右旋布洛芬/蒙脱土复合物的制备及体外释放性能研究

目的:以天然蒙脱土作为药物载体,制备右旋布洛芬/蒙脱土复合物,并对其进行结构表征和体外释药考察.方法:采用溶液插层法制备右旋布洛芬/蒙脱土复合物(S(+)-ibuprofen/montmorillonite,S(+)-IBU/MMT).通过X-射线衍射(XRD)和傅里叶红外变换光谱(FT-IR)对复合物的结构进行表征;采用透析法研究介质的pH值对S(+)-IBU/MMT体外释放的影响.结果蒙脱土层间距由1.25 nm增大到1.31 nm,右旋布洛芬以插层方式进入蒙脱土的层间域;S(+)-IBU/MMT复合物体外释药受释放介质pH值的影响,在pH 1.0、pH4.5和pH 6.8的释放介质中,右旋布洛芬12 h的累积释放百分量分别18％、36％和88％.结论采用溶液插层法所制备S(+)-IBU/MMT复合物具有较好的缓释作用.     

N-甲基-N,N-双十二烷基壳聚糖盐酸盐的合成及自组装囊泡性能

以壳聚糖为原料制备N-甲基-N,N-双十二烷基壳聚糖盐酸盐(TMC),用FT-IR、EA对产物进行表征,溶解性实验表明TMC溶于乙醇等有机溶剂。采用乙醇注射法制备TMC囊泡,研究不同pH值介质中制得的载亲/疏水药物TMC囊泡的Zeta电位、粒径大小及分布、储存稳定性、载药及释放性能。结果表明,制得的TMC自组装囊泡Zeta电位为39.5~46 mV,粒径为50~100 nm,多分散系数为0.17~0.26,静置30天后仍保持稳定。Langmuir膜行为表明在较低pH值下TMC更易自组装,制备介质pH值不同对囊泡的粒径、药物释放行为影响较大,而释药环境pH值对囊泡的药物释放行为影响较小。     

氟尿嘧啶/蒙脱石复合物的制备及其释放性能

以提纯钙基蒙脱石为原料,在一定条件下制备出5-氟尿嘧啶/蒙脱石复合物(5-fluorouracil/montmorillonite,5-FU/MMT),探讨了蒙脱石对5-FU的吸附作用。通过透析法研究了释放介质的pH值和释放时间等因素对5-FU/MMT复合物体外释放的影响规律。采用2种体外释放模型对其释放实验数据进行拟合,探讨了5-FU的释放机理以及蒙脱石作为5-FU缓释载体的可行性。结果表明:蒙脱石与5-FU之间的相互作用主要是物理吸附、化学吸附和插层作用。蒙脱石对5-FU具有较好的缓释作用,是一种性能优异的药物缓释载体;其体外释放能力受释放溶液的pH值影响,在pH=1.2的释放介质中,5-FU的释放浓度和累积释放量最大,分别为9.01mg/L和23.05%,其次为pH=7.4时的,pH=5.0时的最小。一级动力学模型比Korsmeyer–Peppas模型能更好地拟合和描述5-FU在不同pH值释放介质中的体外释放量随时间的变化。拟合结果表明:5-FU从5-FU/MMT复合物中释放的行为主要由物理扩散和药物溶解作用决定,同时5-FU与释放介质之间的离子交换作用对释放过程也有一定贡献。     

β-环糊精/海藻酸钠水凝胶的制备及性能研究

将海藻酸钠(SA)和β-环糊精(β-CD)共混制备了复合水凝胶,并讨论了交联剂浓度、原料配比对水凝胶溶胀性能的影响。结果表明,当两者的共混比例为1∶2、w(交联剂)为6%、交联时间为1h时,水凝胶的溶胀性能较好。水凝胶在pH=1.2时的溶胀率仅为1.2,而在pH=7.4时的溶胀率达到14.2,具有良好的pH敏感性。以牛血清蛋白(BSA)为模型药物,研究了β-CD/SA水凝胶作为药物载体对BSA的负载及释放性能,结果表明:在模拟胃液中的累计释放量较小(21.5%),且释放速率较慢;在模拟肠液中的累计释放量为70.2%,具有良好的pH敏感控制释放性能。     

右旋布洛芬/盐酸改性蒙脱土的制备及体外释放研究

目的：以酸改性蒙脱土为药物载体,制备右旋布洛芬/酸改性蒙脱土复合物,提高右旋布洛芬的载药量,并探索载药复合物在不同释放介质中的释放规律。方法：首先用浓度为5%~20%的盐酸对蒙脱土进行预处理,利用X-射线衍射（XRD）、比表面积测定（BET）、扫面电子显微镜（SEM）等表征方法对蒙脱土进行结构表征,筛选最佳酸处理浓度;然后用溶液插层法将右旋布洛芬负载于酸化后的蒙脱土上,制得右旋布洛芬/酸改性蒙脱土复合物;采用透析法对右旋布洛芬/酸改性蒙脱土复合体系进行体外释放实验。结果：经酸改性后蒙脱土的结构发生改变,当酸浓度为15%时,蒙脱土的比表面积达到最大值246 m2/g。上载右旋布洛芬后,载药量最大可达352.4 mg/g。体外释放实验表明,右旋布洛芬/酸改性蒙脱土的累积释药百分量受pH的影响,当pH为1.2时,其累积释药百分量为18.6%,当pH为6.8时,则为89.3%。结论：盐酸改性蒙脱土有助于提高药物的负载量,右旋布洛芬/酸改性蒙脱土复合物具有良好的缓释作用并有一定的pH响应性,有望制成肠道缓释口服药物制剂。     

壳聚糖改性蒙脱石作为药物控释载体的研究

采用壳聚糖(CS)对钠基蒙脱石(MMT)进行改性制备有机蒙脱石(CS-MMT),对改性后的蒙脱石进行红外光谱(FT-IR)和X射线衍射(XRD)等分析表征.以5-氟尿嘧啶(5-FU)为药物模型制备出壳聚糖改性蒙脱石载药复合物(5-FU/CS-MMT),并以钠基蒙脱石载药复合物(5-FU/MMT)作为对照,探究载药复合物在模拟人工胃液、人工小肠液和人工结肠液中的药物释放情况.结果 表明,当CS的用量是MMT的1.0倍阳离子交换容量时,形成的有机蒙脱石的层间距增大,且对5-FU的载药量达到393 mg/g,而同等情况下,MMT的载药量为239 mg/g.体外释放试验的结果表明,5-FU/CS-MMT中5-FU的体外释放能力主要受释放介质pH值的影响,当pH值为7.4时,5-FU的累积释放率最大,在pH值为1.5时的结果最小.     

纤维素/海藻酸钠基双膜水凝胶的制备及其药物控释研究

用阳离子纤维素(CC)和阴离子海藻酸钠(SA)制备出具有双膜结构的生物相容性水凝胶,探究了水凝胶在不同pH值环境下的药物控制释放行为。结果表明,在pH为7.4,进行单膜水凝胶释放牛血清白蛋白时,纯海藻酸钠水凝胶SA、SA/CC-1水凝胶、SA/CC-2水凝胶的药物释放时间分别为3,6,8 d,累积释放量分别为86%,84%,83%,即纤维素阳离子化程度更高的水凝胶释放药物更缓慢;在pH为2.0的条件下,单膜水凝胶释放牛血清白蛋白的累积释放量的最大值仅为6%,水凝胶的药物释放行为表现出pH敏感性。此外,在pH为7.4条件下,复合药物从双膜水凝胶中有序释放出来,外膜中的茶碱在药物释放的第3 d达到释放平衡,累积释放量为87%;内膜中的牛血清白蛋白在第4 d开始释放,在第11 d达到平衡,累积释放量为84%。该水凝胶有明显的药物控释作用,在生物医学领域有很大的应用前景。     

纤维素/海藻酸钠基双膜水凝胶的制备及其药物控释研究

用阳离子纤维素(CC)和阴离子海藻酸钠(SA)制备出具有双膜结构的生物相容性水凝胶,探究了水凝胶在不同pH值环境下的药物控制释放行为。结果表明,在pH为7.4,进行单膜水凝胶释放牛血清白蛋白时,纯海藻酸钠水凝胶SA、SA/CC-1水凝胶、SA/CC-2水凝胶的药物释放时间分别为3,6,8 d,累积释放量分别为86%,84%,83%,即纤维素阳离子化程度更高的水凝胶释放药物更缓慢;在pH为2.0的条件下,单膜水凝胶释放牛血清白蛋白的累积释放量的最大值仅为6%,水凝胶的药物释放行为表现出pH敏感性。此外,在pH为7.4条件下,复合药物从双膜水凝胶中有序释放出来,外膜中的茶碱在药物释放的第3 d达到释放平衡,累积释放量为87%;内膜中的牛血清白蛋白在第4 d开始释放,在第11 d达到平衡,累积释放量为84%。该水凝胶有明显的药物控释作用,在生物医学领域有很大的应用前景。     

羧甲基壳聚糖离子配位微球的制备及性能研究

以羧甲基壳聚糖(CMCHS)为主要原料,采用静电脉冲液滴发生器制备羧甲基壳聚糖离子配位微球。光学显微镜观察微球具备规整形貌,扫描电镜分析显示干球粒径约为100μm且表面呈多孔结构;红外光谱证明其内部具有由CMCHS上的羧酸根与Ca^2 配位形成的羧酸盐结构。溶胀实验表明,CMCHS溶液浓度、金属离子种类及其浓度等制备条件均影响微球的溶胀性能．且其溶胀行为对pH值较敏感。药物体外释放初步研究表明,CaCl2浓度和释放介质pH值均对微球的释放性能产生影响。研究对其进一步应用于药物释放等领域具有重要意义。     

释放介质对混合药膜包膜体系的影响

制得了5－FU／EVAL混合药膜包膜体系，并对该体系中释放介质的pH值和极性对累积释放量的影响进行研究，通过对膜的微观结构的分析，讨论了影响的原因和方式。     

Biodegradable blend films based on two polysaccharide derivatives and their use as ibuprofen‐releasing matrices

Differential scanning calorimetry (DSC), FTIR, X‐ray diffraction (XRD), and viscosity methods were used to examine the miscibility, interaction, and degradability of cationic guar gum (GG) and sodium carboxymethylcellulose (NaCMC) in their blend films. The experiment results prove that there exist electrostatic interactions and hydrogen bonding between GG and NaCMC. Blend films degrade quicker than pure GG or NaCMC film. Furthermore, the degradation rate of blend films is related to the interactions between GG and NaCMC. Based on the research of blend films as the drug carriers for Ibuprofen, it is found that the blend composition, initial drug concentration, and pH value affect the drug release and the GG/NaCMC blend films have good sustained release performance. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 103: 3553–3559, 2007     

Poly(ethyl glycol) assisting water sorption enhancement of poly(ε‐caprolactone) blend for drug delivery

Poly(ε‐caprolactone) (PCL) has been thermally synthesized, and then fractionated to blend with poly(ethyl glycol) (PEG). Blend films of PCL and PEG have been prepared by solution casting. Fourier transform infrared spectrum and differential scanning calorimetry of the films have been carried out, and the results indicate some hydrogen bonding interaction between the two components, which is resulted from the carbonyl groups of PCL and the hydroxyl end‐groups of the low‐molecular‐weight PEG. Scanning electron microscope images of the blend films reveal porous network structures for their surfaces and for their inner parts and the porous structure becomes more pronounced with the increase of PEG in the blend film. Ibuprofen (IBU) was used as the model drug to test the drug release behavior for the PCL/PEG blend matrices. The results show that IBU could be released from the blend tablets rapidly, and the release rate increases with PEG content. Analysis of the release profiles indicates PCL erosion control release mechanism of pure PCL tablet, but drug diffusion control of the blend tablet, because PEG can absorb water to allow water feasible to diffuse into drug core and dissolve drug. Therefore, the interconnected channels in the blend matrices and the hydrophilic nature of PEG contribute to the improvement of the IBU release rate. The research indicates that drug release rate from PCL based material could be efficiently improved by addition of small amount of hydrophilic low‐molecular‐weight PEG. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2011     

Preparation and characterization of konjac glucomannan and sodium carboxymethylcellulose blend films

The novel blend films of konjac glucomannan (KGM) and sodium carboxymethylcellulose (NaCMC) were prepared by casting the mixed polymer aqueous solutions. The physical properties of the blend films from konjac glucomannan and sodium carboxymethylcellulose were investigated by using FT‐infrared (FTIR), wide‐angle X‐ray diffraction (WAXD), differential thermal analysis (DTA), scanning electron microscopy (SEM), thermogravimetric analysis (TGA), and measurements of mechanical properties. The experimental results showed that the occurrence of the interactions between KGM and NaCMC molecular chains through hydrogen bond formation, and the physical properties of the films largely depend on the blending ratio. The thermal stability, mechanical properties of both tensile strength, and elongation at break of the blend films were improved by blending KGM with NaCMC. The surface morphology of the films observed by SEM was consistent with the results mentioned above. © 2001 John Wiley & Sons, Inc. J Appl Polym Sci 80: 26–31, 2001     

Controlled release of insecticide carbaryl from sodium alginate,sodium alginate/gelatin,and sodium alginate/sodium carboxymethyl cellulose blend beads crosslinked with glutaraldehyde

Interpenetrating network polymeric beads of sodium alginate (NaAlg) and its blend with gelatin (gels) or sodium carboxymethyl cellulose (NaCMC) have been prepared by crosslinking with a common crosslinking agent, glutaraldehyde (GA), for the release of insecticide carbaryl (Carb). The prepared beads were characterized by Fourier transform infrared spectroscopy and scanning electron microscopy. Scanning electron microscopy confirmed the spherical nature and surface morphology of the particles. Bead characteristics, such as carbaryl entrapment efficiency, particle size, equilibrium swelling degree, and carbaryl release kinetics, were determined. The effects of the preparation conditions, such as Carb/NaAlg ratio, time of exposure to GA, blend ratio, and temperature of release medium on the carbaryl release, were investigated for 25 days at 25°C. It was observed that the carbaryl release decreased with increase in crosslinking of network, while it increased with increase in Carb/NaAlg ratio and temperature. The release of carbaryl also increased with increase in Gel or NaCMC content in the blend beads. The highest carbaryl release was found to be 100%, for the beads that were prepared with 1 : 1 NaAlg/Gel at 16 days. The diffusion coefficients have been calculated for the transport of insecticide through the polymeric beads, using initial time approximation method. These values were also consistent with the carbaryl release data. The carbaryl release from most of the bead formulations followed the Fickian trend. © 2005 Wiley Periodicals, Inc. J Appl Polym Sci 99: 1310–1319, 2006     

Biodegradable polymeric microspheres of gelatin and carboxymethyl guar gum for controlled release of theophylline

Carboxymethyl guar gum (CMGG) was synthesized by carboxymethylation of guar gum (GG), which was blended with gelatin (GE) to obtain a novel semi-interpenetrating polymer network (semi-IPN) in the form of microspheres prepared by water-in-oil emulsion method to investigate the controlled release of theophylline (THP), an antiasthmatic drug. Electronic spectroscopy revealed the drug encapsulation ranging from 56 to 74 %. Fourier Transform infrared spectroscopy confirmed the carboxymethylation of GG as well as the semi-IPN structure of the blend polymer. Scanning electron microscopy indicated the smooth surfaces with spherical microspheres. Differential scanning calorimetric and X-ray diffraction studies showed the molecular level dispersion of drug in the microspheres. The in vitro drug release profiles were analyzed to study the effect of polymer blend composition, % drug loading and amount of glutaraldehyde added as a crosslinker. The drug release was extended up to 26 h. The in vitro release data performed in acidic and alkaline media were analyzed using the empirical equations to understand the release profiles of THP.     

Miscibility studies of sodium carboxymethylcellulose/poly(vinyl alcohol) blend membranes for pervaporation dehydration of isopropyl alcohol

Miscibility studies of sodium carboxymethylcellulose/poly(vinyl alcohol) (NaCMC/PVA) blends of different compositions (100/0, 80 : 20, 60 : 40, 50 : 50, 40 : 60, 20 : 80, and 0 : 100) were investigated using viscometric method. NaCMC, PVA, and their blend membranes were prepared by solution‐casting technique and were then crosslinked with glutaraldehyde (GA). The effect of blend composition on mechanical, swelling, and pervaporation results (flux and selectivity) was also investigated in this study. Attenuated total reflectance–Fourier transform infrared spectroscopy (ATR–FTIR) results showed that the blends are miscible over the entire studied composition range and further confirmed the crosslinking reaction with GA. FTIR studies reveal that the blends containing 50 : 50 (NaCMC/PVA) are an optimum miscible blend. Thermogravimetric analysis confirms that the thermal stability increased with increase in NaCMC content in NaCMC/PVA blend membrane. XRD and DSC showed a corresponding decrease in crystallinity and increase in melting point with increase in NACMC content, respectively. NaCMC/PVA blends of all the composition under study were used for dehydration of isopropyl alcohol at different compositions of IPA/water mixture (90 : 10, 87.5 : 12.5, 85 : 15, and 82.5 : 17.5) at 35°C. Swelling studies and PV results reveal that increase in NaCMC content in the blend leads to an increase in flux of water, whereas selectivity decreases. The optimum flux and selectivity were observed for the blend containing 50 : 50 NaCMC/PVA content at a feed ratio of 87.5 : 12.5 IPA/water. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2011     

In-Vitro Release Study of Metoprolol Succinate from the Bioadhesive Films of Pullulan-Polyacrylamide Blends

In the present work, an attempt has been made to investigate the drug release profile of pullulan-polyacrylamide blend films with metoprolol succinate as a model drug. The drug diffusion behavior of pullulan/polyacrylamide films has been established by an open glass diffusion cell at 37 ± 1°C. The diffusion rate of the drug was determined by UV/visible spectroscopy. The kinetics of drug release are fitted to the Higuchi and Koresmeyer–Peppas model. The drug release kinetics for the blend was found to be fast and follows Fickian mechanism. This blend could be a promising approach for formulating a transdermal drug delivery system for immediate release with good film-forming property.     

Morphology,drug release behavior,thermal, and mechanical properties of poly(ethylene oxide) (PEO)/poly(vinyl pyrrolidone) (PVP) blends

Poly(ethylene oxide) (PEO)/poly(vinyl pyrrolidone) (PVP) blends containing different amounts of PVP (0, 10, 25, 50, and 100 wt %) prepared by a solution casting method were characterized in terms of microstructure, thermal, and mechanical properties along with their drug release behavior. Fourier‐transform infrared spectroscopy results confirmed formation of hydrogen bonds between PEO and PVP. Although scanning electron microscopy micrographs showed no phase separation in the blends, the elemental analysis data obtained by energy dispersive X‐ray technique revealed partial miscibility between the blend components. The miscibility of the blend and degree of crystallinity of PEO component of the blend were decreased with increasing PVP content of the blend. The nucleating role of PVP in crystallization of PEO was confirmed by differential scanning calorimetry analysis. A synergistic effect on mechanical properties was obtained as a result of blending PVP with PEO. The results of curcumin release studies from the films indicated that, the blends have lower diffusion coefficients and slower drug release rate as compared to the neat PEO. Theoretical analysis of the drug release data using Peppas's model revealed that the kinetic of drug release from all the films is governed by a non‐Fickian diffusion mechanism. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018 , 135, 46403.     

Rheological properties and drug release characteristics of pH‐responsive hydrogels

Rheological properties, blend compatibility, and gel‐forming capacity of carbopol 940 (CP‐940), sodium alginate (NaAlg), and guar gum (GG) have been studied. These matrices have been used in delivery of timolol maleate for ophthalmic applications. Aqueous solutions of CP‐940, NaAlg, and GG in concentrations between 0.1 and 1% (wt/vol) and their blends have been prepared. In situ gel forming polymeric solutions have shown an increase in viscosity upon exposure to specific pH, ions, and temperature of the eyeball. Blend miscibility was studied by calculating polymer–polymer interaction parameters using viscosity data. Rheological properties viz., torque, viscosity, shear stress, and shear rate were obtained using a Brookfield rheometer. Viscosities of polymer solutions were obtained by a Schott Gerate viscometer. Rheological data were analyzed using Bingham, Casson Standard, and Casson Chocolate equations. The hydrogels were subjected to ex vivo release studies on timolol maleate through the excised bovine cornea using a modified Franz diffusion cell. Results were compared with the conventional drug solution. The release could be extended when the drug is incorporated into hydrogel‐forming solution. © 2004 Wiley Periodicals, Inc. J Appl Polym Sci 94: 2057–2064, 2004     

Preparation,characterization, antibacterial properties,and hemostatic evaluation of ibuprofen‐loaded chitosan/gelatin composite films

Ibuprofen‐loaded chitosan/gelatin (CS/GE) composite films were fabricated in this work. The morphology of the composite film was investigated using scanning electron microscopy. The functional groups of the composite film before and after crosslinking were characterized using Fourier transform infrared spectroscopy. Meanwhile, the mechanical properties, antibacterial performance, cytocompatibility, and hemostatic activity of the composite films were investigated. The results show that the amount of CS affected the mechanical properties and liquid uptake capacities of the composite films. The composite film showed better bactericidal activity against Staphylococcus aureus than Escherichia coli. In vitro drug‐release evaluations showed that crosslinking could control the drug‐release rate and period in wound healing. Both types of CS/GE and drug‐loaded CS/GE composite films also showed excellent cytocompatibility in cytotoxicity assays. The hemostatic evaluation indicated that the composite film crosslinked by glutaraldehyde in rabbit livers had a dramatic hemostatic efficacy. Therefore, ibuprofen‐loaded CS/GE composite films are potentially applicable as a wound dressing material. © 2017 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2017 , 134, 45441.