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Design, Development and Evaluation of Cationic Guar and Hydroxypropylguar BasedIn Situ Gels for Ophthalmic Drug Delivery

Dasankoppa F.S. and Swamy N.G.N


The poor bioavailability and therapeutic response exhibited by the conventional eye drops due to rapidcorneal loss is overcome by the use of ion-activated gel forming systems that are instilled as drops;these undergo gelation in cul-de-sac mode. The present study describes the design, development andevaluation of in situ ophthalmic drug delivery of antibacterial agent, linezolid, based on ion-activatedguar gum derivatives. Novel polymers such as Cationic guar with hydroxypropyl guar are being used asgelling as well as viscosity enhancing agents. Differential scanning calorimetric studies have revealedthat linezolid is compatible with all the excipients in the formulation. The study also aims at rheologicalcharacterization, effect of sterilization (moist heat) and effect of aging on the viscosity of in situ gels bycalculating consistency index (K), flow behaviour index (n value) using power law model. The in vitrodrug diffusion study for the developed formulations has also been carried out. The formulation CGHPG2,exhibiting good physical stability subsequent to sterilization and storage and further retaining theconsistency index (K) and flow behavior index (n value), was chosen as the optimized formulation. Thegel formed in situ revealed the sustained release of the drug for up to 12 hrs. Stability data recordedover a period of 6 months at elevated temperature conditions revealed the formulation to be stable.Invivo ocular toxicity studies revealed non irritant and non toxic nature of the formulation. Therefore, thedeveloped guar gum derivative based ophthalmic in situ gel by virtue of its prolonged corneal residencetime and sustained drug release could be considered a viable alternative to the conventional eye dropformulation in achieving enhanced bioavailability.
Year 2013 | Volume No. 50 | Issue No.1 | Page No. 30
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