Exploring of Taguchi Design in the Optimization of Brinzolamide and Timolol Maleate Ophthalmic in-situ Gel used in Treatment of Glaucoma

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Author(s): Purvi Shah, Vaishali Thakkar*, Vishvas Anjana, Jenee Christiana, Roma Trivedi, Kalpana Patel, Mukesh Gohel, Tejal Gandhi

Journal Name: Current Drug Therapy

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Objective: The present research work focuses on experimental design assisted In-situ gel for fixed dose combination.

Significance: Brinzolamide(BZ) BCS class II drug and timolol maleate(TM), a BCS class I drug is formulated for obtaining sustained effect, increased ocular bioavailability and reduction of dose leading to better patient compliance.

Methods: The material attributes were gelrite, hydroxy propyl methyl cellulose K4M(HPMC K4M) and HP-β-CD and critical quality attribute identified were gel strength, mucoadhesive index and percent of drug release of both drugs. BZ and TM were successfully formulated in ion-triggered In-situ gelling system using Taguchi design with minimum trials.

Results: The final optimized formula 0.5 %w/v gelrite, 0.5 %w/v HPMC K4M, 1:2.5 Ratio of drug to HP-β-CD as well as 150rpm stirring rate exhibited acceptable results with enhanced solubility of BZ. Pharmacodynamic study revealed decrease in intraocular pressure for In-situ gel (17.3) compared to conventional formulation. Moreover, delayed mean residence time and high AUC(61.237 and 4523.65) of In-situ gel indicates prolonged residence time with sustained release.

Conclusion: In conclusion, an excellent ocular tolerance and longer action of gelrite and HPMC K4M. In-situ gel for BZ and TM can be explored as potential alternative to marketed formulation reducing frequency of administration and improving patient compliance in glaucoma.

Keywords: In-situ Gel; HP-β-CD; Taguchi Design; In-vivo animal study

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(E-pub Ahead of Print)
DOI: 10.2174/1574885514666190916151506