Hidradenitis suppurativa is a chronic and debilitating inflammatory condition related to a permanent obstruction of the pilosebaceous units. Until nowadays, therapeutic options are unsatisfactory. Here, we propose nanostructured lipid carriers (NLC) entrapping an association of clindamycin phosphate (CDM) and rifampicin (RIF) as a topical alternative for the treatment of the disease. Chemical compatibility between the drugs was demonstrated using thermal analysis combined with ATR-FTIR and X-ray powder diffraction assays. Nanocarriers’ diameter was narrowly distributed (polydispersity index = 0.2) around 400 ± 14 nm, they possess a negative surface charge (−48.9 ± 0.7 mV) and high drug entrapment efficiencies (80.2 ± 0.4 % and 93.4 ± 0.7 % for CDM and RIF, respectively). The formulation proved to be safe for the topical application, as it was non-irritant on both HET-CAM and reconstructed human epidermis (RHE) assays. Spin-label EPR indicated an NLC affinity for the lipidic domains of stratum corneum, which could benefit the targeting of the sebaceous units. Indeed, when applied on the skin in vitro, even when mimicking the sebaceous condition, NLC accumulated into the hair follicles openings, not altering the amount of accumulated CDM and significantly increasing by 12-fold the uptake of RIF in these structures. In conclusion, developed NLC formulation incorporating the antibiotics CDM and RIF is a promising strategy for the topical treatment of hidradenitis suppurativa or other infections that may affect the pilosebaceous units.

化脓性汗腺炎是一种慢性和衰弱性炎症，与毛囊皮脂腺单位的永久性阻塞有关。直到今天，治疗选择还不能令人满意。在这里，我们提出了一种纳米结构脂质载体（NLC），将克林霉素磷酸酯（CDM）和利福平（RIF）结合起来，作为局部替代药物治疗该疾病。使用热分析结合ATR-FTIR和X射线粉末衍射分析法证明了药物之间的化学相容性。纳米载体的直径在400±14 nm左右狭窄分布（多分散指数= 0.2），它们具有负表面电荷（−48.9±0.7 mV），并且具有较高的药物截留效率（CDM和RIF分别为80.2±0.4％和93.4±0.7％） ， 分别）。事实证明该制剂对局部应用是安全的，因为它在HET-CAM和重建人表皮（RHE）分析中均无刺激性。自旋标记EPR表示对角质层脂质结构域具有NLC亲和力，这可能有利于皮脂单位的靶向。确实，当涂在皮肤上在体外，即使模拟皮脂状况，NLC仍会累积到毛囊开口中，不会改变累积的CDM量，并且在这些结构中的RIF吸收量会显着增加12倍。总之，已开发出的结合了CDM和RIF抗生素的NLC制剂是局部治疗化脓性汗腺炎或其他可能影响菌毛的单位的策略。