Department of Pharmaceutical Science and Technology, Faculty of Pharmacy, Hasanuddin University, Indonesia.
Department of Pharmacy, Faculty of Pharmacy, Hasanuddin University, Indonesia.
Int J Pharm. 2022 Nov 25;628:122323. doi: 10.1016/j.ijpharm.2022.122323. Epub 2022 Oct 21.
This study focused on the incorporation ofchloramphenicol (CAP)intowhey protein (WPI)(CAP-MPs) and was further formulated into a thermoresponsivein situgel for wound healing treatment.CAP microparticleswereproduced by two steps emulsification process.The modification ofthe mixing time and speed, as well as the variation of WPI and CAP concentration, resulted in various particle sizes(0.95 ± 0.07to 8.94 ± 0.32 μm). The optimum formulation was achieved using 15 % WPI in water, and 2 mL CAP in propylene glycol withatotal amount in the mixture was 100 mg, and 5 % oil phase, with homogenization time and speed at 15 min and 7500 rpm, respectively. The characterization of CAP-MP's showed PDI values at 0.110 ± 0.007, drug entrapment efficiency at70.64 ± 1.12 %,and drug loading at 8.80 ± 0.12 %.SEM analysis of CAP-MPs showedspherical, uniform particlesdispersed across the surface of the emulsion droplets.FTIR analysis showed strong development of hydrogen bonds proving the encapsulation was effective. Pluronic® F127, Pluronic® F68, and hydroxypropyl methylcellulose (HPMC)were used for the thermoresponsive hydrogel formulation with desired properties. The gel formulationcouldprovideliquid form at room temperature (25 °C) andformagel at 31 °C.This optimum formula was able to increase the bioadhesivity (28160.92 ± 3902.09 dyne/cm) as well as the percentage of gels skin occlusivity after 24 h (32.82 ± 0.004),and to be considered, it did not show hemolytic activities. In anex vivoantibacterial activity, this combination approach showed a 99.95 % reduction in theStaphylococcus aureus(SA) population.
本研究专注于氯霉素(CAP)在乳清蛋白(WPI)中的掺入(CAP-MPs),并进一步将其制成热响应原位凝胶用于伤口愈合治疗。通过两步乳化法制备 CAP 微球。通过改变混合时间和速度,以及改变 WPI 和 CAP 浓度,得到了不同粒径(0.95±0.07 至 8.94±0.32μm)的微球。最佳配方是在水中使用 15%的 WPI,在丙二醇中使用 2ml CAP,混合物总量为 100mg,油相为 5%,分别以 15min 和 7500rpm 的速度进行均质化。CAP-MP 的特性显示 PDI 值为 0.110±0.007,药物包封效率为 70.64±1.12%,药物载药量为 8.80±0.12%。CAP-MP 的 SEM 分析显示,球形、均匀的颗粒分散在乳液液滴的表面。FTIR 分析表明,氢键的强烈发展证明了包封是有效的。Pluronic®F127、Pluronic®F68 和羟丙基甲基纤维素(HPMC)用于具有所需性能的热响应水凝胶配方。凝胶配方在室温(25°C)下呈液体形式,在 31°C 下呈凝胶形式。这种最佳配方能够提高生物粘附性(28160.92±3902.09 达因/厘米)和 24 小时后凝胶皮肤封闭性的百分比(32.82±0.004),并且可以考虑,它没有显示出溶血活性。在体外抗菌活性中,这种组合方法使金黄色葡萄球菌(SA)的数量减少了 99.95%。