Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, The British University in Egypt (BUE), El Sherouk City, Egypt.
Department of pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Int J Pharm. 2021 Oct 25;608:121114. doi: 10.1016/j.ijpharm.2021.121114. Epub 2021 Sep 20.
Lecithin-chitosan hybrid nanoparticles are emerging as a promising nanocarrier for topical drug delivery. They could achieve a maximized encapsulation of hydrophobic drugs due to the lipophilic nature of lecithin that comprises the core while enhancing retention in the upper skin layers using the positively charged polymeric coat of chitosan. The aim of this study is to incorporate tacrolimus; a hydrophobic anti-proliferative agent into lecithin chitosan hybrid nanoparticles by ethanolic injection technique using a suitable co-solvent to enhance encapsulation of the drug and allow a satisfactory release profile in the upper skin layers. Tacrolimus was successfully incorporated into the synthesized particles using olive oil and Tween 80 as co-solvents, with particle size (160.9 nm ± 15.9 and 118.7 nm ± 13.3, respectively) and EE (88.27% ± 4.3 and 66.72% ± 1.8, respectively). The in vitro drug release profile showed a faster release pattern for the Tween 80-containing particles over a 48-hour period (79.98% vs. 35.57%), hence, were selected for further investigation. The hybrid nanoparticles achieved significantly higher skin deposition than the marketed product (63.51% vs. 34.07%) through a 24-hour time interval, particularly, to the stratum corneum and epidermis skin layers. The in vivo results on IMQ-mouse models revealed superior anti-psoriatic efficacy of the synthesized nanoparticles in comparison to the marketed product in terms of visual observation of the skin condition, PASI score and histopathological examination of autopsy skin samples. Additionally, the in vivo drug deposition showed superior skin deposition of the nanoparticles compared to the marketed product (74.9% vs. 13.4%).
大豆卵磷脂-壳聚糖杂化纳米粒作为一种有前途的新型药物载体，用于局部递药系统。由于大豆卵磷脂的亲脂性，它可以实现疏水性药物的最大包封，而壳聚糖的正电荷聚合物涂层可以增强药物在上皮层的保留。本研究旨在通过乙醇注入技术将他克莫司（一种亲脂性抗增殖剂）包封到大豆卵磷脂-壳聚糖杂化纳米粒中，使用合适的共溶剂来提高药物的包封率，并允许在表皮上层有令人满意的释放特性。他克莫司成功地使用橄榄油和吐温 80 作为共溶剂被包裹到合成的纳米粒中，分别得到粒径（160.9±15.9nm 和 118.7±13.3nm）和 EE（88.27%±4.3 和 66.72%±1.8）。体外药物释放结果显示，在 48 小时内，含有吐温 80 的纳米粒具有更快的释放模式（79.98% vs. 35.57%），因此选择其进行进一步研究。通过 24 小时的时间间隔，杂化纳米粒在皮肤中的沉积量显著高于市售产品（63.51% vs. 34.07%），特别是在角质层和表皮皮肤层。在 IMQ 诱导的小鼠模型中的体内结果表明，与市售产品相比，合成的纳米粒在皮肤状况的视觉观察、PASI 评分和皮肤活检样本的组织病理学检查方面具有更好的抗银屑病疗效。此外，体内药物沉积显示纳米粒的皮肤沉积明显优于市售产品（74.9% vs. 13.4%）。
