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Abstract：
The article aimed to formulate an MLX binary ethosome hydrogel for topical delivery to escalate MLX solubility, facilitate dermal permeation, avoid systemic adverse events, and compare the permeation flux and efficacy with the classical type. MLX ethosomes were prepared using the hot method according to the Box-Behnken experimental design. The formulation was implemented according to 16 design formulas with four center points. Independent variables were (soya lecithin, ethanol, and propylene glycol concentrations) and dependent variables (vesicle size, dispersity index, encapsulation efficiency, and zeta potential). The design suggested the optimized formula (MLX-Ethos-OF) with the highest desirability to perform the best responses formulated and validated. It demonstrates a 169 nm vesicle size, 0.2 dispersity index, 83.1 EE%, and -42.76 mV good zeta potential. MLX-Ethos-OF shows an amorphous form in PXRD and a high in vitro drug release of >90% over 7 h by diffusion and erosion mechanism. MLX-Ethos-OF hyaluronic acid hydrogel was fabricated and assessed. It shows an elegant physical appearance, shear thinning system rheological behavior, good spreadability, and skin-applicable pH value. The ex vivo permeation profile shows a flux rate of 70.45 μg/cm2/h over 12 h. The in vivo anti-inflammatory effect was 53.2% ± 1.3 over 5 h. compared with a 10.42 flux rate and 43% inflammatory inhibition of the classical ethosomal type. The conclusion is that binary ethosome is highly efficient for MLX local delivery rather than classical type.
摘要：
本文旨在配制用于局部递送的MLX二元乙醇体水凝胶，以提高MLX的溶解度，促进皮肤渗透，避免系统性不良事件，并与经典类型的渗透通量和功效进行了比较。根据Box-Behnken实验设计使用热法制备MLX醇质体。该配方是根据具有四个中心点的16个设计配方实施的。自变量是(大豆卵磷脂，乙醇,和丙二醇浓度)和因变量(囊泡大小，分散指数，封装效率，和zeta电位)。该设计建议了具有最高期望的优化配方（MLX-Ethos-OF），以执行制定和验证的最佳响应。它显示出169纳米的囊泡大小，0.2分散性指数，83.1EE%，和-42.76mV良好的ζ电位。MLX-Ethos-OF在PXRD中显示出无定形形式，并且通过扩散和侵蚀机制在7小时内显示出>90％的高体外药物释放。制造并评估MLX-Ethos-OF透明质酸水凝胶。它显示出优雅的物理外观，剪切稀化系统的流变行为，良好的铺展性，和皮肤适用的pH值。离体渗透曲线显示在12小时内的流通量为70.45μg/cm2/h。与经典乙醇型的10.42流通量和43%的炎症抑制相比,体内抗炎作用在5小时内为53.2%±1.3。结论是，二元模型体对于MLX局部递送而不是经典类型是高效的。
