Alhakamy Nabil A, Al-Rabia Mohammed W, Md Shadab, Sirwi Alaa, Khayat Selwan Saud, AlOtaibi Sahar Saad, Hakami Raghad Abkar, Al Sadoun Hadeel, Eldakhakhny Basmah Medhat, Abdulaal Wesam H, Aldawsari Hibah M, Badr-Eldin Shaimaa M, Elfaky Mahmoud A
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Advanced Drug Delivery Research Group, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Pharmaceutics. 2021 Jun 28;13(7):977. doi: 10.3390/pharmaceutics13070977.
Luliconazole is a new topical imidazole antifungal drug for the treatment of skin infections. It has low solubility and poor skin penetration which limits its therapeutic applications. In order to improve its therapeutic efficacy, spanlastics nanoformulation was developed and optimized using a combined mixture-process variable design (CMPV). The optimized formulation was converted into a hydrogel formula to enhance skin penetration and increase the efficacy in experimental cutaneous infections in Swiss mice wounds. The optimized formulation was generated at percentages of Span and Tween of 48% and 52%, respectively, and a sonication time of 6.6 min. The software predicted that the proposed formulation would achieve a particle size of 50 nm with a desirability of 0.997. The entrapment of luliconazole within the spanlastics carrier showed significant ( < 0.0001) antifungal efficacy in the immunocompromised Candida-infected Swiss mice without causing any irritation, when compared to the luliconazole treated groups. The microscopic observation showed almost complete removal of the fungal colonies on the skin of the infected animals (0.2 ± 0.05 log CFU), whereas the control animals had 0.2 ± 0.05 log CFU. Therefore, luliconazole spanlastics could be an effective formulation with improved topical delivery for antifungal activity against .
卢立康唑是一种用于治疗皮肤感染的新型外用咪唑类抗真菌药物。它的溶解度低且皮肤渗透性差，这限制了其治疗应用。为了提高其治疗效果，采用组合混合-工艺变量设计（CMPV）开发并优化了司盘弹性体纳米制剂。将优化后的制剂转化为水凝胶配方，以增强皮肤渗透性并提高在瑞士小鼠伤口实验性皮肤感染中的疗效。优化后的制剂在司盘和吐温的百分比分别为48%和52%以及超声处理时间为6.6分钟的条件下制备而成。软件预测该拟定制剂的粒径将达到50纳米，可取性为0.997。与卢立康唑治疗组相比，卢立康唑在司盘弹性体载体中的包封在免疫受损的念珠菌感染瑞士小鼠中显示出显著的（<0.0001）抗真菌效果，且未引起任何刺激。显微镜观察显示感染动物皮肤上的真菌菌落几乎完全清除（0.2±0.05 log CFU），而对照动物有0.2±0.05 log CFU。因此，卢立康唑司盘弹性体制剂可能是一种有效的制剂，具有改善的局部递送能力，可对抗……的抗真菌活性。
