Mechanism of Drug Release From Temperature-Sensitive Formulations Composed of Low-Melting- Point Microcrystalline Wax
Mechanism of Drug Release From Temperature-Sensitive Formulations Composed of Low-Melting- Point Microcrystalline Wax
复制标题
低熔点微晶蜡温敏制剂的药物释放机制
DOI：
10.1016/j.xphs.2019.01.010
复制
发表时间：
2019
影响因子：
3.8
通讯作者：
Iwao Y.
中科院分区：
文献类型：
--
作者：
Matsumoto K;Kimura SI;Noguchi S;Itai S;Kondo H;Iwao Y.
据报道，由低熔点微晶蜡组成的蜡骨架(WM)颗粒表现出独特的释放行为，在37℃时只释放少量的包埋药物(非扩散控制释放)，而在25℃时以扩散控制的方式释放药物，但药物释放的机制尚不清楚。本研究的目的是利用X射线计算机断层扫描技术确定WM颗粒的药物释放机制。在25℃溶出试验中收集的WM颗粒中，药物释放产生的空隙随着时间的增加而增加，结构没有变化，表明WM颗粒在25℃下释放药物的同时保持了颗粒的形状。在37℃溶出试验中，在初始时间点确定了空隙空间，但在随后的时间点，空隙空间消失了，表面粗糙明显。这种结构变化可能阻碍了外部介质的运输途径，从而抑制了药物的释放。WM颗粒在两个温度下的药物释放机制之间的差异将对开发冷却触发的温度敏感型制剂具有价值。
It was reported that wax matrix (WM) particles composed of low-melting-point microcrystalline wax showed unique release behaviors; the particles released only a small amount of the entrapped drug (non–diffusion-controlled release) at 37°C, whereas it showed comparatively fast drug release in a diffusion-controlled manner at 25°C. However, the mechanism of the drug release is still unclear. The objective of this study was to determine the mechanism of drug release from the WM particles using X-ray computed tomography. In the WM particles collected during dissolution tests at 25°C, the void space derived from drug release increased with increasing time, and there was no change in the structure, indicating that the WM particles released drug while maintaining the particle shape at 25°C. In the WM particles collected during dissolution tests at 37°C, the void space was confirmed at initial time point; however, at subsequent time points, the void space was disappeared, and the roughness of the surface was evident. This structural change may have blocked the conveyance pathway of the outer medium, which would inhibit the drug release. The difference between the drug-release mechanisms of the WM particles at the 2 temperatures will be valuable for developing cooling-triggered, temperature-sensitive formulations.