Mishraki-Berkowitz Tehila, Aserin Abraham, Garti Nissim
The Ratner Chair in Chemistry, Casali Institute of Applied Chemistry, The Institute of Chemistry, The Hebrew University of Jerusalem, Edmond J. Safra Campus, Jerusalem 9190401, Israel.
The Ratner Chair in Chemistry, Casali Institute of Applied Chemistry, The Institute of Chemistry, The Hebrew University of Jerusalem, Edmond J. Safra Campus, Jerusalem 9190401, Israel.
J Colloid Interface Sci. 2017 Jan 15;486:184-193. doi: 10.1016/j.jcis.2016.09.074. Epub 2016 Sep 29.
Insulin loading into the H mesophases was examined as a function of its concentration, with addition of glycerol as a cosolvent and with addition of phosphatidylcholine (PC) as a structural stabilizer. The structural properties, the molecular interactions, the viscoelastic properties, and the dynamic behavior were investigated by SAXS, ATR-FTIR, and rheological measurements. Insulin release was then monitored and analyzed. Insulin incorporation into the H systems shrank the cylinders as it competed with the lipids in water-bonding. Insulin interrupted the interface while increasing τ and creating a more solid-like response. Upon addition of PC, cooperative flow behavior was detected, which is probably the reason for increase in insulin cumulative release from 28% to 52% after 300 min. In the presence of glycerol, the system was less cooperative but insulin was more compactly folded, resulting in a slight improvement in insulin release (up to 6%). Addition of both PC and glycerol caused the maximum release (55%). The addition of additives into the H system demonstrates how structural modifications can improve insulin release, and influence future design of encapsulated drug delivery systems.
研究了胰岛素在H中间相中的负载情况与其浓度的关系，同时添加甘油作为助溶剂以及磷脂酰胆碱（PC）作为结构稳定剂。通过小角X射线散射（SAXS）、衰减全反射傅里叶变换红外光谱（ATR-FTIR）和流变学测量研究了其结构性质、分子相互作用、粘弹性性质和动态行为。然后监测并分析胰岛素的释放情况。胰岛素掺入H体系会使圆柱体收缩，因为它在水合作用中与脂质竞争。胰岛素在增加τ的同时中断了界面，并产生了更类似固体的响应。添加PC后，检测到协同流动行为，这可能是300分钟后胰岛素累积释放从28%增加到52%的原因。在甘油存在的情况下，体系的协同性较差，但胰岛素折叠更紧密，导致胰岛素释放略有改善（高达6%）。同时添加PC和甘油导致最大释放量（55%）。向H体系中添加添加剂证明了结构修饰如何改善胰岛素释放，并影响未来包封药物递送系统的设计。
