Aiedeh Khaled M, Taha Mutasem O, Al-Hiari Yusuf, Bustanji Yasser, Alkhatib Hatim S
Faculty of Pharmacy, University of Jordan, Queen Rania St., Amman 11942, Jordan.
J Pharm Sci. 2007 Jan;96(1):38-43. doi: 10.1002/jps.20764.
Chitosan diacetate (CDA) was prepared by alkylating the amino moieties of chitosan with mono-iodoacetic acid. Subsequently, CDA was cross-linked with Al3+, Zn2+, and Ca2+ ions to yield three ionotropically crosslinked polymeric matrices. These composite matrices were characterized employing infrared spectroscopy (IR) and differential scanning calorimetry (DSC). Subsequently, they were loaded with caffeine, as a model drug, and were assessed as sustained release carriers by evaluating their caffeine release profiles. Interestingly, only CDA-Zn2+ complex sustained the release of caffeine effectively in a zero-order manner. The drug release and thermal behavior of the tested matrices agree with the relative strength of the ionic or coordination character of the bonds. This, in turn, depends on the position of the complexing ions on the electrophilic softness/hardness scale.
通过用一碘乙酸烷基化壳聚糖的氨基部分制备了二乙酸壳聚糖（CDA）。随后，CDA与Al3+、Zn2+和Ca2+离子交联，得到三种离子交联聚合物基质。采用红外光谱（IR）和差示扫描量热法（DSC）对这些复合基质进行了表征。随后，将它们负载咖啡因作为模型药物，并通过评估其咖啡因释放曲线来评价其作为缓释载体的性能。有趣的是，只有CDA-Zn2+络合物能以零级方式有效地维持咖啡因的释放。测试基质的药物释放和热行为与键的离子或配位特性的相对强度一致。反过来，这又取决于络合离子在亲电软度/硬度标度上的位置。
