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Development, skin targeting and antifungal efficacy of topical lipid nanoparticles containing itraconazole.
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-03-07 , DOI: 10.1016/j.ejps.2020.105296 Julia Sapienza Passos 1 , Luiza Capello de Martino 1 , Vanessa Franco Carvalho Dartora 2 , Gabriel L B de Araujo 3 , Kelly Ishida 2 , Luciana B Lopes 2
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-03-07 , DOI: 10.1016/j.ejps.2020.105296 Julia Sapienza Passos 1 , Luiza Capello de Martino 1 , Vanessa Franco Carvalho Dartora 2 , Gabriel L B de Araujo 3 , Kelly Ishida 2 , Luciana B Lopes 2
Affiliation
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Considering the increased incidence of sporotrichosis and other fungal infections in rural and urban areas, and the limitations and adverse effects of oral itraconazole therapy, we studied nanostructured lipid carriers (NLC) as topical delivery systems to increase itraconazole localization in skin lesions and associate efficacy with reduced systemic exposure. Unloaded and itraconazole-loaded NLC showed nanometric size (~216-340 nm), negative zeta potential (~ -17 mV), and high entrapment efficiency (~97%). NLC treatment decreased transepidermal water loss, an index of cutaneous barrier function, in intact skin and in tissues damaged with a linear incision (to mimic lesions) by 23-36%, and reduced drug transdermal delivery by ~2-fold, demonstrating its ability to localize itraconazole within the skin. The unloaded and itraconazole-loaded NLC were considered safe, as indicated by scores of 0.5 and 0.6 in HET-CAM models, respectively, and lack of toxicity (measured by survival and health index) on the Galleria mellonella larvae. The values obtained for minimum inhibitory concentration and minimum fungicidal concentration on Sporothrix brasiliensis yeasts were 0.25 and 32 μg/mL, respectively. The drug in solution displayed similar values, indicating that encapsulation does not hinder itraconazole antifungal effect. NLC treatment improved the survival rate and health index of G. mellonella larvae infected with S. brasiliensis yeasts and C. albicans, demonstrating antifungal efficacy. Taken together, itraconazole encapsulation in NLC represents a viable strategy to optimize cutaneous localization without compromising its efficacy against fungal infections.
中文翻译：
含有伊曲康唑的外用脂质纳米颗粒的开发、皮肤靶向和抗真菌功效。
考虑到农村和城市地区孢子丝菌病和其他真菌感染的发病率增加，以及口服伊曲康唑治疗的局限性和不良反应，我们研究了纳米结构脂质载体（NLC）作为局部给药系统，以增加伊曲康唑在皮肤病变中的定位，并将疗效与减少全身暴露。未负载和负载伊曲康唑的 NLC 显示纳米尺寸（~216-340 nm）、负 zeta 电位（~ -17 mV）和高包封效率（~97%）。 NLC 治疗将完整皮肤和因线性切口（模拟病变）而受损的组织中的经表皮水分流失（皮肤屏障功能的指标）减少了 23-36%，并将药物透皮递送减少了约 2 倍，这证明了其能力将伊曲康唑定位在皮肤内。空载和伊曲康唑负载的 NLC 被认为是安全的，HET-CAM 模型中的得分分别为 0.5 和 0.6，并且对大蜡螟幼虫没有毒性（通过存活和健康指数测量）。获得的对巴西孢子丝菌酵母的最低抑制浓度和最低杀菌浓度值分别为 0.25 和 32 μg/mL。溶液中的药物显示出相似的值，表明封装不会妨碍伊曲康唑的抗真菌作用。 NLC 处理提高了感染巴西沙门氏菌酵母菌和白色念珠菌的大蜡螟幼虫的存活率和健康指数，证明了其抗真菌功效。总而言之，将伊曲康唑封装在 NLC 中代表了一种优化皮肤定位而不损害其抗真菌感染功效的可行策略。
更新日期：2020-04-21
中文翻译：
含有伊曲康唑的外用脂质纳米颗粒的开发、皮肤靶向和抗真菌功效。
考虑到农村和城市地区孢子丝菌病和其他真菌感染的发病率增加，以及口服伊曲康唑治疗的局限性和不良反应，我们研究了纳米结构脂质载体（NLC）作为局部给药系统，以增加伊曲康唑在皮肤病变中的定位，并将疗效与减少全身暴露。未负载和负载伊曲康唑的 NLC 显示纳米尺寸（~216-340 nm）、负 zeta 电位（~ -17 mV）和高包封效率（~97%）。 NLC 治疗将完整皮肤和因线性切口（模拟病变）而受损的组织中的经表皮水分流失（皮肤屏障功能的指标）减少了 23-36%，并将药物透皮递送减少了约 2 倍，这证明了其能力将伊曲康唑定位在皮肤内。空载和伊曲康唑负载的 NLC 被认为是安全的，HET-CAM 模型中的得分分别为 0.5 和 0.6，并且对大蜡螟幼虫没有毒性（通过存活和健康指数测量）。获得的对巴西孢子丝菌酵母的最低抑制浓度和最低杀菌浓度值分别为 0.25 和 32 μg/mL。溶液中的药物显示出相似的值，表明封装不会妨碍伊曲康唑的抗真菌作用。 NLC 处理提高了感染巴西沙门氏菌酵母菌和白色念珠菌的大蜡螟幼虫的存活率和健康指数，证明了其抗真菌功效。总而言之，将伊曲康唑封装在 NLC 中代表了一种优化皮肤定位而不损害其抗真菌感染功效的可行策略。
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