Kaempferol (KMP) belong to flavonoid class have developed in ethosomal formulation and were evaluated for their potential to treat diabetic foot ulcers. Even though ethosomes are highly deformable, they can pass through human skin intact. KMP ethosomes were formulated using the cold method and optimized by Box–Behnken design (BBD) (three‐factor, three‐level (33)). The formulation variables used for optimization are drug concentration of KMP, soylecithin content, and ethanol percentage. The optimized formulation was examined using transmission electronic microscopy (TEM), differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy, in‐vitro release, ex‐vivo permeation studies, and storage stability. The optimized KMP ethosomes was found to have vesicle size (VS) of 283 ± 0.3 nm and zeta potential (ZP) of −29.67 ± 0.3 mV, polydispersity index (PDI) of 0.36, % entrapment efficiency (%EE) of 91.02 ± 0.21%, drug loading (%) of 46.23 ± 2.5% followed by good storage stability at 4°C/60 ± 5% RH. In vitro drug release of optimized KMP ethosomes was 88.2 ± 2.75%, which was approximately double when compared with pure KMP release, that is 49.9 ± 1.89%. The release kinetics for optimized KMP ethosomes follows the Korsmeyer–Peppas model. An apparent permeation coefficient of 356.25 ± 0.5 μg/cm2 was determined and compared with pure KMP (118.46 ± 0.3 μg/cm2) for 24 h. According to the study, ethosomes can be a cutting‐edge strategy that offers a new delivery method for prolonged and targeted distribution of KMP in a variety of dosage forms including oral, topical, transdermal, and so forth.

中文翻译：

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使用 Box-Behnken 统计设计开发和优化负载山奈酚的醇质体：体外和离体评估

山奈酚 (KMP) 属于类黄酮类，已开发成醇质制剂，并对其治疗糖尿病足溃疡的潜力进行了评估。尽管醇质体高度变形，但它们可以完好无损地穿过人体皮肤。KMP 醇质体采用冷法配制，并通过 Box-Behnken 设计 (BBD) 进行优化（三因素、三水平（33））。用于优化的配方变量是 KMP 的药物浓度、大豆卵磷脂含量和乙醇百分比。使用透射电子显微镜 (TEM)、差示扫描量热法 (DSC)、傅里叶变换红外 (FTIR) 光谱检查优化的配方，体外发布，离体渗透研究和储存稳定性。优化后的 KMP 乙醇质体的囊泡大小 (VS) 为 283 ± 0.3 nm，zeta 电位 (ZP) 为 -29.67 ± 0.3 mV，多分散指数 (PDI) 为 0.36，% 包封效率 (%EE) 为 91.02 ± 0.21 %，载药量 (%) 为 46.23 ± 2.5%，并且在 4°C/60 ± 5% RH 下具有良好的储存稳定性。体外优化的 KMP 醇质体的药物释放率为 88.2 ± 2.75%，与纯 KMP 释放率（49.9 ± 1.89%）相比，大约增加了一倍。优化的 KMP 醇质体的释放动力学遵循 Korsmeyer-Peppas 模型。表观渗透系数为356.25±0.5μg/cm2测定并与纯 KMP (118.46 ± 0.3 μg/cm2）24小时。根据这项研究，醇质体可以成为一种前沿策略，它提供了一种新的递送方法，可以以多种剂型（包括口服、外用、透皮等）延长 KMP 的靶向分布。