Novel nicotinamide skin-adhesive hot melt extrudates for treatment of acne

<b>Objectives</b>: Hot melt extrusion is a continuous process with wide industrial applicability. Till current date, there have been no reports on the formulation of extrudates for topical treatment of dermatological diseases. <b>Methods</b>: The aim of the present work was to prepare and characterize medicated hot melt extrudates based on Soluplus polymer and nicotinamide, and to explore their applicability in acne treatment. The extrudates were characterized using DSC, FTIR, XRD, and DVS. The extrudates were also tested for their skin adhesion potential, ability to deposit nicotinamide in different skin layers, and their clinical efficacy in acne patients. <b>Results</b>: The 10% nicotinamide extrudates exhibited amorphous nature which was reserved during storage, with no chemical interaction between nicotinamide and Soluplus. Upon contrasting the skin adhesion and drug deposition of extrudates and nicotinamide gel, it was evident that the extrudates displayed significantly higher adhesion and drug deposition reaching 4.8 folds, 5.3 folds, and 4.3 folds more in the stratum corneum, epidermis and dermis, respectively. Furthermore, the extrudates significantly reduced the total number of acne lesions in patients by 61.3% compared to 42.14% with the nicotinamide gel. <b>Conclusion</b>: Soluplus extrudates are promising topical drug delivery means for the treatment of dermatological diseases.

<b>研究目的</b>：热熔挤出（Hot melt extrusion）是一种具备广泛工业应用价值的连续化工艺。截至目前，尚无针对皮肤病局部治疗用挤出物制剂的研究报道。<b>研究方法</b>：本研究旨在制备并表征以Soluplus聚合物与烟酰胺（nicotinamide）为基质的药用热熔挤出物，并探究其在痤疮治疗中的应用潜力。本研究采用差示扫描量热法（DSC）、傅里叶变换红外光谱（FTIR）、X射线衍射（XRD）与动态蒸汽吸附法（DVS）对挤出物进行表征；同时测试了该挤出物的皮肤黏附性能、烟酰胺在不同皮肤层中的沉积能力，以及其在痤疮患者中的临床疗效。<b>研究结果</b>：含10%烟酰胺的挤出物呈现无定形结构，且该结构在储存过程中得以保持，烟酰胺与Soluplus之间未发生化学反应。对比挤出物与烟酰胺凝胶的皮肤黏附性能及药物沉积效果后发现，挤出物的黏附能力与药物沉积量显著更优：在角质层、表皮与真皮中的药物沉积量分别较凝胶高出4.8倍、5.3倍与4.3倍。此外，相较于烟酰胺凝胶组的42.14%皮损改善率，挤出物可使患者的痤疮皮损总数显著减少61.3%。<b>研究结论</b>：Soluplus基挤出物是一种极具应用前景的皮肤病局部治疗药物递送制剂。