Purpose

Adapalene (AD) is one of the main retinoids used in the topical therapy of acne, an extremely common skin disease usually associated with psychological morbidity. However, like other retinoids, AD is frequently associated with skin irritation. To overcome the skin irritation, we proposed the encapsulation of AD in solid lipid nanoparticles (SLNs) using the ion pair strategy.

Methods

The developed SLN-AD was characterized by high-performance liquid chromatography, differential scanning calorimetry, X-ray diffraction, synchrotron small-angle X-ray scattering, and transmission electron microscopy. In vitro permeation tests using porcine skin and in vivo mice skin irritation test were performed to evaluate, respectively, the drug’s skin distribution and the skin irritation.

Results

The characterization studies were able to demonstrate that the proposed strategy effectively provided high AD encapsulation in SLNs and its incorporation into a hydrophilic gel. Sustained release, epidermal targeting, and less skin irritation were observed for SLN-AD gel in comparison to the marketed AD gel.

Conclusions

The studies demonstrated that the encapsulation of AD in SLNs through the formation of an ion pair is a valuable alternative to diminish the adverse skin reactions caused by AD and can optimize patient adherence to treatment.

中文翻译：

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固体脂质纳米颗粒中的离子对策略：通过控制Adapalene释放来改善表皮靶向性的靶向方法，从而降低皮肤刺激性。

目的

阿达帕林（AD）是痤疮局部治疗中使用的主要类维生素A之一，痤疮是一种极为常见的皮肤疾病，通常与心理疾病相关。但是，像其他类维生素A一样，AD经常与皮肤刺激有关。为了克服对皮肤的刺激，我们建议使用离子对策略将AD封装在固体脂质纳米颗粒（SLN）中。

方法

研制的SLN-AD具有高效液相色谱，差示扫描量热法，X射线衍射，同步加速器小角X射线散射和透射电子显微镜的特点。进行了使用猪皮肤的体外渗透测试和体内小鼠皮肤刺激测试，以分别评估药物的皮肤分布和皮肤刺激。

结果

表征研究能够证明所提出的策略有效地提供了SLNs中的高AD封装以及将其并入亲水性凝胶中。与市售的AD凝胶相比，SLN-AD凝胶具有持续释放，表皮靶向性和较少的皮肤刺激性。

结论

研究表明，通过形成离子对将AD包裹在SLN中是减少AD引起的不良皮肤反应并可以优化患者对治疗依从性的有价值的替代方法。