Faculty of Pharmacy, DIT University, Mussoorie, Diversion Road, Makkawala, Uttarakhand 248009, India.
Hygia Institute of Pharmaceutical education and research, Faizullahganj, Prabandh Nagar, Ghaila road, Lucknow 226020, India.
Biomed Mater. 2024 Nov 22;20(1). doi: 10.1088/1748-605X/ad920e.
This study aimed to optimize mesalamine (MES)-nanoparticles (NPs) using Box Behnken Design and investigate itsantioxidant potential in colon drug targeting. The formulation was prepared using oil/water (O/W) emulsion solvent evaporation technique for time dependent colonic delivery. The optimal formulation with the following parameters composition was selected: polymer concentration (% w/w) (A) = 0.63, surfactant concentration (% w/w) (B) = 0.71, sonication duration (min) (C) = 6. The outcomes showed that ethyl cellulose (EC) NP containing MES has particles size of 142 ± 2.8 nm, zeta potential (ZP) of -24.8 ± 2.3 mV, % EE of 87.9 ± 1.6%, and PDI of 0.226 ± 0.15. Scanning electron microscopy revealed NPs has a uniform and spherical shape. Therelease data disclosed that the EC NPs containing MES showed bursts release of 52% ± 1.6% in simulated stomach media within 2 h, followed by a steady release of 93% ± 2.9% in simulated intestinal fluid that lasted for 48 h. The MES release from NP best match with the Korsmeyer-Peppas model (= 0.962) and it followed Fickian diffusion case I release mechanism. The formulation stability over six-months at 25 °C ± 2 °C with 65% ± 5% relative humidity, and 40 °C ± 2 °C with 75% ± 5% relative humidity showed no significant changes in colour, EE, particle sizes and ZP. As perresults, MES-NP effectively increased glutathione, SOD level and reduces the LPO level as compared to other treatment groups. The findings hold promise that the developed formulation can suitably give in ulcerative colitis.
本研究旨在使用 Box Behnken 设计优化美沙拉嗪（MES）纳米粒子（NPs），并研究其在结肠药物靶向中的抗氧化潜力。该配方采用油/水（O/W）乳液溶剂蒸发技术制备，用于时间依赖性结肠递药。选择具有以下参数组成的最佳配方：聚合物浓度（%w/w）（A）=0.63、表面活性剂浓度（%w/w）（B）=0.71、超声持续时间（min）（C）=6。结果表明，载有 MES 的乙基纤维素（EC）NP 的粒径为 142±2.8nm、Zeta 电位（ZP）为-24.8±2.3mV、%EE 为 87.9±1.6%、PDI 为 0.226±0.15。扫描电子显微镜显示 NPs 具有均匀的球形形状。释放数据显示，载有 MES 的 EC NPs 在模拟胃液中 2 小时内释放 52%±1.6%，随后在模拟肠液中以 93%±2.9%的速度稳定释放，持续 48 小时。MES 从 NP 中的释放最符合 Korsmeyer-Peppas 模型（=0.962），遵循菲克第一扩散释放机制。在 25°C±2°C、相对湿度 65%±5%和 40°C±2°C、相对湿度 75%±5%的条件下，配方在六个月内保持稳定，颜色、EE、粒径和 ZP 没有显著变化。结果表明，与其他治疗组相比，MES-NP 能有效增加谷胱甘肽、SOD 水平，降低 LPO 水平。研究结果表明，所开发的配方可适用于溃疡性结肠炎的治疗。
