluronic F68/127 (PLF68/127) were prepared by the emulsion–solvent evaporation method. Repaglinide, an antidiabetic drug with a very short half‐life, was successfully encapsulated into the blend MS. Various formulations were prepared by varying the ratio of PLGA and PLF68/127. Drug encapsulation up to 91% was achieved as measured by UV spectroscopy. Scanning electron microscopy showed that MS have smooth surfaces even after incorporation of PLF68/127. Particle size, as measured by using laser light scattering technique, gave an average size ranging from 12 to 47 μm. Differential scanning calorimetry (DSC) was performed to understand the crystalline nature of the drug after encapsulation into MS. DSC revealed the crystalline dispersion in the polymer matrix. In vitro release experiments performed in simulated intestinal fluid, indicated the dependence of release rate on the amount of PLF68/127 present in the MS; slow release was extended up to 153 h. Release data have been fitted to an empirical equation to compute the diffusional exponent (n), which indicated that the release mechanism to be non‐Fickian type. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2010  相似文献   

3.
5‐Fluorouracil (5‐Fu) loaded poly(glycolide‐co‐lactide‐co‐caprolactone) (PGLC) nanoparticles were prepared by modified spontaneous emulsification solvent diffusion method (modified‐SESD method) and characterized by dynamic light scattering, scanning electron microscopy and 1H NMR determination. It was found that the obtained nanoparticles showed near spherical shape and was controllable with the radius range of 30–100 nm. Compared with the nanoparticles prepared by polylactide and poly (lactide‐co‐glycolide) (PLGA) under the similar preparation condition, yield of PGLC nanoparticles was the highest, which reached to about 100%. On the other hand, drug entrapment efficiency of PGLC nanoparticles was also higher than that of PLGA and PLLA nanoparticles. 5‐Fu release behavior of PGLC nanoparticles in vitro showed that 5‐Fu release of PGLC nanoparticles showed a near zero‐order release profile, and 5‐Fu release rate of PGLC nanoparticles was faster than that of PLLA and PLGA nanoparticles. According to degradation behavior of PGLC nanoparticles, it could be proposed that the kinetic of degradation controlled release played an important role in the release process of PGLC nanoparticles. It revealed that the PGLC nanoparticles could be a promising drug carrier. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2007  相似文献   

4.
Poly(hydroxybutyrate‐co‐hydroxyvalerate) (PHBV) was electrospun into ultrafine fibrous nonwoven mats. Different from the conventional electrospinning process, which involves a positively charged conductive needle and a grounded fiber collector (i.e., positive voltage (PV) electrospinning), pseudo‐negative voltage (NV) electrospinning, which adopted a setup such that the needle was grounded and the fiber collector was positively charged, was investigated for making ultrafine PHBV fibers. For pseudo‐NV electrospinning, the effects of various electrospinning parameters on fiber morphology and diameter were assessed systematically. The average diameters of PHBV fibers electrospun via pseudo‐NVs were compared with those of PHBV fibers electrospun via PVs. With either PV electrospinning or pseudo‐NV electrospinning, the average diameters of electrospun fibers ranged between 500 nm and 4 μm, and they could be controlled by varying the electrospinning parameters. The scientific significance and technological implication of fiber formation by PV electrospinning and pseudo‐NV electrospinning in the field of tissue engineering were discussed. POLYM. ENG. SCI., 2011. © 2011 Society of Plastics Engineers  相似文献   

5.
Electrospinning is a direct, continuous, and useful technique to prepare nanofiber by applying electrostatic forces. In this study, poly(lactic‐co‐glycolic acid)/poly(ethylene glycol) (PLGA/PEG) nanofiber mats were prepared, and electrospinning process was optimized to obtain appropriate fiber diameter and hydrophilicity for anti‐adhesion application. Optimization of applied voltage, PEG content, and feeding rate was investigated using response surface methodology. A total of 15 trials were designed to optimize the parameters. Fiber diameter was measured using scanning electron microscopy. Individual and interactive effects of the solution properties were determined. Moreover, the adequacy of the models was verified by validation experiments. For anti‐adhesion test, a nanofiber mat was produced based on the suggested optimum electrospinning conditions. Results showed that optimum fiber diameters were obtained using 7.5% PEG content, applied voltage of 19 kV, and flow rate of 3 mL/h. Experimental results were in good agreement with the predicted fiber diameters. Furthermore, a rat model of sidewall defect‐cecum abrasion was employed to investigate the efficacy of PEG/PLGA in preventing postoperative peritoneal adhesions. Hence, this study provides an overview on the fabrication of PLGA/PEG nanofibers with targeted diameter, which may be used in anti‐adhesion. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018 , 135, 46282.  相似文献   

6.
Temperature‐responsive polymers have become increasingly attractive as carrier for the injectable drug delivery systems. In the present work, we have studied the preparation of poly(N‐isopropylacrylamide‐acrylamide‐vinilpyrrolidone) (NIPAAm‐AAm‐VP terpolymer) nanoparticulated terpolymer and its blend with poly(lactide‐co‐glycolide, PLGA; molar ratio of lactide/glycolid 1/3). Thermosensitive terpolymer, poly(NIPAAm‐AAm‐VP) was prepared by free‐radical polymerization in aqueous solution. The nanoparticles of poly(NIPAAm‐AAm‐VP) and its blend with PLGA containing naltrexone were prepared using the evaporation and w/o emulsion‐solvent evaporation methods, respectively. Nanoparticles prepared from terpolymer‐PLGA blend at low polymer concentration (5%) shows larger particle size (>300 nm) and higher drug content%. Various types of nanoparticles showed a burst release of less than 10% after 24 h . The results suggest that by regulating different variables, desired release profiles of naltrexone can be achieved using a blend of PLGA‐poly(NIPAAm‐AAm‐VP) nanoparticulate system. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2009  相似文献   

7.
Poly(2‐hydroxyethyl methacrylate)‐co‐polylactide (PHEMA‐co‐PLA) and its corresponding cyhalothrin‐loaded ultrafine particles were successfully synthesized and prepared, respectively. The chemical structures of the copolymers have been confirmed by Fourier transform infrared spectroscopy (FTIR), 1H‐nuclear magnetic resonance (1H‐NMR), 13C‐nuclear magnetic resonance (13C‐NMR), and thermogravimetric analysis (TGA). Furthermore, the particle size, the cyhalothrin loading content (LC), and the cyhalothrin release behavior were investigated. PHEMA‐co‐PLA proved to be a good material for the preparation of ultrafine particles for lipophilic pesticide delivery. The developed cyhalothrin‐loaded PHEMA‐co‐PLA ultrafine particles showed good dispersity in water and sustained release behavior. In addition, it is easy to be prepared by both nanoprecipitation method and emulsion/solvent evaporation method. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2013  相似文献   

8.
Ultrafine fibrous webs of poly(lactide‐co‐glycolic acid) (PLGA) containing the bactericidal antibiotic drug rifampin were prepared by electrospinning, and their properties were investigated for wound‐dressing applications. Because PLGA is a biodegradable and biocompatible polymer, it is one of the best materials for the preparation of wound‐dressing substrates. Through this investigation of PLGA/rifampin electrospun webs, we found that the in vitro degradation reached approximately 60% in 10 days, and the drug release from the webs showed a fast and constant profile suitable for wound‐dressing applications. Also, we observed that both the web‐degradation rate and the drug‐release rate increased as the drug concentration in the PLGA/rifampin electrospun webs and the content level of glycolide units in the PLGA polymer matrix increased. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012  相似文献   

9.
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   

10.
Surfactant‐free nanoparticles of poly(DL ‐lactide‐co‐glycolide) (PLGA) nanoparticles were prepared with or without poly(L ‐lactide)‐poly(ethylene oxide) (LE) diblock copolymer (abbreviated as PLGA/LE and PLGA nanoparticles) by dialysis method. LE diblock copolymer was used to make PLGA nanoparticles to alternate conventional surfactant. The size of PLGA and PLGA/LE nanoparticles was 295.3 ± 171.3 and 307.6 ± 27.2 nm, respectively, suggesting LE diblock copolymer might be coated onto the surface of nanoparticles. Observation of scanning electron microscope (SEM) showed that PLGA/LE nanoparticles have spherical shapes ranging ~ 200–500 nm. In 1H‐NMR study, characteristic peaks of the methyl protons of PLGA disappeared in D2O, whereas characteristic peaks of the methyl proton of both PEG and PLGA were shown in both CDCl3 and D2O, indicating that LE diblock copolymer coated on the surface of the PLGA nanoparticles. The higher the initial content of drug, the higher the drug contents and the lower the loading efficiency. PLGA/LE nanoparticles at higher drug contents resulted in slower adriamycin·HCl (ADR) release rate than that of lower drug contents. Also, slower release rate of ADR was achieved by entrapped into the PLGA/LE nanoparticles, whereas LE polymeric micelles showed rapid ADR release. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 89: 1116–1123, 2003  相似文献   

11.
Poly(N‐vinylpyrrolidone) (PVP) groups were grafted onto poly(3‐hydroxybutyrate‐co‐3‐hydroxyvalerate) (PHBV) backbone to modify the properties of PHBV and synthesize a new novel biocompatible graft copolymer. Based on these graft copolymers, electrospun fiber mats and commonly cast films were explored as drug delivery vehicles using tetracycline hydrochloride as a model drug. Toward that end, the fibers were electrospun and the films were cast from chloroform solutions containing a small amount of methanol to solubilize the drug. The Brookfield viscosities of the solution were determined to achieve the optimal electrospinning conditions. The vitro release of the tetracycline hydrochloride from these new drug delivery systems was followed by UV–vis spectroscopy. To probe into the factors affected on the release behavior of these drug delivery systems, their water absorbing abilities in phosphate buffer solution were investigated, together with their surface hydrophilicity, porosity and crystallization properties were characterized by water contact angles, capillary flow porometer, DSC, and WAXD, respectively. The morphological changes of these drug delivery vehicles before and after release were also observed with SEM. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012  相似文献   

12.
Ultrafine hexanitrohexaazaisowurtzitane (CL‐20) samples were prepared by a ultrasound‐ and spray‐assisted precipitation method. Raw CL‐20 and ultrafine CL‐20 samples were characterized by SEM, FT‐IR spectroscopy, XRD, and particle size analysis. The impact sensitivity and thermal stability of two CL‐20 samples were also tested and compared. The results indicate that by this recrystallization process, the mean particle size of CL‐20 is 470 nm, and the particle size distribution was in the range from 400–700 nm. The particle morphology is nearly spheric with a smooth surface. Compared with raw CL‐20, the impact sensitivity of the ultrafine sample is significantely reduced and the drop height (H50) is increased from 12.8 to 37.9 cm. The critical explosion temperature of ultrafine CL‐20 decreased from 235.6 to 229.0 °C, which suggests that the thermal stability of ultrafine CL‐20 is lower than that of raw CL‐20.  相似文献   

13.
This article explores the application of spray drying technique to produce microparticles of poly(D ,L ‐lactide‐co‐glycolic acid) (PLGA), as well as di‐block copolymer of polylactic acid (PLA) and polyethylene glycol (PEG) (PLA‐PEG), containing zidovudine (AZT), an anti‐HIV drug, to achieve its controlled release over an extended period of time. Of the two polymers studied, PLGA is hydrophobic, whereas PLA‐PEG is hydrophilic and the drug, AZT is water‐soluble. Formulations were developed containing 10 and 25 wt % of AZT giving encapsulation efficiencies (EE) of 66 to 86% for PLGA and 90 to 94% for PLA‐PEG di‐block copolymer. All the formulations were characterized by Fourier transform spectroscopy (FTIR) to investigate the interaction of AZT with polymers and to characterize PLA‐PEG. NMR was also employed to confirm the formation of PLA‐PEG. X‐ray diffraction was used to understand the molecular level dispersion of AZT within the polymeric matrices, while differential scanning calorimetry was employed to assess thermal properties. Scanning electron microscopy was employed to understand the surface morphology of AZT‐loaded microparticles. In vitro release experiments performed in pH 7.4 buffer media extended the release of AZT up to 125 h with PLGA, whereas 30 h were required for releasing AZT through PLA‐PEG microparticles. Cumulative release data were fitted to an empirical equation to understand the nature of release characteristics. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci 000: 000–000, 2011  相似文献   

14.
Sea‐island polyurethane (PU)/polycarbonate (PC) composite nanofibers were obtained through electrospinning of partially miscible PU and PC in 3 : 7 (v/v) N,N‐dimethylformamide (DMF) and tetrahydrofuran (THF) mixture solvent. Their structures, mechanical, and thermal properties were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared (FTIR) spectroscopy, thermogravimetric (TG), and differential scanning calorimetry (DSC). The structures and morphologies of the nanofibers were influenced by composition ratio in the binary mixtures. The pure PC nanofiber was brittle and easy to break. With increasing the PU content in the PU/PC composite nanofibers, PU component not only facilitated the electrospinning of PC but improved the mechanical properties of PU/PC nanofibrous mats. In a series of nanofibrous mats with varied PU/PC composition ratios, PU/PC 70/30 showed excellent tensile strength of 9.60 Mpa and Young's modulus of 55 Mpa. After selective removal of PC component in PU/PC composite nanofibers by washing with acetone, the residual PU maintained fiber morphology. However, the residual PU nanofiber became irregular and contained elongated indents and ridges along the fiber surface. PU/PC composite fibers showed sea‐island nanofiber structure due to phase separation in the spinning solution and in the course of electrospinning. At PC content below 30%, the PC domains were small and evenly dispersed in the composite nanofibers. As PC content was over 50%, the PC phases became large elongated aggregates dispersed in the composite nanofibers. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2010  相似文献   

15.
Electrospinning is a facile method for preparing nanocomposite materials in fiber form. Nanomaterials that have been incorporated within such fibers are usually inorganic in nature. Recently, nanocomposite nanofibers based on poly(vinyl alcohol) (PVA) as the matrix and nanocrystals of α‐chitin (i.e. chitin whiskers; ca 31 nm in width and ca 549 nm in length on average) as the nanofiller have been successfully prepared. In the study reported here, the fibers were further investigated using X‐ray diffraction (XRD) and dynamic mechanical analyses in comparison with the corresponding solvent‐cast films. The average diameters of the PVA/chitin whiskers fibers ranged between 175 and 218 nm. Careful analysis of the wide‐angle XRD patterns of the fiber mats and the films showed that PVA was partially crystalline, and the incorporation of the whiskers within the fibers was confirmed by peaks characteristic to α‐chitin crystals. Dynamic mechanical analysis showed that the fiber mats were weaker than the films and that the relaxation temperatures associated with the glass transition (Tg) of the fiber mats were greater than those of the films. The addition and increasing the amount of the whiskers caused the crystallinity of PVA within the nanocomposite materials to decrease and Tg to increase. The present study shows that the geometry of nanocomposite materials plays a major role in determining their properties. Copyright © 2009 Society of Chemical Industry  相似文献   

16.
BACKGROUND: Vitamin B12 is an essential vitamin required by all mammals. Absorption of vitamin B12 is facilitated by binding of intrinsic factor–vitamin B12 complex to specific receptors in the ileum. In humans a deficiency of this vitamin or a lack of intrinsic factor leads to pernicious anaemia. The major objective of the present study was to prepare intrinsic factor–vitamin B12 complex‐loaded poly[lactic‐co‐(glycolic acid)] (PLGA)‐based microparticles and to investigate their release kinetics. RESULTS: PLGA copolymer was synthesized by the ring‐opening polymerization method and characterized using gel permeation chromatography, Fourier transform infrared spectroscopy and 1H NMR. The glass transition temperature measurement showed a single Tg at 40 °C. The intrinsic factor–vitamin B12 complex‐loaded PLGA microspheres were prepared by a water‐in‐oil‐in‐water double emulsion solvent extraction/evaporation technique. An environmental scanning electron microscopy investigation demonstrated that the PLGA particles had a mean particle diameter of 38 µm. Interestingly, different drug release patterns (bi‐ and triphasic ones) were observed for vitamin B12‐loaded and intrinsic factor–vitamin B12 complex‐loaded microspheres. In contrast to the rapid release of vitamin B12 by itself, in vitro release tests showed that intrinsic factor and vitamin B12 in the complex were released from PLGA microspheres in a sustained manner over 15 days. CONCLUSION: PLGA microspheres can be an effective carrier for the intrinsic factor–vitamin B12 complex. Copyright © 2007 Society of Chemical Industry  相似文献   

17.
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   

18.
A two‐step direct melt copolymerization process of l ‐lactic acid (L ‐LA)/glycolic acid (GA) was developed: poly(l ‐lactic acid) (PLLA) and poly(glycolic acid) (PGA) with different molecular weight was first synthesized respectively by binary catalyst (tin chloride/p‐toluenesulfonic or tin chloride); and then poly(l ‐lactic‐co‐glycolic acid) (b‐PLGA) was produced by melt polymerization of the as‐prepared PLLA and PGA, wherein the composition and chain structure of b‐PLGA copolymers could be controlled by the molecular weight of PLLA. The chain structure and thermal properties of copolymers were studied by Wide‐angle X‐ray diffraction, nuclear magnetic resonance, differential scanning calorimetry, and thermogravimetric analysis. In comparison with the random PLGA (r‐PLGA) synthesized by one‐step direct melt polymerization, the average l ‐lactic blocks length (LLA) in b‐PLGA was longer while the average glycolic blocks length (LGA) in b‐PLGA was shorter which further resulted in the improved crystallinity and thermostability. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 41566.  相似文献   

19.
To improve the efficacy of salmon calcitonin (SCT) on disuse osteoporosis‐induced bone fracture, the sustained‐release vehicles delivered to bone fractures should be developed. In this study, SCT‐loaded poly(d ,l ‐lactic‐co‐glycolic acid) microspheres (SCT‐PLGA MS) with 20 kDa‐COOH and 40 kDa‐COOH (SCT‐PLGA‐20 COOH MS and SCT‐PLGA‐40 COOH MS) are incorporated into calcium phosphate cement (CPC) at various mass ratios. The cumulative release and mechanical properties of SCT‐PLGA MS/CPC composites decrease as PLGA MS/CPC mass ratio increase. Scanning electron microscopy images and the mass loss of composites indicate the MS from 20% SCT‐PLGA MS/CPC composites have mostly degraded after 8 weeks. In addition, SCT released from the 20% SCT‐PLGA‐20 MS/CPC composites significantly facilitate proliferation and differentiation of MC3T3‐E1 cells. In conclusion, 20% SCT‐PLGA‐20 COOH MS/CPC composites exhibit the sustained drug release, proper CPC degradation, good mechanical properties, and preferable osteoblast proliferation, which would be beneficial to their in vivo applications. © 2017 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2017 , 134, 45486.  相似文献   

20.
Chemical and thermal characterization of poly(d ,l ‐lactide‐co‐glycolide) (PLGA) composites filled with hydroxyapatite (HA) or carbon nanotubes (CNT) were evaluated by infrared spectroscopy, differential scanning calorimetry, thermogravimetry, and dynamic–mechanical–thermal analysis. The morphology and distribution of the nanoparticles were studied by transmission electron microscopy. The composites were prepared by solvent casting using 30% HA or 1, 3, and 5% of pristine and functionalized CNT as nanoparticles and PLGA 75:25 and PLGA 50:50 as copolymer matrix. The Coats–Redfern and E2 function methodologies were used to calculate the reaction order and the activation energy (Ea) of the thermal degradation process. It was found that the addition of nanoparticles increased the glass transition temperature (Tg) of the composites. Also, higher degradation temperatures and Ea values were obtained for PLGA–HA composites and compared with the neat copolymer, and the opposite behavior was exhibited by PLGA–CNT composites. The thermal and mechanical properties were highly dependent on the morphology and dispersion of the filler. The functionalization process of CNT promoted, to some extent, a better distribution and dispersion of CNT into the matrix, and these composites exhibited a slight enhancement on storage modulus. On the other hand, PLGA–HA composites showed a good dispersion but no improvement on the storage modulus below Tg. POLYM. ENG. SCI., 2013. © 2012 Society of Plastics Engineers  相似文献   

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