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以胰岛素为目标药物,以丝素(SF)和羟丙基壳聚糖(HPCS)为包药材料,复凝聚法制备SF-HPCS载药微球。采用红外光谱(FTIR)、扫描电镜(SEM)、X射线衍射(XRD)、热重分析(TGA)等对载药微球的结构、外部形貌及热性能等进行了表征。结果表明,所制备的载药微球表面密实,平均粒径22.4μm,呈正态分布;载药微球对胰岛素的包埋率达73.6%,大于HPCS载药微球(64.3%)及壳聚糖(CS)载药微球(57.1%);SF-HPCS载药微球在人工胃液中4h内累计释药率为21.3%,在人工肠液中24h内累计释药率达81.2%,48h累计释药率为92.2%,释放过程平稳、缓慢。 相似文献
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将聚乙二醇单甲醚(mPEG)醛化改性后,通过西佛碱反应接枝到自制的O-季铵化壳聚糖的NH2上,硼氢化钠还原制得N-mPEG接枝O-季铵化壳聚糖(QACS-mPEG),反相悬浮法制备二乙烯基砜交联QACS-mPEG微球。用FTIR、1 H NMR、EA和SEM对产物进行表征,并且以酮洛芬为模型药物研究微球的载药性能及释放行为。结果表明,mPEG和季铵盐基团的引入提高了N-mPEG-O-季铵化壳聚糖微球的载药量,为4.31mg/mg;载药N-mPEG-O-季铵化壳聚糖微球在模拟肠液的缓释效果优于胃液,微球释药具有pH响应性。 相似文献
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利用毛细管共挤出技术结合静电吸附和仿生硅化的方法,制备了海藻酸钙-壳聚糖/精蛋白/二氧化硅(ACPSi)复合微胶囊。ACPSi复合微胶囊的平均粒径约3.18 mm,单分散性好,囊壁最外层的二氧化硅层可抑制其在肠液pH环境中的溶胀,增强囊的机械稳定性。将羟丙甲基纤维素邻苯二甲酸酯(HPMCP)肠溶微球作为释药“微阀门”,嵌入囊壁可以更好地控制微胶囊的释药行为。以吲哚美辛为模型药物,当药物浓度为22.5 mg/ml时,ACPSi载药微胶囊在pH 2.5模拟胃液中3 h时累计释药率仅为0.33%,而转移至pH 6.8模拟肠液中19 h时累计释药率为77.78%;囊壁嵌入HPMCP微球后,22 h时累计释药率可提高约4%。因此,该复合微胶囊具有良好的肠靶向作用和控释特性,作为口服肠靶向缓控释制剂具有良好的应用前景。 相似文献
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针对口服给药体系如何保护药物分子免受人体内环境影响这一挑战,采用乳化凝胶法设计合成了一种pH值敏感性的海藻酸钠(SA)-蒙脱石(MMT)复合微球MMT/SA,用以负载抗癌药物盐酸阿霉素(DOX),在保护药物分子的同时克服了胃肠道的生物化学屏障。探索了MMT处理工艺和合成配比的不同对微球形貌的影响,最终控制微球尺寸在20μm以内,且分布均一。复合载药微球DOX/MMT/SA的载药率为14.7%,在模拟人工胃液和人工肠液环境中表现出不同的药物缓释效果,在模拟人工肠液中的累计释放率(31.7%)明显高于在人工胃液中的释放率(15.8%),且对人结肠癌细胞有明显的杀伤效果。 相似文献
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针对穿心莲内酯(AND)口服给药存在药物苦极问题,拟制备一种有效掩蔽药物苦味且能实现药物控释的微球载体。以海藻酸钠(Na-Alg)和N-异丙基丙烯酰胺(NIPAM)为制备材料,采用静电液滴偶联单体聚合工艺制备了核-壳型AND/Ca-Alg/pNIPAM微球。采用扫描电微观测、红外光谱分析、溶胀实验和体外释药实验等表征微球结构与性能。结果表明:与Ca-Alg微球相比,Ca-Alg/pNIPAM微球具有清晰的核-壳结构;微球平衡溶胀率在32—36℃突降14.6%;微球在模拟胃液中2 h内药物累积释放率低于10%,而在模拟肠液中6—8 h即达到释放平衡且释药动力学符合Reter-Peppas模型。核-壳结构使Ca-Alg/pNIPAM微球在高效负载药物的同时掩蔽了药物苦味,并赋予微球温度/pH双重响应特性,实现了药物肠靶向释放。 相似文献
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以阿司匹林为药物模型分子,制备了载阿司匹林明胶微球。SEM研究表明,明胶微球在载药后,表面结构变得更为紧实。载药性能探讨表明,当阿司匹林的投药量为16mg时,明胶微球的载药性能较优(载药量为7.3%,包封率为57.5%)。对明胶微球在人工体液中的释药性能研究显示,载阿司匹林明胶微球具有良好的缓释性能。由于具有较大的酸性和胃蛋白酶的存在,微球在人工胃液中药物释放效率较高,在人工胃液和人工肠液中药物的释放率分别为40%和28%,且一级动力学模型对微球的体外药物释放情况拟合度较高。 相似文献
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针对氧化锌易被仔猪胃里的酸性胃液分解,导致饲料中的氧化锌添加量较高,对环境造成污染,长期使用反而会抑制仔猪的生长的情况,以海藻酸钠为载体,制备了海藻酸钠肠溶包被氧化锌微球。考察了各组分配比对药物粒径、收率、载药量、包封率及在胃液和肠液中释放时间的影响。结果表明,较为理想的微球的配方为:海藻酸钠、氯化钙、壳聚糖的质量分数分别为3%、3%、0.25%,氧化锌投加质量分数为10%。所制得的微球在形态、粒径、包封率、体外释放溶出的实验等方面均表现优秀,在pH为6.8的模拟肠液中,所制得微球在0.5 h内的释药量大于80%。 相似文献
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采用双乳化-凝胶法制备了单分散的海藻酸钙凝胶微球,并通过正交试验系统考察了海藻酸钠浓度、氯化钙浓度、表面活性剂浓度、搅拌速度和油水比对海藻酸钙凝胶微球粒径及形貌的影响。在优化的条件下,制备出了平均粒径为4μm、单分散和球形度好的海藻酸钙凝胶微球。包埋模型药物牛血清白蛋白(BSA)的过程中,以去离子水作为洗涤液洗涤海藻酸钙微球时,BSA的包封率仅为13%左右;当水洗液的pH值为3.2时,BSA的包封率提高到66%左右,载药率可达16%,这是海藻酸钙pH值响应溶胀和BSA与海藻酸盐之间静电作用的结果。微球中BSA的体外释放曲线表明,该系统具有在模拟胃液中释药速率慢、释药量低、模拟肠液中释药迅速的特性。因此,双乳化-凝胶法制备海藻酸钙微球有望成为制备蛋白类药物控释制剂的一种新方法,以达到靶向快速给药的目的。 相似文献
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可生物降解药物载体——纳米/亚微米壳聚糖微球的制备及性能 总被引:9,自引:2,他引:9
利用聚电解质的离子凝胶反应,在溶液中壳聚糖为聚阳离子电解质与带反相电荷的聚阴离子三聚磷酸钠(TPP)发生离子凝胶反应,在合适的浓度和适当的搅拌速度下,得到亚微米级的壳聚糖微球。利用环己烷作为油相,以壳聚糖溶液为水相,配制澄清透明的W/O反相微乳清液,滴加质量浓度为5mg/mL的TPP溶液于已配制好的微乳清液中,制得纳米级壳聚糖微球。采用上述两种方法制得的纳米/亚微米壳聚糖微球用作生物降解药物载体,载药实验结果表明,释放初期无明显暴释现象,具有良好的药物缓释作用。 相似文献
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B. Yerri Swamy C. Venkata Prasad C. L. N. Reddy P. Sudhakara Ildoo Chung M. C. S. Subha K. Chowdoji Rao 《应用聚合物科学杂志》2012,125(1):555-561
Sodium alginate (NaAlg)/poly (vinyl alcohol) (PVA) blend microspheres (MS) were prepared by water-in-oil (w/o) emulsion method. These polymer microspheres were crosslinked with glutaraldehyde and loaded with metformin hydrochloride (MHC). The microspheres were characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and X-ray diffraction (XRD) analysis to confirm the molecular dispersion of the drug, thermal stability, morphological properties, and crystallinity of the polymer matrix before and after blending. SEM of the microspheres suggested the formation of microspheres in spherical structure. Drug release data were analyzed using an empirical equation to understand the nature of drug transport through polymeric matrices. The controlled release (CR) characteristics of the polymer matrices was investigated in pH 7.4 media and from the results it was obtained that the drug was released in controlled manner up to 10 h. The physico-chemical properties of the microspheres were studied by calculating drug entrapment efficiency and drug release kinetics. Percent of encapsulation efficiency (% EE) decreased with increase in crosslinking agent (GA) and PVA content in the microspheres. The optimum % EE (80%) was observed in case of MS containing 40% of PVA with 15% MHC. The release profiles indicate that the release of MHC decreases with increasing the PVA/NaAlg (w/w) and drug/polymer ratio. At the end of 10 h, the highest release of MHC was found to be 96% for MS containing PVA/NaAlg (40 : 60) and 15 wt % drug loaded. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012 相似文献
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V. Ramesh Babu K. S. V. Krishna Rao M. Sairam B. Vijaya Kumar Naidu Kallappa M. Hosamani Tejraj M. Aminabhavi 《应用聚合物科学杂志》2006,99(5):2671-2678
pH‐Sensitive interpenetrating network (IPN) microgels (MGs) of sodium alginate (NaAlg) and acrylic acid have been prepared by using water‐in‐oil (W/O) emulsion technique. The MGs were characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X‐ray diffractometer (X‐RD). The release of ibuprofen (IB), an anti‐inflammatory drug, from these MGs was studied in pH 1.2 and 7.4 media. MG network consists of NaAlg, which disintegrates in the intestinal fluid, while poly(acrylic acid) provides pH‐sensitivity to the microgel network. The system developed in this study showed a pH‐sensitivity for the release of IB, which was attributed to the diffusion controlled release of the drug through the surfaces of MGs that undergo disintegration after swelling, depending upon the chemical composition of MGs and pH of the medium. © 2005 Wiley Periodicals, Inc. J Appl Polym Sci, 2006 相似文献
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双丙酮丙烯酰胺与海藻酸钠接枝聚合制备双亲性药物载体 总被引:1,自引:0,他引:1
双丙酮丙烯酰胺(DAAM)与海藻酸钠(SA)进行接枝聚合反应,过硫酸钾作为引发剂,制备了海藻酸钠-双丙酮丙烯酰胺两亲性共聚物,接枝率可以达到43%,该产物在水相中发生自聚集,形成直径300~500 nm的胶束。用红外光谱(FTIR)、热重分析(TGA)、荧光光谱(FS)、元素分析(EA)、扫描电镜(SEM)和Zeta电位对产物进行了表征。结果表明,胶体粒子表面带负电荷,在水中分散,结构稳定。将其用钙离子交联后形成凝胶,对于模型药物布洛芬(ibuprofen)有较好的负载率和缓释行为,载药率可以达到12%。 相似文献
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用溶液共混法制备聚乙烯醇-海藻酸钠(PVA-SA)复合微球,考察了SA质量分数、PVA质量分数、CaCl2质量分数、m(PVA)/m(SA)和干燥方式对PVA-SA复合微球制备的影响,并测定了微球的含水率、溶胀率、载药量和包封率,通过红外光谱(FTIR)对微球进行了表征,研究了不同m(PVA)/m(SA)的PVA-SA复合微球对药物的缓释作用。结果表明,SA质量分数为6%,PVA质量分数为10%,CaCl2质量分数为5%,m(PVA)/m(SA)为1∶3时,可以制备出各项性能较好的微球,其载药率30.24%,包封率90.11%,并且有良好的缓释效果。 相似文献
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Carboxymethyl chitosan sodium salt (CMCS)/sodium alginate (SA), a pH-sensitive hydrogel composed of CMCS and SA crosslinked by 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide (EDC) and N-hydroxysuccinimide, has been evaluated in vitro as a potential carrier for protein drug delivery of bovine serum albumin (BSA). The crosslinked structures, pore morphologies, and mechanical properties of the composite CMCS/SA hydrogel at different pH have been characterized by Fourier-transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and dynamic mechanical analysis (DMA). The swelling behavior of the prepared hydrogel was assessed at different pH values, 1.2, 4.0, 6.86, 7.4, and 9.0. The in vitro slow release ability of the CMCS/SA hydrogel was assessed at 37°C and pH 1.2 or pH 7.4 to simulate gastrointestinal and mouth environments in vivo. The efficiency was found to be greater than 90% at pH 7.4. The composite CMCS/SA hydrogel showed no cytotoxic effect toward L-929 cells according to the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test. These findings demonstrate that the composite hydrogel has promising potential for drug delivery. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019 , 136, 46911. 相似文献
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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 相似文献
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Juan C. Sánchez‐Díaz Fausto Becerra‐Bracamontes Alejandro González‐Álvarez L. Emilio Cruz‐Barba Agustín Martínez‐Ruvalcaba 《应用聚合物科学杂志》2010,117(6):3595-3600
An ionically crosslinked polymer network composed of chitosan and sodium hexametaphosphate (SHMP) was synthesized to determine their swelling and ascorbic acid release kinetics at various SHMP concentrations. The chitosan/SHMP hydrogels were synthesized using an acetic acid aqueous solution (1% v/v). Ionization constants (pKb) of the SHMP were obtained by potentiometric titration. The results show that the SHMP was hydrolyzed in acidic medium forming orthophosphate and trimetaphosphate. The swelling percentages were measured at different swelling media pH's; the higher swelling capacities were for the systems that were swollen in neutral solution. Also, it was studied the ionic crosslinking degree by turbidimetric titration, comparing the electrostatic interactions between the chitosan and the SHMP; the results shows that electrostatic interactions between the amine groups of the chitosan and the anionic groups of the SHMP are dependent of the swelling medium pH. The ascorbic acid diffusion inside the hydrogel follows the second law of Fick, and the diffusion coefficients were obtained for different SHMP concentrations. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2010 相似文献