pH、离子强度敏感性壳聚糖水凝胶的合成及其对辅酶A的控制释放

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.     

海藻酸钠-g-聚丙烯酰胺/氧化石墨烯复合水凝胶的制备及控释行为

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。     

海藻酸钠-g-聚丙烯酰胺/氧化石墨烯复合水凝胶的制备及控释行为EI北大核心CSCD

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。     

pH敏感型海藻酸钙多孔凝胶微球的制备及溶胀性能的研究

以海藻酸钠作为基材,制备了一种在pH值为7.4环境下具有敏感性的多孔水凝胶微球。通过正交试验得到了较佳的制备条件为:海藻酸钠溶液浓度为2%(质量分数),氯化钙溶液浓度为3%(质量分数),水浴温度为60℃,保温时间为40min。在此条件下制得的凝胶微球,在pH值为7.4(结肠pH值环境)的磷酸盐缓冲溶液中溶胀30min后,溶胀比可达21.8;而在去离子水(pH值6左右)和pH值1.2(胃液pH值环境)的缓冲溶液中同样时间的溶胀比仅为1.5。通过添加不同类型和浓度的成孔剂,如PEG200、NaCl等,提高了凝胶微球的溶胀响应速率。结果表明,在没有成孔剂存在的条件下,此凝胶微球在pH值为7.4的缓冲溶液中溶胀到最大溶胀比所需时间为30min,而在添加了适量PEG200、NaCl后,均提高了其溶胀响应速率,分别在10、15min即可达到最大溶胀比。     

聚丙烯酸/活性炭复合凝胶的制备及溶胀行为

采用自由基溶液聚合的方法,以过硫酸铵(APS)为引发剂,N,N′-亚甲基双丙烯酰胺(NNMBA)为交联剂,制备了聚丙烯酸(PAA)复合活性炭凝胶(PAA/AC)。考察了凝胶在生理盐水和不同pH值缓冲溶液中的平衡溶胀比及溶胀动力学,结果表明,活性炭能有效提高PAA凝胶的平衡溶胀比。蒸馏水中PAA/AC凝胶的平衡溶胀比可达到303(g/g),约为PAA凝胶平衡溶胀比的2.3倍;生理盐水(0.9%g/mL NaCl水溶液)中PAA/AC凝胶的平衡溶胀比可达到60(g/g),约为PAA凝胶平衡溶胀比的2.4倍;在实验设计的pH范围内PAA/AC凝胶的平衡溶胀比比PAA凝胶更高,具有更好的pH值敏感特性。     

超大孔水凝胶P(AA-co-DMAA)的制备及释放性能

以丙烯酸(AA)和N,N-二甲基丙烯酰胺(DMAA)为单体,采用泡沫分散聚合法制备P(AA-co-DMAA)超大孔水凝胶及载有盐酸小檗碱的载药凝胶,研究单体配比、温度、pH值和NaCl浓度对载药凝胶释放性能的影响。结果表明,凝胶具有超大孔结构及pH敏感性;n(AA)∶n(DMAA)=1∶1的载药凝胶释放率最小;升高温度使载药凝胶的释放率增大;在pH=1的HCl溶液和pH=6.8的磷酸盐缓冲溶液中,载药凝胶释放率远大于蒸馏水;NaCl溶液浓度越大,载药凝胶的释放率越大。     

pH敏感水凝胶PMAA对布洛芬的控制释放

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...     

聚甲基丙烯酸-N,N-二甲氨基乙酯/聚乙烯醇半互穿网络水凝胶的溶胀行为

以甲基丙烯酸-N,N-二甲氨基乙酯(DMAEMA)和聚乙烯醇(PVA)为原料,通过自由基聚合法制备了一系列半互穿网络水凝胶(PDVA)。研究了原料配比对该系列半互穿网络水凝胶最低临界溶解温度(LCST)的影响,以及介质pH值、温度对半互穿网络水凝胶溶胀行为的影响。结果表明,PVDA系列半互穿网络水凝胶的LCST随PVA含量的增加而升高,在酸性和碱性条件下该系列水凝胶的溶胀度与温度之间的变化关系恰恰相反;当温度低于LCST时,水凝胶的溶胀度随介质pH值的增大呈现先增大后减小的变化趋势,而当温度高于LCST时,PDVA系列水凝胶的溶胀度几乎不随介质pH值的变化而变化。     

形状记忆型水凝胶的制备及其在药物控制释放中的应用

以戊二醛为交联剂,制备了pH敏感性明胶-果胶水凝胶(GT-PT)和明胶-辛基果胶水凝胶(GT-OPT),研究了交联剂用量、温度、pH值对凝胶溶胀性能的影响及溶胀-消溶胀性能。结果表明,当温度在30～60℃时,凝胶的溶胀率随温度的升高而增大;且具有明显的pH敏感性,碱性条件下的溶胀率大于酸性条件下的溶胀率;不同pH值条件下,明胶-果胶水凝胶具有"形状记忆"功能。包埋在水凝胶中的牛血清蛋白在pH=1.0时的释药率大于pH=7.8和pH=9.18时的释药率。此类水凝胶有望用于蛋白质的pH值及温度控制释放。     

pH敏感性壳聚糖/聚乙烯醇水凝胶的制备及其性能研究

制备了pH敏感性壳聚糖/聚乙烯醇(CS-PVA)水凝胶,研究了该水凝胶在室温下不同pH值介质中的溶胀比。发现在酸性溶液中,凝胶的溶胀比远大于在碱性溶液中的溶胀比,且其在不同pH值溶液中具有可逆溶胀-收缩行为,对药物氟哌酸具有缓释效果。     

壳聚糖透明质酸复合水凝胶的制备及性能

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。     

In vitro release dynamics of model drugs from psyllium and acrylic acid based hydrogels for the use in colon specific drug delivery

Psyllium is medicinally important gel forming polysaccharides. Keeping in view, the pharmacological importance of psyllium and drug delivery devices based on hydrogels, psyllium, if suitably tailored to prepare the hydrogels, can act as the double potential candidates for the novel drug delivery systems. Therefore, it is an attempt to prepared psyllium and acrylic acid based pH sensitive novel hydrogels by using N,N'-methylenebisacrylamide (N,N-MBAAm) as crosslinker and ammonium persulfate (APS) as initiator for the use in colon specific drug delivery. The present paper discusses the swelling kinetics of the hydrogels and release dynamics of model drugs (tetracycline hydrochloride, insulin and tyrosine) from drug-loaded hydrogels, for the evaluation of the swelling mechanism and drug release mechanism from the polymeric networks .The effect of pH on the swelling kinetics and release pattern of drugs have been studied by varying the pH of the release medium. It has been observed that swelling and release of drugs from the hydrogels occurred through non-Fickian or anomalous diffusion mechanism in distilled water and pH 7.4 buffer. It shows that the rate of polymer chain relaxation and the rate of drug diffusion from these hydrogels are comparable.     

Preparation and characterization of hybrid pH-sensitive hydrogels of chitosan-co-acrylic acid for controlled release of verapamil

In the present work crosslinked hydrogels based on chitosan (CS) and acrylic acid (AA) were prepared by free radical polymerization with various feed compositions using N,N methylenebisacrylamide (MBA) as crosslinking agent. Benzoyl peroxide was used as catalyst. Fourier transform infrared spectra (FTIR) confirmed the formation of the crosslinked hydrogels. This hydrogel is formed due to electrostatic interaction between cationic groups in CS and anionic groups in AA. Prepared hydrogels were used for dynamic and equilibrium swelling studies. For swelling behavior, effect of pH, polymeric and monomeric compositions and degree of crosslinking were investigated. Swelling studies were performed in USP phosphate buffer solutions of varying pH 1.2, 5.5, 6.5 and 7.5. Results showed that swelling increased by increasing AA contents in structure of hydrogels in solutions of higher pH values. This is due to the presence of more carboxylic groups available for ionization. On the other hand by increasing the chitosan content swelling increased in a solution of acidic pH, but this swelling was not significant and it is due to ionization of amine groups present in the structure of hydrogel. Swelling decreased with increase in crosslinking ratio owing to tighter hydrogel structure. Porosity and sol-gel fraction were also measured. With increase in CS and AA contents porosity and gel fraction increased, whereas by increasing MBA content porosity decreased and gel fraction increased. Furthermore, diffusion coefficient (D) and the network parameters i.e., the average molecular weight between crosslinks (M_c), polymer volume fraction in swollen state (V_2s), number of repeating units between crosslinks (M_r) and crosslinking density (q) were calculated using Flory-Rehner theory. Selected samples were loaded with a model drug verapamil. Release of verapamil depends on the ratios of CS/AA, degree of crosslinking and pH of the medium. The release mechanisms were studied by fitting experimental data to model equations and calculating the corresponding parameters. The result showed that the kinetics of drug release from the hydrogels in both pH 1.2 and 7.5 buffer solutions was mainly non-Fickian diffusion.     

Synthesis and characterization of a pH/temperature responsive glycine-mediated hydrogel for drug release

In this work, a pH/temperature responsive hydrogel (PMEA) from N-acryloylglycine methyl ester (NAGME), N-acryloylglycine ethyl ester (NAGEE), and acrylic acid (AAc) was synthesized by free radical polymerization. The swelling behaviors and drug release properties of hydrogels were systematically investigated at different temperature, pH, and AAc content. It was found that the hydrogel PMEA demonstrated pH and temperature responsive nature. The caffeine-release behaviors showed that only 49.1% caffeine was released from PMEA in pH 2.70 phosphate buffer solution (PBS) after 500 minutes, whereas more than 93.9% caffeine was gradually diffused into the medium in pH 7.49 PBS over the same time interval. In addition, the caffeine release was much higher at 37°C than that at 14°C in deionized water. As seen from the results, the PMEA seems to be a potential drug carrier with pH-temperature responsiveness.     

聚丙烯酸类水凝胶的制备及其在碱性溶液中的pH敏感性

以（NH₄）₂S₂O₈和NaHSO₃为氧化-还原引发剂、N,N′-亚甲基双丙烯酰胺（MBA）为交联剂,采用自由基水溶液聚合方法,分别合成了聚丙烯酸（PAAc）、聚丙烯酰胺（PAAm）和系列丙烯酸（AAc）质量分数（fAAc）不同的聚（丙烯酸-co-丙烯酰胺）（P（AAc-co-AAm））水凝胶。进而分别对其在碱性缓冲溶液和NaOH溶液中的pH敏感行为进行了探讨。结果表明,PAAc和P（AAc-co-AAm）凝胶在2种溶液中均具有优良的pH响应行为,且在NaOH溶液中的溶胀比大于缓冲溶液中;而PAAm凝胶仅在NaOH溶液中具有pH敏感性。2种溶液中,随f（AAc）的增加,P（AAc-co-AAm）凝胶的平衡溶胀比（ESR）增大;但在缓冲溶液中,当f（AAc）≥20%时,P（AAc-co-AAm）凝胶的溶胀行为与PAAc相似,而当f（AAc）<20%时,其溶胀则同时表现出PAAc和PAAm凝胶的溶胀特性。溶胀机理分析表明,凝胶的溶胀主要受聚合物网络内静电排斥作用和离子屏蔽效应控制。     

Swelling behavior of polyacrylamide/laponite clay nanocomposite hydrogels: pH-sensitive property

In this study, an investigation is carried out on the influence of varying clay contents (25–43%), pH values (2–11 buffer solutions), heat treatment, temperatures (25–60 °C) and ionic strengths (saline solution, 10^?7–0.1 M) on the water absorbency of polyacrylamide (PAAm)/laponite nanocomposite (NC) hydrogels in the absence of polyelectrolyte. For the influence of pH value on swelling behaviors, a maximum swelling ratio occurs at pH 11. Heat treatment of the hydrogels significantly improved the swelling capacity and created an obvious pH sensitive area (pH 3–4). The swelling capacity of the hydrogels was enhanced by increasing the temperature of the absorbing media. The results of swelling at different ionic strengths also indicate that the ionic strength can considerably weaken the swelling abilities of the NC hydrogels.     

Synthesis and characterization of a pH/temperature responsive glycine-mediated hydrogel for drug release

In this work, a pH/temperature responsive hydrogel (PMEA) from N-acryloylglycine methyl ester (NAGME), N-acryloylglycine ethyl ester (NAGEE), and acrylic acid (AAc) was synthesized by free radical polymerization. The swelling behaviors and drug release properties of hydrogels were systematically investigated at different temperature, pH, and AAc content. It was found that the hydrogel PMEA demonstrated pH and temperature responsive nature. The caffeine-release behaviors showed that only 49.1% caffeine was released from PMEA in pH 2.70 phosphate buffer solution (PBS) after 500 minutes, whereas more than 93.9% caffeine was gradually diffused into the medium in pH 7.49 PBS over the same time interval. In addition, the caffeine release was much higher at 37°C than that at 14°C in deionized water. As seen from the results, the PMEA seems to be a potential drug carrier with pH-temperature responsiveness.