Liu Zhiyu, Song Hangling, Chen Xia, Han Aichun, Chen Rong, Liu Guiting, Guo Shaoyun
The State Key Laboratory of Polymer Materials Engineering, Polymer Research Institute of Sichuan University, Sichuan Provincial Engineering Laboratory of Plastic/Rubber Complex Processing Technology, Sichuan University, Chengdu 610065, China.
Polymers (Basel). 2021 Sep 13;13(18):3076. doi: 10.3390/polym13183076.
Hot-melt blending has been widely used in the pharmaceutical industry to produce drug delivery systems, however, realizing the controlled drug release behavior of a hot-melt blended medicament it is still a tough challenge. In this study, we developed a simple and effective heat treatment method to adjust the drug release behavior, without the addition of any release modifiers. Thin metoprolol tartrate (MPT)/poly(ε-caprolactone) (PCL) tablets were prepared through hot-melt processing, and different morphologies of MPT were obtained by altering processing temperatures and the following heat treatment. MPT particles with different particle sizes were obtained under different processing temperatures, and fibrous crystals of MPT were fabricated during the following heat treatment. Different morphological structures of MPT adjusted the drug diffusion channel when immersed in phosphate-buffered saline (PBS), and various drug release behaviors were approached. After being immersed for 24 h, 7% of the MPT was released from the blend processed at 130 °C, while more than 95% of the MPT were released after the following heat treatment of the same sample. Thus, flexible drug release behaviors were achieved using this simple and effective processing manufacture, which is demonstrated to be of profound importance for biomedical applications.
热熔共混已在制药行业中广泛用于生产药物递送系统，然而，要实现热熔共混药物的可控释药行为仍是一项艰巨的挑战。在本研究中，我们开发了一种简单有效的热处理方法来调节药物释放行为，无需添加任何释放调节剂。通过热熔工艺制备了薄型酒石酸美托洛尔（MPT）/聚（ε-己内酯）（PCL）片剂，并通过改变加工温度和随后的热处理获得了不同形态的MPT。在不同的加工温度下获得了不同粒径的MPT颗粒，并在随后的热处理过程中制备了MPT的纤维状晶体。当MPT浸入磷酸盐缓冲盐水（PBS）中时，其不同的形态结构调节了药物扩散通道，并呈现出各种药物释放行为。浸泡24小时后，在130℃下加工的共混物中有7%的MPT释放出来，而对同一样品进行后续热处理后，超过95%的MPT释放出来。因此，通过这种简单有效的加工制造方法实现了灵活的药物释放行为，这对于生物医学应用具有深远的重要意义。
