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Sci. Pharm. 2008, 76(3), 515-532; doi:10.3797/scipharm.0803-17 (registering DOI)

Formulation and Evaluation of a Novel In Situ Gum Based Ophthalmic Drug Delivery System of Linezolid

1
Pharmacy, Rajiv Gandhi University of Health Sciences, Vidyanagar, Hubli–580031, Karnataka, India
2
Government College of Pharmacy, Rajiv Gandhi University of Health sciences, Bangalore, Subbiah Circle-580027, Karnataka, India
*
Author to whom correspondence should be addressed.
Received: 19 March 2008 / Accepted: 21 May 2008 / Published: 18 August 2008
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Abstract

Abstract A major problem in ocular therapeutics is the attainment of optimal drug concentration at the site of action, which is compromised mainly due to precorneal loss resulting in only a small fraction of the drug being ocularly absorbed [1]. The effective dose administered may be altered by increasing the retention time of medication into the eye by using in situ gel forming systems. The aim of the present investigation is to prepare and evaluate novel in situ gum based ophthalmic drug delivery system of linezolid. Hydroxypropyl guar (HPG) and xanthum (XG) were used as gum with the combination of hydroxyethyl cellulose (HEC), carbopol (CP), and sodium alginate as viscosity enhancing agents. Suitable concentrations of buffering agents were used to adjust the pH to 7.4. All the formulations were sterilized in an autoclave at 121°C for 15mins. The formulations were evaluated for clarity, pH measurement, gelling capacity, drug content estimation, rheological study, in vitro diffusion study, antibacterial activity, isotonicity testing, eye irritation testing. The developed formulations exhibited sustained release of drug from formulation over a period of 6hr thus increasing residence time of the drug. The optimized formulations were tested for eye irritation on albino rabbit (male) using the Draize test protocol with crossover studies. The formulations were found to be non-irritating with no ocular damage or abnormal clinical signs to the cornea, iris or conjunctiva observed. Thus these in situ gelling systems containing gums may be a valuable alternative to the conventional systems.
Keywords: Linezolid; In situ gel; Draize test; Gelling capacity; Rheological evaluation; In vitro diffusion study Linezolid; In situ gel; Draize test; Gelling capacity; Rheological evaluation; In vitro diffusion study
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

HIREMATH, S.S.P.; DASANKOPPA, F.S.; NADAF, A.; JAMAKANDI, V.G.; MULLA, J.S.; A., S.S.; SHOLAPUR, H.N.; AEZAZAHMED; G., N.N. Formulation and Evaluation of a Novel In Situ Gum Based Ophthalmic Drug Delivery System of Linezolid. Sci. Pharm. 2008, 76, 515-532.

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