Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman, Jordan.
Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman, Jordan.
Int J Pharm. 2019 Oct 30;570:118684. doi: 10.1016/j.ijpharm.2019.118684. Epub 2019 Sep 7.
The aim of this study was to develop an ibuprofen microemulsion (IBU-ME) incorporated into in situ gels (microgels) for local delivery into periodontal pockets. The IBU-ME was prepared at a concentration of 1% w/v IBU. Various concentrations of the thermosensitive Pluronic® F127 (P127) solution and a series of combinations of the P127 solution and IBU-ME at a 1:1 ratio were initially developed and tested to determine their sol-gel transition temperatures (T). Based on these studies, a constant concentration of P127 (11.1% w/v) and variable concentrations of IBU-ME were used to prepare the microgels. The mechanical properties (T, gelling time (T), viscosity, and viscoelastic properties) of the microgels were evaluated. The release of IBU from the microgels was determined in vitro. Rheological stability studies were performed to investigate the mechanical properties of the microgels after one month. The transition behavior studies demonstrated that the microgels are thermosensitive systems with pseudoplastic flow and their viscoelastic properties indicated that the elastic property was greater than the viscous property (G' > G″). The results showed that the mechanical properties of the microgels depend on the concentration of IBU-ME. In addition, rheological stability studies demonstrated that T and T are increased after one month, whereas the viscosity and viscoelastic properties are decreased after one month. Owing to the rigid structure of the microgels, the release of IBU from the microgels followed a controlled-release pattern.
本研究旨在开发一种布洛芬微乳液(IBU-ME),将其纳入局部递送至牙周袋的原位凝胶(微凝胶)中。IBU-ME 的浓度为 1% w/v IBU。最初开发并测试了各种浓度的热敏性 Pluronic® F127(P127)溶液和一系列 P127 溶液与 1:1 比例的 IBU-ME 的组合,以确定其溶胶-凝胶转变温度(T)。基于这些研究,使用恒定浓度的 P127(11.1% w/v)和可变浓度的 IBU-ME 来制备微凝胶。评估了微凝胶的机械性能(T、胶凝时间(T)、粘度和粘弹性)。体外测定了 IBU 从微凝胶中的释放情况。进行了流变稳定性研究,以研究微凝胶在一个月后的机械性能。转变行为研究表明,微凝胶是具有假塑性流动的热敏体系,其粘弹性性质表明弹性性质大于粘性性质(G' > G")。结果表明,微凝胶的机械性能取决于 IBU-ME 的浓度。此外,流变稳定性研究表明,一个月后 T 和 T 增加,而一个月后粘度和粘弹性降低。由于微凝胶的刚性结构,IBU 从微凝胶中的释放遵循控制释放模式。