Khan Barkat Ali, Ahmad Sajeel, Khan Muhammad Khalid, Hosny Khaled M, Bukhary Deena M, Iqbal Haroon, Murshid Samar S, Halwani Abdulrahman A, Alissa Mohammed, Menaa Farid
Drug Delivery and Cosmetic Lab (DDCL), Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, Pakistan.
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Gels. 2022 Sep 22;8(10):608. doi: 10.3390/gels8100608.
The aim of this study was to fabricate and characterize a pharmaceutical emulgel co-loaded with naproxen/eugenol for transdermal delivery to improve the analgesic and anti-inflammatory effects and to eliminate GIT adverse reactions. Emulgel was prepared using a slow emulsification method and evaluated for physical appearance, thermodynamic stability, viscosity, pH, spreadability, extrudability, in-vitro drug release, drug content, ex-vivo permeation, drug retention studies and in-vivo studies. The emulgel exhibited good physical attributes, being thermodynamically stable with no phase separation, having excellent homogeneity, and pH 5.5 to 6.5. Slight changes in viscosity, spreadability and extrudability with respect to high temperature were observed (p > 0.05). The drug content was 96.69 ± 1.18% and 97.24 ± 1.27% for naproxen and eugenol, respectively. The maximum release of naproxen after 12 h was 85.14 ± 1.11%, whereas eugenol was 86.67 ± 1.23% from emulgel following anomalous non-Fickian mechanism. The maximum % permeation of naproxen across skin was 78.5 ± 1.30, whereas maximum % permeation of eugenol was 83.7 ± 1.33 after 12 h. The skin retention of eugenol and naproxen was 8.52 ± 0.22% and 6.98 ± 0.24%, respectively. The optimized emulgel inhibited the carrageenan induced paw edema. The pain reaction times of optimized emulgel and standard marketed product (Voltral®) were 11.16 ± 0.17 and 10.36 ± 0.47, respectively, with no statistically significant difference (p > 0.05). This study concluded that transdermal delivery of naproxen-eugenol emulgel synergized the anti-inflammatory and analgesic effects of naproxen and eugenol.
本研究的目的是制备并表征一种载有萘普生/丁香酚的药用乳胶凝胶用于透皮给药，以提高镇痛和抗炎效果，并消除胃肠道不良反应。采用缓慢乳化法制备乳胶凝胶，并对其外观、热力学稳定性、粘度、pH值、铺展性、挤出性、体外药物释放、药物含量、离体渗透、药物滞留研究和体内研究进行评估。该乳胶凝胶具有良好的物理特性，热力学稳定，无相分离，具有优异的均匀性，pH值为5.5至6.5。观察到粘度、铺展性和挤出性随高温有轻微变化（p>0.05）。萘普生和丁香酚的药物含量分别为96.69±1.18%和97.24±1.27%。按照非菲克反常机制，12小时后乳胶凝胶中萘普生的最大释放率为85.14±1.11%，而丁香酚为86.67±1.23%。12小时后，萘普生透过皮肤的最大渗透率为78.5±1.30，而丁香酚的最大渗透率为83.7±1.33。丁香酚和萘普生在皮肤中的滞留率分别为8.52±0.22%和6.98±0.24%。优化后的乳胶凝胶可抑制角叉菜胶诱导的爪肿胀。优化后的乳胶凝胶和市售标准产品（扶他林®）的疼痛反应时间分别为11.16±0.17和10.36±0.47，无统计学显著差异（p>0.05）。本研究得出结论，萘普生-丁香酚乳胶凝胶的透皮给药协同了萘普生和丁香酚的抗炎和镇痛作用。
