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Cow ghee fortified ocular topical microemulsion; in vitro, ex vivo, and in vivo evaluation.
Journal of Microencapsulation ( IF 3.0 ) Pub Date : 2019-09-09 , DOI: 10.1080/02652048.2019.1662121
Aashu Gupta 1 , Kritika Nayak 1 , Manju Misra 1
Affiliation  

Aim: Utility of cow ghee (CG) as permeation enhancer in development of topical ocular microemulsion (ME) for delivery of fluocinolone acetonide (FA) to posterior eye.

Methods: 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 ex vivo permeation and irritation. In vivo pharmacokinetic studies were performed on Sprague dawley rats.

Results: 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. Ex vivo study revealed higher permeation and non-irritancy. In vivo pharmacokinetic study showed retention of CG fortified ME in posterior rat eye.

Conclusion: Present investigation established CG as permeation enhancer for ocular topical formulation.



中文翻译:

牛酥油增强了眼用局部微乳剂;体外,离体和体内评估。

目的:使用牛油酥油(CG)作为渗透促进剂,用于局部用眼用微乳状液(ME),以将氟轻松将乙酰氟轻松(FA)输送至后眼。

方法:为制备ME,根据FA的溶解度筛选油,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率。已开发的ME的特征在于其物理化学性质,例如大小,多分散指数,ζ电位和稳定性等。对它们进行了离体渗透和刺激性评估。Sprague dawley大鼠上进行了体内药代动力学研究。

结果:选择了月桂醇为油,拉布拉索尔为表面活性剂,反式角酚为助表面活性剂。油:表面活性剂:助表面活性剂:水的最佳比例为4:23:23:50。表征了以CG强化的已开发FA负载ME。体外研究显示较高的渗透性和无刺激性。体内药代动力学研究表明,在大鼠后眼中保留了CG增强的ME。

结论:目前的研究建立了CG作为眼外用制剂的渗透促进剂。

更新日期:2019-09-09
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