Chitosan/Polyethylene Glycol Beads Crosslinked with Tripolyphosphate and Glutaraldehyde for Gastrointestinal Drug Delivery
Chitosan/Polyethylene Glycol Beads Crosslinked with Tripolyphosphate and Glutaraldehyde for Gastrointestinal Drug Delivery
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DOI：
10.1208/s12249-010-9483-z
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发表时间：
2010-09-01
影响因子：
3.3
通讯作者：
Muangsin, Nongnuj
中科院分区：
文献类型：
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作者：
Buranachai, Thawachinee;Praphairaksit, Nalena;Muangsin, Nongnuj
本研究报告了使用双氯芬酸钠（DFNa）作为模型药物制备壳聚糖（CS）/聚乙二醇（PEG）水凝胶珠。在优化聚合物与药物的比例后，通过与三聚磷酸钠（TPP）进行离子交联来修饰壳聚糖珠。 CS/PEG/DFNa 珠子的 (w/w/w) 比例为 1/0.5/0.5，在 pH 6.0 的 10% (w/v) TPP 中交联 30 分钟，产生优异的 DFNa 封装水平，负载效率超过 90%。 CS/PEG/DFNa 珠中 DFNa 的溶出曲线表明，该制剂能够维持约 8 小时的延长药物释放。在测试的制剂中，与 TPP（10%（w/v）30 分钟）和戊二醛（GD）（5%（w/v））组合交联的 CS/PEG/DFNa（1/0.5/1（w/w/w））珠能够在胃和十二指肠模拟液（pH 分别为 1.2 和 6.8）中提供最小的 DFNa 释放，从而在 24 小时内基本上逐渐释放药物。肠道（空肠和回肠）模拟液体（pH 7.4）。因此，总体而言，与 TPP 和 GD 交联的 CS/PEG 珠看起来是一种有前途的新型替代胃肠道药物释放系统。
This study reports on the preparation of chitosan (CS)/polyethylene glycol (PEG) hydrogel beads using sodium diclofenac (DFNa) as a model drug. Following the optimization of the polymer to drug ratio, the chitosan beads were modified by ionic crosslinking with sodium tripolyphosphate (TPP). The CS/PEG/DFNa beads obtained from a (w/w/w) ratio of 1/0.5/0.5 with crosslinking in 10% (w/v) TPP at pH 6.0 for 30 min yielded excellent DFNa encapsulation levels with over 90% loading efficiency. The dissolution profile of DFNa from CS/PEG/DFNa beads demonstrated that this formulation was able to maintain a prolonged drug release for approximately 8 h. Among the formulations tested, the CS/PEG/DFNa (1/0.5/1 (w/w/w)) beads crosslinked with a combination of TPP (10% (w/v) for 30 min) and glutaraldehyde (GD) (5% (w/v)) were able to provide minimal DFNa release in the gastric and duodenal simulated fluids (pH 1.2 and 6.8, respectively) allowing for a principally gradual drug release over 24 h in the intestinal (jejunum and ileum) simulated fluid (pH 7.4). Thus, overall the CS/PEG beads crosslinked with TPP and GD look to be a promising and novel alternative gastrointestinal drug release system.