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Nano-elastic liposomes as multidrug carrier of sodium stibogluconate and ketoconazole: A potential new approach for the topical treatment of cutaneous Leishmaniasis.
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-02-04 , DOI: 10.1016/j.ejps.2020.105256 M Junaid Dar 1 , Sidra Khalid 1 , Sanjay Varikuti 2 , Abhay R Satoskar 2 , Gul Majid Khan 1
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-02-04 , DOI: 10.1016/j.ejps.2020.105256 M Junaid Dar 1 , Sidra Khalid 1 , Sanjay Varikuti 2 , Abhay R Satoskar 2 , Gul Majid Khan 1
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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 IC50 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.
中文翻译：
纳米弹性脂质体作为stibogluconate钠和ketoconazole的多药载体：皮肤利什曼病局部治疗的潜在新方法。
本研究评估了在纳米弹性脂质体（NELs）中与酮康唑（KTZ）共同负载的司妥葡萄糖酸钠（SSG）与皮肤利什曼病（CL）的局部治疗的疗效。开发了SSG-KTZ共装载NEL，并评估了各种理化特性和抗利什曼原虫的潜力。优化的纳米囊泡的平均粒径为212.8±3.1 nm，包封效率为61.2±2.9％。与药物溶液相比，SSG-KTZ共装载的NELs显示SSG的皮肤渗透率高5.37倍。SSG和KTZ表现出协同相互作用，流式细胞仪显示DsRed Leishmania mexicana对感染巨噬细胞的杀灭作用增强。与普通SSG解决方案相比，体外和体内抗Leishmanial研究表明IC50值降低了10.67倍，寄生负担降低了35.33倍。
更新日期：2020-02-04
中文翻译：
纳米弹性脂质体作为stibogluconate钠和ketoconazole的多药载体：皮肤利什曼病局部治疗的潜在新方法。
本研究评估了在纳米弹性脂质体（NELs）中与酮康唑（KTZ）共同负载的司妥葡萄糖酸钠（SSG）与皮肤利什曼病（CL）的局部治疗的疗效。开发了SSG-KTZ共装载NEL，并评估了各种理化特性和抗利什曼原虫的潜力。优化的纳米囊泡的平均粒径为212.8±3.1 nm，包封效率为61.2±2.9％。与药物溶液相比，SSG-KTZ共装载的NELs显示SSG的皮肤渗透率高5.37倍。SSG和KTZ表现出协同相互作用，流式细胞仪显示DsRed Leishmania mexicana对感染巨噬细胞的杀灭作用增强。与普通SSG解决方案相比，体外和体内抗Leishmanial研究表明IC50值降低了10.67倍，寄生负担降低了35.33倍。
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