Aqueous-Based Nanoemulsion Containing (-)-α-Bisabolol for Topical Treatment of Skin burns

E. D. A. Almeida, Ricardo Ferreira-Nunes, B. R. L. Aguiar, P. E. D. dos Reis, Taís Gratieri, Marcilio Cunha-Filho, G. M. Gelfuso
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Abstract

α-Bisabolol (BIS) is a sesquiterpene extracted from chamomile flowers, which has been used to topically treat burnt skin has been reported. High lipophilicity of BIS, however, is a problem for both skin application and washing. The present study aimed to prepare and characterize a stable and safe aqueous-based nanoemulsion to incorporate BIS and favor skin penetration focusing on skin burns' topical treatment. Oil-in-water nanoemulsions were obtained from a pseudo-ternary phase diagram. The selected nanoemulsion was characterized (droplet size, PDI, and zeta potential), and the stability was assessed for 60 days at 6ºC and room temperature. The irritability of the formulation was determined by HET-CAM. Skin permeation studies were carried out in vitro intact skin, hot water burn skin, and hot plate burn skin. The nanoemulsion incorporated 1% (w/w) BIS, presented droplets' size of 14.0±0.8 nm (PDI= 0.13±0.02), the zeta potential of +7.5±1.9 mV, and was physically stable over 60 days. The HET-CAM did not show any irritability process provided by the nanoformulation. In the skin permeation experiments, when compared to an oily control solution of BIS, nanoemulsion increased 3.7-fold penetration of the drug in intact skin, likely because the nanoformulation acted as an absorption drug enhancer. On a hot water burn skin model, the increase in drug penetration was 1.7-fold, and in the hot plate burn skin, it was 2.3-fold. The nanoemulsion seems to be a promising alternative for skin burns' topical treatment using this natural active substance.
含有(-)-α-双abolol的水基纳米乳局部治疗皮肤烧伤
α-双abolol (bisabolol, BIS)是从洋甘菊中提取的倍半萜,已被报道用于局部治疗烧伤皮肤。然而,BIS的高亲脂性对皮肤应用和洗涤都是一个问题。本研究旨在制备一种稳定、安全的水基纳米乳,用于皮肤烧伤的局部治疗。利用伪三元相图制备了水包油纳米乳液。对所选择的纳米乳进行了表征(液滴大小、PDI和zeta电位),并在6℃和室温条件下评估了60天的稳定性。用ht - cam测定制剂的激惹性。在体外完整皮肤、热水烧伤皮肤和热板烧伤皮肤中进行皮肤渗透研究。加入1% BIS (w/w)的纳米乳液,微滴尺寸为14.0±0.8 nm (PDI= 0.13±0.02),zeta电位为+7.5±1.9 mV, 60 d内物理稳定。HET-CAM没有显示出纳米配方提供的任何过敏性过程。在皮肤渗透实验中,与BIS的油性对照溶液相比,纳米乳在完整皮肤中的药物渗透增加了3.7倍,可能是因为纳米制剂起到了吸收药物的促进作用。在热水烧伤皮肤模型中,药物渗透增加了1.7倍,在热板烧伤皮肤模型中,药物渗透增加了2.3倍。纳米乳液似乎是使用这种天然活性物质局部治疗皮肤烧伤的一种很有前途的选择。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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