In vitro & in vivo Studies on Lornoxicam Loaded Nanoemulsion Gels for Topical Application
In vitro & in vivo Studies on Lornoxicam Loaded Nanoemulsion Gels for Topical Application
复制标题
DOI：
10.2174/15672018113106660063
复制
发表时间：
2014-02-01
影响因子：
2.4
通讯作者：
Mazumder, Bhaskar
中科院分区：
文献类型：
--
作者：
Dasgupta, Sandipan;Ghosh, Surajit K.;Mazumder, Bhaskar
本工作的目的是增加氯诺昔康半固体外用制剂的溶解度和体外皮肤渗透性，并考察纳米乳制剂的体内潜力。采用自发乳化法制备了优化的氯诺昔康纳米乳剂，其粒径在102~200 nm范围内稳定。稳定的纳米乳液配方通过粘度、液滴大小、透射电子显微镜和折射率进行了表征。测定了氯诺昔康纳米乳和常规凝胶剂的体外透皮速率。与常规凝胶(L-G)相比，纳米乳剂Ne8和纳米凝胶NG8的稳态通量(J(Ss))、渗透系数(K-p)和增强率(E-r)等渗透性参数显著增加。体内研究表明，与常规凝胶剂相比，LX的抗炎作用显著增强。NG8制剂的抗炎作用与空白对照相比，百分率抑制值显著增加，差异有非常显著意义(P<；0.001)。这项工作首次表明，氯诺昔康可以制成纳米乳剂，并可能在提高溶解度和渗透性方面显示出希望。
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 (J(ss)), permeability coefficient (K-p), and enhancement ratio (E-r) were significantly increased in nanoemulsion NE8 and the nanogel NG8 as compared to conventional gel (L-G). 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.