Characterization of pH-responsive hydrogels of poly(itaconic acid-g-ethylene glycol) prepared by UV-initiated free radical polymerization as biomaterials for oral delivery of bioactive agents.
Characterization of pH-responsive hydrogels of poly(itaconic acid-g-ethylene glycol) prepared by UV-initiated free radical polymerization as biomaterials for oral delivery of bioactive agents.
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DOI：
10.1002/jbm.a.32510
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发表时间：
2010-04
影响因子：
4.9
通讯作者：
Peppas, Nicholas A.
中科院分区：
文献类型：
--
作者：
Betancourt, Tania;Pardo, Juan;Soo, Ken;Peppas, Nicholas A.
蛋白质的有效口服递送受到胃肠道中陡峭的pH梯度和蛋白水解酶以及由于其大小、电荷或溶解度导致的蛋白质进入血流的低吸收的阻碍。本工作合成了pH响应性聚衣康酸与聚乙二醇接枝复合水凝胶，并将其应用于口服给药。这些水凝胶预期在低pH下由于聚（衣康酸）羧基和聚（乙二醇）之间的氢键而处于塌陷构型，并且由于去质子化的羧酸基团之间的电荷排斥而随着pH增加而溶胀。使用四甘醇作为交联剂和Irgacure® 2959作为引发剂，通过UV引发的自由基聚合制备水凝胶。考察了单体配比、交联度和溶剂用量对水凝胶性能的影响。通过FTIR证实了水凝胶的组成。平衡溶胀的pH值范围为1.2至7的研究表明，溶胀的程度随着pH值的增加而增加，直到pH值约为6时，没有进一步的羧酸去质子化发生。在Caco-2结肠直肠癌细胞中的研究证实了这些材料在高达5 mg/ml浓度下的细胞相容性。
Effective oral delivery of proteins is impeded by steep pH gradients and proteolytic enzymes in the gastrointestinal tract, as well as low absorption of the proteins into the bloodstream due to their size, charge or solubility. In the present work, pH-responsive complexation hydrogels of poly(itaconic acid) with poly(ethylene glycol) grafts were synthesized for applications in oral drug delivery. These hydrogels were expected to be in collapsed configuration at low pH due to hydrogen bonding between poly(itaconic acid) carboxyl groups and poly(ethylene glycol), and to swell with increasing pH because of charge repulsion between deprotonated carboxylic acid groups. Hydrogels were prepared by UV-initiated free radical polymerization using tetraethylene glycol as the crosslinking agent and Irgacure® 2959 as the initiator. The effect of monomer ratios, crosslinking ratio and solvent amount on the properties of the hydrogels were investigated. The composition of the hydrogels was confirmed by FTIR. Equilibrium swelling studies in the pH range of 1.2 to 7 revealed that the extent of swelling increased with increasing pH up to a pH of about 6, when no further carboxylic acid deprotonation occurred. Studies in Caco-2 colorectal carcinoma cells confirmed the cytocompatibility of these materials at concentrations of up to 5 mg/ml.
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影响因子：
10.8
作者：
Torres-Lugo, M;García, M;Peppas, NA
通讯作者：
Peppas, NA
影响因子：
3
作者：
Jeria-Orell, M;Pizarro, GDC;Geckeler, KE
通讯作者：
Geckeler, KE
影响因子：
4
作者：
NAGAI, S
通讯作者：
NAGAI, S
DOI：
10.1016/j.ejpb.2005.10.011
发表时间：
2006-05-01
影响因子：
4.9
作者：
Serra, L;Doménech, J;Peppas, NA
通讯作者：
Peppas, NA
影响因子：
6
作者：
Stanojevic, M;Krusic, MK;Stupar, M
通讯作者：
Stupar, M