Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research , Gandhinagar , Gujarat , India.
J Microencapsul. 2019 Nov;36(7):603-621. doi: 10.1080/02652048.2019.1662121. Epub 2019 Sep 9.
Utility of cow ghee (CG) as permeation enhancer in development of topical ocular microemulsion (ME) for delivery of fluocinolone acetonide (FA) to posterior eye. For ME preparation, oil, surfactant and cosurfactant were screened based on solubility of FA. Pseudoternary phase diagrams were constructed to determine their ratios. The developed MEs were characterised for their physicochemical properties like size, polydispersity index, zeta potential, and stability etc. They were evaluated for permeation and irritation. pharmacokinetic studies were performed on Sprague dawley rats. Lauroglycol as oil, labrasol as surfactant and Transcutol as cosurfactant were selected. The optimised ratio of oil:surfactant:cosurfactant:water was 4:23:23:50. The developed FA loaded ME fortified with CG was characterised. study revealed higher permeation and non-irritancy. pharmacokinetic study showed retention of CG fortified ME in posterior rat eye. Present investigation established CG as permeation enhancer for ocular topical formulation.
牛脂（CG）作为透皮促进剂在开发用于眼部后段递氟轻松丙酮（FA）的局部眼用微乳（ME）中的应用。 为了制备 ME，根据 FA 的溶解度筛选油相、表面活性剂和助表面活性剂。构建伪三元相图以确定它们的比例。对所开发的 ME 的物理化学性质（如大小、多分散指数、Zeta 电位和稳定性等）进行了表征。评价了它们的渗透性和刺激性。在 Sprague dawley 大鼠上进行了药代动力学研究。选择了月桂酰基聚乙二醇甘油酯（Lauroglycol）作为油相，月桂醇聚氧乙烯醚（Labrasol）作为表面活性剂， 丙二醇（Transcutol）作为助表面活性剂。优化的油相：表面活性剂：助表面活性剂：水的比例为 4：23：23：50。对含有 CG 的 FA 负载 ME 进行了表征。研究表明 CG 可增加 FA 的透皮吸收且无刺激性。药代动力学研究表明 CG 强化 ME 在大鼠眼后段的滞留。本研究确立了 CG 作为眼部局部制剂的透皮促进剂。
