Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, 6th of October City, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Cairo, Egypt.
Drug Deliv. 2022 Dec;29(1):2784-2795. doi: 10.1080/10717544.2022.2108939.
Levocetirizine hydrochloride (LVC) is an antihistaminic drug that is repurposed for the treatment of alopecia. This investigation is targeted for formulating LVC into cationic ceramide/phospholipid composite (CCPCs) for the management of alopecia. CCPCs were fabricated by ethanol-injection approach, through a central composite experiment. CCPCs were evaluated by inspecting their entrapment efficiency (EE%), polydispersity index (PDI), particle size (PS), and zeta potential (ZP). The optimum CCPCs were additionally studied by , , , and studies. The fabricated CCPCs had acceptable EE%, PS, PDI, and ZP values. The statistical optimization elected optimum CCPCs composed of 5 mg hyaluronic acid, 10 mg ceramide III, and 5 mg dimethyldidodecylammonium bromide employing phytantriol as a permeation enhancer. The optimum CCPCs had EE%, PS, PDI, and ZP of 88.36 ± 0.34%, 479.00 ± 50.34 nm, 0.377 ± 0.0035, and 20.20 ± 1.13 mV, respectively. The optimum CCPC maintained its stability for up to 90 days. It also viewed vesicles of tube shape via transmission electron microscope. The assessment resulted in better interaction and stability between LVC and vesicle components in water. The and assessments showed satisfactory skin retention of LVC from optimum CCPCs. The histopathological assessment verified the safety of optimum CCPCs to be topically applied. Overall, the optimum CCPCs could be utilized as a potential system for the topical management of alopecia, with a prolonged period of activity, coupled with reduced LVC shortcomings.
左西替利嗪盐酸盐（LVC）是一种抗组胺药物，现被重新用于治疗脱发。本研究旨在将 LVC 制成阳离子神经酰胺/磷脂复合（CCPC）用于脱发的治疗。CCPC 是通过乙醇注入法，采用中心复合实验来制备的。通过考察包封效率（EE%）、多分散指数（PDI）、粒径（PS）和 Zeta 电位（ZP）来评估 CCPC。通过体外释放、稳定性、经皮渗透和组织病理学研究进一步研究最佳的 CCPC。制备的 CCPC 具有可接受的 EE%、PS、PDI 和 ZP 值。统计优化选择了最佳的 CCPC，由 5mg 透明质酸、10mg 神经酰胺 III 和 5mg 二甲基双十二烷基溴化铵组成，使用植物三醇作为渗透增强剂。最佳 CCPC 的 EE%、PS、PDI 和 ZP 分别为 88.36±0.34%、479.00±50.34nm、0.377±0.0035 和 20.20±1.13mV。最佳 CCPC 在长达 90 天内保持稳定。通过透射电子显微镜观察到最佳 CCPC 呈管状囊泡。评估结果表明，LVC 与囊泡成分在水中具有更好的相互作用和稳定性。评估结果表明，最佳 CCPC 可使 LVC 有较好的皮肤滞留性。组织病理学评估证实最佳 CCPC 局部应用具有安全性。总体而言，最佳 CCPC 可作为治疗脱发的潜在系统，具有延长的活性期，并减少 LVC 的缺点。
