Shahid Mudassar, Hussain Afzal, Khan Azmat Ali, Ramzan Mohhammad, Alaofi Ahmed L, Alanazi Amer M, Alanazi Mohammad M, Rauf Mohd Ahmar
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Pharmaceutical Biotechnology Laboratory, Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
ACS Omega. 2022 May 30;7(23):20267-20279. doi: 10.1021/acsomega.2c02219. eCollection 2022 Jun 14.
An attempt has been made to optimize ketoconazole (KTZ)-loaded cationic nanoemulsion for topical delivery followed by , , and evaluations. Central composite design suggested a total of 13 outcomes at 3 factors and 2 levels against 6 responses. Formulations were characterized for globular size, polydispersity index, pH, ζ potential, % entrapment efficiency (% EE), and drug content. Moreover, the optimized KTZ-CNM13 was compared against drug suspension (KTZ-SUS), commercial cream, and anionic nanoemulsion for drug release, permeation, hemolysis, antifungal assay, dermal irritancy, and long-term stability. KTZ-CNM13 was found to have a low size (239 nm), an optimal ζ potential (+22.7 mV), a high % EE (89.1%), a spherical shape, a high drug content (98.9%), and a high numerical desirability value (1.0). drug release behavior of KTZ from KTZ-CNM13 was 7.54- and 1.71-folds higher than those of KTZ-ANM13 and KTZ-SUS, respectively, at 24 h. The permeation rate values were ordered as KTZ-CNM13 > KTZ-ANM13 > KTZ-MKT > KTZ-SUP due to various studied factors. High values of zone of inhibition for KTZ-CNM13 were observed against , , and as compared to KTZ-SUS. hemolysis and irritation studied confirmed the safety concern of the nanoemulsion at the explored composition. Long-term stability result revealed a stable product at the explored temperature for a year. Conclusively, cationic nanoemulsion is a promising approach to deliver KTZ for high permeation and therapeutic efficacy.
已尝试优化负载酮康唑（KTZ）的阳离子纳米乳剂用于局部给药，随后进行了[此处原文缺失具体评价内容]评价。中心复合设计表明，在3个因素和2个水平下，针对6个响应共有13个结果。对制剂进行了球形尺寸、多分散指数、pH值、ζ电位、包封率（%EE）和药物含量的表征。此外，将优化后的KTZ-CNM13与药物混悬液（KTZ-SUS）、市售乳膏和阴离子纳米乳剂进行了药物释放、[此处原文缺失具体评价内容]渗透、[此处原文缺失具体评价内容]溶血、抗真菌试验、[此处原文缺失具体评价内容]皮肤刺激性和长期稳定性的比较。发现KTZ-CNM13具有较小的尺寸（239nm）、最佳的ζ电位（+22.7mV）、较高的包封率（89.1%）、球形形状、较高的药物含量（98.9%）和较高的数值可取性值（1.0）。在24小时时，KTZ从KTZ-CNM13的药物释放行为分别比KTZ-ANM13和KTZ-SUS高7.54倍和1.71倍。由于各种研究因素，渗透速率值的顺序为KTZ-CNM13＞KTZ-ANM13＞KTZ-MKT＞KTZ-SUP。与KTZ-SUS相比，观察到KTZ-CNM13对[此处原文缺失具体真菌名称]、[此处原文缺失具体真菌名称]、[此处原文缺失具体真菌名称]和[此处原文缺失具体真菌名称]的抑菌圈值较高。[此处原文缺失具体评价内容]溶血和[此处原文缺失具体评价内容]刺激性研究证实了纳米乳剂在所探索组成下的安全性问题。长期稳定性结果表明，在所探索的温度下，该产品在一年内稳定。总之，阳离子纳米乳剂是一种有前景的方法，可用于高渗透和治疗效果的KTZ给药。
