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

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

Journal Name: Current Drug Therapy

Volume 15 , Issue 5 , 2020

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Graphical Abstract:


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 the 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 attributes identified were gel strength, mucoadhesive index and percentage 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. The pharmacodynamic study revealed a decrease in intraocular pressure for In-situ gel (17.3) compared to conventional marketed suspension. 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, 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 the frequency of administration and improving patient compliance in glaucoma.

Keywords: In-situ gel, HP-β-CD, taguchi design, in-vivo animal study, brinzolamide, Glaucoma.

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Article Details

Year: 2020
Published on: 22 January, 2021
Page: [524 - 542]
Pages: 19
DOI: 10.2174/1574885514666190916151506

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