Alyami Mohammad H, Alyami Hamad S, Abdo Asmaa M, A Sabry Shereen, El-Nahas Hanan M, Ayoub Margrit M
Department of Pharmaceutics, College of Pharmacy, Najran University, Najran 66462, Saudi Arabia.
Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt.
Pharmaceutics. 2024 Aug 1;16(8):1026. doi: 10.3390/pharmaceutics16081026.
In an effort to tackle the skin reactions frequently observed with topical application of ivermectin (IVM), a study was conducted to develop and optimize transethosomes (TESMs) loaded with IVM for scabies treatment. A three-factor, two-level (2) full factorial design was employed. Soyabean phosphatidylcholine concentration (A), ethanol concentration (B) and Span 60 amount (C) were studied as independent factors, while entrapment efficiency (EE), particle size (PS), polydispersity index (PDI), zeta potential (ZP) and drug release after 6 h (Q6h) were characterized. The skin sensitivity of the optimized formulation was evaluated by skin irritation test and histopathological examination. The EE% ranged from 88.55 ± 0.576% to 94.13 ± 0.305%, PS was from 318.033 ± 45.61 nm to 561.400 ± 45.17 nm, PDI was from 0.328 ± 0.139 to 0.671 ± 0.103, ZP was from -54.13 ± 1.09 mV to -60.50 ± 2.34 mV and Q6h was from 66.20 ± 0.30% to 93.46 ± 0.86%. The IVM-loaded transethosomal cream showed lower skin irritation and a more intact epidermal layer with intact keratinocyte, compared to the marketed cream which showed severe destruction of the keratin layer. Therefore, patient compliance can be improved by encapsulating IVM within TESMs to minimize its skin reactions.
为了解决局部应用伊维菌素(IVM)时经常观察到的皮肤反应,开展了一项研究,旨在开发并优化负载IVM的传递体(TESMs)用于疥疮治疗。采用三因素两水平(2³)全因子设计。将大豆磷脂酰胆碱浓度(A)、乙醇浓度(B)和司盘60用量(C)作为独立因素进行研究,同时对包封率(EE)、粒径(PS)、多分散指数(PDI)、zeta电位(ZP)和6小时后的药物释放量(Q6h)进行表征。通过皮肤刺激性试验和组织病理学检查评估优化制剂的皮肤敏感性。EE%范围为88.55±0.576%至94.13±0.305%,PS为318.033±45.61 nm至561.400±45.17 nm,PDI为0.328±0.139至0.671±0.103,ZP为-54.13±1.09 mV至-60.50±2.34 mV,Q6h为66.20±0.30%至93.46±0.86%。与显示角质层严重破坏的市售乳膏相比,负载IVM的传递体乳膏显示出较低的皮肤刺激性,且表皮层更完整,角质形成细胞完整。因此,将IVM包裹在TESMs中以尽量减少其皮肤反应,可以提高患者的依从性。