Sahiner Mehtap, Yilmaz Aynur S, Ayyala Ramesh S, Sahiner Nurettin
Department of Bioengineering, Faculty of Engineering, Canakkale Onsekiz Mart University Terzioglu Campus, Canakkale 17100, Turkey.
Department of Chemistry, Faculty of Sciences & Arts, and Nanoscience and Technology Research and Application Center (NANORAC), Canakkale Onsekiz Mart University Terzioglu Campus, Canakkale 17100, Turkey.
Pharmaceutics. 2023 Jan 23;15(2):384. doi: 10.3390/pharmaceutics15020384.
Glycerol (Gly) is a well-known, FDA-approved molecule posing three hydroxyl groups. Since Gly is biocompatible, here, it was aimed to prepare poly(Glycerol) (p(Gly)) particles directly for the first time for the delivery of therapeutic agents. Micrometer-sized particles of p(Gly) were successfully synthesized via the micro-emulsion method with an average size of 14.5 ± 5.6 µm. P(Gly) microparticles up to 1.0 g/mL concentrations were found biocompatible with 85 ± 1% cell viability against L929 fibroblasts. Moreover, p(Gly) microparticles were tested for hemocompatibility, and it was found that up to 1.0 mg/mL concentrations the particles were non-hemolytic with 0.4 ± 0.1% hemolysis ratios. In addition, the blood compatibility index values of the prepared p(Gly) particles were found as 95 ± 2%, indicating that these microparticles are both bio- and hemocompatible. Furthermore, Quercetin (QC) flavonoid, which possessed high antioxidant properties, was loaded into p(Gly) microparticles to demonstrate drug-carrying properties of the particles with improved bioavailability, non-toxicity, and high biocompatibility. The results of this study evidently revealed that p(Gly) particles can be directly prepared from a cost-effective and easily accessible glycerol molecule and the prepared particles exhibited good biocompatibility, hemocompatibility, and non-toxicity. Therefore, p(Gly) particles were found as promising vehicles for drug delivery systems in terms of their higher loading and release capability as well as for sustained long term release profiles.
甘油(Gly)是一种广为人知且已获美国食品药品监督管理局(FDA)批准的分子,带有三个羟基。由于甘油具有生物相容性,因此本文首次旨在直接制备聚甘油(p(Gly))颗粒用于治疗剂的递送。通过微乳液法成功合成了微米级的p(Gly)颗粒,平均尺寸为14.5±5.6 µm。发现浓度高达1.0 g/mL的p(Gly)微粒与L929成纤维细胞具有生物相容性,细胞活力为85±1%。此外,对p(Gly)微粒进行了血液相容性测试,发现浓度高达1.0 mg/mL时,这些颗粒无溶血现象,溶血率为0.4±0.1%。此外,所制备的p(Gly)颗粒的血液相容性指数值为95±2%,表明这些微粒具有生物相容性和血液相容性。此外,将具有高抗氧化性能的槲皮素(QC)类黄酮负载到p(Gly)微粒中,以证明该颗粒具有载药性能,同时具有提高的生物利用度、无毒性和高生物相容性。本研究结果清楚地表明,p(Gly)颗粒可以直接由成本效益高且易于获取的甘油分子制备而成,所制备的颗粒具有良好的生物相容性、血液相容性和无毒性。因此,就其更高的负载和释放能力以及持续的长期释放特性而言,p(Gly)颗粒被认为是药物递送系统的有前途的载体。