In vivo temperature-sensitive drug release system trigged by cooling using low-melting-point microcrystalline wax
In vivo temperature-sensitive drug release system trigged by cooling using low-melting-point microcrystalline wax
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DOI：
10.1016/j.jconrel.2019.04.029
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发表时间：
2019-06-10
影响因子：
10.8
通讯作者：
Iwao, Yasunori
中科院分区：
文献类型：
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作者：
Matsumoto, Kohei;Kimura, Shin-ichiro;Iwao, Yasunori
温度敏感制剂是一种有吸引力的控释制剂，它通过外部温度刺激引起的体温变化释放掺入的药物。最近，有报道称，由低熔点微晶蜡（MCW）组成的蜡基质（WM）颗粒在37℃时仅释放少量药物，而在25℃时药物释放速度更快。本研究开发了由低熔点微晶蜡组成的温度敏感配方，该配方通过冷却而不是加热触发药物释放。在体外溶出试验中，将试验介质从37℃反复冷却至25℃，实现了促进和抑制药物释放的控制。经冷却处理的大鼠血浆中药物浓度明显高于未冷却处理的大鼠，表明在体外和体内冷却均促进了药物的释放。因此，由低熔点MCW组成的颗粒对于开发冷却触发的温度敏感配方是有用的。
Temperature-sensitive formulations are attractive controlled-release formulations, which release an incorporated drug by changes in body temperature induced by external temperature stimulation. Recently, it has been reported that wax matrix (WM) particles composed of a low-melting-point microcrystalline wax (MCW) released only a small amount of the drug at 37 degrees C, whereas faster drug release occurred at 25 degrees C. In this study, temperature-sensitive formulations composed of low-melting-point MCW that release drugs triggered by cooling, rather than heating, were developed. In an in vitro dissolution test in which the test medium was repeatedly cooled from 37 to 25 degrees C, control of the promotion and suppression of drug release was achieved. The drug concentration in the plasma of rats administered the particles was significantly increased by cooling compared with non-cooling, indicating that the drug release from the particles was promoted by cooling both in vitro and in vivo. Therefore, particles composed of low-melting-point MCW should be useful for the development of cooling-triggered, temperature-sensitive formulations.