Upputuri Ravi Theaj Prakash, Mandal Abul Kalam Azad
School of Bio Sciences and Technology, Vellore Institute of Technology, Vellore-632014, Tamil Nadu, India.
Iran J Pharm Res. 2019 Summer;18(3):1137-1146. doi: 10.22037/ijpr.2019.1100715.
Drug release kinetics plays an important role in determining the mechanism of drug release, which in turn helps in formulating controlled/sustained release formulations. In our study, different concentrations of green tea polyphenols (GTP) were encapsulated into casein nanoparticles which showed a maximum encapsulation efficiency (76.9%) at a GTP concentration of 5 mg/mL. The casein nanoparticles were characterized through particle size analysis, zeta potential, AFM, and HR SEM, followed by molecular docking studies, which confirmed the binding of GTP to casein nanoparticles. release studies carried out at different temperatures and pH showed no significant difference in the release pattern, but the release was prolonged even up to 48 h. On varying pH of the release medium, an increase in the percentage of release was observed as the pH shifted from acidic to basic. All release data showed good correlation with Zero order kinetics, an ideal model for release of drugs from nanoparticulate sustained release formulations, with anomalous mode of drug transport. Antioxidant activity of the released GTP determined through DPPH assay showed potent antioxidant effect of GTP even after 48 h of its release. Our data indicated that casein nanoparticles could be used as a potent vehicle for the delivery of GTP for achieving a sustained release.
药物释放动力学在确定药物释放机制方面起着重要作用，这反过来又有助于制定控释/缓释制剂。在我们的研究中，不同浓度的绿茶多酚（GTP）被包裹在酪蛋白纳米颗粒中，在GTP浓度为5 mg/mL时显示出最大包封效率（76.9%）。通过粒度分析、zeta电位、原子力显微镜和高分辨率扫描电子显微镜对酪蛋白纳米颗粒进行了表征，随后进行了分子对接研究，证实了GTP与酪蛋白纳米颗粒的结合。在不同温度和pH值下进行的释放研究表明，释放模式没有显著差异，但释放甚至延长至48小时。随着释放介质pH值从酸性转变为碱性，观察到释放百分比增加。所有释放数据与零级动力学具有良好的相关性，零级动力学是纳米颗粒缓释制剂药物释放的理想模型，具有异常的药物转运模式。通过DPPH测定法测定的释放的GTP的抗氧化活性表明，即使在其释放48小时后，GTP仍具有强大的抗氧化作用。我们的数据表明，酪蛋白纳米颗粒可作为一种有效的载体用于递送GTP以实现持续释放。
