Section of Pharmaceutical Technology Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, 15784 Athens, Greece.
Theoretical and Physical Chemistry Institute, National Hellenic Research Foundation, 11635 Athens, Greece.
Acta Pharm. 2020 Dec 1;70(4):527-538. doi: 10.2478/acph-2020-0037.
A variety of commonly used hydrogels were utilized in the preparation of calcium alginate beads, which incorporate the chronobiotic hormone melatonin (MLT). The in vitro release of the hormone in aqueous media at pH 1.2 and 6.8 was probed in the conjunction with the swelling of the beads and their thermal degradation properties. It has been found that the release of MLT from the beads was reversibly proportional to the extent of their expansion, which depends on the molecular mass/viscosity of the biopolymers present in the beads; the higher the molecular mass/viscosity of the hydrogels the greater the beads swelling and the less the MLT's release. Thermogravimetric analysis (TGA) data support the presence of the components in the hybrid hydrogel beads and elucidate their effects on the thermal stability of the systems. Thus, the physicochemical properties of the biopolymers used, along with their stereoelectronic features modulate the release of MLT from the beads, providing formulations able to treat sleep onset related problems or dysfunctions arising from poor sleep maintenance.
各种常用的水凝胶被用于制备海藻酸钙珠，其中包含生物钟激素褪黑素（MLT）。在 pH 值为 1.2 和 6.8 的水性介质中，研究了激素在珠内的体外释放以及珠的溶胀和热降解特性。研究发现，MLT 从珠中的释放与珠的膨胀程度成正比，而膨胀程度取决于珠中存在的生物聚合物的分子量/粘度；水凝胶的分子量/粘度越高，珠的溶胀越大，MLT 的释放越少。热重分析（TGA）数据支持了混合水凝胶珠中各成分的存在，并阐明了它们对体系热稳定性的影响。因此，所使用的生物聚合物的物理化学性质及其立体电子特性调节了 MLT 从珠中的释放，提供了能够治疗与睡眠开始相关的问题或因睡眠维持不良而引起的功能障碍的配方。
