Int. J. Pharm. Sci. Rev. Res., 66(1), January - February 2021; Article No. 22, Pages: 136-141 ISSN 0976 – 044X International Journal of Pharmaceutical Sciences Review and Research Available online at www.globalresearchonline.net ©Copyright protected. Unauthorised republication, reproduction, distribution, dissemination and copying of this document in whole or in part is strictly prohibited. 136 B.Padmasri 1* , R.Nagaraju 2 1. Department of Pharmaceutical Technology, Sri Venkateswara College of Pharmacy, Etherla, Srikakulam, India. 2 .Department of Pharmaceutics, Institute of Pharmaceutical Technology, Sri Padmavathi Mahila, Viswa Vidylayam, Tirupati, India. *Corresponding author’s E-mail: padmasripharma@gmail.com Received: 21-10-2020; Revised: 26-12-2020; Accepted: 03-01-2021; Published on: 15-01-2021. ABSTRACT Ophthalmic In-situ gel systems refers to polymer solution which can be administered as liquid and undergoes a sol-to-gel transition upon exposure to physiological environment i.e., pH, Temperature, ions in the lachrymal fluid. The main important aim of the current study was ocular itraconazole in situ gel systems development and evaluation for its enhancing ocular bioavailability and in-vitro antifungal activity assessment. The keratomycosis is a chronic illness that can may leads to vision loss if not treated effectively. Itraconazole is low soluble drug due to this nature in present study we selected solid dispersion formulation (F12) to prepare in-situ gelling formulations of itraconazole. The pH-triggered in-situ gel formulations were prepared by using different grades of polymers like Carbopol along with of HPMC. The prepared formulations were assessed to know physical appearance, pH, viscosity, content of drug, gelling capacity and time, in-vitro permeation studies, rheological properties and antifungal studies. All the prepared formulations are exhibiting quite consistent drug content. Furthermore in-vitro studies of drug release and antifungal activity of these formulations were also evaluated. Drug release study of all the formulations showed sustained release properties. The antimycotic effectiveness of the optimized preparation against C.albicans and Asperigillus niger confirmed that designed formulation has enhanced effect and retained its properties against fungal infection. In conclusion, hence formulation (F3) was selected as optimized formulations could be offered as shows potential approach for ocular drug delivery for the treatment of fungal keratitis to overcome the drawbacks of conventional ophthalmic solutions. Keywords: Itraconazole, Ocular drug delivery, In-situ gels, Carbopol 934, HPMC. QUICK RESPONSE CODE → DOI: 10.47583/ijpsrr.2021.v66i01.022 DOI link: http://dx.doi.org/10.47583/ijpsrr.2021.v66i01.022 INTRODUCTION ne of the principal predicaments faced in ophthalmic therapeutics is the attainment and retention of optimal ophthalmic drug concentration at the place of action, which is undermined predominantly on account of pre corneal loss resultant a diminutive ocular absorption of drug fraction such as only 10% drug concentrations available at the place of action within the eye 1 . Various ophthalmic preparations like drops, gels, balms or ointments and polymeric ocular inserts have been explored trying to broaden the ocular residence period of drug for ophthalmic therapy 2 . The effectual dosage administer might be distorted by amplifying the retention period of ophthalmic drug by utilizing in-situ gel forming methods. Ophthalmic drug delivery is an incredibly fascinating and highly challenging goal in the management of ophthalmic therapy 3, 4 . The ophthalmic drops have extremely low bioavailability because of their quick washout during lacrimation (tears pool because of poor drainage) in eyes. The majority of the systems are applied as suspensions or solutions. The fast pre corneal quick elimination was observed by means of conservative ophthalmic preparations ends in poor therapeutics bioavailability. Ease of drug management in case of gel forms and highly viscous solutions impede its utilization and compliance of patient. The obscured vision and the lacrimation are related with the drug dosage involving within the gel form. Hence, these might be conquering by manufacturing the medicine as a formulation that goes through immediate in- situ gelation upon administration to the eyes. They go through gelation after drug instillation because of physico- chemical alterations take place in the eyes. It builds the precorneal contact time and improved bioavailability of preparation can be accomplished by formulating in-situ gel systems. The present study describes “Development and evaluation of itraconazole loaded ocular In-situ gel formulations for enhancing ocular bioavailability” METERIALS AND METHODS Itraconazole was acquired from Glenmark Pharma private Ltd, Mumbai, India. All the polymers received were of pharmaceutical grade (HPMC K4, HPMC LVCR-100 are obtained from Lepid Life Sciences Pvt Ltd, Delhi, India and Carbopol-934 and Carbopol-980 are obtained from Sigma- Aldrich, Germany were used as received. Benzalkonium chloride was obtained from S.D Fine chemicals, Mumbai, Formulation Development and Evaluation of Itraconazole Ocular In-situ Gel for Enhancement of Ocular Bioavailability: In-vitro Antifungal Activities Assessment O Research Article