Al-Suwayeh Saleh A, Badran Mohamed M, Alhumoud Ghada O, Taha Ehab I, Ashri Lubna Y, Kazi Mohsin
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, P.O. Box 2457, Saudi Arabia.
Saudi Pharm J. 2023 Jun;31(6):889-903. doi: 10.1016/j.jsps.2023.04.004. Epub 2023 Apr 15.
The present study aimed to evaluate the impact of ultrafine nanoemulsions on the transdermal delivery of lornoxicam (LOR) for management of the inflammation. The transdermal administration of LORNE could increase the efficacy of LOR with a reduction in side effects. Merging the beneficial properties of ultrafine nanoemulsions and their components (penetration enhancers) can lead to good solubilization, a small droplet size, and more effective LOR carriers. Therefore, this study aims to develop and evaluate the potential use of ultrafine nanoemulsions of LOR (LORNE) to elucidate their skin targeting for the treatment of inflammation. Based on solubility and pseudo ternary phase diagram tests, ultrafine LORNE composed of Labrafil M 2125 CS, Cremophor RH40, and Transcutol HP to deliver LOR was developed and characterized for its physicochemical properties, emulsification, and release. The selected LORNE was incorporated into carbopol gel (LORNE-Gel) and examined for skin permeation, retention, dermatokinetics, anti-inflammatory efficacy, and skin irritation. The selected LORNE12-Gel could improve skin permeation, retention, and dermatokinetic results significantly (p < 0.05) with enhanced C and AUC compared to LOR-Gel. Moreover, LORNE12-Gel showed a remarkable anti-inflammatory effect compared to LOR-Gel after topical application. No signs of skin irritation were observed following treatment, indicating the safety of LORNE12-Gel. Thus, this study demonstrated that LOR-loaded LORNE12-Gel could be promising as an efficient transdermal nanocarrier for an anti-inflammatory alternative.
本研究旨在评估超细纳米乳剂对氯诺昔康（LOR）经皮给药治疗炎症的影响。LORNE经皮给药可提高LOR的疗效并减少副作用。将超细纳米乳剂及其成分（渗透促进剂）的有益特性相结合，可实现良好的增溶效果、小液滴尺寸以及更有效的LOR载体。因此，本研究旨在开发并评估LOR超细纳米乳剂（LORNE）的潜在用途，以阐明其在炎症治疗中的皮肤靶向性。基于溶解度和伪三元相图测试，开发了由Labrafil M 2125 CS、聚氧乙烯蓖麻油RH40和二乙二醇单乙基醚制成的用于递送LOR的超细LORNE，并对其理化性质、乳化和释放进行了表征。将选定的LORNE加入卡波姆凝胶（LORNE - Gel）中，并检测其皮肤渗透、滞留、皮肤动力学、抗炎疗效和皮肤刺激性。与LOR - Gel相比，选定的LORNE12 - Gel可显著改善皮肤渗透、滞留和皮肤动力学结果（p < 0.05），C和AUC增加。此外，局部应用后，LORNE12 - Gel与LOR - Gel相比显示出显著的抗炎作用。治疗后未观察到皮肤刺激迹象，表明LORNE12 - Gel的安全性。因此，本研究表明，负载LOR的LORNE12 - Gel有望成为一种高效的经皮纳米载体，作为抗炎替代品。
