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1.
以海藻酸、丙烯酰胺为单体,氧化石墨烯为原料制备了海藻酸钠-g-聚丙烯酰胺/氧化石墨烯(NaAlg-g-PAAm/GO)复合水凝胶,采用傅里叶变换红外光谱和扫描电镜对其结构和形貌进行了表征;当GO的质量分数从0.6%增至3.2%时,溶胀率从37%减至21%;阳离子对水凝胶的溶胀性的影响能力是Fe3+Ca2+K+;以5-氟尿嘧啶(5-FU)为抗癌药物模型,模拟胃腔和小肠的环境,研究了在pH=1.2和pH=7.4的缓冲溶液中复合水凝胶的控制释放行为,实验结果表明水凝胶在pH=7.4的缓冲溶液中的累积释放率明显高于在pH=1.2的溶液中的累积释放率,所以该类水凝胶有望成为靶向药物释放的载体。  相似文献   

2.
以海藻酸、丙烯酰胺为单体,氧化石墨烯为原料制备了海藻酸钠-g-聚丙烯酰胺/氧化石墨烯(NaAlg-g-PAAm/GO)复合水凝胶,采用傅里叶变换红外光谱和扫描电镜对其结构和形貌进行了表征;当GO的质量分数从0.6%增至3.2%时,溶胀率从37%减至21%;阳离子对水凝胶的溶胀性的影响能力是Fe3+>Ca2+>K+;以5-氟尿嘧啶(5-FU)为抗癌药物模型,模拟胃腔和小肠的环境,研究了在pH=1.2和pH=7.4的缓冲溶液中复合水凝胶的控制释放行为,实验结果表明水凝胶在pH=7.4的缓冲溶液中的累积释放率明显高于在pH=1.2的溶液中的累积释放率,所以该类水凝胶有望成为靶向药物释放的载体。  相似文献   

3.
以5-氨基水杨酸(5-ASA)为模型药物分子,pH敏感水凝胶聚甲基丙烯酸(PMAA)为载体,采用浸渍法实现了药物在载体上的负载,载药量约为23.3wt%。通过体外模拟释放实验,研究了该凝胶在不同pH值模拟胃液(pH=1.2)和模拟肠液(pH=7.5)中的释药行为。结果表明,药物在pH值较低的模拟胃液中释放的较慢,且最大累积释药率较低(~10.4%);在pH值较高的模拟肠液中释放的较快,最大累积释药率达~47.6%,并揭示了释药机理。因此,PMAA可实现药物5-ASA在模拟肠液中的靶向释放,在智能药物控释系统领域具有潜在的应用价值。  相似文献   

4.
采用离子凝胶法制备了欧车前胶-g-聚丙烯酸/凹凸棒黏土/海藻酸钠(PSY-g-PAA/APT/SA)载药复合凝胶小球,以双氯芬酸钠为模型药物,考察了pH敏感性和凹凸棒黏土含量对凝胶小球的包封率、载药率、溶胀性能和药物释放行为的影响。结果表明,当释放介质为模拟胃液(pH=1.2)时,药物基本不释放;而为模拟肠液(pH=6.8)时,5h后累积释放率超过90%,复合凝胶小球具有明显的pH敏感性。随着凝胶小球中凹凸棒黏土含量的增加,溶胀率和药物累积释放率均减小,表明凹凸棒黏土的引入可以减缓药物的突释效应。  相似文献   

5.
以不同烷基侧链的N-乙烯基咪唑类离子液体为单体,设计合成了3种具有pH/盐双敏感性的交联网状孔洞结构的聚咪唑类离子液体凝胶(PC_nvimBr,n=2,4,6)。在微观结构、溶胀特性和刺激响应行为研究基础上,探讨了侧链微增长对聚离子液体凝胶结构与性能的调节控制,并根据凝胶的构效关系情况进行相应药物的体外控制释放研究,研究表明,PC_nvimBr凝胶具有良好的pH/盐刺激双响应性以及溶胀可逆性。在pH=7.4的弱碱性环境下,三种聚离子液体凝胶均具有较强的敏感性及溶胀可逆性,其中PC_2vimBr凝胶的pH响应性最为敏感,其平衡溶胀率高达1422.3%。同时,以NaCl盐溶液为模拟模型,相对而言,PC_2vimBr凝胶在弱碱性条件下具有良好的盐敏感性。此外,结合人体肠道呈弱碱性特点,以肠道杀菌药物环丙沙星(CIP)为载药模型,在pH=7.4时药物控制释放的体外模拟实验研究发现,PC_2vimBr凝胶10 h内的累积释放率为67.78%,是PC_4vimBr、PC_6vimBr凝胶的1.42和3.38倍,这与pH/盐刺激双响应性的研究结果一致。因此,烷基侧链微增长对凝胶结构具有较强的调控作用,pH/盐双敏感性的PC_2vimBr凝胶在肠道杀菌药物的控制释放具有潜在的应用价值。  相似文献   

6.
用零长度的1-乙基-(3-二甲基氨基丙基)碳二亚胺盐酸盐(EDC·HCl)和N-羟基丁二酰亚胺(NHS)作为偶联剂和稳定剂制备了壳聚糖基透明质酸复合水凝胶,探讨了溶液pH值对该类水凝胶溶胀性的影响。溶液的pH在4.0时,该类水凝胶的溶胀率最低,升高和降低溶液的pH,该类水凝胶的溶胀率均升高,文中还对水凝胶的降解率进行了研究,实验发现,交联后的水凝胶具有一定的稳定性。包埋在此水凝胶中的牛血清蛋白(BSA)释放随载药介质pH值的变化而显著不同,pH 7.4条件下载药的水凝胶释药率大于pH 1.2条件下的释药率。因此,具有pH敏感性的壳聚糖透明质酸复合水凝胶在药物运输领域具有潜在的应用。  相似文献   

7.
以壳聚糖(CS),L-天冬氨酸(ASP)和戊二醛(GA)为原料,合成了具有pH、离子强度敏感性的壳聚糖水凝胶CS-GA-ASP.研究了交联剂含量、pH、离子强度对水凝胶溶胀率的影响和水凝胶对辅酶A的控制释放.结果表明,水凝胶在酸性溶液中,溶胀率最大,在中性溶液中溶胀率最小;水凝胶在不同pH或不同离子强度的溶液中交替放置时,表现出良好的溶胀-退胀可逆性;在室温下,pH=3.7、6.8、9的缓冲溶液中,辅酶A的累积释放率分别为78%、92%和87%,且在pH=6.8的缓冲溶液中,辅酶A释放速率最快,在pH=3.7的缓冲溶液中时,辅酶A释放速率最慢.  相似文献   

8.
pH敏感水凝胶PMAA对布洛芬的控制释放   总被引:1,自引:1,他引:0  
采用自由基聚合法制备了pH敏感水凝胶聚甲基丙烯酸(PMAA),研究了该凝胶在不同pH值溶液中的溶胀性能.结果表明,PMAA凝胶在pH=2时的溶胀率仅为2.6,而在pH=10时的溶胀率达15.8,具有明显的pH敏感性能.以疏水性布洛芬为模型药物,研究了PMAA水凝胶作为药物载体对布洛芬的负载及释放性能,结果显示:PMAA...  相似文献   

9.
研究了用静电纺丝制备聚苯乙烯-马来酸酐共聚物(SMA)/醋酸纤维素(CA)复合超细纤维。通过一缩二乙二醇(DEG)交联,并在0.05mol/L NaOH/乙醇溶液中水解制得SMA-Na-DEG/纤维素超细纤维水凝胶。对其结构和拉伸性能进行了分析和测试,结果表明:该水凝胶pH响应良好,pH=9.1时,溶胀比达到最大值27.6g/g;加入纤维素后,水凝胶的力学性能明显提高。此外,还以水杨酸为药物,评估了SMA-Na-DEG/纤维素水凝胶的药物释放行为,并探讨了其释放机理。  相似文献   

10.
聚天冬氨酸交联温敏性水凝胶的药物缓释性能   总被引:1,自引:0,他引:1  
选用牛血清蛋白(BSA)和5-氟尿嘧啶(5-FU)为模型药物,以聚天冬氨酸交联温敏性水凝胶为载体材料,采用包埋法制备了载药水凝胶,研究了水凝胶的载药和释药性能。水凝胶对BSA和5-FU的包埋率均大于98%。37℃时,水凝胶中丙烯酸用量越大,BSA的释放率越低;交联剂用量对BSA的释放率无显著影响。25℃时,丙烯酸用量越大,5-FU的释放率越大;交联剂用量越大,5-FU的释放率越小。37℃时,丙烯酸用量越小,5-FU的释放率越大;交联剂用量越大,5-FU的释放率越小。  相似文献   

11.
Objective: The aim of this study was to prepare pH-sensitive ofloxacin (OFL)/montmorillonite (MMT)/chitosan (CTS) nanocomposite microspheres that improve the burst release effect of the drug by the solution intercalation technique and emulsification cross-linking techniques. Methods: First, OFL/MMT hybrids were prepared through the solution intercalation technique. Then, OFL/MMT-intercalated OFL/MMT/CTS nanocomposite microspheres were obtained through emulsification cross-linking technology. The intercalated nanocomposite was confirmed by Fourier-transform infrared spectroscopy and X-ray diffraction. Finally, in vitro release of OFL from the microspheres was performed in simulated gastric fluids and simulated intestinal fluids. The effect of MMT content on drug encapsulation efficiency and the drug release of the nanocomposite microspheres were investigated. Results: The results showed that the release rate of OFL from the nanocomposite microspheres at pH 7.4 was higher than that at pH 1.2. Compared with pure CTS microspheres, the incorporation of certain amount of MMT in the nanocomposite microspheres can enhance the drug encapsulation efficiency and reduce the burst release. Conclusion: A sustained release particulate system can be obtained by incorporating MMT into the nanocomposite microspheres and can improve the burst release effect of the drug.  相似文献   

12.
Chitosan-prednisolone conjugate microspheres (Ch-SP-MS) were prepared, and Eudragit coating was applied in order to efficiently deliver the microspheres and drug to the intestinal disease sites. The Eudragit L100-coated microspheres (Ch-SP-MS/EuL100) were examined for particle characteristics and the release of drug and Ch-SP-MS in different pH media at 37°C. Ch‐SP-MS were spherical, with a mean size of 4.5 μm and prednisolone content of 3.3% (w/w). Ch-SP-MS/EuL100 were fairly spherical, with a mean size of 22. 5 μm and drug content of 0.32% (w/w). At pH 1.2, the release extent was less than 5% even at 48 h, and Eudragit coating tended to suppress the release. In contrast, at pH 6.8 and 7.4, Ch-SP-MS/EuL100 tended to show somewhat faster drug release than Ch-SP-MS. Ch-SP-MS/EuL100 displayed a release extent of 23 and 27% at pH 6.8 and 7.4, respectively. Ch-SP-MS aggregated at pH 1.2, but almost kept their initial size and shape at pH 6.8 and 7.4. Ch-SP-MS/EuL100 almost maintained their original shape and size at pH 1.2, and gradually released Ch-SP-MS at pH 6.8 and 7.4 due to dissolution of the Eudragit layer. Eudragit coating is suggested to be useful to efficiently deliver Ch-SP-MS to the intestinal disease sites.  相似文献   

13.
Chitosan-prednisolone conjugate microspheres (Ch-SP-MS) were prepared, and Eudragit coating was applied in order to efficiently deliver the microspheres and drug to the intestinal disease sites. The Eudragit L100-coated microspheres (Ch-SP-MS/EuL100) were examined for particle characteristics and the release of drug and Ch-SP-MS in different pH media at 37°C. Ch-SP-MS were spherical, with a mean size of 4.5 μm and prednisolone content of 3.3% (w/w). Ch-SP-MS/EuL100 were fairly spherical, with a mean size of 22. 5 μm and drug content of 0.32% (w/w). At pH 1.2, the release extent was less than 5% even at 48 h, and Eudragit coating tended to suppress the release. In contrast, at pH 6.8 and 7.4, Ch-SP-MS/EuL100 tended to show somewhat faster drug release than Ch-SP-MS. Ch-SP-MS/EuL100 displayed a release extent of 23 and 27% at pH 6.8 and 7.4, respectively. Ch-SP-MS aggregated at pH 1.2, but almost kept their initial size and shape at pH 6.8 and 7.4. Ch-SP-MS/EuL100 almost maintained their original shape and size at pH 1.2, and gradually released Ch-SP-MS at pH 6.8 and 7.4 due to dissolution of the Eudragit layer. Eudragit coating is suggested to be useful to efficiently deliver Ch-SP-MS to the intestinal disease sites.  相似文献   

14.
The microspheres of crosslinked starch have been prepared and characterized by IR spectral analysis and SEM technique. The prepared microspheres were loaded with an anticoagulant drug ‘heparin’ and the kinetics of in-vitro release of heparin was investigated spectrophotometrically at physiological pH (7.4) and body temperature (37 °C). The influence of percent loading of heparin, chemical architecture of the microspheres and pH of the release medium were examined on the release profiles of the drug. The chemical stability of heparin was tested in phosphate buffer saline (pH 7.4) and the release was also studied in various simulated biological fluids.  相似文献   

15.
Nanomaterials are at the leading edge of the rapidly developing field of nanotechnology. The use of nanoparticles as drug delivery vehicles for anticancer therapeutics has great potential to revolutionize the future of cancer therapy. The present paper concerns both the optimizations of anticancer drug loading and its release from polymeric nanoparticles. The major aim of this study was to design poly (HEMA) nanoparticles as swelling controlled drug release system for anticancer drug. The prepared nanoparticles were characterized by Infra-Red (IR) Spectra, Particle size Analysis, and Scanning Electron Microscopy (SEM). The nanoparticles were loaded with widely used anticancer drug, 5-Fluorouracil, and controlled release of drug was investigated to observe the effects of various parameters such as percent loading of the drug, chemical architecture of the nanocarriers, pH, temperature, and nature of release media on the release profiles. The chemical stability of 5-Fluorouracil (5-FU) was also tested in phosphate buffer saline (PBS) (pH = 7.4) and release was studied in various simulated biological fluids. The prepared nanoparticles could provide a possible pathway for controlled and targeted delivery of anticancer drug, thus causing lower side effects and higher efficacy.  相似文献   

16.
The aim of this study was to develop colon-specific delivery systems for 5-aminosalicylic acid (5-ASA) using guar gum as a carrier. Core tablets containing 5-ASA were prepared by wet granulation with starch paste and were compression coated with coating formulations containing different quantities of guar gum (300, 200, 150, and 125 mg). In vitro drug release studies were carried out in simulated gastric and intestinal fluids and in pH 6.8 buffer containing rat cecal contents. The application of 175 mg of coating formulation containing 150 mg of guar gum over 5-ASA core tablets resulted in the release of less than 2% drug in simulated gastric and intestinal fluids and about 93% of 5-ASA in pH 6.8 buffer containing rat cecal contents. Differential scanning calorimetric (DSC) studies showed the absence of any interaction between 5-ASA and the excipients on storage at 45°C for 12 weeks. The study confirmed that selective delivery of 5-ASA to the colon can be achieved using guar gum as a carrier in the form of a compression coating over the drug core.  相似文献   

17.
The aim of this study was to develop colon-specific delivery systems for 5-aminosalicylic acid (5-ASA) using guar gum as a carrier. Core tablets containing 5-ASA were prepared by wet granulation with starch paste and were compression coated with coating formulations containing different quantities of guar gum (300, 200, 150, and 125 mg). In vitro drug release studies were carried out in simulated gastric and intestinal fluids and in pH 6.8 buffer containing rat cecal contents. The application of 175 mg of coating formulation containing 150 mg of guar gum over 5-ASA core tablets resulted in the release of less than 2% drug in simulated gastric and intestinal fluids and about 93% of 5-ASA in pH 6.8 buffer containing rat cecal contents. Differential scanning calorimetric (DSC) studies showed the absence of any interaction between 5-ASA and the excipients on storage at 45°C for 12 weeks. The study confirmed that selective delivery of 5-ASA to the colon can be achieved using guar gum as a carrier in the form of a compression coating over the drug core.  相似文献   

18.
Eudragit S100 coated microsponges for Colon targeting of prednisolone   总被引:1,自引:0,他引:1  
Context: Microsponge is a novel approach for targeting the drug to the colon for the management of colon ailments such as inflammatory bowel disease.

Objective: Prednisolone loaded microsponges (PLMs) were prepared and coated with Eudragit S 100 (ES) and evaluated for colon-specific drug delivery.

Materials and methods: PLMs were prepared using quasi emulsion solvent diffusion technique using ethyl cellulose, triethylcitrate (1% v/v, plasticizer) and polyvinyl alcohol (Mol. Wt. 72?kDa, emulsifying agent). The developed microsponges were compressed into tablets via direct compression technique using sodium carboxymethyl cellulose (Na CMC) and magnesium stearate as super-disintegrant and lubricant, respectively. The tablets were then coated with ES to provide protection against harsh gastric environment and manifest colon-specific drug release.

Results: PLMs were found to be nano-porous spherical microstructures with size around 35?µm and 86% drug encapsulation efficiency. Finally, they were compressed into tablets which were coated with Eudragit S 100 In vitro drug release from ES coated tablets was carried out at various simulated gastrointestinal fluids i.e. 1?hr in SGF (pH 1.2), 2 to 3?h in SIF (pH 4.6), 4–5?h in SIF (pH 6.8), and 6–24?h in SCF (pH 7.4) and the results showed the biphasic release pattern indicating prolonged release for about 24?h.

Discussion and conclusion: In vitro drug release studies revealed that drug starts releasing after 5?h by the time PLMs may enter into the proximal colon. Hence maximum amount of drug could be released in the colon that may result in reduction in dose and dose frequency as well as side effects of drug as observed with the conventional dosage form of prednisolone.  相似文献   

19.
A simple pH-controlled drug release system was successfully prepared by coating pH-sensitive polymer hydroxypropyl methylcellulose phthalate (HPMCP) on drug-loaded mesoporous SBA-15 tablet. Using famotidine (Famo) as a model drug, the effects of coating times and drying temperature on drug release were studied in detail to optimize the drug release system. In simulated gastric fluid (SGF, pH 1.2), it took only 2 h for Famo to be completely released from mesoporous silica tablet without HPMCP coating. Also in SGF, with the increase of coating times and drying temperature, the release of Famo was greatly delayed by HPMCP coating. For the tablet with twice coating of HPMCP and dried at 80 °C, only 4.0 wt.% of Famo could be released within 4 h. However, in simulated intestinal fluid (SIF, pH 7.4), HPMCP coating did not show obvious effect on the release of Famo.  相似文献   

20.
Abstract

Enteric-coated epichlorohydrin crosslinked dextran microspheres containing 5-Fluorouracil (5-FU) for colon drug delivery was prepared by emulsification-crosslinking method. The formulation variables studied includes different molecular weights of dextran, volume of crosslinking agent, stirring speed, time and temperature. Dextran microspheres showed mean entrapment efficiencies ranging between 77 and 87% and mean particle size ranging between 10 and 25?µm. About 90% of drug was released from uncoated dextran microspheres within 8?h, suggesting the fast release and indicated the drug loaded in uncoated microspheres, released before they reached colon. Enteric coating (Eudragit-S-100 and Eudragit-L-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method. The release study of 5-FU from coated dextran microspheres was complete retardation in simulated gastric fluid (pH 1.2) and once the coating layer of enteric polymer was dissolved at higher pH (7.4 and 6.8), a controlled release of the drug from the microspheres was observed. Further, the release of drug was found to be higher in the presence of dextranase and rat caecal contents, indicating the susceptibility of dextran microspheres to colonic enzymes. Organ distribution and pharmacokinetic study in albino rats was performed to establish the targeting potential of optimized formulation in the colon.  相似文献   

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