Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh-786004, Assam, India.
Curr Drug Deliv. 2014;11(1):132-8. doi: 10.2174/15672018113106660063.
The objective of this work was to increase the solubility, in vitro skin permeability of lornoxicam from semisolid topical formulations and also to investigate the in vivo potential of nanoemulsion formulation. Optimized lornoxicam loaded nanoemulsion was prepared successfully by spontaneous self-emulsification method and the size of the stable formulations was found within the range of 102 to 200 nm. The stable nanoemulsion formulations characterized for viscosity, droplet size, transmission electron microscopy (TEM) and refractive index. In vitro permeation rate of nanoemulsion and conventional gel of lornoxicam (LX) were determined. Prmeability parameters like steady-state flux (Jss), permeability coefficient (Kp), and enhancement ratio (Er) were significantly increased in nanoemulsion NE8 and the nanogel NG8 as compared to conventional gel (LG). In vivo studies revealed a significant increase in anti-inflammatory effects as compared with conventional gel of LX. The anti-inflammatory effects of formulation NG8 showed a significant increase in percent inhibition value when compared with control, this difference was found to be highly significant (p<0.001). This work shows for the first time that lornoxicam can be formulated into nanoemulsions and may show promise in enhancing solubility and permeation.
本工作旨在提高洛索洛芬半固体制剂的溶解度、体外皮肤透过性，并研究纳米乳制剂的体内潜力。通过自发自乳化法成功制备了优化的载洛索洛芬纳米乳，其稳定制剂的粒径在 102nm 至 200nm 范围内。对稳定的纳米乳制剂进行了粘度、粒径、透射电子显微镜（TEM）和折射率的表征。测定了纳米乳和洛索洛芬常规凝胶（LX）的体外透皮率。与常规凝胶（LG）相比，纳米乳 NE8 和纳米凝胶 NG8 的稳态通量（Jss）、渗透系数（Kp）和增强比（Er）显著增加。体内研究表明，与洛索洛芬常规凝胶相比，纳米凝胶 NG8 的抗炎作用显著增加。与对照组相比，制剂 NG8 的抗炎作用的抑制率百分比显著增加，这种差异具有高度显著性（p<0.001）。本工作首次表明，洛索洛芬可以制成纳米乳剂，可能在提高溶解度和渗透性方面具有潜力。
