Abstract

The purpose of this research was to enhance the transdermal delivery of diclofenac sodium niosomal formulations. To characterise the obtained niosomes, SEM, XRPD, DSC and ATR-FTIR were employed. The size of the niosomes increased from 158.00 ± 6.17 to 400.87 ± 4.99 nm when cholesterol was incorporated into the formulations. It was observed that the zeta potential of niofenac varies from −25.40 ± 1.352 to −43.13 ± 1.171 mV when the cholesterol percentage decreased from 2% to 0.2%. The higher entrapment efficiency percentage (63.70 ± 0.18%) was obtained for the formulations with larger particle sizes and higher cholesterol content. The optimised niofenac formulation showed a controlled release fashion where 61.71 ± 0.59% of the drug released within 24 h. The results showed that the value of permeated diclofenac sodium through the skin layers was higher for the niofenac gel formulation (242.3 ± 31.11 µg/cm²) compared to simple gel formulation (127.40 ± 27.80 µg/cm²). Besides, niofenac formulation outperformed the anti-inflammatory activities in the formalin test compared to the control and diclofenac simple gel group. The licking time was significantly lower in both early (40.2 ± 7.3 s) and late stages (432.4 ± 31.7 s) for niofenac compared to conventional formulation (early stage 130.4 ± 8.73 s and late stage 660.6 ± 123.73 s). This study indicates that niosomal formulations can improve drug therapeutic effects by increasing drug delivery to specific sites.

摘要

本研究的目的是增强双氯芬酸钠 niosomal 制剂的透皮递送。为了表征获得的 niosomes，使用了 SEM、XRPD、DSC 和 ATR-FTIR。当将胆固醇掺入制剂中时，niosomes 的大小从 158.00 ± 6.17 增加到 400.87 ± 4.99 nm。据观察，当胆固醇百分比从 2% 下降到 0.2% 时，niofenac 的 zeta 电位从 -25.40 ± 1.352 到 -43.13 ± 1.171 mV 变化。对于具有较大粒径和较高胆固醇含量的配方，获得了较高的包封率百分比 (63.70 ± 0.18%)。优化的尼芬酸制剂表现出控释方式，其中 61.71 ± 0.59% 的药物在 24 小时内释放。² ) 与简单的凝胶配方 (127.40 ± 27.80 µg/cm ² ) 相比。此外，与对照组和双氯芬酸简单凝胶组相比，在福尔马林试验中，尼芬酸制剂的抗炎活性优于对照组。与传统制剂（早期 130.4 ± 8.73 秒和晚期 660.6 ± 123.73 秒）相比，尼芬酸的早期（40.2 ± 7.3 秒）和晚期（432.4 ± 31.7 秒）的舔舐时间显着降低。该研究表明，niosomal 制剂可以通过增加药物输送到特定部位来提高药物治疗效果。