Bao Wenting, Zhang Xianlong, Wu Hong, Chen Rong, Guo Shaoyun
The State Key Laboratory of Polymer Materials Engineering, Polymer Research Institute of Sichuan University, Chengdu 610065, China.
Aviation Fuel & Chemical Airworthiness Certification Center of CAAC, The Second Research Institute of Civil Aviation Administration of China, Chengdu 610207, China.
Polymers (Basel). 2019 May 14;11(5):880. doi: 10.3390/polym11050880.
In this paper, the synergistic effect of ultrasound and polyethylene glycol (PEG) on the controlled release of a water soluble drug from polylactide (PLA) matrices was studied. When ultrasound was used following the hot melt extrusion (HME) of the PLA/model drug release system, the release of the model drug (Methylene Blue (MB)) from the PLA when immersed in phosphate buffered saline (PBS) was affected by the variation of the parameters of ultrasound. It was found that no more than 2% PLA dissolved during the in-vitro release study, and the release of the MB from the PLA was diffusion controlled and fit well with the Higuchi diffusion model. Polyethylene glycol (PEG), which has high hydrophilicity and rapid dissolution speed, was blended with the PLA during the melt extrusion to enhance the release of the MB. The analysis of the structure and properties of the in-vitro release tablets of PLA/PEG/MB indicated that the ultrasound could improve the dispersion of MB in the PLA/PEG blends and it could also change the structure and properties of the PLA/PEG blends. Due to the dissolution of the PEG in PBS, the release of the MB from the PLA/PEG drug carrier was a combination of diffusion and erosion controlled release. Thus a new mechanism combining of diffusion and erosion models and modified kinetics model was proposed to explain the release behavior.
本文研究了超声与聚乙二醇(PEG)对水溶性药物从聚乳酸(PLA)基质中控释的协同作用。当在PLA/模型药物释放系统的热熔挤出(HME)之后使用超声时,浸入磷酸盐缓冲盐水(PBS)中的PLA中模型药物(亚甲基蓝(MB))的释放受超声参数变化的影响。发现在体外释放研究期间溶解的PLA不超过2%,并且MB从PLA中的释放受扩散控制,与Higuchi扩散模型拟合良好。具有高亲水性和快速溶解速度的聚乙二醇(PEG)在熔融挤出过程中与PLA共混,以提高MB的释放。对PLA/PEG/MB体外释放片的结构和性能分析表明,超声可以改善MB在PLA/PEG共混物中的分散性,并且还可以改变PLA/PEG共混物的结构和性能。由于PEG在PBS中的溶解,MB从PLA/PEG药物载体中的释放是扩散和溶蚀控制释放的组合。因此,提出了一种结合扩散和溶蚀模型以及修正动力学模型的新机制来解释释放行为。