Harwansh Ranjit K, Mukherjee Pulok K, Bahadur Shiv, Biswas Rajarshi
School of Natural Product Studies, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
School of Natural Product Studies, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
Life Sci. 2015 Nov 15;141:202-11. doi: 10.1016/j.lfs.2015.10.001. Epub 2015 Oct 5.
The study was aimed to develop a ferulic acid (FA) loaded nanoemulsion based gel in order to ensure the enhanced permeability and maximum antioxidant activity against UVA induced oxidative stress in rat.
The optimized ferulic acid loaded nanoemulsion 3 (FA-NE3) was prepared by spontaneous nano-emulsification method with an appropriate ratio (20:30:50% w/w) of the oil (isostearyl isostearate), aqueous system and Smix [surfactant (labrasol) and co-surfactant (plurol isostearique)] respectively. FA-NE3 was characterized by measuring their droplet size, zeta potential, refractive index, transmission electron microscopy (TEM), ultraviolet (UV), fourier transform infrared spectroscopy (FTIR) and rheological characteristics. Ex vivo skin permeation and in vivo UVA protection activity of FA-NE3 based nano-gels (FA-NG3) along with placebo were studied through the rat skin.
FA-NE3 exhibited sustained-release profile, better permeability and ultraviolet A (UVA) protection activity as compared to conventional dosage form. This phenomenon may be attributed towards increased solubility of the drug and enhanced permeability from nanoemulsion. FA-NE3 based nanogel (FA-NG3) could elevate the level of skin marker enzymes against oxidative stress mediated by UVA.
The gel formulation exhibited significant (P<0.01) skin permeability and antioxidant activity in the current investigations. The nanogel could be promising nanocarriers for topical delivery of FA in response to better skin protection activity against UVA rays in a sustained manner.
本研究旨在开发一种负载阿魏酸（FA）的纳米乳凝胶，以确保增强渗透性，并对大鼠紫外线A（UVA）诱导的氧化应激具有最大抗氧化活性。
采用自发纳米乳化法，分别以适当比例（20:30:50% w/w）的油（异硬脂酸异硬脂酯）、水相体系和混合表面活性剂[表面活性剂（Labrasol）和助表面活性剂（异硬脂酸聚甘油酯）]制备优化的负载阿魏酸纳米乳3（FA-NE3）。通过测量其粒径、zeta电位、折射率、透射电子显微镜（TEM）、紫外（UV）、傅里叶变换红外光谱（FTIR）和流变学特性对FA-NE3进行表征。通过大鼠皮肤研究了基于FA-NE3的纳米凝胶（FA-NG3）与安慰剂的离体皮肤渗透和体内UVA防护活性。
与传统剂型相比，FA-NE3表现出缓释特性、更好的渗透性和紫外线A（UVA）防护活性。这种现象可能归因于药物溶解度的增加和纳米乳渗透性的增强。基于FA-NE3的纳米凝胶（FA-NG3）可以提高皮肤标记酶的水平，以抵抗UVA介导的氧化应激。
在当前研究中，该凝胶制剂表现出显著（P<0.01）的皮肤渗透性和抗氧化活性。由于对UVA射线具有更好的持续皮肤保护活性，纳米凝胶可能是用于FA局部递送的有前景的纳米载体。
