a Department of Pharmaceutics , KLE University's College of Pharmacy , Bengaluru , India.
b Institute for Drug Delivery and Biomedical Research , Bengaluru , India.
Pharm Dev Technol. 2018 Oct;23(8):806-814. doi: 10.1080/10837450.2017.1369110. Epub 2017 Aug 31.
The aim of the study was to enhance the transdermal delivery of diclofenac potassium (DP) from hydrogels by constant voltage iontophoresis (CVI). The other objective was to establish the safety and efficacy of CVI in rats.
Hydrogels of DP were developed using hydroxyethyl cellulose as matrix material and geraniol, l-menthol and thymol as iontophoretic efficiency enhancers (IEE). In vitro permeation of hydrogels under CVI (1.5 V) was performed in Franz diffusion cells across porcine skin. The ability of CVI to deliver therapeutic amount of DP in vivo was assessed in rat paw edema model.
CVI significantly (p < 0.05) increased the steady state flux of DP compared to the passive. The hydrogels containing geraniol and l-menthol enhanced the iontophoretic flux of DP by ∼4.75 and ∼4.49 fold, respectively compared to passive control. The in vivo studies indicated that CVI in combination with IEE, significantly reduced (p < 0.05) area under the curve (AUC) of % inflammation compared to passive treatment. An excellent correlation (r = 0.996) was noted between in vitro flux values and AUC of % inflammation.
The preclinical studies conclusively demonstrated that CVI in combination with IEE's such as geraniol or l-menthol has the potential to safely deliver therapeutic amounts of DP.
本研究旨在通过恒电压离子电渗（CVI）增强双氯芬酸钾（DP）从水凝胶中的透皮传递。另一个目的是确定 CVI 在大鼠中的安全性和有效性。
使用羟乙基纤维素作为基质材料和橙花醇、薄荷醇和百里香作为离子电渗效率增强剂（IEE）开发 DP 的水凝胶。在 Franz 扩散细胞中，通过 CVI（1.5V）在猪皮上进行水凝胶的体外渗透。在大鼠足肿胀模型中评估 CVI 体内输送治疗量 DP 的能力。
与被动相比，CVI 显著（p<0.05）增加了 DP 的稳态通量。与被动对照相比，含有橙花醇和薄荷醇的水凝胶分别将 DP 的离子电渗通量增强了约 4.75 倍和 4.49 倍。体内研究表明，与被动治疗相比，CVI 联合 IEE 显著降低（p<0.05）了炎症的 AUC。体外通量值与炎症 AUC 之间存在极好的相关性（r=0.996）。
临床前研究明确表明，CVI 联合 IEE（如橙花醇或薄荷醇）有可能安全地输送治疗量的 DP。
