A novel accelerated in vitro release method to evaluate the release of thymopentin from PLGA microspheres

作者：Xie, Xiangyang; Li, Zhiping; Zhang, Ling; Chi, Qiang; Yang, Yanfang; Zhang, Hui; Yang, Yang; Mei, Xingguo^*

来源：Pharmaceutical Development and Technology, 2015, 20(5): 633-640.

DOI：10.3109/10837450.2014.892131

• Accelerated release
• gradient heating program
• peptide release
• PLGA microspheres
• thymopentin

A novel accelerated method of good correlations with "real-time'' release to evaluate in vitro thymopentin release from poly (D, L-lactide-co-glycolide) (PLGA) microsphere was developed. Thymopentin-loaded microspheres were made from three types of PLGA, and peptide release was studied in various conditions. Incomplete release of peptide (<60%) from microspheres was found in accelerated testing with two typical release media. This problem was circumvented by adding organic solvents to the release media and varying the temperature in the media heating process. Release media containing three kinds of organic solvents at 50 degrees C were tested, respectively, and hydro-alcoholic solution was selected for further study. After the surfactant concentration (0.06%, W/V) and ethanol concentration (20%, V/V) were fixed, a gradient heating program, consisting of three stages and each stage with a different temperature, was introduced to enhance the correlations between the short-and long-term release. After adjusting the heating time of each stage, a good correlation (R-2 = 9896, formulation 8 K; R-2 = 0.9898, formulation 13 K; R-2 = 0.9886, formulation 28 K) between accelerated and "real-time'' release was obtained. By optimizing the conditions as ethanol concentration and temperature gradients, this accelerated method may be appropriate for similar peptide formulations that not well correlate with "real-time'' release.

• 出版日期2015
• 单位中国人民武装警察部队学院; 中国人民解放军广州军区武汉总医院