首页 | 官方网站   微博 | 高级检索  
相似文献
 共查询到20条相似文献,搜索用时 15 毫秒
1.
Sustained release Miglitol-loaded poly (d, l-lactide-co-glycolide) (PLGA) microparticles were prepared using high pressure homogenization-solvent evaporation method. 23 full factorial design was employed to study effect of independent variables (X1-Polymer amount; X2-Surfactant concentration and X3-Homogenization Pressure) on percent encapsulation efficiency (%EE) as response. The microparticles produced were characterized for particle size, morphology, % EE, drug polymer compatibility and in vitro drug release. An average particle size of Miglitol-loaded PLGA microparticles was 230.1?nm and found almost spherical with smooth surface. % EE ranged from 58.7%?±?2.11 to 86.5%?±?0.24 depending on the polymer amount, surfactant concentration and homogenization pressure. An absence of chemical interaction between drug-polymer and reduction in % crystallinity of drug was confirmed by FTIR and X-ray diffraction analysis respectively. In vitro release studies showed a sustained release of Miglitol from microparticles up to 12?hrs.  相似文献   

2.
Multiple unit delivery dosage forms of biodegradable gelatin microspheres containing the anticancer drug methotrexate (GMM) of various mean particle sizes (1–5, 5–10, and 15–20 μm) were prepared by the polymer dispersion technique and were crosslinked with glutaraldehyde. The GMM were coated with biodegradable natural polymers, namely alginate (AGMM) and chitosan (CGMM), which differ in their pH sensitivity, to obtain two different types of pH dependent delivery systems for oral delivery of methotrexate (MTX). The in vitro release profiles of MTX from AGMM and CGMM were determined in simulated gastric medium, intestinal medium, and in media simulating gastrointestinal tract conditions. The effect of the concentration of coating polymer and particle size on the release rate of MTX from both AGMM and CGMM were also studied. Both AGMM and CGMM provided controlled release of MTX following a zero-order release pattern in gastric and intestinal fluids for prolonged periods of time. The release rate of MTX decreased with an increase in concentration of the coating polymer as well as an increase in particle size of the microspheres. Both AGMM and CGMM showed good potential as pH dependent multiple unit delivery systems for the controlled release of MTX in oral administration. © 1995 John Wiley & Sons, Inc.  相似文献   

3.
Biodegradable carboxylated polyurethanes with three molecular weights were synthesized to prepare a nanoparticulate sustained delivery system of raloxifene hydrochloride, the drug with poor bioavailability. The nanoparticles were prepared by coprecipitation method. Optimal conditions for the preparation of nanoparticles were obtained using Box–Behnken design. Independent factors were ratio of polymer to drug, Mw of polymer and speed of magnetic stirrer. Dependent variables include zeta potential, polydispersity index (PdI), particle size, and loading efficacy (LE). Results of the fractional factorial design based on an analysis of variance demonstrated that the model for particle size, zeta potential, PdI and loading efficacy was statistically significant. The size of nanoparticles in design experiments were 46–96 nm in diameter and had entrapment efficiency of 84–92%. The nanoparticles were evaluated for in vitro release and showed a sustained release profile (24.19% ± 4.35% after 4 weeks), following the Fickian diffusion‐based release mechanism. © 2013 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 39668.  相似文献   

4.
采用快速膜乳化法制备了聚(乳酸-羟基乙酸)(PLGA)微球,得到制备PLGA微球的优化条件为:过膜压力5 kPa,水相中PVA浓度19 g/L,油/水相体积比1:10,该条件下所制空白微球的平均粒径约为24 mm,粒径分布系数Span<0.7. 在此基础上制备载生长激素释放肽-6(GHRP-6)微球,油相乳化剂浓度2.5 g/L、外水相中NaCl浓度10 g/L条件下所制载GHRP-6微球包埋率最高可达85%,初乳制备方式对药物包埋率及体外释放行为均有较大影响,超声法制备的初乳所得微球内部结构紧密,药物包埋率较高(85%),但释药缓慢;而均质法制备的初乳所得微球内部结构疏松,药物包埋率较低(76.8%),但在体外释放更完全.  相似文献   

5.
The preparation of microcapsules containing perphenazine by solvent evaporation using ethyl cellulose is described. The microparticles are formed after solvent evaporation and polymer precipitation. The drug was dissolved in a polymer solution and emulsified into an aqueous phase to form microcapsules. To study the effects on particle size, encapsulation efficiency and morphology, three different molecular weights of ethyl cellulose (Mw=47000, 71000 and 99000) were used. Covalent bonding of drugs to polymers via hydrolytically or enzymatically cleavable covalent bond was achieved for sustained drug delivery. The release rate of perphenazine from these systems was investigated. © 1998 Society of Chemical Industry  相似文献   

6.
Matrix metalloproteases are key regulatory molecules in the breakdown of extracellular matrix and in inflammatory processes. Matrix metalloproteinase-1 (MMP-1) can significantly enhance muscle regeneration by promoting the formation of myofibers and degenerating the fibrous tissue. Herein, we prepared novel MMP-1-loaded poly(lactide-co-glycolide-co-caprolactone) (PLGA-PCL) nanoparticles (NPs) capable of sustained release of MMP-1. We established quadratic equations as mathematical models and employed rotatable central composite design and response surface methodology to optimize the preparation procedure of the NPs. Then, characterization of the optimized NPs with respect to particle size distribution, particle morphology, drug encapsulation efficiency, MMP-1 activity assay and in vitro release of MMP-1 from NPs was carried out. The results of mathematical modeling show that the optimal conditions for the preparation of MMP-1-loaded NPs were as follows: 7 min for the duration time of homogenization, 4.5 krpm for the agitation speed of homogenization and 0.4 for the volume ratio of organic solvent phase to external aqueous phase. The entrapment efficiency and the average particle size of the NPs were 38.75 ± 4.74% and 322.7 ± 18.1 nm, respectively. Further scanning electron microscopy image shows that the NPs have a smooth and spherical surface, with mean particle size around 300 nm. The MMP-1 activity assay and in vitro drug release profile of NPs indicated that the bioactivity of the enzyme can be reserved where the encapsulation allows prolonged release of MMP-1 over 60 days. Taken together, we reported here novel PLGA-PCL NPs for sustained release of MMP-1, which may provide an ideal MMP-1 delivery approach for tissue reconstruction therapy.  相似文献   

7.
Vildagliptin (VLG), an antihyperglycemic drug, having high water solubility and shorter elimination half-life. This leads to administer VLG frequently to maintain its therapeutic efficacy. Hence the goal of this work was to formulate sustained release polymeric VLG microparticles by spray drying technique using 32 full factorial design (Design-Expert Software). Ethyl cellulose (EC) and span-80 were used as encapsulating material and surfactant, respectively. This work furthermore assessed the probability of encapsulating VLG by single emulsion oil in oil (o/o) solvent evaporation technique. The resultant microparticles from these two methods were evaluated to demonstrate the significant differences in their particle size, percentage yield, drug loading (DL), encapsulation efficiency (EE), in vitro drug release, surface morphology, and drug–polymer compatibility. EE of microparticles prepared by spray drying and solvent evaporation technique was in the range of 71.42–89.87% and 51.79–64.03%, respectively. The in vitro drug release study from the microparticles prepared by both methods was conducted for 12?h. Microparticles prepared by solvent evaporation technique showed incomplete VLG release in 12?h. To visualize the effects of independent factors (polymer and surfactant amount) on dependent factors (EE and DL), 2D contour and 3D surface plots were constructed. Significant variations in microparticles’ physicochemical properties were observed with two formulation techniques. Optimum EE and sustained drug release of VLG–EC microparticles were conclusive using spray drying and solvent evaporation techniques.  相似文献   

8.
The grafting of acrylamide onto a chitosan backbone was carried out at three acrylamide concentrations (polymer/monomer ratio = 1:1, 1:2, and 1:3). The synthesis of the grafted polymer was achieved by K2S2O8‐induced free‐radical polymerization. Microspheres of polyacrylamide‐g‐chitosan crosslinked with glutaraldehyde were prepared to encapsulate nifedipine (NFD), a calcium channel blocker and an antihypertensive drug. The microspheres of polyacrylamide‐g‐chitosan were produced by a water‐in‐oil emulsion technique with three different concentrations of glutaraldehyde as the crosslinking agent. Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC) were used to characterize the grafted copolymers, and the microspheres were prepared from them. FTIR and DSC were also used to analyze the extent of crosslinking. The microspheres were characterized by the particle size; the water transport into these microspheres, as well as the equilibrium water uptake, were studied. Scanning electron microscopy confirmed the spherical nature of the particles, which had a mean particle size of 450 μm. Individual particle dynamic swelling experiments suggested that with an increase in crosslinking, the transport became case II. The release of NFD depended on the crosslinking of the network and on the amount of drug loading. Calculating the drug diffusion coefficients with the initial time and later time approximation method further supported this. The drug release in all 27 formulations followed case II transport, and this suggested that the time dependence of the NFD release followed zero‐order kinetics. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 89: 2940–2949, 2003  相似文献   

9.
The non-steroidal anti-inflammatory drug naproxen (NAP) has been coprecipitated with two different biopolymers, Eudragit (EUD) and poly(l-lactic acid) (PLA), by a supercritical antisolvent process (SAS). NAP release profiles were determined in simulated gastric and intestinal fluids in order to identify the best polymer to use for different administration routes. The in vitro release profiles of the NAP–EUD and NAP–PLA systems showed a slower and more controlled release in comparison to the untreated NAP. Moreover, the effects of pressure, temperature, initial concentration of the solution and drug-to-polymer ratio on the particle size and morphology of these drug-polymer systems have been evaluated. Although the morphology was spherical for both kinds of system, the NAP–PLA particles are larger than the NAP–EUD particles. A larger particle size is also obtained on using a lower pressure. However, the temperature did not influence, or only had a slight influence on, the particle size of NAP–PLA systems but it did have an influence on NAP–EUD systems.  相似文献   

10.
Dissolution rate of lovastatin is slow, only 30% of the oral dose is absorbed, and it undergoes extensive first‐pass extraction resulting in low and variable bioavailability. The objective of this research was to enhance the dissolution rate through preparing polymeric microparticles. Coacervation‐phase separation method through the addition of a non‐solvent was used to prepare polymeric microparticles. The method was optimized through studying effects of the type of solvent, the type of polymer, drug : polymer ratio and concentration of surfactant on particle size, particle size distribution, and in‐vitro drug release. Optimized polymeric microparticles and unprocessed drug were characterized using different techniques (SEM, FTIR, DSC, and PXRD) and their flow properties were evaluated. The optimum microparticles were prepared using ethanol as a solvent, Eudragit® L 100 as a polymer in a drug:polymer ratio of 1:2 and SDS in a concentration of 0.25%. Characterization techniques indicated a change from the crystalline form to an amorphous form that was molecularly dispersed into the polymer. Flow properties of these microparticles were improved as compared to unprocessed drug. Drug release was enhanced 4‐ to 5‐folds probably due to precipitation of the drug in an amorphous form; wetting enhancement; size reduction and stabilization by polymers and surfactants. In conclusion the selection of proper process parameters enhanced drug release 5 folds. The use of DMSO as a solvent and the preparation of physical mixtures in this research provided a means for controlled or prolonged release. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 43277.  相似文献   

11.
A laboratory scale spray dryer was used to encapsulate vildagliptin (VLG), an antihyperglycemic drug, into different polymers such as poly(dl-lactide) (PDLA), poly(dl-lactide-glycolide)-50:50 (PLGA 50:50), and poly(dl-lactide-glycolide)-75:25 (PLGA 75:25). Response surface methodology (RSM) was employed to evaluate the effects of process and formulation factors on the encapsulation efficiency (EE). The physicochemical properties of the drug-loaded micro-/nanoparticles, mainly the drug loading (DL), particle size distribution, surface morphology, drug–polymer compatibility, and release rate were investigated. % EE of drug-loaded micro-/nanoparticles were in the range of 57.10% to 76.44%. PLGA50:50 micro-/nanoparticles showed highest EE as compared to PDLA and PLGA75:25 micro-/nanoparticles. The mean particle size of the micro-/nanoparticles containing PLGA 50:50, PLGA 75:25, and PDLA polymers were 428?nm, 640?nm, and 1.22 µm, respectively. Surface morphology study revealed smooth, spherical and nonporous surface structures of the micro-/nanoparticles. Fourier transform infrared spectroscopy studies confirmed the drug–polymer compatibility. Powder X-ray diffraction analysis of micro-/nanoparticles revealed that VLG was present in the amorphous form within the micro-/nanoparticles formulations. In vitro release study demonstrated that VLG is slowly released from micro-/nanoparticles for 12?h and the drug release rate was influenced by type and viscosity of polymers used. This work suggests that PDLA, PLGA 50:50, and PLGA75:25 polymers are able to sustain the VLG release rates from micro-/nanoparticles.  相似文献   

12.
The aim of this study is to fabricate polymer/hydroxyapatite (HA) particle composite fibers for drug encapsulation and sustained release. Firstly, drug‐loaded hydroxyapatite particles are synthesized in one step, then by electrospinning of the blends of drug‐loaded hydroxyapatite particles and polymer solution the drug‐loaded polymer/hydroxyapatite particle composite fibers are successfully prepared. Effect of loading ratio of drug‐loaded hydroxyapatite particles in the fibers and pH value of the release medium on the drug release kinetics are both investigated, and the results demonstrate that, as compared with the polymer/drug electrospun fibers, the drug in the polymer/drug‐loaded hydroxyapatite particle composite fibers shows a sustained release manner, and the drug release rate can be regulated by both the loading ratio of drug‐loaded hydroxyapatite particles in the composite fibers and pH value of the buffer solution. The results indicate that the developed drug‐loaded polymer/hydroxyapatite particle composite fibers show great potential in bone regeneration and other related biomedical fields. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 42871.  相似文献   

13.
The use of copolymers grafted on starch for controlled‐release technology is an interesting proposal, since a modification of a natural polymer is more suitable than synthetic polymers because of its biocompatibility and biodegradability. The aim of this paper is to synthesize acrylic polymers grafted on carbohydrates to investigate the release kinetic of different solubility drugs from polymeric matrix systems and to observe the effect of grafted copolymers and drug solubility on the release mechanism. Copolymer variables such as carbohydrate content, stereoregularity of grafted chains, particle size, morphology, sensitivity to hydration, and rheological properties are discussed. Tablets were prepared by direct compression of the graft copolymer and drug. The drugs' release in vitro kinetics was studied by dissolution testing. Drug release from tablets depends on polymer matrix, polymer content, drug, and pH. An increase in drug solubility results in an increase in the rate of dissolution, as in the case of a poor hydrophilic matrix. © 2005 Wiley Periodicals, Inc. J Appl Polym Sci 96: 523–536, 2005  相似文献   

14.
Monodisperse ethyl cellulose (EC) microspheres (MSs) of three size groups (20–35, 55–60, and 80–105 μm in diameter) were fabricated to study the effect of the MS size on the drug‐release profiles with a novel scheme combining mechanical and hydrodynamic forces. More than 90% of the MSs were within ±3 μm of the average diameter, regardless of the EC viscosities used in the study. The effect of the polymer viscosity was also examined with ECs with two distinct viscosities (4 and 45 cp). The encapsulation efficiencies (EEs) of piroxicam and rhodamine were 6.4–51 and 63–80%, respectively. The drug distribution in the MSs showed a higher concentration near the particle surface, and this was more distinct with rhodamine. An approximately zero‐order release was observed with the small MSs of 4‐cp EC during 24 h without evident initial bursts. The MS size affected the surface‐area‐to‐volume ratio, EE, and intraparticle drug distribution, affecting the drug‐release profiles. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2009  相似文献   

15.
The aim of the present study was to investigate the effect of formulation and operating parameters of the laboratory spray dryer on polymeric microspheres intended to be used for sustaining drug delivery of diclofenac sodium (DS). Four operating and four formulation parameters were investigated by Plackett–Burman design to enhance the encapsulation efficiency (EE). The independent variables were air inlet temperature, aspirator, feed flow rate, spray nozzle diameter, amount of drug, amount of polymers, and volume of organic solvent. The resultant microspheres were characterized for their EE. The microspheres having high EE were further characterized for particle size, morphology, and in vitro drug release. Interaction between the drug and the polymer were investigated by Fourier transform infrared (FTIR) spectroscopy and X-ray powder diffractometry (XRPD). The Pareto chart showed that amount of Eudragit® RS100, amount of ethylcellulose, and aspirator were identified as significant factors. The microspheres showed high EE (47.55?±?0.006% to 67.99?±?0.007%). The microspheres were found to be discrete, spherical with smooth surface. The FTIR analysis confirmed the compatibility of DS with the polymers without interaction. The XRPD revealed the dispersion of drug within microspheres formulation. The in vitro drug release from these DS-loaded microspheres showed sustained release of DS over a period of 12?h and followed the Korsmeyer–Peppas model [R2?=?0.9920 (Run 1) and 0.9957 (Run 13)] with a value of the slope (n)?≤?0.43. This n value, however, appears to indicate that Fickian release is the dominant mechanism of drug release with these formulations.  相似文献   

16.
This study was to investigate the kinetics of drug release from polymer/TiO2 nanotubes composite. Lidocaine and carprofen were selected as model drugs to represent weak base and weak acid drugs, respectively. Mathematical models used to fit the in vitro drug release experimental data indicate that at higher pH, the drug release was first order diffusion controlled. At lower pH, the release of the two drugs exhibits two staged controlled release mechanism. The first phase is due to drug diffusion and the second stage is a result of poly(lactic‐co‐glycolic acid) (PLGA) polymer degradation. The rate of drug release from polymer/TiO2 nanotubes drug carrier was mainly controlled by three pH dependent factors: the solubility of the drug, the degree of polymer swelling/degradation, and the electrostatic force between polymer and drug. This study suggests that controlled release could be achieved for polymer/TiO2 nanotubes drug carrier via the modulation of pKa values of polymers and drug solubility. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 41570.  相似文献   

17.
An inverse suspension polymerization method for the preparation of thermoresponsive hydrogel microspheres based on N‐isopropylacrylamide was described in this article. The polymerization reaction was carried out at 200 rpm stirring rate and the microspheres obtained were in the size range of 71–500 μm in the swollen states. The particles were sieved by using ASTM sieves. The selected fraction (180–250 μm) of poly(N‐isopropylacrylamide) (PNIPAAm) microspheres was used for radiation‐induced modification with itaconic acid (IA) to obtain PNIPAAm/poly(itaconic acid) graft copolymer. Viagra and lidocaine were used as model drugs for the investigation of controlled‐release behavior of the microspheres. Incorporation of IA graft chains onto microspheres enhanced significantly the uptake of both drugs and further controlled release at specific pH values. The release studies showed that some of the basic parameters affecting the drug‐loading and ‐release behavior of the microspheres were pH, temperature, particle size, and chemical nature of drug. © 2005 Wiley Periodicals, Inc. J Appl Polym Sci 97: 1115–1124, 2005  相似文献   

18.
Self‐assembled nanoparticles prepared from amphiphilic chitosan/oleic acid (Ch/OA) have shown antibacterial activity and potential application as a carrier for hydrophobic anticancer drugs. In this study, a low molecular weight chitosan was modified with oleic acid obtaining a degree of substitution (DS) of 12%. The critical aggregation concentration (CAC) of the Ch/OA polymer obtained (0.025 mg mL?1) is lower in comparison with some systems of chitosan‐fatty acids. The self‐assembled Ch/OA nanoparticle size was optimized by changing polymer concentration, solvent, method, and time of homogenization to obtain particles with sizes around 300 nm and positive zeta potential. The drug loading about 7 μg mL?1 and encapsulation efficiency of 75.8 ± 3.6% for Celecoxib was affected by the drug concentration. In vitro release behavior performed in (PBS, pH 7.4) and MES buffer (pH 6) indicated a pH‐dependent drug release behavior. The self‐assembled systems show stability during 4 weeks after the encapsulation of the hydrophobic drug. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2017 , 134 , 44472.  相似文献   

19.
2‐Hydroxyethyl methacrylate was copolymerized with acrylamide, N‐vinyl‐2‐pyrrolidone, and n‐butyl methacrylate by free‐radical solution polymerization with α,α′‐azobisisobutyronitrile as an initiator at 70 ± 1°C. The average molecular weights and molar compositions of the resultant copolymers were determined with gel permeation chromatography and 1H‐NMR spectroscopy data, respectively. Diclofenac or 2‐[(2,6‐dichlorophenyl)amino]benzene acetic acid, a nonsteroidal anti‐inflammatory drug, was chemically attached to the copolymers by transesterification reaction in the presence of N,N′‐dicyclohexylcarbodiimide to give macromolecular prodrugs. All the synthesized polymers were characterized with Fourier transform infrared, 1H‐, and 13C‐NMR spectroscopy techniques. The polymer–drug conjugates were hydrolyzed in cellophane member dialysis bags containing aqueous buffered solutions (pH 8) at 37°C, and the hydrolysis solutions were detected by UV spectrophotometer at selected intervals. The results showed that the drug could be released by selective hydrolysis of the ester bond from the side chain of the drug moiety. The release profiles of the drug indicated that the hydrolytic behavior of polymeric prodrugs strongly depends on the hydrophilicity of the polymer. The results suggest that the synthesized copolymers could be useful carriers for the release of diclofenac in controlled‐release systems. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci 104: 2403–2409, 2007  相似文献   

20.
The aim of this study was to investigate the in vitro drug release behavior of sweet potato starch (SPS) microparticles intended for controlled drug delivery applications. Diclofenac sodium (DS) was used as a model drug candidate in the present study. SPS microparticles were prepared using a spray-drying technique by varying the polymer concentration and drug loading. The mean particles size of drug-loaded spray-dried SPS microparticles was between 10.3 and 13.1 µm. The mean particle size increased slightly with increase in the concentration of SPS. The mean particle size of spray-dried SPS microparticles increased from 10.3 to 13.1 µm when the concentration of SPS increased from 2 to 4% w/v. Under the current spray-drying conditions, the percentage yield of spray-dried SPS microparticles did not vary much among the various formulations and it was between 65.2 and 70.1%. The encapsulation efficiencies of SPS microparticles formulations was between 95.1–98.2%, suggesting good encapsulating ability of the SPS polymer by spary drying. Drug release from all the formulations of spray-dried SPS microparticles was controlled over period of 6 h. The cumulative amount of drug release from the spray-dried SPS microparticles decreased with an increase in the concentration of SPS, while it increases as the drug loading is increased. Release of the drug from spray-dried SPS microparticles followed Fick's law of diffusion since a good correlation coefficient (R2) was observed with the Higuchi plots (R2 = 0.9928 to 0.9979).  相似文献   

设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司    京ICP备09084417号-23

京公网安备 11010802026262号