Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320, Pakistan.
Department of Pathology, Ohio State University Medical Center, Columbus, Ohio 43201, USA.
Eur J Pharm Sci. 2020 Mar 30;145:105256. doi: 10.1016/j.ejps.2020.105256. Epub 2020 Feb 4.
The present study evaluates the efficacy of sodium stibogluconate (SSG) co-loaded with ketoconazole (KTZ) in nano-elastic liposomes (NELs) for the topical treatment of cutaneous leishmaniasis (CL). SSG-KTZ co-loaded NELs were developed and assessed for various physicochemical properties and anti-leishmanial potential. The optimized nano-vesicles have an average size of 212.8 ± 3.1 nm and entrapment efficiency of 61.2 ± 2.9%. SSG-KTZ co-loaded NELs displayed 5.37-fold higher skin permeation of SSG as compared to drug solution. SSG and KTZ displayed a synergistic interaction and flow cytometry revealed enhanced killing of DsRed Leishmania mexicana in infected macrophages. In-vitro and in-vivo anti-leishmanial studies indicated a 10.67-fold lower IC value and a 35.33-fold reduced parasitic burden as compared with plain SSG solution, respectively. SSG-KTZ co-loaded NELs were found to be a promising approach for the topical treatment of CL.
本研究评估了载酮康唑（KTZ）的葡甲酸钠（SSG）纳米弹性脂质体（NEL）在治疗皮肤利什曼病（CL）中的疗效。制备并评估了 SSG-KTZ 载药 NEL 的各种理化性质和抗利什曼原虫效果。优化后的纳米囊泡平均粒径为 212.8±3.1nm，包封率为 61.2±2.9%。与药物溶液相比，SSG-KTZ 载药 NEL 使 SSG 的皮肤渗透增加了 5.37 倍。SSG 和 KTZ 表现出协同作用，流式细胞术显示，载药 NEL 增强了对感染巨噬细胞中 DsRed 墨西哥利什曼原虫的杀伤作用。体外和体内抗利什曼原虫研究表明，与普通 SSG 溶液相比，IC 值降低了 10.67 倍，寄生虫载量降低了 35.33 倍。SSG-KTZ 载药 NEL 有望成为治疗 CL 的一种新的局部给药方法。
