Nano-delivery systems have gained remarkable recognition for targeted delivery of therapeutic payload, reduced off-target effects, and improved biopharmaceutical profiles of drugs. Therefore, we aimed to fabricate polymeric nanoparticles (NPs) to deliver tacrolimus (TCS) to deeper layers of the skin in order to alleviate its systemic toxicity and improved therapeutic efficacy against atopic dermatitis (AD). To further optimize the targeting efficiency, TCS-loaded NPs were coated with hyaluronic acid (HA). Following the various physicochemical optimizations, the prepared HA-TCS-CS-NPs were tested for in vitro drug release kinetics, drug permeation across the stratum corneum, percentage of drug retained in the epidermis and dermis, and anti-AD efficacy. Results revealed that HA-TCS-CS-NPs exhibit sustained release profile, promising drug permeation ability, improved skin retention, and pronounced anti-AD efficacy. Conclusively, we anticipated that HA-based modification of TCS-CS-NPs could be a promising therapeutic approach for rationalized management of AD, particularly in children as well as in adults having steroid phobia.

纳米递送系统已获得针对治疗性负载的靶向递送，减少脱靶效应以及改善药物的生物制药特性的卓越认可。因此，我们旨在制造聚合物纳米颗粒（NPs）以将他克莫司（TCS）递送至皮肤的更深层，以减轻其全身毒性并提高对特应性皮炎（AD）的治疗功效。为了进一步优化靶向效率，将负载TCS的NP涂上透明质酸（HA）。在进行了各种理化优化之后，对制备的HA-TCS-CS-NPs进行了体外测试药物释放动力学，穿过角质层的药物渗透，保留在表皮和真皮中的药物百分比以及抗AD功效。结果显示，HA-TCS-CS-NPs表现出持续释放特征，有希望的药物渗透能力，改善的皮肤滞留性和明显的抗AD功效。结论是，我们预计基于HA的TCS-CS-NPs修饰可能是合理管理AD的有前途的治疗方法，尤其是对于患有类固醇恐惧症的儿童以及成人。