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Encapsulation in lipid-core nanocapsules improves topical treatment with the potent antileishmanial compound CH8.
Nanomedicine: Nanotechnology, Biology and Medicine ( IF 4.2 ) Pub Date : 2019-10-28 , DOI: 10.1016/j.nano.2019.102121 Douglas O Escrivani 1 , Milene Valéria Lopes 1 , Fernanda Poletto 2 , Stela Regina Ferrarini 3 , Ariane J Sousa-Batista 1 , Patrick G Steel 4 , Sílvia Stanisçuaski Guterres 3 , Adriana Raffin Pohlmann 2 , Bartira Rossi-Bergmann 1
Nanomedicine: Nanotechnology, Biology and Medicine ( IF 4.2 ) Pub Date : 2019-10-28 , DOI: 10.1016/j.nano.2019.102121 Douglas O Escrivani 1 , Milene Valéria Lopes 1 , Fernanda Poletto 2 , Stela Regina Ferrarini 3 , Ariane J Sousa-Batista 1 , Patrick G Steel 4 , Sílvia Stanisçuaski Guterres 3 , Adriana Raffin Pohlmann 2 , Bartira Rossi-Bergmann 1
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Cutaneous leishmaniasis (CL) is a neglected parasitic disease conventionally treated by multiple injections with systemically toxic drugs. Aiming at a more acceptable therapy, we developed lipid-core nanocapsules (LNCs) entrapping the potent antileishmanial chalcone (CH8) for topical application. Rhodamine-labeled LNC (Rho-LNC-CH8) was produced for imaging studies. LNC-CH8 and Rho-LNC-CH8 had narrow size distributions (polydispersity index <0.10), with similar mean sizes (~180 nm) by dynamic light scattering. In vitro, Rho-LNC-CH8 was rapidly internalized by extracellular Leishmania amazonensis parasites macrophages in less than 15 min. LNC-CH8 activated macrophage oxidative mechanisms more efficiently than CH8, and was more selectively toxic against the intracellular parasites. In vivo, topically applied Rho-LNC-CH8 efficiently permeated mouse skin. In L. amazonensis-infected mice, LNC-CH8 reduced the parasite load by 86% after three weeks of daily topical treatment, while free CH8 was ineffective. In conclusion, LNC-CH8 has strong potential as a novel topical formulation for CL treatment.
中文翻译：
脂质核心纳米胶囊中的封装改善了用强效抗疟疾化合物CH8进行的局部治疗。
皮肤利什曼病（CL）是一种被忽视的寄生虫病，通常通过多次注射全身毒性药物来治疗。为了获得更可接受的治疗方法，我们开发了包埋强效抗衰老查尔酮（CH8）的脂质核心纳米胶囊（LNC），用于局部应用。罗丹明标记的LNC（Rho-LNC-CH8）用于成像研究。LNC-CH8和Rho-LNC-CH8具有窄的尺寸分布（多分散指数<0.10），通过动态光散射具有相似的平均尺寸（〜180 nm）。在体外，Rho-LNC-CH8在不到15分钟的时间内被胞外利什曼原虫亚马逊巨噬细胞迅速内在化。LNC-CH8比CH8更有效地激活巨噬细胞的氧化机制，并且对细胞内的寄生虫更具选择性。体内，局部应用的Rho-LNC-CH8有效地渗透了小鼠皮肤。每天局部治疗三周后，在感染L. Amazonensis的小鼠中，LNC-CH8将寄生虫负荷降低了86％，而游离CH8无效。总之，LNC-CH8作为治疗CL的新型局部用药具有强大的潜力。
更新日期：2019-10-28
中文翻译：
脂质核心纳米胶囊中的封装改善了用强效抗疟疾化合物CH8进行的局部治疗。
皮肤利什曼病（CL）是一种被忽视的寄生虫病，通常通过多次注射全身毒性药物来治疗。为了获得更可接受的治疗方法，我们开发了包埋强效抗衰老查尔酮（CH8）的脂质核心纳米胶囊（LNC），用于局部应用。罗丹明标记的LNC（Rho-LNC-CH8）用于成像研究。LNC-CH8和Rho-LNC-CH8具有窄的尺寸分布（多分散指数<0.10），通过动态光散射具有相似的平均尺寸（〜180 nm）。在体外，Rho-LNC-CH8在不到15分钟的时间内被胞外利什曼原虫亚马逊巨噬细胞迅速内在化。LNC-CH8比CH8更有效地激活巨噬细胞的氧化机制，并且对细胞内的寄生虫更具选择性。体内，局部应用的Rho-LNC-CH8有效地渗透了小鼠皮肤。每天局部治疗三周后，在感染L. Amazonensis的小鼠中，LNC-CH8将寄生虫负荷降低了86％，而游离CH8无效。总之，LNC-CH8作为治疗CL的新型局部用药具有强大的潜力。
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