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chitosan, (pHâ€sensitive polymer also acts as a permeation enhancer) was used in temperature and pHâ€triggered in situ gelling systems while gellan alone was used in ionâ€activated in situ gelling system. The formulation allows its easy instillation into the eye as a liquid (drops), forms transparent gel, and spreads over the corneal surface. At the formulation pH, transcorneal permeation profile of ofloxacin was comparable to that of in vitro release profile. In situ gelâ€forming ability of the developed systems significantly controls precorneal drainage as studied by gamma scintigraphy. Thus, increased residence time in the
eye would help to increase the ocular bioavailability.The formulation was also found to be nonirritant and well tolerable. Cmax of in situ gelling formulation was found to be 1.5 times higher than marketed eye drops solution at the similar Tmax of 1 h.
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Kaur IP, Garg A, Singla AK, Aggarwal D. Vesicular systems in ocular drug delivery: An overview. Int J Pharm 2004;269:1â€14.
Shell JW. Pharmacokinetics of topically applied ophthalmic drugs. Surv
Bourlais CL, Acar L, Zia H, Sado PA, Needham T, Leverge R. Ophthalmic
drug delivery systemsâ€“Recent advances. Prog Retin Eye Res
Bourlais CL, Acar LT, Rhodes CT, Sado PA, Leverge R. New ophthalmic
drug delivery systems. Drug Dev Ind Pharm 1995;21:19â€59.
Lin HR, Sung KC. Carbopol/pluronic phase change solutions for
ophthalmic drug delivery. J Control Release 2000;69:379â€88.
Srividya B, Cardoza RM, Amin PD. Sustained ophthalmic delivery of
ofloxacin from a pH triggered in situ gelling system. J Control Release
Wilson CG. Assessing ocular drug delivery with lachrimal scintigraphy.
Pharm Sci Technolo Today 1999;2:321â€6.
Rossomondo RM, Carlton WH, Trueblood JH, Thomas RP. A new method
of evaluating lacrimal drainage. Arch Ophthalmol 1972;88:523â€5.
Snibson GR, Greaves JL, Soper ND, Tiffany JM, Wilson CG, Bron AJ.
Ocular surface residence times of artificial tear solutions. Cornea
Greaves JL, Wilson CG, Birmingham AT. Assessment of the precorneal
residence of an ophthalmic ointment in healthy subjects. Br J Clin
Nagarsenker MS, Londhe VY, Nadkarni GD. Preparation and evaluation
of liposomal formulations of tropicamide for ocular delivery. Int J Pharm
Alany RG, Rades T, Nicoll J, Tucker IG, Davies NM. W/O microemulsions for ocular delivery: Evaluation of ocular irritation and precorneal retention. J Control Release 2006;111:145â€52.
Wei G, Xu H, Ding PT, Li SM, Zheng JM. Thermosetting gels with
modulated gelation temperature for ophthalmic use: The rheological
and gamma scintigraphic studies. J Control Release 2002;83:65â€74.
Liu Z, Li J, Nie S, Liu H, Ding P, Pan W. Study of an alginate/HPMCâ€based
in situ gelling ophthalmic delivery system for gatifloxacin. Int J Pharm
Gupta H, Velpandian T, Jain S. Ionâ€and pHâ€activated novel inâ€situ
gel system for sustained ocular drug delivery. J Drug Target
Khan S, Singhara D, Yeole P. Temperature induced in situ gel of lidocaine
hydrochloride for periodontal anesthesia. Indian Drugs 2005;42:519â€24.
Gilbert J, Richardson J, Davies M, Palin K, Hadgraft J. The effect of solutes
and polymers on the gelation properties of Pluronic F127 solutions for
controlled drug delivery. J Control Release 1987;5:113â€8.
Choi H, Jung J, Ryu J, Yoon S, Oh Y, Kim C. Development of in situâ€gelling
and mucoadhesive acetaminophen liquid suppository. Int J Pharm
Gonjari ID, Hosmani AH, Karmarkar AB, Godage AS, Kadam SB,
Dhabale PN. Formulation and evaluation of in situ gelling thermoreversible
mucoadhesive gel of fluconazole. Drug Discov Ther 2009;3:6â€9.
Elâ€Kamel A, Alâ€Dosari H, Alâ€Jenoobi F. Environmentally responsive
ophthalmic gel formulation of carteolol hydrochloride. Drug Deliv
Zignani M, Tabatabay C, Gurny R. Topical semiâ€solid drug delivery: Kinetics
and tolerance of ophthalmic hydrogels. Adv Drug Deliv Rev 1995;16:51â€60.
Sanzgiri Y, Mashi S, Crescenzi V, Callegaro L, Topp M, Stella V. Gellanâ€based
systems for ophthalmic sustained delivery of methylprednisolone.
J Control Release 1993;26:195â€201.
Gunning FP, Greve EL, Bron AM, Bosc JM, Royer JG, George JL, et al., Two
topical carbonic anhydrase inhibitors sezolamide and dorzolamide in
Gelrite vehicle: A multipleâ€dose efficacy study. Graefes Arch Clin Exp
Johnson DH, Epstein DL, Allen RC, Boysâ€Smith J, Campbell D,
Rosenquist R, et al., A oneâ€year multicenter clinical trial of pilocarpine
gel. Am J Ophthalmol 1984;97:723â€9.
Diamond JP, White L, Leeming JP, Bing Hoh H, Easty DL. Topical 0.3%
ciprofloxacin, norfloxacin, and ofloxacin in treatment of bacterial
keratitis: A new method for comparative evaluation of ocular drug
penetration. Br J Ophthalmol 1995;79:606â€9.