In Situ Ophthalmic Gel of Ciprofloxacin Hydrochloride for Once a Day Sustained Delivery

Abstract

This article focuses on preparation and evaluation of a once a day ophthalmic delivery system for ciprofloxacin hydrochloride based on the concept of pH-triggered in situ gelation. The in situ gelling system involves the use of polyacrylic acid (Carbopol ® 980NF) as a phase transition polymer, hydroxypropyl methylcellulose (Methocel ® K100LV) as a release retardant, and ion exchange resin as a complexing agent. Ciprofloxacin hydrochloride was complexed with ion exchange resin to avoid incompatibility between drug and polyacrylic acid. The developed formulation was stable, and nonirritant to rabbit eyes and in vitro drug release was found to be around 98% over a period of 24 hours.Keywords pH-triggered in situ gel; ciprofloxacin hydrochloride; Carbopol ® ; hydroxypropyl methylcellulose; once a day ocular delivery system INTRODUCTIONToday, topical ophthalmic application is considered the preferred way to achieve therapeutic levels of active medicament used to treat ocular diseases. Solutions, suspensions, and semisolids like ointments and gels are conventionally available as ophthalmic delivery systems. From a biopharmaceutical standpoint, their use has met some criticism over their efficiency as drug delivery systems. Bioavailability, particularly for ocular solutions, ranges from 1% to 10% of the total administered dose. This could be due to the rapid precorneal kinetics resulting from reflex tearing and blinking. The basic disadvantage associated with the use of ocular formulation is rapid loss of both solutions and suspended solid. Ophthalmic ointments give blurred vision, leading to poor patient acceptance (Olejnic, 1993).

New method for ophthalmic delivery of azithromycin by poloxamer/carbopol-based in situ gelling system

“…These systems are more acceptable for patients since they are administered into the eye as solutions, after which they undergo transition into gels. These ocular drug delivery systems can be classified as pH-triggered systems, thermosensitive systems, and ion-activated systems (El-Kamel et al, 2006;Jain et al, 2008;Ma et al, 2008).…”

Newer Trends in In Situ Gelling Systems for Controlled Ocular Drug Delivery

“…To avoid incompatibility between drug and polyacrylic acid, ciprofloxacin hydrochloride was complexed with ion exchange resin. The formulation was observed to be stable and nonirritant to rabbit's eye and showed 98% in vitro drug release over a period of 24 hours [15].…”

“…In situ ophthalmic gel of fluroquinolone antibiotic ciprofloxacin hydrochloride using polyacrylic acid (Carbopol ® 980NF) as pH sensitive phase transition polymer was prepared by Jain et al [15]. HPMC (Methocel ® K100LV) was added as a release retardant, and ion exchange resin as a complexing agent.…”

“…A wide variety of drug molecules and materials of therapeutic advantages such as antibiotics (Ofloxacin, Ciprofloxacin, Gatifloxacin), beta blockers (Timolol, Carteolol), NSAIDs (Ketorolac Tromethamine, Indomethacin), Pilocarpine hydrochloride, Puerarin, Recombinant rhEGF, Antivirals (Acyclovir) has been delivered through in situ gelling systems, which shows the importance of in situ gelling formulations as the future drug delivery systems [7][8][9][11][12][13][14][15][16][17][18][19][20][21][22][23][24][25].…”

Design and Evaluation of a Brinzolamide Drug–Resin <i>in Situ</i> Thermosensitive Gelling System for Sustained Ophthalmic Drug Delivery

“…DSC was carried out by heating four substances (drug, resin, drug-resin complex and drug-resin physical mixture) separately from 40 to 270°C at the heating rate of 10°C/min under a nitrogen environment. 19) The instrument used was a DSC-60A (Shimadzu Corp., Kyoto, Japan).…”