Vipul Sansare et al., Int. J. Res. Pharm. Sci., 2021, 12(2), 1003-1008 SčĔėę CĔĒĒĚēĎĈĆęĎĔē IēęĊėēĆęĎĔēĆđ JĔĚėēĆđ Ĕċ RĊĘĊĆėĈč Ďē PčĆėĒĆĈĊĚęĎĈĆđ SĈĎĊēĈĊĘ Published by JK Welfare & Pharmascope Foundation Journal Home Page: www.pharmascope.org/ijrps Design, fabrication and evaluation of clotrimazole loaded polymeric microsphere based in situ ophthalmic gel Manish Kumar Gupta 1 , Vipul Sansare *1 , Birendra Shrivastava 1 , Santosh Jadhav 2 1 School of Pharmaceutical Sciences, Jaipur National University, Jaipur- 302017, India 2 SVPM’S College of Pharmacy, Malegaon, Maharashtra- 413115, India Article History: Received on: 05 Jan 2021 Revised on: 10 Feb 2021 Accepted on: 22 Feb 2021 Keywords: Clotrimazole, Corneal fungal infection, In situ gel, PLGA, Polymeric microsphere AćĘęėĆĈę The present study was started with aim to design clotrimazole loaded poly- meric microsphere based in situ ophthalmic gel for management of corneal fungal infections. The clotrimazole loaded microsphere was fabricated using various percentage of polylactide-co-glycolide polymer by solvent evapora- tion technique and evaluated for particle size, zeta potential and encapsula- tion efϐiciency. The polyvinyl alcohol was used as stabilizer. The formulation batch which showed good particle size and entrapment efϐiciency was selected for further study. The in situ ophthalmic gel of optimized drug loaded micro- sphere was formulated using various ratios of sodium alginate and hydroxy propyl methyl cellulose. The formulated gel was evaluated with respect to pH, in vitro gelling capacity, clarity, viscosity, in vitro antifungal activity and in vitro transcorneal permeation behavior. The fabricated drug loaded micro- spheres revealed acceptable particle size, zeta potential and encapsulation efϐiciency. The prepared in situ gels were clear and exhibited acceptable pH, rheological properties and in vitro gelation. The drug loaded microsphere based gel revealed superior in vitro antifungal activity against Aspergillus niger than conventional formulation and sufϐicient drug permeation across goat cornea. Thus, formulated clotrimazole loaded microsphere based in situ gel based systems can be a promising approach for sustained ophthalmic delivery of antifungal agents. * Corresponding Author Name: Vipul Sansare Phone: +91-8692930764 Email: avipulsansare@gmail.com ISSN: 0975-7538 DOI: https://doi.org/10.26452/ijrps.v12i2.4617 Production and Hosted by Pharmascope.org © 2021 | All rights reserved. INTRODUCTION Fungal eye infection is extremely rare but major cause of ocular morbidity. Mycotic eye infections are commonly caused by yeast Candida albicans which is the most common cause of endogenous Endophthalmitis (Klotz et al., 2000). The fungi such as Fusarium solani and Aspergillus ϔlavus are also responsible for one-third of all traumatic infectious keratitis. Endophthalmitis is an infection of the inside of the eye i.e. the vitreous and/or aqueous humor whereas keratitis is an infection of the cornea of eye (Müller et al., 2013). Clotrimazole (CLZ), 1- [(2-chlorophenyl)diphenylmethyl]-1H-imidazole is well known antifungal drug containing imidazole ring. Conventional ophthalmic drug administration involves local administration of antifungal drug by topical route (Mohanty et al., 2015). However con- ventional ophthalmic drug delivery is challenging due to barrier properties of cornea and conjunc- tiva. The unique anatomy and physiology cornea presents constant challenge for formulators to cir- cumvent the protective barriers of eyes. In addition to this, poor ocular residence time of drug due to its © International Journal of Research in Pharmaceutical Sciences 1003