Dapsone (DAP) is a long-established molecule that remains a promising therapeutic agent for various diseases mainly because it combines antimicrobial and anti-inflammatory activities. Its oral application, however, is limited by the dose-dependent hematological side effects that may rise from systemic exposure. As an alternative to overcome this limitation, the administration of DAP to the skin has witnessed prominent interest in the past 20 years, particularly when applied to the treatment of dermatological disorders. In this review, all technological strategies proposed to the topical delivery of DAP are presented. Most of the reported studies have been devoted to the clinical use and safety of a gel formulation containing both solubilized and microcrystalline drug, however, the technological characteristics of such preparation are still missing. In parallel, the incorporation of DAP into vesicular and particulate carriers (e.g. nano- and microemulsions, niosomes, invasomes, bilosomes, cubosomes, solid lipid nanoparticles, nanostructured lipid carriers, polymeric nanocapsules and polymer-lipid-polymer hybrid nanoparticles) appears to be an alternative to provide greater drug release control, enhanced drug solubilization and follicular targeting. Indeed, the main application of DAP topical formulations reported in the literature was the treatment of acne vulgaris, a disease located in the hair follicle. Other diseases affecting different regions of the skin (e.g. cutaneous lupus erythematosus and cutaneous leishmaniasis), however, may also benefit from a topical therapeutic regimen containing DAP. Therefore, the investigation of appendageal route in comparison to passive transmembrane diffusion as a function of targeted disease, as well as pharmacokinetic studies, are perspectives highlighted herein. Such studies may drive future efforts towards the rational development of safe and effective technologies to deliver DAP to the skin.

氨苯砜 (DAP) 是一种历史悠久的分子，它仍然是各种疾病的有前途的治疗剂，主要是因为它结合了抗菌和抗炎活性。然而，其口服应用受到全身暴露可能引起的剂量依赖性血液学副作用的限制。作为克服这一限制的替代方法，在过去的 20 年中，将 DAP 施用于皮肤引起了人们极大的兴趣，特别是在应用于治疗皮肤病时。在这篇综述中，介绍了针对 DAP 局部给药提出的所有技术策略。大多数报道的研究都致力于含有溶解和微晶药物的凝胶制剂的临床使用和安全性，但是，这种制剂的技术特征仍然缺失。例如纳米和微乳液、niosomes、invasomes、bilosomes、cubosomes、固体脂质纳米颗粒、纳米结构脂质载体、聚合物纳米胶囊和聚合物-脂质-聚合物混合纳米颗粒）似乎是提供更好的药物释放控制、增强的药物溶解和滤泡的替代方案目标。事实上，文献中报道的 DAP 局部制剂的主要应用是治疗寻常痤疮，这是一种位于毛囊中的疾病。影响皮肤不同区域的其他疾病（例如然而，皮肤红斑狼疮和皮肤利什曼病）也可能受益于含有 DAP 的局部治疗方案。因此，与被动跨膜扩散相比，作为靶向疾病的函数的附肢途径的研究以及药代动力学研究是本文强调的观点。这些研究可能会推动未来努力合理开发安全有效的技术，将 DAP 输送到皮肤。