University of Chemistry and Technology Prague, Faculty of Chemical Technology, Department of Organic Technology, Technická 5, 166 28 Prague, Czech Republic.
University of Chemistry and Technology Prague, Faculty of Chemical Technology, Department of Organic Technology, Technická 5, 166 28 Prague, Czech Republic.
Int J Pharm. 2022 Nov 25;628:122264. doi: 10.1016/j.ijpharm.2022.122264. Epub 2022 Oct 7.
The transdermal application of actives offers numerous advantages over other conventional routes. Namely, a stable level of drugs in the bloodstream and reduced side effects are the argument for topical administration. Unfortunately, the exceptional skin barrier and unsuitable physico-chemical properties of drugs are the limiting factors for the transdermal passage. It is possible to overcome this by incorporating the drug into nano-carriers to enhance its permeation through the skin barrier. For this purpose, we prepared lipid nanocapsules (LNCs) to modulate skin passage of three pharmaceutically important drugs - indomethacin (IND), diclofenac sodium (DF) and caffeine (CF). We present a stable system prepared by the phase inversion temperature method with particle size under 100 nm and PDI < 0.1 with great encapsulation efficiency for indomethacin and diclofenac. By FTIR it was possible to confirm (for IND and DF) or disprove (in case of CF) the incorporation of a drug into the LNCs. By ex vivo permeation experiments on porcine skin, we confirmed the superior effect of the LNCs on the APIs skin passage. The drug permeated through the skin with higher intensity when delivered from LNCs compared to other standard formulations. We show that lipid nanocapsules play an important role in enhanced topical application of actives.
经皮给药相对于其他传统途径有许多优势。也就是说，血液中药物的稳定水平和减少副作用是局部给药的论据。不幸的是，皮肤屏障的特殊性和药物的物理化学性质不合适是经皮传递的限制因素。可以通过将药物纳入纳米载体来增强其穿过皮肤屏障的渗透来克服这一问题。为此，我们制备了脂质纳米胶囊（LNC）来调节三种药物 - 吲哚美辛（IND）、双氯芬酸钠（DF）和咖啡因（CF） - 的经皮传递。我们展示了一种通过相转变温度法制备的稳定系统，粒径小于 100nm，PDI<0.1，对吲哚美辛和双氯芬酸钠具有很高的包封效率。通过傅里叶变换红外光谱（FTIR）可以确认（对于 IND 和 DF）或否定（对于 CF）药物是否被包封在 LNC 中。通过猪皮的体外渗透实验，我们证实了 LNC 对 API 经皮传递的优越效果。与其他标准制剂相比，LNC 给药时药物透过皮肤的强度更高。我们表明，脂质纳米胶囊在增强活性药物的局部应用中发挥着重要作用。
