Department of dermatology, The First Affiliated Hospital, Xi'an Medical College, Xi'an, 710077, China.
Department of Pharmaceutics, Faculty of Pharmacy, Umm Al-Qura University, Makkah, Saudi Arabia; Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Egypt.
Carbohydr Polym. 2018 Oct 1;197:478-489. doi: 10.1016/j.carbpol.2018.06.023. Epub 2018 Jun 6.
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.
纳米传递系统因其能够靶向输送治疗有效载荷、减少脱靶效应以及改善药物的生物制药特性而备受关注。因此,我们旨在制备聚合物纳米颗粒(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)的治疗效果。为了进一步提高靶向效率,将 TCS 负载的 NPs 用透明质酸(HA)进行包衣。经过各种物理化学优化后,对制备的 HA-TCS-CS-NPs 进行了体外药物释放动力学、药物穿过角质层的渗透、表皮和真皮中药物滞留的百分比以及抗 AD 功效的测试。结果表明,HA-TCS-CS-NPs 具有持续释放的特点,具有良好的药物渗透能力、改善的皮肤保留效果和显著的抗 AD 功效。总之,我们预计 TCS-CS-NPs 的基于 HA 的修饰可能是一种有前途的治疗方法,可用于合理管理 AD,特别是在儿童以及对类固醇有恐惧症的成人中。