Editor-in-Chief İlkay Küçükgüzel Associate Editor Aslı Türe Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2020 , Vol 24 , Issue 6
Ocular delivery of ketorolac tromethamine using microemulsion as a vehicle: Design, evaluation, and transcorneal permeation
Anayatollah SALIMI1,Marzieh BEHROUZIFAR2
1Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran
2Department of Pharmaceutics, Faculty of pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran
DOI : 10.35333/jrp.2020.252 Ketorolac is a nonsteroidal anti-inflammatory drug with analgesic properties. Different clinical studies have established the safeness and efficacy of using 0.5% ketorolac formulations for alleviating ocular inflammation and pain. Ketorolac’s eye drops have a short period of action because of its solubility in tear fluids, which resulting to its quick drainage from the eye, meaning that the patient has to administer it frequently. The present study describes the design of an microemulsion vehicle to be used for the ocular delivery of ketorolac. Ketorolac-loaded microemulsion (ME) was supplied using oleic acid-Transcutol P (oily phase), Tween 80, Span 20 (surfactant), and propylene glycol (co-surfactant). The physicochemical properties of the prepared MEs were evaluated according to their viscosities, pH, droplet sizes, surface tension, physical and chemical stability, drug release, and transcorneal rabbit permeation. The drug release profile revealed that 23.65-38.64% of the drug was released during the 24-hour experiment. The maximum permeated drug percentage was observed for ME-K-1 (9.041%). The whole of prepared MEs with various components and properties significantly increased the cornea permeation rate and permeation percentage after 6 hours (%P6h) from the rabbit cornea. The flux and diffusivity coefficient in ME-K-2 formulation were obtained 0.125 mg/cm2/h and 0.0126 cm2/h, which are 3.49 and 6.464 times higher, respectively, then the values for ketorolac drops (KT 0.5%). The MEs developed in the present work were within the range of acceptable droplet sizes for ocular use and possessed physical and chemical stability. Furthermore, the values recorded for the physicochemical parameters support their suitability for ophthalmic use. Keywords : Transcorneal permeation; microemulsion; ketorolac; rabbit; release
Marmara University