Department of Pharmaceutics, Faculty of Pharmacy, University of Karachi, Karachi, Pakistan.
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.
Biomed Res Int. 2017;2017:4654958. doi: 10.1155/2017/4654958. Epub 2017 Sep 27.
The aim of the study was to develop a reservoir-type transdermal patch for a controlled delivery of dexibuprofen and to evaluate its in vivo anti-inflammatory activity in Albino Wistar rats. In order to develop these patches, six formulations of dexibuprofen microemulsion comprising ethyl oleate, Tween 80: PG (2 : 1), and water were prepared by simplex lattice design and characterized. The reservoir compartment was filled with these microemulsions and in vitro release and skin permeation were assessed. The optimized patch was obtained on the basis of the responses: and flux. The impact of drug loading, surface area, membrane thickness, adhesive, and agitation speed on drug release and permeation was also studied. The skin sensitivity reaction and in vivo anti-inflammatory activity of optimized patch were evaluated. Stability study at three different temperatures for three months was carried out. The result suggests that a membrane based patch with zero-order release rate, of 79.13 ± 3.08%, and maximum flux of 331.17 g/cmh can be obtained exhibiting suitable anti-inflammatory activity with no visible skin sensitivity reaction. The outcomes of stability study recommend storage of patches at 4°C having shelf-life of 6.14 months. The study demonstrates that the reservoir-type transdermal patch of dexibuprofen microemulsion has a potential of delivering drug across skin in controlled manner with required anti-inflammatory activity.
本研究旨在开发一种用于控制地昔布非诺酯释放的储库型透皮贴剂,并评估其在白化 Wistar 大鼠体内的抗炎活性。为了开发这些贴片,我们通过单纯形格子设计制备了包含油酸乙酯、吐温 80:PG(2:1)和水的六种地昔布非诺酯微乳配方,并对其进行了表征。储库室填充了这些微乳,评估了体外释放和皮肤渗透。根据响应: 和通量,选择了优化的贴片。还研究了药物载药量、表面积、膜厚度、粘合剂和搅拌速度对药物释放和渗透的影响。评估了优化贴片的皮肤敏感性反应和体内抗炎活性。进行了为期三个月的三个不同温度的稳定性研究。结果表明,可获得具有零级释放速率、 的 79.13±3.08%和最大通量为 331.17μg/cmh 的基于膜的贴片,表现出适当的抗炎活性,无明显的皮肤敏感性反应。稳定性研究的结果建议将贴片储存在 4°C 下,保质期为 6.14 个月。该研究表明,地昔布非诺酯微乳的储库型透皮贴剂具有通过皮肤以受控方式输送药物的潜力,并具有所需的抗炎活性。