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一种通过氧化还原策略来调节 Fe(III)-海藻酸钠气凝胶释放性能的方法,用于口服药物传递。

A redox strategy to tailor the release properties of Fe(III)-alginate aerogels for oral drug delivery.

机构信息

Department of Inorganic and Analytical Chemistry, University of Debrecen, Egyetem tér 1, Debrecen, Hungary.

Department of Physical Chemistry and Materials Science, University of Szeged, Rerrich B. tér 1, Szeged, Hungary.

出版信息

Carbohydr Polym. 2018 May 15;188:159-167. doi: 10.1016/j.carbpol.2018.01.098. Epub 2018 Feb 3.

DOI:10.1016/j.carbpol.2018.01.098
PMID:29525152
Abstract

Iron(III)-crosslinked alginate aerogel beads (d = 3-5 mm) were prepared and loaded with ibuprofen by using the technique of adsorptive deposition from supercritical CO. Additional formulations were prepared where the aerogels were co-impregnated by ibuprofen and ascorbic acid. The release of ibuprofen from the Fe(III)-alginate is much faster in pH = 7.4 (PBS) than in pH = 2.0 (HCl), which can be explained by the faster dissolution and higher swelling of the alginate matrix in PBS. By decreasing the size of the beads and using a higher G content alginate the release rate could be slightly increased. A marked acceleration of drug release was achieved in both HCl and PBS by incorporating ascorbic acid into the Fe(III)-alginate aerogel preparations. The explanation is that in aqueous media ascorbic acid in situ reduces the crosslinking Fe(III) to Fe(II). The latter does not interact strongly with alginate, which promotes the hydration of the chains, thus the erosion and dissolution of the carrier matrix.

摘要

铁(III)交联的海藻酸盐气凝胶珠(d=3-5mm)被制备并通过超临界 CO2 的吸附沉积技术负载布洛芬。还制备了其中气凝胶被布洛芬和抗坏血酸共同浸渍的制剂。在 pH=7.4(PBS)时,铁(III)-海藻酸盐中布洛芬的释放速度比在 pH=2.0(HCl)时快得多,这可以通过 PBS 中海藻酸盐基质更快的溶解和更高的溶胀来解释。通过减小珠粒的尺寸并使用更高 G 含量的海藻酸盐,可以略微提高释放速率。通过将抗坏血酸掺入 Fe(III)-海藻酸盐气凝胶制剂中,可以在 HCl 和 PBS 中明显加速药物释放。这是因为在水介质中,抗坏血酸原位将交联的 Fe(III)还原为 Fe(II)。后者与海藻酸盐的相互作用不强,促进了链的水合作用,从而促进了载体基质的侵蚀和溶解。

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